dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d7098213ef994e7f871969c33d7d6733
CCCCO.Oc1ccc(Br)cc1F>>CCCCOc1ccc(Br)cc1F
N(=NC(=O)OC(C)C)C(=O)OC(C)C.BrC1=CC(=C(C=C1)O)F.C(CCC)O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>BrC1=CC(=C(C=C1)OCCCC)F
O[CH2:4][CH2:3][CH2:2][CH3:1].[OH:5][c:6]1[cH:7][cH:8][c:9]([Br:10])[cH:11][c:12]1[F:13]>>[CH3:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]([Br:10])[cH:11][c:12]1[F:13]
CCCCO.Oc1ccc(Br)cc1F
CCCCOc1ccc(Br)cc1F
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
86bfb73617450d22f9456ed5ce4d96a73f1f8fc0c016bebae57fda68e2da86a2
2258bd14c3b5449b92dc09cf9fa522f88d5071b4af20f7e968b60aa1ae6db0cf
c1ccccc1
O-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
95.6
[{"value": 95.6, "product": "BrC1=CC(=C(C=C1)OCCCC)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
0.315 mol of each of 4-bromo-2-fluorophenol (1), 1-butanol and triphenylphosphine were dissolved in 1000 ml of tetrahydrofuran, and 0.315 mol of diisopropyl azodicarboxylate was added dropwise at about 20° C. After the mixture had been stirred overnight, the solvent was removed by distillation in a rotary evaporator, a...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Aromatic alcohol
Ether
null
null
c1ccccc1
HO-
O1CCCC1
null
8
CCCCO.Oc1ccc(Br)cc1F>O1CCCC1>CCCCOc1ccc(Br)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d72ec14bcd7c4423a145eaa149263f3b
CCCCOc1ccc(-c2ccc(OCC)c(F)c2)cc1F.COC(=O)OC>>O=C1C=CC=C2C1=Cc1ccccc12
C(OC)(OC)=O.C(CCC)[Li].Cl.C(C)OC1=C(C=C(C=C1)C1=CC(=C(C=C1)OCCCC)F)F>>C1(C=CC=C2C3=CC=CC=C3C=C12)=O
CCCCO[c:12]1[cH:11][cH:10][c:9](-[c:4]2[cH:3][c:8](F)[c:7](OCC)[cH:6][cH:5]2)[cH:14][c:13]1F.CO[C:2](OC)=[O:1]>>[O:1]=[C:2]1[CH:3]=[CH:4][CH:5]=[C:6]2[C:7]1=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]12
CCCCOc1ccc(-c2ccc(OCC)c(F)c2)cc1F.COC(=O)OC
O=C1C=CC=C2C1=Cc1ccccc12
null
null
O1CCCC1.CCCCCC
C-C Coupling
OtherReaction
e5b15ba84b2ba37cd733f78a51dce674bd6285e4b29a5f812aac175df36f2b0e
15a1940e22270f845f5603712729e7f951ae2ac4f5fe74812a8b111b8bc3cb17
O=C1C=CC=C2C1=Cc1ccccc12
C-C-C-C-O-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c;H0;D3;+0:4](-[c;H0;D3;+0:5]2:[cH;D2;+0:6]:[c;H0;D3;+0:7](-F):[c;H0;D3;+0:8](-O-C-C):[cH;D2;+0:9]:[cH;D2;+0:10]:2):[cH;D2;+0:11]:[c;H0;D3;+0:12]:1-F.C-O-[C;H0;D3;+0:13](=[O;D1;H0:14])-O-C>>[O;D1;H0:14]=[C;H0;D3;+0:13]1-[CH;D2;+0:6]=[CH;D2;+0:5]-[CH;D2;+0:10]=[C;H0;D3;+0:9]2-[C;H0...
null
[]
-70
CELSIUS
2
HOUR
60 mmol of 4-ethoxy-3,3′-difluoro-4′-butoxybiphenyl (5) are introduced into 200 ml of tetrahydrofuran, and the mixture is cooled to −70° C. 120 mmol of a 1.6 M solution of n-butyllithium in hexane are added dropwise, and the mixture is stirred at this temperature for 2 hours. 60 mmol of dimethyl carbonate are subsequen...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Carbonic Ester.Ether.Ether
Ketone.Conjugated diene
c1ccccc1.c1ccccc1
C1=CCC2=Cc3ccccc3C2=C1
C1=CCC2=Cc3ccccc3C2=C1
HF
O1CCCC1.CCCCCC
-70
2
CCCCOc1ccc(-c2ccc(OCC)c(F)c2)cc1F.COC(=O)OC>O1CCCC1.CCCCCC>O=C1C=CC=C2C1=Cc1ccccc12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-eca79e3229d14634afded7b73fa277ff
Brc1ccc(I)cc1.CCOc1ccc(B(O)O)c(F)c1F>>CCOc1ccc(C2(Br)C=CC=CC2)c(F)c1F
BrC1=CC=C(C=C1)I.Cl.[NH3+]N.FC1=C(C=CC(=C1F)OCC)B(O)O.B(=O)[O-].[Na+]>>BrC1(CC=CC=C1)C1=C(C(=C(C=C1)OCC)F)F
I[c:12]1[cH:11][cH:10][c:8]([Br:9])[cH:14][cH:13]1.OB(O)[c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:17]([F:18])[c:15]1[F:16]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C:8]2([Br:9])[CH:10]=[CH:11][CH:12]=[CH:13][CH2:14]2)[c:15]([F:16])[c:17]1[F:18]
Brc1ccc(I)cc1.CCOc1ccc(B(O)O)c(F)c1F
CCOc1ccc(C2(Br)C=CC=CC2)c(F)c1F
null
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl
O.O1CCCC1
C-C Coupling
OtherReaction
24147e6c17b57f1fbe9654a7dfabfddb33df908fb9bb12bacd88530f88c84429
26a064b072c3f632170c6bc35a0d0971310fe79472b0652670ca7488a1dfe506
C1=CCC(c2ccccc2)C=C1
I-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[c;H0;D3;+0:4](-[Br;D1;H0:5]):[cH;D2;+0:6]:[cH;D2;+0:7]:1.O-B(-O)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[F;D1;H0:12]):[c:13]>>[Br;D1;H0:5]-[C;H0;D4;+0:4]1(-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11](-[F;D1;H0:12]):[c:13])-[CH2;D2;+0:6]-[CH;D2;+0:7]=[CH;D2;+0:1]-[CH;D2;+0:2]=[CH;D2;...
null
[]
20
CELSIUS
5
MINUTE
0.450 mol of sodium metaborate are introduced into 240 ml of water. 0.012 mol of bis(triphenylphosphine)palladium(II) chloride, 0.6 mol of 4-bromo-1-iodobenzene (11) and 0.012 mol of hydrazinium hydrochloride are added, and the mixture is stirred at about 20° C. for 5 minutes. 0.6 mol of 2,3-difluoro-4-ethoxyphenylboro...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Boronic acid
Tertiary halide.Conjugated diene
c1ccccc1.c1ccccc1
c1ccccc1.C1=CCCC=C1
c1ccccc1.C1=CCCC=C1
I-.B
Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.O.O1CCCC1
20
0.083333
Brc1ccc(I)cc1.CCOc1ccc(B(O)O)c(F)c1F>Cl[Pd]([P](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3)([P](C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6)Cl.O.O1CCCC1>CCOc1ccc(C2(Br)C=CC=CC2)c(F)c1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0b9a94fdaf9742109279595824d5e13c
CCOc1ccc(-c2ccccc2B(O)O)c(F)c1F.c1ccc(P(c2ccccc2)c2ccccc2)cc1>>c1ccc(-c2ccccc2-c2ccccc2)cc1
FC1=C(C=CC(=C1F)OCC)C=1C(=CC=CC1)B(O)O.BrC1=CC(=C(C=C1)I)F.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C([O-])([O-])=O.[Na+].[Na+]>>C1(=CC=CC=C1)C=1C(=CC=CC1)C1=CC=CC=C1
CCOc1ccc(-[c:10]2[c:5](B(O)O)[cH:6][cH:7][cH:8][cH:9]2)c(F)c1F.c1ccc(P([c:4]2[cH:3][cH:2][cH:1][cH:18][cH:17]2)[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)cc1>>[cH:1]1[cH:2][cH:3][c:4](-[c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2-[c:11]2[cH:12][cH:13][cH:14][cH:15][cH:16]2)[cH:17][cH:18]1
CCOc1ccc(-c2ccccc2B(O)O)c(F)c1F.c1ccc(P(c2ccccc2)c2ccccc2)cc1
c1ccc(-c2ccccc2-c2ccccc2)cc1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
O.C(C)(C)O
C-C Coupling
OtherReaction
f8945fe9c079a69871e2c5a84e61f8ea58863b43334dfad26abc5ead49040606
77a9334ff309e7ea03168ea8c67a45d16cf2750ac0108bbb5ee5802c9501105d
c1ccc(-c2ccccc2-c2ccccc2)cc1
C-C-O-c1:c:c:c(-[c;H0;D3;+0:1]2:[c:2]:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6]:2-B(-O)-O):c(-F):c:1-F.[c:7]:[c:8]:[c;H0;D3;+0:9](-P(-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14])-c1:c:c:c:c:c:1):[c:15]:[c:16]>>[c:7]:[c:8]:[c;H0;D3;+0:9](-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6]:1-[c;H0;D3;+0:10](:[c:11]:[c:12]):...
null
[]
null
null
null
null
0.047 mol of 2′,3′-difluoro-4′-ethoxybiphenylboronic acid (14), 0.05 mol of 1-bromo-3-fluoro-4-iodobenzene (15), 1 mmol of palladium acetate, 2 mmol of triphenylphosphine, 25 ml of saturated sodium carbonate solution, 20 ml of water and 100 ml of isopropanol are initially introduced and refluxed overnight. Conventional...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ether.Boronic acid
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
HF.B
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].O.C(C)(C)O
null
null
CCOc1ccc(-c2ccccc2B(O)O)c(F)c1F.c1ccc(P(c2ccccc2)c2ccccc2)cc1>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].O.C(C)(C)O>c1ccc(-c2ccccc2-c2ccccc2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d9f85d7ffa8444e78678cc9498e7bd8a
ClN1C=Cc2ccccc2C1.OB(O)c1ccccc1>>c1ccc(-c2nccc3ccccc23)cc1
ClN1CC2=CC=CC=C2C=C1.C1(=CC=CC=C1)B(O)O.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C([O-])([O-])=O.[K+].[K+]>>C1(=CC=CC=C1)C1=NC=CC2=CC=CC=C12
Cl[N:6]1[CH2:5][c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[CH:8]=[CH:7]1.OB(O)[c:4]1[cH:3][cH:2][cH:1][cH:16][cH:15]1>>[cH:1]1[cH:2][cH:3][c:4](-[c:5]2[n:6][cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]23)[cH:15][cH:16]1
ClN1C=Cc2ccccc2C1.OB(O)c1ccccc1
c1ccc(-c2nccc3ccccc23)cc1
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-]
C(OC)COC
C-C Coupling
OtherReaction
a68c8cee464e8b848d31a64c983925882ceef8ec8515b34c884232707601f1dd
0bd0588c783a70e7d53efd630a4969b18d3b156f02f4c1f8e8551696045d6d66
c1ccc(-c2nccc3ccccc23)cc1
Cl-[N;H0;D3;+0:1]1-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5](:[c:6])-[CH;D2;+0:7]=[CH;D2;+0:8]-1.O-B(-O)-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[c:6]:[c:5]1:[cH;D2;+0:7]:[cH;D2;+0:8]:[n;H0;D2;+0:1]:[c;H0;D3;+0:2](-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]):[c:3]:1:[c:4]
96.9
[{"value": 96.9, "product": "C1(=CC=CC=C1)C1=NC=CC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.9, "product": "C1(=CC=CC=C1)C1=NC=CC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2-Chloro-isoquinoline (28.8 g, 0.176 mol), phenylboronic acid (25.7 g 0.211 mol), triphenylphosphine (4.6 g 17.6 mmol), palladium acetate (0.99 g 4.4 mmol) and 2M solution of potassium carbonate (65.7 g 0.475 mol) were added to 270 ml of dimethoxyethane. This mixture was stirred at reflux for 17 hrs. The mixture was th...
10.6084/m9.figshare.5104873.v1
null
Enamine.Boronic acid
null
C1=Cc2ccccc2C[NH]1.c1ccccc1
c1ccccc1.c1ccc2cnccc2c1
c1ccccc1.c1ccc2cnccc2c1
HCl.B
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(OC)COC
null
null
ClN1C=Cc2ccccc2C1.OB(O)c1ccccc1>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C(OC)COC>c1ccc(-c2nccc3ccccc23)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f9a41ba85d96457aa547e1997e89c67d
C=C(C)C(=O)O.CC(C)(C)OC(=O)CBr>>C=C(C)C(=O)OCC(=O)OC(C)(C)C
N#N.C(C(=C)C)(=O)O.BrCC(=O)OC(C)(C)C.C1CCC2=NCCCN2CC1>>C(C)(C)(C)OC(COC(C(=C)C)=O)=O
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[OH:6].Br[CH2:7][C:8](=[O:9])[O:10][C:11]([CH3:12])([CH3:13])[CH3:14]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][C:8](=[O:9])[O:10][C:11]([CH3:12])([CH3:13])[CH3:14]
C=C(C)C(=O)O.CC(C)(C)OC(=O)CBr
C=C(C)C(=O)OCC(=O)OC(C)(C)C
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
d0f2e7dd04291aff91491624f6ba09bd6ae2852adc109edeabfddd534d9ccfd8
ebb133741743004d799d6738504ddfd5b4a53248a4f85602c0fff1c33566ad58
null
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8].[C;D1;H2:9]=[C:10](-[C;D1;H3:11])-[C:12](=[O;D1;H0:13])-[OH;D1;+0:14]>>[C;D1;H2:9]=[C:10](-[C;D1;H3:11])-[C:12](=[O;D1;H0:13])-[O;H0;D2;+0:14]-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5](-[C;D1;H3:6])(-[C;D1;H3:7])-[C;D1;H3:8]
null
[]
null
null
1
HOUR
Methacrylic acid (8.06 g, 0.10 mole), t-butyl bromoacetate (19.50 g, 0.10 mole) and 1,8-diazabicyclo[5.4.0]undoc-7-ene, DBU, (15.20 g, 0.10 mole) and 150 ml toluene were combined in a 500 ml 3-neck flask equipped with condenser, nitrogen inlet, thermometer and magnetic stirrer bar. The reaction mixture was stirred at r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester.Ester
null
null
null
HBr
C1(=CC=CC=C1)C
null
1
C=C(C)C(=O)O.CC(C)(C)OC(=O)CBr>C1(=CC=CC=C1)C>C=C(C)C(=O)OCC(=O)OC(C)(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8ffe0e1859a94fc688a47d34ee7139b2
CC(=O)Cl.CCN(CCO)c1ccccc1>>CCN(CCOC(C)=O)c1ccccc1
O.C(C)N(C1=CC=CC=C1)CCO.C(C)N(CC)CC.C(C)(=O)Cl>>C(C)(=O)OCCN(C1=CC=CC=C1)CC
Cl[C:7]([CH3:8])=[O:9].[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][OH:6])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][O:6][C:7]([CH3:8])=[O:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1
CC(=O)Cl.CCN(CCO)c1ccccc1
CCN(CCOC(C)=O)c1ccccc1
null
null
CC(=O)C
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
c1ccccc1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
99.9
[{"value": 99.9, "product": "C(C)(=O)OCCN(C1=CC=CC=C1)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
51.8 g of 2-(N-ethylanilino)ethanol and 31.7 g of triethylamine were dissolved in 320 ml of acetone, and to this solution 24.9 g of acetyl chloride was slowly added dropwise while stirring under ice cooling. This mixture was stirred for 3 hours at room temperature, and the reaction solution was poured into 500 ml of wa...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
c1ccccc1
HCl
CC(=O)C
null
null
CC(=O)Cl.CCN(CCO)c1ccccc1>CC(=O)C>CCN(CCOC(C)=O)c1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-34275707ff204c1a9665c1e2feedc6dc
CCN(CCOC(C)=O)c1ccc(C=O)cc1.O=C1CCCCC1.[OH-]>>CCN(CCO)c1ccc(C=C2CCCC(=Cc3ccc(N(CC)CCO)cc3)C2=O)cc1
C(C)(=O)OCCN(C1=CC=C(C=C1)C=O)CC.C1(CCCCC1)=O.[OH-].[Na+]>>C(C)N(C1=CC=C(C=C1)C=C1C(C(CCC1)=CC1=CC=C(C=C1)N(CCO)CC)=O)CCO
O=[C:2]([CH3:1])[O:6][CH2:5][CH2:4][N:3]([c:7]1[cH:8][cH:9][c:10]([CH:11]=O)[cH:32][cH:33]1)[CH2:23][CH3:24].[CH2:12]1[CH2:13][CH2:19][CH2:20][C:21](=[O:31])[CH2:30]1.[OH-:27]>>[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][OH:6])[c:7]1[cH:8][cH:9][c:10]([CH:11]=[C:12]2[CH2:13][CH2:14][CH2:15][C:16](=[CH:17][c:18]3[cH:19][cH:20][c...
CCN(CCOC(C)=O)c1ccc(C=O)cc1.O=C1CCCCC1.[OH-]
CCN(CCO)c1ccc(C=C2CCCC(=Cc3ccc(N(CC)CCO)cc3)C2=O)cc1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
b192ce4c3d5c99a43991cddb805f904196d7633978bb5776af97c92a55a07b63
78009ba978d0ceae9d1dc423bbe7021c0591263ff5884ce533831826b7b1437a
O=C1C(=Cc2ccccc2)CCCC1=Cc1ccccc1
O=[CH;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[c:5](-[N;H0;D3;+0:6](-[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:10](=O)-[C;D1;H3:11])-[CH2;D2;+0:12]-[C;D1;H3:13]):[c:14]:[c:15]:1.[O;H0;D1;+0:16]=[C;H0;D3;+0:17]1-[CH2;D2;+0:18]-[CH2;D2;+0:19]-[CH2;D2;+0:20]-[CH2;D2;+0:21]-[CH2;D2;+0:22]-1.[OH-;D0:23]>>[C;D1;H3:11]-[CH2;D2;+0:10]-[N;H0;...
185.2
[{"value": 185.2, "product": "C(C)N(C1=CC=C(C=C1)C=C1C(C(CCC1)=CC1=CC=C(C=C1)N(CCO)CC)=O)CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
23.5 g of 2-(ethyl(4-formylphenyl)amino)ethyl acetate, 4.91 g of cyclohexanone and 150 ml of ethanol were mixed and to this was added an aqueous solution (25 ml) of 2.2 g of sodium hydroxide while stirring at 50° C. This mixture was further stirred for 5 hours. After cooling to room temperature, a precipitate was filtr...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone.Ester.Tertiary amine
Ketone.Primary alcohol.Primary alcohol.Tertiary amine.Tertiary amine
C1CCCCC1
C1CCCCC1.c1ccccc1
c1ccccc1.C1CCCCC1.c1ccccc1
null
C(C)O
50
null
CCN(CCOC(C)=O)c1ccc(C=O)cc1.O=C1CCCCC1.[OH-]>C(C)O>CCN(CCO)c1ccc(C=C2CCCC(=Cc3ccc(N(CC)CCO)cc3)C2=O)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-276671e04862474aa4387e04ebc7e0b5
Nc1ccc2c(=O)[nH][nH]c(=O)c2c1>>Nc1cccc2c(=O)[nH][nH]c(=O)c12
CN(C)C=O.C1=CC2=C(C=C1N)C(=O)NNC2=O>>C1=CC2=C(C(=C1)N)C(=O)NNC2=O
[NH2:1][c:2]1[cH:3][c:13]2[c:6]([cH:5][cH:4]1)[c:7](=[O:8])[nH:9][nH:10][c:11]2=[O:12]>>[NH2:1][c:2]1[cH:3][cH:4][cH:5][c:6]2[c:7](=[O:8])[nH:9][nH:10][c:11](=[O:12])[c:13]12
Nc1ccc2c(=O)[nH][nH]c(=O)c2c1
Nc1cccc2c(=O)[nH][nH]c(=O)c12
null
null
null
Miscellaneous
OtherReaction
2958a78cdf1571124dfc971b67140b8b51f8a1fd9b61f3100d91245dc9f6104a
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=c1[nH][nH]c(=O)c2ccccc12
[N;D1;H2:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[c;H0;D3;+0:4]2:[c:5](=[O;D1;H0:6]):[#7;a:7]:[#7;a:8]:[c:9](=[O;D1;H0:10]):[c:11]:2:[c:12]:[cH;D2;+0:13]:1>>[N;D1;H2:1]-[c;H0;D3;+0:2]1:[cH;D2;+0:3]:[cH;D2;+0:13]:[c:12]:[c:11]2:[c:9](=[O;D1;H0:10]):[#7;a:8]:[#7;a:7]:[c:5](=[O;D1;H0:6]):[c;H0;D3;+0:4]:2:1
null
[]
null
null
null
null
About 1 mg of Vitamin D binding protein, DBP, is buffer exchanged three times with 100 mM PBS at pH 8.2. The final volume was 200 uL. Succinyl-amino-buty-ethyl-isoluminol NHS ester (4.6 mg) is dissolved in DMF. The isoluminol (17 uL) is added to the DBP and the mixture is maintained at room temperature for about 1 hour...
10.6084/m9.figshare.5104873.v1
null
null
null
C1=c2ccccc2=CNN1
C1=c2ccccc2=CNN1
C1=c2ccccc2=CNN1
null
null
null
null
Nc1ccc2c(=O)[nH][nH]c(=O)c2c1>>Nc1cccc2c(=O)[nH][nH]c(=O)c12
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-34edcaa7e3ba4173928e329654c5e7d9
O=C(CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21)NCCCCCC(=O)ON1C(=O)CC(S(=O)(=O)[O-])C1=O>>O=C(O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21
C([O-])(O)=O.C1[C@H]2[C@@H]([C@@H](S1)CCCCC(=O)NCCCCCC(=O)ON3C(=O)CC(C3=O)S(=O)(=O)[O-])NC(=O)N2.[Na+]>>OC(=O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@H]12
O=C(CCCCCN[C:2](=[O:1])[CH2:4][CH2:5][CH2:6][CH2:7][C@@H:8]1[S:9][CH2:10][C@@H:11]2[NH:12][C:13](=[O:14])[NH:15][C@H:16]12)ON1C(=O)CC(S(=O)(=O)[O-])C1=O>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][CH2:6][CH2:7][C@@H:8]1[S:9][CH2:10][C@@H:11]2[NH:12][C:13](=[O:14])[NH:15][C@H:16]12
O=C(CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21)NCCCCCC(=O)ON1C(=O)CC(S(=O)(=O)[O-])C1=O
O=C(O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21
null
null
O
Miscellaneous
Oxidation of amide to carboxylic acid
62e278fda2673d37ab1043207b8d7b8eea62f64281613e4dde1953cdd8fd288d
a579c296c52361ddbd71a28ea32c062e3bd81eb84137ee3f44c507ab24af7ec9
O=C1N[C@H]2CSC[C@H]2N1
O=C(-C-C-C-C-C-N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4])-O-N1-C(=O)-C-C(-S(=O)(=O)-[O-])-C-1=O>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;D1;H1:5]
null
[]
null
null
4
MINUTE
About 2.0 mg of DBP is buffer exchanged with 20 mM bicarbonate at pH 9.6 three times to give a final volume of 1.0 mL. Two aliquots of sulfo-NHS-LC-biotin (Pierce) are dissolved in water to give a 1 mg/mL solution just prior to addition. The first aliquot (10 uL) is added and the reaction is maintained at room temperat...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Tertiary amide.Tertiary amide.Sulfonic acid
Carboxylic acid
C1CCNC1
null
C1N[C@H]2CSC[C@H]2N1
HO-
O
null
0.066667
O=C(CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21)NCCCCCC(=O)ON1C(=O)CC(S(=O)(=O)[O-])C1=O>O>O=C(O)CCCC[C@@H]1SC[C@@H]2NC(=O)N[C@@H]21
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a58080e00e764f4f9ecc3343f178b2be
O=C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO>>OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O
CC1([C@@H](N2[C@H](S1)[C@@H](C2=O)NC(=O)[C@@H](C=3C=CC=CC3)N)C(=O)O)C.CC1([C@@H](N2[C@H](S1)[C@@H](C2=O)NC(=O)[C@@H](C=3C=CC=CC3)N)C(=O)O)C.CC(C1CCC(C(O1)OC2C(CC(C(C2O)OC3C(C(C(CO3)(C)O)NC)O)N)N)N)NC.O=C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO.C[C@@H]1CC(=O)[C@]2([C@@H](O1)O[C@@H]3[C...
[OH:1][CH2:2][C@@H:3]([OH:4])[C@@H:11]([C@@H:9]([C@H:7]([CH:5]=[O:6])[OH:8])[OH:10])[OH:12]>>[OH:1][CH2:2][C@H:3]1[O:4][CH:5]([OH:6])[C@H:7]([OH:8])[C@@H:9]([OH:10])[C@H:11]1[OH:12]
O=C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO
OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O
null
null
OCC(O)CO
Heteroatom Alkylation and Arylation
OtherReaction
dd33a789286640dba431fbee315fe5133b49e36a8cf19e8a8c4cb319208abf4a
125aab717b417847558f582772c0fc28476c151b88628553e6b2e16bfc3d5da7
C1CCOCC1
[C:1]-[C:2](-[OH;D1;+0:3])-[C:4]-[C:5]-[C:6](-[O;D1;H1:7])-[CH;D2;+0:8]=[O;H0;D1;+0:9]>>[C:1]-[C:2]1-[C:4]-[C:5]-[C:6](-[O;D1;H1:7])-[CH;D3;+0:8](-[OH;D1;+0:9])-[O;H0;D2;+0:3]-1
null
[]
null
null
8
HOUR
Eight co-integrants each from the crosses summarized in Table 2 were streaked for single colonies (from cultures cryo-preserved in 10% glycerol; described in Section 6.4)) on Luria broth plates with ampicillin (100 μg/ml), spectinomycin (50 μg/ml) and gentamycin (10 μg/ml). Single colonies were inoculated into Luria br...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary alcohol
Ether.Secondary alcohol
null
C1CCOCC1
C1CCOCC1
null
OCC(O)CO
null
8
O=C[C@H](O)[C@@H](O)[C@@H](O)[C@H](O)CO>OCC(O)CO>OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@H]1O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d94a106a50a34f4c8ff61ec4d39c08b9
CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)OCc3ccccc3)cc2cc1Cl>>CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)O)cc2cc1Cl
[H][H].C(CCC)(=O)OC1=C(C=C2C=C(C(OC2=C1)=O)C(=O)NCC(=O)OCC1=CC=CC=C1)Cl.C(C)(=O)O.[H][H]>>C(CCC)(=O)OC1=C(C=C2C=C(C(OC2=C1)=O)C(=O)NCC(=O)O)Cl
c1ccc(C[O:20][C:18]([CH2:17][NH:16][C:14]([c:13]2[c:11](=[O:12])[o:10][c:9]3[cH:8][c:7]([O:6][C:4]([CH2:3][CH2:2][CH3:1])=[O:5])[c:24]([Cl:25])[cH:23][c:22]3[cH:21]2)=[O:15])=[O:19])cc1>>[CH3:1][CH2:2][CH2:3][C:4](=[O:5])[O:6][c:7]1[cH:8][c:9]2[o:10][c:11](=[O:12])[c:13]([C:14](=[O:15])[NH:16][CH2:17][C:18](=[O:19])[OH...
CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)OCc3ccccc3)cc2cc1Cl
CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)O)cc2cc1Cl
null
[Pd]
O1CCOCC1
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=c1ccc2ccccc2o1
[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]
null
[]
null
null
null
null
7-Butyryloxy-3-carboxymethylaminocarbonyl-6-chlorocoumarin was prepared as follows. 920 mg (2 mMol) 7-butyryloxy-3-benzyloxycarbonylmethylaminocarbonyl-6-chlorocoumarin were dissolved in 50 ml dioxane. 100 mg palladium on carbon (10%) and 100 microliters acetic acid were added to the solution and the suspension stirred...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccc2occcc2c1
Other
[Pd].O1CCOCC1
null
null
CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)OCc3ccccc3)cc2cc1Cl>[Pd].O1CCOCC1>CCCC(=O)Oc1cc2oc(=O)c(C(=O)NCC(=O)O)cc2cc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-dd15db25f90240b191400b49b2751000
COc1ccc(CSCCCCCCCCCCCCBr)cc1.O=C(O)CCCCCCCCCCCS>>COc1ccc(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)cc1
COC1=CC=C(CSCCCCCCCCCCCCBr)C=C1.SCCCCCCCCCCCC(=O)O.C[O-].CO.CO>>COC1=CC=C(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)C=C1
Br[CH2:20][CH2:19][CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][S:8][CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:37][cH:36]1.[SH:21][CH2:22][CH2:23][CH2:24][CH2:25][CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][C:33](=[O:34])[OH:35]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH...
COc1ccc(CSCCCCCCCCCCCCBr)cc1.O=C(O)CCCCCCCCCCCS
COc1ccc(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)cc1
null
null
CCOC(=O)C.C(C)(=O)O
Heteroatom Alkylation and Arylation
thioether_nucl_sub
77cd742b5ba20df0e225494f6e5f3d958ee82ce9a1b16fd99a2d9f8350b4fdc8
b05f7dda7dad719ae1868a84c33eeaf5bf649036fc64173cf4774a5eb4d70181
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[SH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:6]-[C:5]-[C:4]
49
[{"value": 49.0, "product": "COC1=CC=C(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.7, "product": "COC1=CC=C(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
MINUTE
Na (116 mg, 5 mmol) was dissolved it dry MeOH. 12-mercapto-1-dodecanoic acid (340 mg, 1.46 mmol)—synthesized according to JACS 115, 3458–3474, 1993—was added to the methoxide solution. After stirring with some heating for 5 min, (2) (497 mg, 1.24 mmol) was added to the reaction. The reaction became very viscous and an ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aliphatic thiol
Monosulfide
null
null
c1ccccc1
HBr
CCOC(=O)C.C(C)(=O)O
null
0.083333
COc1ccc(CSCCCCCCCCCCCCBr)cc1.O=C(O)CCCCCCCCCCCS>CCOC(=O)C.C(C)(=O)O>COc1ccc(CSCCCCCCCCCCCCSCCCCCCCCCCCC(=O)O)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2ab4c69ffe444c58afdc1046b831250f
C[N+](C)(C)CC(O)CCl.[Cl-]>>C[N+](C)(C)CCCO.[Cl-]
OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.[Cl-].ClCC(C[N+](C)(C)C)O.[OH-].[Na+].OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO>>[Cl-].OCCC[N+](C)(C)C.OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
Cl[CH2:7][CH:6]([CH2:5][N+:2]([CH3:1])([CH3:3])[CH3:4])[OH:8].[Cl-:21]>>[CH3:1][N+:2]([CH3:3])([CH3:4])[CH2:5][CH2:6][CH2:7][OH:8].[Cl-:21]
C[N+](C)(C)CC(O)CCl.[Cl-]
C[N+](C)(C)CCCO.[Cl-]
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
fc951f63d0c998ede5197f634065a1790ab013a6437aa03e3288e50bfe0f5e60
83c338d888ff405ee347e0cb1ab22bb61cb7dfdd74f9374da3ce0a74792dced1
null
Cl-[CH2;D2;+0:1]-[CH;D3;+0:2](-[OH;D1;+0:3])-[C:4]-[#7;+:5]>>[#7;+:5]-[C:4]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[OH;D1;+0:3]
null
[]
null
null
null
null
Herein is provided a synthesis procedure for the chloride salt of hydroxypropyltrimonium sorbitol (also referred to as ‘Sorbitol Monoquat’). A round bottom 250 ml flask was fitted with a mechanical stirrer. Into the flask was charged a mixture of sorbitol (10 g, 55.0 mmol) and 3-chloro-2-hydroxypropyl trimethylammonium...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary alcohol
Primary alcohol
null
null
null
Other
null
null
null
C[N+](C)(C)CC(O)CCl.[Cl-]>>C[N+](C)(C)CCCO.[Cl-]
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b7b3ed40ed644461b6f858f1a00c0109
C(=NC1CCCCC1)=NC1CCCCC1.CCNCC.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1.Oc1cccc2[nH]nnc12>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
C(C)NCC.C1(CCCCC1)N=C=NC1CCCCC1.Cl.NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.OC1=CC=CC=2NN=NC21>>Cl.Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)CC=1N=CNC1
C1CCC(N=[C:31]=[N:32]C2CCCCC2)CC1.C[CH2:35][NH:36][CH2:37]C.[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[C:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28].c1c[c:29]([OH:30])[c:34]2[c:33](c1)[nH]n[n:38]2>>[CH3:1][O:2][C...
C(=NC1CCCCC1)=NC1CCCCC1.CCNCC.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1.Oc1cccc2[nH]nnc12
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
null
null
CN(C=O)C
Acylation
OtherReaction
473e366d878e6f02fc99238eb9646fb1dcba650de30ad2973ed38753b5eb9ca0
3ca32cd4aad0c21eca7cfaa8c2b6f616c4b02f5e2f2fcbf465c0d443b194706c
O=C(CCc1c[nH]cn1)NCCc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1
C-[CH2;D2;+0:1]-[NH;D2;+0:2]-[CH2;D2;+0:3]-C.C1-C-C-C(-N=[C;H0;D2;+0:4]=[N;H0;D2;+0:5]-C2-C-C-C-C-C-2)-C-C-1.[C:6]-[C:7](-[NH2;D1;+0:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C;D1;H3:12].[O;D1;H0:13]=[C:14]1-[#16:15]-[C;H0;D3;+0:16](=[CH;D2;+0:17]-[c:18](:[c:19]):[c:20])-[C:21](=[O;D1;H0:22])-[#7:23]-1.[OH;D1;+0:24]-[c;H0;D3;+...
163.8
[{"value": 79.0, "product": "Cl.Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)CC=1N=CNC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 163.8, "product": "Cl.Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)CC=1N=CNC1", "details": "CALCULATEDPERCENTYIELD", "is_desire...
null
null
24
HOUR
Diethylamine (1.04 ml, 6.0 mmol) and N,N′-dicyclohexylcarbodiimide (0.64 g, 3.13 mmol) were added to the stirred suspension of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzylidene]thiazolidin-2,4-dione hydrochloride (1.3 g, 3.0 mmol), 2-N-t-butoxycarbonylamino-4-imidazole propionic acid (0.8 g, 3.13 mmol) and hy...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol.Primary amine.Secondary amine.Monosulfide
Secondary amide.Primary amine.Monosulfide
C1CCCCC1.C1CCCCC1.C1CSCN1.c1ccc2[nH]nnc2c1
C1CSCN1.c1c[nH]cn1
c1ccccc1.c1ccccc1.C1CSCN1.c1c[nH]cn1
Other
CN(C=O)C
null
24
C(=NC1CCCCC1)=NC1CCCCC1.CCNCC.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1.Oc1cccc2[nH]nnc12>CN(C=O)C>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-26ebee2f65de419a88e12f4b2597d1eb
C(=NC1CCCCC1)=NC1CCCCC1.CN(C)C=O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
O.Cl.NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.CN(C=O)C.C1(CCCCC1)N=C=NC1CCCCC1>>Cl.Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)CC=1N=CNC1
C1CCC([N:32]=[C:31]=[N:38][CH:34]2[CH2:33]CCC[CH2:35]2)CC1.C[N:36]([CH:29]=[O:30])[CH3:37].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[C:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]...
C(=NC1CCCCC1)=NC1CCCCC1.CN(C)C=O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
null
null
null
Acylation
OtherReaction
20b01e7dfa9851a73e9e8c5479f0a8661b682b55c889bfc071b442603174a3e5
1a4d3415d2184a745da04c57f5f66f1606ca66eda2f7c1d8c081f34200c7f7da
O=C(CCc1c[nH]cn1)NCCc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1
C-[N;H0;D3;+0:1](-[CH3;D1;+0:2])-[CH;D2;+0:3]=[O;D1;H0:4].C1-C-C-C(-[N;H0;D2;+0:5]=[C;H0;D2;+0:6]=[N;H0;D2;+0:7]-[CH;D3;+0:8]2-[CH2;D2;+0:9]-C-C-C-[CH2;D2;+0:10]-2)-C-C-1.[C:11]-[C:12](-[NH2;D1;+0:13])-[C:14](=[O;D1;H0:15])-[#8:16]-[C;D1;H3:17].[O;D1;H0:18]=[C:19]1-[#16:20]-[C;H0;D3;+0:21](=[CH;D2;+0:22]-[c:23](:[c:24]...
51
[{"value": 51.0, "product": "Cl.Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)CC=1N=CNC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
A solution of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzylidene]thiazolidin-2,4-dione hydrochloride (6 g, 13.7 mmol) and 2-N-t-butoxy-carbonylamino-4-imidazole propionic acid (5.2 g, 20.3 mmol) in N,N-dimethylformamide (200 ml) was stirred for 1 h at −10° C. N,N′-Dicyclohexylcarbodiimide (4.5 g, 21.8 mmol) wa...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Primary amine.Monosulfide
Secondary amide.Primary amine.Monosulfide
C1CCCCC1.C1CCCCC1.C1CSCN1
C1CSCN1.c1c[nH]cn1
c1ccccc1.c1ccccc1.C1CSCN1.c1c[nH]cn1
Other
null
null
12
C(=NC1CCCCC1)=NC1CCCCC1.CN(C)C=O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)Cc1c[nH]cn1.Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-63d709e139114d61af6aab85262e9c8f
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
O.Cl.NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.C(=O)(OC(C)(C)C)N1C(CCC1)C(=O)O.C1(CCCCC1)N=C=NC1CCCCC1>>C(C)(C)(C)OC(=O)N1C(CCC1)C(NC(CC1=CC=C(C=C1)OC1=CC=C(C=C1)C=C1C(NC(S1)=O)=O)C(=O)OC)=O
O[C:29](=[O:30])[CH:31]1[CH2:32][CH2:33][CH2:34][N:35]1[C:36](=[O:37])[O:38][C:39]([CH3:40])([CH3:41])[CH3:42].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[C:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28]>>[CH3:1][O:2...
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
null
null
C(C)(=O)OCC.CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C1NC(=O)C(=Cc2ccc(Oc3ccc(CCNC(=O)C4CCCN4)cc3)cc2)S1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:13].[C:14]-[C:15](-[NH2;D1;+0:16])-[C:17](=[O;D1;H0:18])-[#8:19]-[C;D1;H3:20]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:16]-[C:15](-[C:14])-[C:17](=[O;D1;H0:18])-[#8:19]-[C;D1;...
32.4
[{"value": 32.4, "product": "C(C)(C)(C)OC(=O)N1C(CCC1)C(NC(CC1=CC=C(C=C1)OC1=CC=C(C=C1)C=C1C(NC(S1)=O)=O)C(=O)OC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 32.1, "product": "C(C)(C)(C)OC(=O)N1C(CCC1)C(NC(CC1=CC=C(C=C1)OC1=CC=C(C=C1)C=C1C(NC(S1)=O)=O)C(=O)OC)=O", "details": "CALCULATEDPERCENTYIELD",...
null
null
10
HOUR
A solution of 5[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzylidene]thiazolidin-2,4-dione hydrochloride (2.5 g, 5.76 mmol) and N-Boc-pyrolidin-2-carboxylic acid (1.238 g, 5.76 mmol) in dimethyl formamide (25 ml) was stirred for 60 minutes at 0° C. N,N′-Dicyclohexylcarbodiimide (1.423 g, 6.91 mmol) was added to it ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.C1CSCN1.C1CC[NH]C1
HO-
C(C)(=O)OCC.CN(C=O)C
null
10
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>C(C)(=O)OCC.CN(C=O)C>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-964f5c140dda483dbe6b8a944fee6afc
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
O.Cl.NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.C(C)(C)(C)OC(=O)N1C(CCC1)C(=O)O.C1(CCCCC1)N=C=NC1CCCCC1>>C(C)(C)(C)OC(=O)N1C(CCC1)C(NC(CC1=CC=C(C=C1)OC1=CC=C(C=C1)CC1C(NC(S1)=O)=O)C(=O)OC)=O
O[C:29](=[O:30])[CH:31]1[CH2:32][CH2:33][CH2:34][N:35]1[C:36](=[O:37])[O:38][C:39]([CH3:40])([CH3:41])[CH3:42].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH2:16][CH:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28]>>[CH3:1][O:...
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
null
null
C(C)(=O)OCC.CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C1NC(=O)C(Cc2ccc(Oc3ccc(CCNC(=O)C4CCCN4)cc3)cc2)S1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:13].[C:14]-[C:15](-[NH2;D1;+0:16])-[C:17](=[O;D1;H0:18])-[#8:19]-[C;D1;H3:20]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:16]-[C:15](-[C:14])-[C:17](=[O;D1;H0:18])-[#8:19]-[C;D1;...
51.2
[{"value": 51.2, "product": "C(C)(C)(C)OC(=O)N1C(CCC1)C(NC(CC1=CC=C(C=C1)OC1=CC=C(C=C1)CC1C(NC(S1)=O)=O)C(=O)OC)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzyl]thiazolidin-2,4-dione hydrochloride (2.03 g, 4.65 mmol) and N-t-butoxycarbonylpyrrolidin-2-carboxylic acid (1 g, 4.65 mmol) in N,N-dimethylformamide (20 ml) was stirred for 1 h at 0° C. N,N′-Dicyclohexylcarbodiimide (0.96 g, 4.65 mmol) was added to th...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.C1CSCN1.C1CC[NH]C1
HO-
C(C)(=O)OCC.CN(C=O)C
null
2
CC(C)(C)OC(=O)N1CCCC1C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1>C(C)(=O)OCC.CN(C=O)C>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C1CCCN1C(=O)OC(C)(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0b5223ecf85040698165df61d6191fd1
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
O.Cl.NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.C(C)(C)(C)OC(=O)NC(C(=O)O)C.C1(CCCCC1)N=C=NC1CCCCC1>>C(C)(C)(C)OC(=O)NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C
O[C:29](=[O:30])[CH:31]([CH3:32])[NH:33][C:34](=[O:35])[O:36][C:37]([CH3:38])([CH3:39])[CH3:40].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH2:16][CH:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28]>>[CH3:1][O:2][C:3](=[O:4])...
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
null
null
C(C)(=O)OCC.O1CCCC1
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[C:13]-[C:14](-[NH2;D1;+0:15])-[C:16](=[O;D1;H0:17])-[#8:18]-[C;D1;H3:19]>>[C:13]-[C:14](-[NH;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]...
23
[{"value": 23.0, "product": "C(C)(C)(C)OC(=O)NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1.5
HOUR
A solution of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzyl]thiazolidin-2,4-dione hydrochloride (2.3 g, 5.27 mmol) and 2-t-butoxycarbonylaminopropionic acid (0.997 g, 5.27 mmol) in tetrahydrofuran (20 ml) was stirred for 1 h at 0° C. N,N′-Dicyclohexylcarbodiimide (1.086 g, 5.27 mmol) was added to this solution...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.C1CSCN1
HO-
C(C)(=O)OCC.O1CCCC1
null
1.5
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1>C(C)(=O)OCC.O1CCCC1>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9c8ede02f9314b8780028afe08414a5a
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)N
C(C)(C)(C)OC(=O)NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C.Cl>>Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C
CC(C)(C)OC(=O)[NH:33][CH:31]([C:29]([NH:28][CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH2:16][CH:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)=[O:30])[CH3:32]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11...
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)N
null
null
ClCCl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]-[C:8](-[#8:9])=[O;D1;H0:10]>>[#8:9]-[C:8](=[O;D1;H0:10])-[C:7]-[#7:6]-[C:4](=[O;D1;H0:5])-[C:2](-[C;D1;H3:3])-[NH2;D1;+0:1]
66.3
[{"value": 66.3, "product": "Cl.NC(C(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 5-[4-(4-(2-(2-t-butoxycarbonylaminopropanamido}2-methoxycarbonylethyl)phenoxy)benzyl]thiazolidin-2,4-dione (1 g, 1.75 mmol) in dichloromethane (10 ml) was bubbled with HCl gas at −10° C. for 50 minutes. The excess HCl gas was removed by N2 bubbling and concentrated to dryness to afford the title compound ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.c1ccccc1.C1CSCN1
HO-
ClCCl
null
null
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C>ClCCl>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)N
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-69940fd1468f471fa545f355ebf47133
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
O.Cl.NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.C(C)(C)(C)OC(=O)NC(C(=O)O)C.C1(CCCCC1)N=C=NC1CCCCC1>>C(C)(C)(C)OC(=O)NC(C(=O)NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C
O[C:29](=[O:30])[CH:31]([CH3:32])[NH:33][C:34](=[O:35])[O:36][C:37]([CH3:38])([CH3:39])[CH3:40].[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[C:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)[NH2:28]>>[CH3:1][O:2][C:3](=[O:4])[...
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
null
null
C(C)(=O)OCC.CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C1NC(=O)C(=Cc2ccc(Oc3ccccc3)cc2)S1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[C:13]-[C:14](-[NH2;D1;+0:15])-[C:16](=[O;D1;H0:17])-[#8:18]-[C;D1;H3:19]>>[C:13]-[C:14](-[NH;D2;+0:15]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]...
36.3
[{"value": 36.3, "product": "C(C)(C)(C)OC(=O)NC(C(=O)NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of 5-[4-(4-(2-amino-2-methoxycarbonylethyl)phenoxy)benzylidene]thiazolidin-2,4-dione hydrochloride (2 g, 4.6 mmol) and 2-t-butoxycarbonylamino propionic acid (0.87 g, 4.6 mmol) in dimethyl formamide (10 ml) was stirred for 1 h at 0° C. N,N′-Dicyclohexylcarbodiimide (1.139 g, 5.5 mmol) was added to this solut...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1.C1CSCN1
HO-
C(C)(=O)OCC.CN(C=O)C
null
2
CC(NC(=O)OC(C)(C)C)C(=O)O.COC(=O)C(N)Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1>C(C)(=O)OCC.CN(C=O)C>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(C)NC(=O)OC(C)(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9e01c3eb0ed740a29320f8d952f36727
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CNC(=O)OC(C)(C)C>>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CN
C(C)(C)(C)OC(=O)NCC(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC.Cl>>Cl.NCC(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC
CC(C)(C)OC(=O)[NH:32][CH2:31][C:29]([NH:28][CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH2:16][CH:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)=[O:30]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[...
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CNC(=O)OC(C)(C)C
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CN
null
null
ClCCl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C1NC(=O)C(Cc2ccc(Oc3ccccc3)cc2)S1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]-[C:7](-[#8:8])=[O;D1;H0:9]>>[#8:8]-[C:7](=[O;D1;H0:9])-[C:6]-[#7:5]-[C:3](=[O;D1;H0:4])-[C:2]-[NH2;D1;+0:1]
78.8
[{"value": 78.8, "product": "Cl.NCC(=O)NC(CC1=CC=C(OC2=CC=C(CC3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 5-[4-(4-(2-(2-t-butoxycarbonylaminoacetamido)-2-methoxycarbonylethyl)phenoxy)benzyl]thiazolidin-2,4-dione (0.73 g, 1.31 mmol) in dichloromethane (30 ml) was bubbled with HCl gas at −10° C. for 1.25 h. The excess HCl gas was removed by N2 bubbling and the solvent was removed by distillation to provide the ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.c1ccccc1.C1CSCN1
HO-
ClCCl
null
null
COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CNC(=O)OC(C)(C)C>ClCCl>COC(=O)C(Cc1ccc(Oc2ccc(CC3SC(=O)NC3=O)cc2)cc1)NC(=O)CN
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-25127b0bf1854ea0bc85f57270ceb0a7
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(CCSC)NC(=O)OC(C)(C)C>>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)CCSC
CSCCC(C(=O)NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)NC(=O)OC(C)(C)C.Cl>>Cl.CSCCC(C(=O)NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)N
CC(C)(C)OC(=O)[NH:32][CH:31]([C:29]([NH:28][CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][c:7]1[cH:8][cH:9][c:10]([O:11][c:12]2[cH:13][cH:14][c:15]([CH:16]=[C:17]3[S:18][C:19](=[O:20])[NH:21][C:22]3=[O:23])[cH:24][cH:25]2)[cH:26][cH:27]1)=[O:30])[CH2:33][CH2:34][S:35][CH3:36]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]([CH2:6][c:7]1[cH...
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(CCSC)NC(=O)OC(C)(C)C
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)CCSC
null
null
ClCCl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
O=C1NC(=O)C(=Cc2ccc(Oc3ccccc3)cc2)S1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6]-[C:7]-[C:8](-[#8:9])=[O;D1;H0:10]>>[#8:9]-[C:8](=[O;D1;H0:10])-[C:7]-[#7:6]-[C:4](=[O;D1;H0:5])-[C:2](-[C:3])-[NH2;D1;+0:1]
80.6
[{"value": 80.6, "product": "Cl.CSCCC(C(=O)NC(CC1=CC=C(OC2=CC=C(C=C3C(NC(S3)=O)=O)C=C2)C=C1)C(=O)OC)N", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 5-[4-(4-(2-(4-methylthio-2-t-butoxycarbonylaminobutyramido)-2-methoxycarbonylethyl)phenoxy)benzylidene]thiazolidin-2,4-dione (1.38 g, 2.2 mmol) in dichloromethane (30 ml) was bubbled with HCl gas at −10° C. for 80 minutes. The excess HCl gas was removed by N2 bubbling and the solvent was removed by distil...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1.c1ccccc1.C1CSCN1
HO-
ClCCl
null
null
COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(CCSC)NC(=O)OC(C)(C)C>ClCCl>COC(=O)C(Cc1ccc(Oc2ccc(C=C3SC(=O)NC3=O)cc2)cc1)NC(=O)C(N)CCSC
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b693a864a5f84c91904645550a8b9dac
COC(=O)c1ccc(C=O)cc1.c1ccc([P+](c2ccccc2)(c2ccccc2)C2CC2)cc1>>COC(=O)c1ccc(C=C2CC2)cc1
O.[Br-].C1(CC1)[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.[H-].[Na+].COC(=O)C1=CC=C(C=C1)C=O>>C1(CC1)=CC1=CC=C(C(=O)OC)C=C1
O=[CH:9][c:8]1[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:14][cH:13]1.c1ccc([P+](c2ccccc2)(c2ccccc2)[CH:10]2[CH2:11][CH2:12]2)cc1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH:9]=[C:10]2[CH2:11][CH2:12]2)[cH:13][cH:14]1
COC(=O)c1ccc(C=O)cc1.c1ccc([P+](c2ccccc2)(c2ccccc2)C2CC2)cc1
COC(=O)c1ccc(C=C2CC2)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
bd381618bc151c1640636a375a39e59b35fa6d8a00d5cfbbe1b09d2ed0b3fba6
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
C(=C1CC1)c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]1-[C:6]-[CH;D3;+0:7]-1-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[c:3]:[c:2](-[CH;D2;+0:1]=[C;H0;D3;+0:7]1-[C:5]-[C:6]-1):[c:4]
69.8
[{"value": 69.8, "product": "C1(CC1)=CC1=CC=C(C(=O)OC)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
2
HOUR
To a suspension of sodium hydride (60%, 0.27 g) in tetrahydrofuran (40 mL) was added cyclopropyltriphenylphosphonium bromide (2.6 g), and the mixture was stirred at 70° C. for 2 hours. To the reaction mixture was added methyl terephthalaldehydate (1.0 g), and the mixture was stirred at 70° C. for 7 days. Water was adde...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccccc1.c1ccccc1.c1ccccc1.C1CC1
C1CC1
c1ccccc1.C1CC1
HO-
O1CCCC1
70
2
COC(=O)c1ccc(C=O)cc1.c1ccc([P+](c2ccccc2)(c2ccccc2)C2CC2)cc1>O1CCCC1>COC(=O)c1ccc(C=C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-777da998342d4afdbf69846fb21072a8
COC(=O)c1ccc(C=C2CC2)cc1>>OCc1ccc(C=C2CC2)cc1
[H-].[Al+3].[Li+].[H-].[H-].[H-].C1(CC1)=CC1=CC=C(C(=O)OC)C=C1.O>>C1(CC1)=CC1=CC=C(CO)C=C1
CO[C:2](=[O:1])[c:3]1[cH:4][cH:5][c:6]([CH:7]=[C:8]2[CH2:9][CH2:10]2)[cH:11][cH:12]1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[C:8]2[CH2:9][CH2:10]2)[cH:11][cH:12]1
COC(=O)c1ccc(C=C2CC2)cc1
OCc1ccc(C=C2CC2)cc1
null
null
O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
C(=C1CC1)c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
101.3
[{"value": 101.3, "product": "C1(CC1)=CC1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a suspension of lithium aluminum hydride (0.16 g) in tetrahydrofuran (30 mL) was added methyl 4-(cyclopropylidenemethyl)benzoate (0.80 g), and the mixture was stirred at room temperature for 5 hours. Water (0.4 mL) was added to the reaction mixture, and the mixture was stirred for 3 days. Insoluble materials were re...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1.C1CC1
Other
O1CCCC1
null
5
COC(=O)c1ccc(C=C2CC2)cc1>O1CCCC1>OCc1ccc(C=C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9ebaaf178676404ebfef3fc9396de50d
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(C=C2CC2)cc1>>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
CC1=C(C(NN1)=O)CC1=CC=C(C=C1)C=C1CC1.CC(=O)OC[C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)Br)OC(=O)C)OC(=O)C)OC(=O)C>>CC1=C(C(=NN1)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)CC1=CC=C(C=C1)C=C1CC1
Br[C@H:8]1[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:37]([O:38][C:39]([CH3:40])=[O:41])[C@H:32]([O:33][C:34]([CH3:35])=[O:36])[C@H:27]1[O:28][C:29]([CH3:30])=[O:31].[O:9]=[c:10]1[nH:11][nH:12][c:13]([CH3:14])[c:15]1[CH2:16][c:17]1[cH:18][cH:19][c:20]([CH:21]=[C:22]2[CH2:23][CH2:24]2)[cH:25][cH:26]1>>[CH3:1][C:...
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(C=C2CC2)cc1
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
null
C([O-])([O-])=O.[Ag+2]
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
49b04419fad6ce95036469eff0b0bfaaabc2fb3bd31dcfbbcd47a76a3bff025b
5cef8b32be1a1b6849554821131ec7ae3bfda59406cde9d9abe4b3a7d689dd3d
C(=C1CC1)c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
Br-[C@@H;D3;+0:1](-[#8:2]-[C:3])-[C:4](-[#8:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8])-[C:9].[C:10]-[c:11]1:[c:12](-[C;D1;H3:13]):[#7;a:14]:[nH;D2;+0:15]:[c;H0;D3;+0:16]:1=[O;H0;D1;+0:17]>>[C:10]-[c:11]1:[c:12](-[C;D1;H3:13]):[#7;a:14]:[n;H0;D2;+0:15]:[c;H0;D3;+0:16]:1-[O;H0;D2;+0:17]-[C@H;D3;+0:1](-[#8:2]-[C:3])-[C:4](-[#8:5...
16.2
[{"value": 16.2, "product": "CC1=C(C(=NN1)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)CC1=CC=C(C=C1)C=C1CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
8
HOUR
To a suspension of 5-methyl-4-{[4-(cyclopropylidenemethyl)phenyl]methyl}-1,2-dihydro-3H-pyrazol-3-one (0.026 g) and acetobromo-α-D-glucose (0.049 g) in tetrahydrofuran was added silver carbonate (0.036 g), and the mixture was stirred at 60° C. overnight under light shielding. The reaction mixture was purified by column...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether
Ether.Ether
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1.c1ccccc1.C1CC1
HBr
C([O-])([O-])=O.[Ag+2].O1CCCC1
60
8
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(C=C2CC2)cc1>C([O-])([O-])=O.[Ag+2].O1CCCC1>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-19e9a998f28946868815e06a318ccf88
Brc1ccc(C2CC2)cc1.CN(C)C=O>>O=Cc1ccc(C2CC2)cc1
[Cl-].[NH4+].C(C)(C)(C)[Li].C1(CC1)C1=CC=C(C=C1)Br.CN(C=O)C>>C1(CC1)C1=CC=C(C=O)C=C1
Br[c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9]2)[cH:10][cH:11]1.CN(C)[CH:2]=[O:1]>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9]2)[cH:10][cH:11]1
Brc1ccc(C2CC2)cc1.CN(C)C=O
O=Cc1ccc(C2CC2)cc1
null
null
O1CCCC1
C-C Coupling
Bouveault aldehyde synthesis
4664d189e1ff40b394aee0a7d0943c7bfc06c1f81f238cff6865649dda594153
afd09ced98f25d311f21cc04ba6a50fe7e5516de47e17484683ded13d323b1b2
c1ccc(C2CC2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].C-N(-C)-[CH;D2;+0:6]=[O;D1;H0:7]>>[O;D1;H0:7]=[CH;D2;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
-78
CELSIUS
30
MINUTE
To a solution of 4-bromostylene (1.83 g) in dichloromethane (5 mL) was added diethylzinc (1 mol/L, 30 mL) under an argon atmosphere at 0° C., and the mixture was stirred at the same temperature for 10 minutes. Chloroiodomethane (4.3 mL) was added to the mixture, and the mixture was warmed to room temperature and stirre...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Tertiary amide
Aldehyde
c1ccccc1
c1ccccc1
c1ccccc1.C1CC1
HBr
O1CCCC1
-78
0.5
Brc1ccc(C2CC2)cc1.CN(C)C=O>O1CCCC1>O=Cc1ccc(C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-621039449c2a4a8292dc2cf8bcf28ed2
O=Cc1ccc(C2CC2)cc1>>OCc1ccc(C2CC2)cc1
O.C1(CC1)C1=CC=C(C=O)C=C1.[BH4-].[Li+]>>C1(CC1)C1=CC=C(CO)C=C1
[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9]2)[cH:10][cH:11]1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9]2)[cH:10][cH:11]1
O=Cc1ccc(C2CC2)cc1
OCc1ccc(C2CC2)cc1
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccc(C2CC2)cc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
95.9
[{"value": 95.9, "product": "C1(CC1)C1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 4-cyclopropylbenzaldehyde (0.71 g) in methanol (10 mL) was added lithium borohydride (2 mol/L tetrahydrofuran solution, 3.7 mL), and the mixture was warmed to room temperature and stirred for 30 minutes. To the reaction mixture was added water, and the mixture was extracted with diethyl ether. The orga...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1.C1CC1
null
CO
null
0.5
O=Cc1ccc(C2CC2)cc1>CO>OCc1ccc(C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6e4a81ed99724d89ab0593aba47b36bc
CCC=O.CCP(=O)(CC)Cc1ccc(C(=O)OC)cc1>>CC/C=C/c1ccc(C(=O)OC)cc1
[Cl-].[NH4+].C(C)P(=O)(CC)CC1=CC=C(C(=O)OC)C=C1.[H-].[Na+].C(CC)=O>>C(=C\CC)/C1=CC=C(C(=O)OC)C=C1
O=[CH:3][CH2:2][CH3:1].CCP(=O)(CC)[CH2:4][c:5]1[cH:6][cH:7][c:8]([C:9](=[O:10])[O:11][CH3:12])[cH:13][cH:14]1>>[CH3:1][CH2:2]/[CH:3]=[CH:4]/[c:5]1[cH:6][cH:7][c:8]([C:9](=[O:10])[O:11][CH3:12])[cH:13][cH:14]1
CCC=O.CCP(=O)(CC)Cc1ccc(C(=O)OC)cc1
CC/C=C/c1ccc(C(=O)OC)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
43d4e2f03e758941ee99f59641d5d56e6475fe935434d251d75d5cdebbe19869
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
c1ccccc1
C-C-P(=O)(-C-C)-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].O=[CH;D2;+0:5]-[C:6]-[C;D1;H3:7]>>[C;D1;H3:7]-[C:6]/[CH;D2;+0:5]=[CH;D2;+0:1]/[c:2](:[c:3]):[c:4]
null
[]
null
null
30
MINUTE
To a suspension of sodium hydride (60%, 0.97 g) in tetrahydrofuran (80 mL) was added methyl 4-(diethylphosphorylmethyl)benzoate (5.8 g) at 0° C., and the mixture was stirred for 30 minutes. To the reaction mixture was added a solution of propionaldehyde (1.6 mL) in tetrahydrofuran (10 mL), and the mixture was stirred a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
null
null
c1ccccc1
HO-
O1CCCC1
null
0.5
CCC=O.CCP(=O)(CC)Cc1ccc(C(=O)OC)cc1>O1CCCC1>CC/C=C/c1ccc(C(=O)OC)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ca3864fed8fc4967bdbb8ce498ef21c7
CCC=Cc1ccc(C(=O)OC)cc1>>CC/C=C/c1ccc(CO)cc1
C(=CCC)C1=CC=C(C(=O)OC)C=C1.[H-].[Al+3].[Li+].[H-].[H-].[H-].[OH-].[Na+].O.O>>C(=C\CC)/C1=CC=C(CO)C=C1
CO[C:9]([c:8]1[cH:7][cH:6][c:5]([CH:4]=[CH:3][CH2:2][CH3:1])[cH:12][cH:11]1)=[O:10]>>[CH3:1][CH2:2]/[CH:3]=[CH:4]/[c:5]1[cH:6][cH:7][c:8]([CH2:9][OH:10])[cH:11][cH:12]1
CCC=Cc1ccc(C(=O)OC)cc1
CC/C=C/c1ccc(CO)cc1
null
null
C(C)OCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
89.1
[{"value": 89.1, "product": "C(=C\\CC)/C1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
To a suspension of lithium aluminum hydride (1.2 g) in diethyl ether (100 mL) was added a solution of methyl 4-(but-1-en-1-yl)benzoate (2.5 g) in diethyl ether (20 mL) at 0° C., and the mixture was heated under reflux for 30 mixture. After the reaction mixture was cooled to 0° C., to the mixture were added water (1.2 m...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1
Other
C(C)OCC
0
null
CCC=Cc1ccc(C(=O)OC)cc1>C(C)OCC>CC/C=C/c1ccc(CO)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e24f573036ff4a2aaa16817ca2bb8277
COCCl.OCc1ccc(Br)cc1>>COCOCc1ccc(Br)cc1
O.BrC1=CC=C(CO)C=C1.C(C)(C)N(CC)C(C)C.COCCl>>BrC1=CC=C(C=C1)COCOC
Cl[CH2:3][O:2][CH3:1].[OH:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([Br:10])[cH:11][cH:12]1>>[CH3:1][O:2][CH2:3][O:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([Br:10])[cH:11][cH:12]1
COCCl.OCc1ccc(Br)cc1
COCOCc1ccc(Br)cc1
null
null
ClCCl
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
27244342195fcd168f26a709ba63fe92c20aa8622e0ab7a8f8d1433cf4454d5d
6b7bcf6411652db3d69b48a8c20d1194484df28a33661f5a192e999e8e5bbb75
c1ccccc1
Cl-[CH2;D2;+0:1]-[#8:2]-[C;D1;H3:3].[OH;D1;+0:4]-[C:5]-[c:6]>>[C;D1;H3:3]-[#8:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[C:5]-[c:6]
86.7
[{"value": 86.7, "product": "BrC1=CC=C(C=C1)COCOC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
To a solution of 4-bromobenzyl alcohol (2.8 g) and diisopropylethylamine (2.5 g) in dichloromethane (30 mL) was added chloromethyl methyl ether (1.3 g) at 0° C., and the mixture was stirred at room temperature for 14 hours. To the reaction mixture was water, and the mixture was extracted diethyl ether. The organic laye...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary alcohol
Ether.Ether
null
null
c1ccccc1
HCl
ClCCl
null
14
COCCl.OCc1ccc(Br)cc1>ClCCl>COCOCc1ccc(Br)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-bf427509761f45f6aaacfa11f5e1b9a1
CC(C)OB(OC(C)C)OC(C)C.COCOCc1ccc(Br)cc1>>COCOCc1ccc(OB(O)O)cc1
Cl.B(OC(C)C)(OC(C)C)OC(C)C.BrC1=CC=C(C=C1)COCOC.C(CCC)[Li]>>COCOCC1=CC=C(C=C1)OB(O)O
CC(C)[O:10][B:11]([O:12]C(C)C)[O:13]C(C)C.Br[c:9]1[cH:8][cH:7][c:6]([CH2:5][O:4][CH2:3][O:2][CH3:1])[cH:15][cH:14]1>>[CH3:1][O:2][CH2:3][O:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([O:10][B:11]([OH:12])[OH:13])[cH:14][cH:15]1
CC(C)OB(OC(C)C)OC(C)C.COCOCc1ccc(Br)cc1
COCOCc1ccc(OB(O)O)cc1
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
e9dbfb9f314e618f498ba931f950b90cc87acea41f31fcecb8d08ba23aa7f8e1
e3660767655c50df0f92afc78c794dd2af7cf646bf1430960eafd30c23bf3fa7
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].C-C(-C)-[O;H0;D2;+0:6]-[#5:7](-[O;H0;D2;+0:8]-C(-C)-C)-[O;H0;D2;+0:9]-C(-C)-C>>[OH;D1;+0:8]-[#5:7](-[OH;D1;+0:9])-[O;H0;D2;+0:6]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
90.8
[{"value": 90.8, "product": "COCOCC1=CC=C(C=C1)OB(O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 1-bromo-4-[(methoxymethyloxy)methyl]benzene (3.0 g) in tetrahydrofuran (52 mL) was added n-butyllithium (1.6 mol/L hexane solution, 9.3 mL) at −78° C., and the mixture was stirred for 30 minutes. To the reaction mixture was added triisopropyl borate (2.6 g), and the mixture was stirred at room temperat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1
c1ccccc1
c1ccccc1
HBr
O1CCCC1
null
0.5
CC(C)OB(OC(C)C)OC(C)C.COCOCc1ccc(Br)cc1>O1CCCC1>COCOCc1ccc(OB(O)O)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-260a63fadb674591b1c496508b6d04c3
Brc1nccs1.COCOCc1ccc(OB(O)O)cc1>>COCOCc1ccc(-c2nccs2)cc1
COCOCC1=CC=C(C=C1)OB(O)O.BrC=1SC=CN1.[F-].[Cs+]>>COCOCC1=CC=C(C=C1)C=1SC=CN1
Br[c:10]1[n:11][cH:12][cH:13][s:14]1.OB(O)O[c:9]1[cH:8][cH:7][c:6]([CH2:5][O:4][CH2:3][O:2][CH3:1])[cH:16][cH:15]1>>[CH3:1][O:2][CH2:3][O:4][CH2:5][c:6]1[cH:7][cH:8][c:9](-[c:10]2[n:11][cH:12][cH:13][s:14]2)[cH:15][cH:16]1
Brc1nccs1.COCOCc1ccc(OB(O)O)cc1
COCOCc1ccc(-c2nccs2)cc1
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
O.COCCOC.C(C)O
C-C Coupling
OtherReaction
c5d70f44da54f3e70cb2853a91e1281ef6956874f04660e612a73059bc40890b
48892094855745f5c51f8910c27ce7c101e08ad3f9da2a58d5512e3d9c1b432f
c1ccc(-c2nccs2)cc1
Br-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[#7;a:5]:1.O-B(-O)-O-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:8]:[c:7]:[c;H0;D3;+0:6](-[c;H0;D3;+0:1]1:[#16;a:2]:[c:3]:[c:4]:[#7;a:5]:1):[c:9]:[c:10]
46.5
[{"value": 46.5, "product": "COCOCC1=CC=C(C=C1)C=1SC=CN1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
85
CELSIUS
24
HOUR
To a solution of 1-bromo-4-[(methoxymethyloxy)methyl]benzene (3.0 g) in tetrahydrofuran (52 mL) was added n-butyllithium (1.6 mol/L hexane solution, 9.3 mL) at −78° C., and the mixture was stirred for 30 minutes. To the reaction mixture was added triisopropyl borate (2.6 g), and the mixture was stirred at room temperat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1cscn1.c1ccccc1
c1ccccc1.c1cscn1
c1ccccc1.c1cscn1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.COCCOC.C(C)O
85
24
Brc1nccs1.COCOCc1ccc(OB(O)O)cc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.COCCOC.C(C)O>COCOCc1ccc(-c2nccs2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ba1b19d3ae524c2aa76779742eed3d65
COCOCc1ccc(-c2nccs2)cc1>>OCc1ccc(-c2nccs2)cc1
O.Cl.COCOCC1=CC=C(C=C1)C=1SC=CN1.Cl>>S1C(=NC=C1)C1=CC=C(CO)C=C1
COC[O:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[n:8][cH:9][cH:10][s:11]2)[cH:12][cH:13]1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[n:8][cH:9][cH:10][s:11]2)[cH:12][cH:13]1
COCOCc1ccc(-c2nccs2)cc1
OCc1ccc(-c2nccs2)cc1
null
null
C(C)O
Reduction
Cleavage of alkoxy ethers to alcohols
c466c3bec39e9af8d3c14d52e5e6f58679d038f05bc956e4b63094a922799541
a4561cbdd42f56679299e19ea8b11070a39a15f6a95fb8a877e677f11b7ff57f
c1ccc(-c2nccs2)cc1
C-O-C-[O;H0;D2;+0:1]-[C:2]-[c:3]>>[OH;D1;+0:1]-[C:2]-[c:3]
50.8
[{"value": 50.8, "product": "S1C(=NC=C1)C1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
5
HOUR
To a solution of 1-bromo-4-[(methoxymethyloxy)methyl]benzene (3.0 g) in tetrahydrofuran (52 mL) was added n-butyllithium (1.6 mol/L hexane solution, 9.3 mL) at −78° C., and the mixture was stirred for 30 minutes. To the reaction mixture was added triisopropyl borate (2.6 g), and the mixture was stirred at room temperat...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Primary alcohol
null
null
c1ccccc1.c1cscn1
HO-
C(C)O
50
5
COCOCc1ccc(-c2nccs2)cc1>C(C)O>OCc1ccc(-c2nccs2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9ea8bc6bb4054a54a4711a5394da890f
CCOC(=O)CP(=O)(OCC)OCC.CCOC(OCC)c1ccc(C=O)cc1>>CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1
[Cl-].[NH4+].CCOC(C1=CC=C(C=C1)C=O)OCC.C(C)OP(=O)(OCC)CC(=O)OCC.[H-].[Na+]>>C(C)OC(C1=CC=C(C=CC(=O)OCC)C=C1)OCC
CCOP(=O)(OCC)[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].O=[CH:7][c:8]1[cH:9][cH:10][c:11]([CH:12]([O:13][CH2:14][CH3:15])[O:16][CH2:17][CH3:18])[cH:19][cH:20]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]=[CH:7][c:8]1[cH:9][cH:10][c:11]([CH:12]([O:13][CH2:14][CH3:15])[O:16][CH2:17][CH3:18])[cH:19][cH:20]1
CCOC(=O)CP(=O)(OCC)OCC.CCOC(OCC)c1ccc(C=O)cc1
CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1
null
null
O.O1CCCC1
C-C Coupling
Wittig with Phosphonium
a86984aeb4a9963534e0b081b0ecca18455fda1775f36ce168d1ca4cf966df3e
203dd34a20dceaf1737adbf20e01b43c2424e4e4b1722d942d1a796d895396e6
c1ccccc1
C-C-O-P(=O)(-O-C-C)-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].O=[CH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH;D2;+0:1]=[CH;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
null
null
10
MINUTE
To a solution of ethyl diethylphosphonoacetate (4.4 mL) in tetrahydrofuran (40 mL) was added sodium hydride (60%, 0.88 g) at 0° C., and the mixture was stirred for 10 minutes. To the reaction mixture was added a solution of terephthalaldehyde mono-(diethyl acetal) (4.2 g) in tetrahydrofuran (10 mL), and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Ester
null
null
c1ccccc1
HO-
O.O1CCCC1
null
0.166667
CCOC(=O)CP(=O)(OCC)OCC.CCOC(OCC)c1ccc(C=O)cc1>O.O1CCCC1>CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-5594bc4ab0f641049337d59474f1dcda
CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1>>CCOC(OCC)c1ccc(CCCO)cc1
C(C)OC(C1=CC=C(C=CC(=O)OCC)C=C1)OCC>>C(C)OC(C1=CC=C(C=C1)CCCO)OCC
CCO[C:14]([CH:13]=[CH:12][c:11]1[cH:10][cH:9][c:8]([CH:4]([O:3][CH2:2][CH3:1])[O:5][CH2:6][CH3:7])[cH:17][cH:16]1)=[O:15]>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][CH2:14][OH:15])[cH:16][cH:17]1
CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1
CCOC(OCC)c1ccc(CCCO)cc1
null
[Pt]
O1CCCC1
Reduction
OtherReaction
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccccc1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[CH;D2;+0:3]=[CH;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[c:5](:[c:6]):[c:7]
94.6
[{"value": 94.6, "product": "C(C)OC(C1=CC=C(C=C1)CCCO)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
HOUR
To a solution of ethyl diethylphosphonoacetate (4.4 mL) in tetrahydrofuran (40 mL) was added sodium hydride (60%, 0.88 g) at 0° C., and the mixture was stirred for 10 minutes. To the reaction mixture was added a solution of terephthalaldehyde mono-(diethyl acetal) (4.2 g) in tetrahydrofuran (10 mL), and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1
Other
[Pt].O1CCCC1
null
10
CCOC(=O)C=Cc1ccc(C(OCC)OCC)cc1>[Pt].O1CCCC1>CCOC(OCC)c1ccc(CCCO)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f8d46507f5dc462fa621f54e904a8352
BrCc1ccccc1.CCOC(OCC)c1ccc(CCCO)cc1>>CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1
O.C(C1=CC=CC=C1)Br.C(C)OC(C1=CC=C(C=C1)CCCO)OCC.[H-].[Na+]>>C(C)OC(C1=CC=C(C=C1)CCCOCC1=CC=CC=C1)OCC
Br[CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1.[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][CH2:14][OH:15])[cH:23][cH:24]1>>[CH3:1][CH2:2][O:3][CH:4]([O:5][CH2:6][CH3:7])[c:8]1[cH:9][cH:10][c:11]([CH2:12][CH2:13][CH2:14][O:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21]...
BrCc1ccccc1.CCOC(OCC)c1ccc(CCCO)cc1
CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
dd3f9c60e1f90d961a7c01d970ae213561355ee1451f276a3b04696e4b6fae5c
46a6e883cf919b4006e69abfdfd883f458f55c08b3200960c6a5b57c4139fbca
c1ccc(CCCOCc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
5
MINUTE
To a solution of ethyl diethylphosphonoacetate (4.4 mL) in tetrahydrofuran (40 mL) was added sodium hydride (60%, 0.88 g) at 0° C., and the mixture was stirred for 10 minutes. To the reaction mixture was added a solution of terephthalaldehyde mono-(diethyl acetal) (4.2 g) in tetrahydrofuran (10 mL), and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
CN(C=O)C
null
0.083333
BrCc1ccccc1.CCOC(OCC)c1ccc(CCCO)cc1>CN(C=O)C>CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-77a21fdd8bff4c069bfb526f3490207b
CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1>>OCc1ccc(CCCOCc2ccccc2)cc1
O.C(C)OC(C1=CC=C(C=C1)CCCOCC1=CC=CC=C1)OCC.Cl>>C(C1=CC=CC=C1)OCCCC1=CC=C(CO)C=C1
CCO[CH:2]([O:1]CC)[c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][O:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1
CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1
OCc1ccc(CCCOCc2ccccc2)cc1
null
null
O1CCCC1
Reduction
OtherReaction
c466c3bec39e9af8d3c14d52e5e6f58679d038f05bc956e4b63094a922799541
a4561cbdd42f56679299e19ea8b11070a39a15f6a95fb8a877e677f11b7ff57f
c1ccc(CCCOCc2ccccc2)cc1
C-C-O-[CH;D3;+0:1](-[O;H0;D2;+0:2]-C-C)-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
74.1
[{"value": 74.1, "product": "C(C1=CC=CC=C1)OCCCC1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of ethyl diethylphosphonoacetate (4.4 mL) in tetrahydrofuran (40 mL) was added sodium hydride (60%, 0.88 g) at 0° C., and the mixture was stirred for 10 minutes. To the reaction mixture was added a solution of terephthalaldehyde mono-(diethyl acetal) (4.2 g) in tetrahydrofuran (10 mL), and the mixture was...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Primary alcohol
null
null
c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
1
CCOC(OCC)c1ccc(CCCOCc2ccccc2)cc1>O1CCCC1>OCc1ccc(CCCOCc2ccccc2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-455c633b370b4a5898ab60ef54ef475f
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.O=c1[nH][nH]c(C(F)(F)F)c1Cc1ccc(CCCOCc2ccccc2)cc1>>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C(F)(F)F)c2Cc2ccc(CCCOCc3ccccc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
C(C1=CC=CC=C1)OCCCC1=CC=C(C=C1)CC=1C(NNC1C(F)(F)F)=O.CC(=O)OC[C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)Br)OC(=O)C)OC(=O)C)OC(=O)C.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)OCCCC1=CC=C(C=C1)CC=1C(=NNC1C(F)(F)F)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
Br[C@H:8]1[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:47]([O:48][C:49]([CH3:50])=[O:51])[C@H:42]([O:43][C:44]([CH3:45])=[O:46])[C@H:37]1[O:38][C:39]([CH3:40])=[O:41].[O:9]=[c:10]1[nH:11][nH:12][c:13]([C:14]([F:15])([F:16])[F:17])[c:18]1[CH2:19][c:20]1[cH:21][cH:22][c:23]([CH2:24][CH2:25][CH2:26][O:27][CH2:28][c...
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.O=c1[nH][nH]c(C(F)(F)F)c1Cc1ccc(CCCOCc2ccccc2)cc1
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C(F)(F)F)c2Cc2ccc(CCCOCc3ccccc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
null
null
C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
49b04419fad6ce95036469eff0b0bfaaabc2fb3bd31dcfbbcd47a76a3bff025b
5cef8b32be1a1b6849554821131ec7ae3bfda59406cde9d9abe4b3a7d689dd3d
c1ccc(COCCCc2ccc(Cc3c[nH]nc3O[C@H]3CCCCO3)cc2)cc1
Br-[C@@H;D3;+0:1](-[#8:2]-[C:3])-[C:4](-[#8:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8])-[C:9].[C:10]-[c:11]1:[c:12](-[C:13](-[F;D1;H0:14])(-[F;D1;H0:15])-[F;D1;H0:16]):[#7;a:17]:[nH;D2;+0:18]:[c;H0;D3;+0:19]:1=[O;H0;D1;+0:20]>>[C:10]-[c:11]1:[c:12](-[C:13](-[F;D1;H0:14])(-[F;D1;H0:15])-[F;D1;H0:16]):[#7;a:17]:[n;H0;D2;+0:18]:[...
41.8
[{"value": 41.8, "product": "C(C1=CC=CC=C1)OCCCC1=CC=C(C=C1)CC=1C(=NNC1C(F)(F)F)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
20
HOUR
To a solution of 4-({4-[3-(benzyloxy)propyl]phenyl}methyl)-5-trifluoromethyl-1,2-dihydro-3H-pyrazole-3-one (0.83 g) and acetobromo-α-D-glucose (1.5 g) in acetonitrile (12 mL) was added potassium carbonate (0.55 g), and the mixture was stirred at 60° C. for 20 hours. Insoluble materials were removed by filtration, and t...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether
Ether.Ether
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1.c1ccccc1.c1ccccc1
HBr
C(C)#N
60
20
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.O=c1[nH][nH]c(C(F)(F)F)c1Cc1ccc(CCCOCc2ccccc2)cc1>C(C)#N>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C(F)(F)F)c2Cc2ccc(CCCOCc3ccccc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-646484b9805f4ab1801c6600e812a249
CC(C)[P+](c1ccccc1)(c1ccccc1)c1ccccc1.COC(=O)c1ccc(C=O)cc1>>COC(=O)c1ccc(C=C(C)C)cc1
[Cl-].[NH4+].C(CCC)[Li].[I-].C(C)(C)[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.COC(=O)C1=CC=C(C=C1)C=O>>CC(=CC1=CC=C(C(=O)OC)C=C1)C
c1ccc([P+](c2ccccc2)(c2ccccc2)[CH:10]([CH3:11])[CH3:12])cc1.O=[CH:9][c:8]1[cH:7][cH:6][c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:14][cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([CH:9]=[C:10]([CH3:11])[CH3:12])[cH:13][cH:14]1
CC(C)[P+](c1ccccc1)(c1ccccc1)c1ccccc1.COC(=O)c1ccc(C=O)cc1
COC(=O)c1ccc(C=C(C)C)cc1
null
null
O1CCCC1
C-C Coupling
OtherReaction
cb5f277ac55a0e763ef643becc05f1522019cc4161daceb249ed2d634b78153b
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[CH;D3;+0:6](-[C;D1;H3:7])-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[C;D1;H3:5]-[C;H0;D3;+0:6](-[C;D1;H3:7])=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
88.9
[{"value": 88.9, "product": "CC(=CC1=CC=C(C(=O)OC)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
To a suspension of isopropyltriphenylphosphonium iodide (9.5 g) in tetrahydrofuran (90 mL) was added n-butyllithium (1.5 mol/L hexane solution, 15 mL) at 0° C., and the mixture was stirred for 15 minutes. To the reaction mixture was added a solution of methyl terephthalaldehydate (3.3 g) in tetrahydrofuran (10 mL), and...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1
HO-
O1CCCC1
null
0.25
CC(C)[P+](c1ccccc1)(c1ccccc1)c1ccccc1.COC(=O)c1ccc(C=O)cc1>O1CCCC1>COC(=O)c1ccc(C=C(C)C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e354b1f01bf5458aaf4bf38d80edc405
COC(=O)c1ccc(C=C(C)C)cc1>>CC(C)=Cc1ccc(CO)cc1
CC(=CC1=CC=C(C(=O)OC)C=C1)C.O.[OH-].[Na+].O.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>CC(=CC1=CC=C(CO)C=C1)C
CO[C:9]([c:8]1[cH:7][cH:6][c:5]([CH:4]=[C:2]([CH3:1])[CH3:3])[cH:12][cH:11]1)=[O:10]>>[CH3:1][C:2]([CH3:3])=[CH:4][c:5]1[cH:6][cH:7][c:8]([CH2:9][OH:10])[cH:11][cH:12]1
COC(=O)c1ccc(C=C(C)C)cc1
CC(C)=Cc1ccc(CO)cc1
null
null
C(C)OCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
96.6
[{"value": 96.6, "product": "CC(=CC1=CC=C(CO)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
30
MINUTE
To a suspension of isopropyltriphenylphosphonium iodide (9.5 g) in tetrahydrofuran (90 mL) was added n-butyllithium (1.5 mol/L hexane solution, 15 mL) at 0° C., and the mixture was stirred for 15 minutes. To the reaction mixture was added a solution of methyl terephthalaldehydate (3.3 g) in tetrahydrofuran (10 mL), and...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1
Other
C(C)OCC
0
0.5
COC(=O)c1ccc(C=C(C)C)cc1>C(C)OCC>CC(C)=Cc1ccc(CO)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c7e2282149994952b0a66f32c7b5a32d
BrC(Br)(Br)Br.CC(C)=Cc1ccc(CO)cc1>>CC(C)=Cc1ccc(CBr)cc1
O.CC(=CC1=CC=C(CO)C=C1)C.C(Br)(Br)(Br)Br.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>CC(=CC1=CC=C(CBr)C=C1)C
BrC(Br)(Br)[Br:10].O[CH2:9][c:8]1[cH:7][cH:6][c:5]([CH:4]=[C:2]([CH3:1])[CH3:3])[cH:12][cH:11]1>>[CH3:1][C:2]([CH3:3])=[CH:4][c:5]1[cH:6][cH:7][c:8]([CH2:9][Br:10])[cH:11][cH:12]1
BrC(Br)(Br)Br.CC(C)=Cc1ccc(CO)cc1
CC(C)=Cc1ccc(CBr)cc1
null
null
ClCCl
Functional Group Interconversion
Appel reaction
752e1807cd47d8316010cc3f92eab16c5a89ffb844d9514fcae469ba993c78dd
2c6b51fb1e17cb2c93d565e0423c75825df2c8e11c870e0c98b278f20ba9f3ad
c1ccccc1
Br-C(-Br)(-Br)-[Br;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
3.5
HOUR
To a solution of 4-(2-methylprop-1-en-1-yl)benzyl alcohol (0.60 g) and carbon tetrabromide (1.2 g) in dichloromethane (12 mL) was added triphenylphosphine (0.97 g) at 0° C., and the mixture was stirred at room temperature for 3.5 hours. To the reaction mixture was added water, and the mixture was extracted with hexane....
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Tertiary halide.Primary alcohol
Primary halide
null
null
c1ccccc1
HBr
ClCCl
null
3.5
BrC(Br)(Br)Br.CC(C)=Cc1ccc(CO)cc1>ClCCl>CC(C)=Cc1ccc(CBr)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-d817accfc9194d7d8c056a712cc00b72
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(Br)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.OB(O)c1ccc(F)cc1>>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(F)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
BrC1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.FC1=CC=C(C=C1)B(O)O.[F-].[Cs+]>>FC1=CC=C(C=C1)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
Br[c:20]1[cH:19][cH:18][c:17]([CH2:16][c:15]2[c:10]([O:9][C@@H:8]3[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:40]([O:41][C:42]([CH3:43])=[O:44])[C@H:35]([O:36][C:37]([CH3:38])=[O:39])[C@H:30]3[O:31][C:32]([CH3:33])=[O:34])[n:11][nH:12][c:13]2[CH3:14])[cH:29][cH:28]1.OB(O)[c:21]1[cH:22][cH:23][c:24]([F:25])[cH:2...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(Br)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.OB(O)c1ccc(F)cc1
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(F)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
null
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1
O.COCCOC.C(C)O
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccc(Cc3c[nH]nc3O[C@H]3CCCCO3)cc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-B(-O)-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:6](:[c:7]:[c:8]):[c:9]:[c:10]):[c:4]:[c:5]
60.1
[{"value": 60.1, "product": "FC1=CC=C(C=C1)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
85
CELSIUS
18
HOUR
A mixture of 4-[(4-bromophenyl)methyl]-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.099 g), 4-fluorophenylboronic acid (0.046 g), cesium fluoride (0.050 g) and tetrakis(triphenylphosphine)palladium(0) (0.0038 g) in 1,2-dimethoxyethane (1.3 mL), ethanol (0.3 mL) and water (0.3 mL) was stirred...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
C1CCOCC1.c1cn[nH]c1.c1ccccc1.c1ccccc1
HBr.B
C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.COCCOC.C(C)O
85
18
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(Br)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.OB(O)c1ccc(F)cc1>C=1C=CC(=CC1)[P](C=2C=CC=CC2)(C=3C=CC=CC3)[Pd]([P](C=4C=CC=CC4)(C=5C=CC=CC5)C=6C=CC=CC6)([P](C=7C=CC=CC7)(C=8C=CC=CC8)C=9C=CC=CC9)[P](C=1C=CC=CC1)(C=1C=CC=CC1)C=1C=CC=CC1.O.COCCOC.C(C)O>CC(=O)OC[C@H]1O[C@@H](O...
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-97bf7a716be548b498b33e3b8c7e9ac9
BrC1CCC1.O=Cc1ccc(O)cc1>>O=Cc1ccc(OC2CCC2)cc1
[OH-].[Na+].OC1=CC=C(C=O)C=C1.C([O-])([O-])=O.[Cs+].[Cs+].C1(CCC1)Br>>C1(CCC1)OC1=CC=C(C=O)C=C1
Br[CH:8]1[CH2:9][CH2:10][CH2:11]1.[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([OH:7])[cH:12][cH:13]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]2[CH2:9][CH2:10][CH2:11]2)[cH:12][cH:13]1
BrC1CCC1.O=Cc1ccc(O)cc1
O=Cc1ccc(OC2CCC2)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
6d96532a86b84488fc6bd0e5287d56cd1fadd66f51758349138c69702e9daf1b
cf768afb66ed5041aefdce1fa6d1e40995a1ab7c4b4a4ca47544fe49ee1e629f
c1ccc(OC2CCC2)cc1
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-1.[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[c:7]:[c:6](-[O;H0;D2;+0:5]-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-1):[c:8]
75.1
[{"value": 75.1, "product": "C1(CCC1)OC1=CC=C(C=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
8
HOUR
To a suspension of 4-hydroxybenzaldehyde (0.12 g) and cesium carbonate (0.49 g) in N,N-dimethylformamide (2 mL) was added cyclobutyl bromide (0.15 g), and the mixture was stirred at 65° C. overnight. To the reaction mixture was added 1 mol/L aqueous sodium hydroxide solution, and the mixture was extracted with diethyl ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol
Ether
C1CCC1
C1CCC1
c1ccccc1.C1CCC1
HBr
CN(C=O)C
65
8
BrC1CCC1.O=Cc1ccc(O)cc1>CN(C=O)C>O=Cc1ccc(OC2CCC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-5f4ff8e070b54cb8ac8ee5860bef04f3
O=Cc1ccc(OC2CCC2)cc1>>OCc1ccc(OC2CCC2)cc1
Cl.C1(CCC1)OC1=CC=C(C=O)C=C1.[BH4-].[Na+]>>C1(CCC1)OC1=CC=C(CO)C=C1
[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]2[CH2:9][CH2:10][CH2:11]2)[cH:12][cH:13]1>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([O:7][CH:8]2[CH2:9][CH2:10][CH2:11]2)[cH:12][cH:13]1
O=Cc1ccc(OC2CCC2)cc1
OCc1ccc(OC2CCC2)cc1
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccc(OC2CCC2)cc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
91.3
[{"value": 91.3, "product": "C1(CCC1)OC1=CC=C(CO)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a suspension of 4-hydroxybenzaldehyde (0.12 g) and cesium carbonate (0.49 g) in N,N-dimethylformamide (2 mL) was added cyclobutyl bromide (0.15 g), and the mixture was stirred at 65° C. overnight. To the reaction mixture was added 1 mol/L aqueous sodium hydroxide solution, and the mixture was extracted with diethyl ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1.C1CCC1
null
CO
null
8
O=Cc1ccc(OC2CCC2)cc1>CO>OCc1ccc(OC2CCC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e4b9bbe846834bb582b1056ba6ea5d4b
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(OCc4ccccc4)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(O)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
C(C1=CC=CC=C1)OC1=CC=C(C=C1)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O>>OC1=CC=C(C=C1)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
c1ccc(C[O:25][c:24]2[cH:23][cH:22][c:21](-[c:20]3[cH:19][cH:18][c:17]([CH2:16][c:15]4[c:10]([O:9][C@@H:8]5[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:40]([O:41][C:42]([CH3:43])=[O:44])[C@H:35]([O:36][C:37]([CH3:38])=[O:39])[C@H:30]5[O:31][C:32]([CH3:33])=[O:34])[n:11][nH:12][c:13]4[CH3:14])[cH:29][cH:28]3)[cH:2...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(OCc4ccccc4)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(O)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
null
[C].[Pd]
CO
Deprotection
Hydroxyl benzyl deprotection
36869d1fe85185a14d9eb30bf05178c600a9b6eca277ffaf3803578c30e0bf5d
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc(-c2ccc(Cc3c[nH]nc3O[C@H]3CCCCO3)cc2)cc1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C-c1:c:c:c:c:c:1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
58.2
[{"value": 58.2, "product": "OC1=CC=C(C=C1)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
11
HOUR
To a solution of 4-({4-[4-(benzyloxy)phenyl]phenyl}methyl)-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.14 g) in methanol (3 mL) was added 10% palladium-carbon powder (0.030 g), and the mixture was stirred at room temperature under a hydrogen atmosphere for 11 hours. Insoluble materials were...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
c1ccccc1
null
C1CCOCC1.c1cn[nH]c1.c1ccccc1.c1ccccc1
Other
[C].[Pd].CO
null
11
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(OCc4ccccc4)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>[C].[Pd].CO>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(-c3ccc(O)cc3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-6744837d271542169edc181f1b3dfcd3
Cc1ccc(-c2ccccn2)cc1.O=C1CCC(=O)N1Cl>>ClCc1ccc(-c2ccccn2)cc1
C1(=CC=C(C=C1)C1=NC=CC=C1)C.ClN1C(CCC1=O)=O>>N1=C(C=CC=C1)C1=CC=C(CCl)C=C1
[CH3:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][n:12]2)[cH:13][cH:14]1.O=C1CCC(=O)N1[Cl:1]>>[Cl:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][cH:11][n:12]2)[cH:13][cH:14]1
Cc1ccc(-c2ccccn2)cc1.O=C1CCC(=O)N1Cl
ClCc1ccc(-c2ccccn2)cc1
null
CC(C)(C#N)N=NC(C)(C)C#N
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Chlorination
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccc(-c2ccccn2)cc1
O=C1-C-C-C(=O)-N-1-[Cl;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
53.8
[{"value": 53.8, "product": "N1=C(C=CC=C1)C1=CC=C(CCl)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2-(p-tolyl)pyridine (1.7 g) and N-chlorosuccinimide (1.5 g) in carbon tetrachloride (30 mL) was added α,α-azobisisobutyronitrile (0.033 g), and the mixture was heated under reflux for 5 hours. Insoluble materials were removed by filtration, and the filtrate was concentrated under reduced pressure. The ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1.c1ccncc1
HO-
CC(C)(C#N)N=NC(C)(C)C#N.C(Cl)(Cl)(Cl)Cl
null
null
Cc1ccc(-c2ccccn2)cc1.O=C1CCC(=O)N1Cl>CC(C)(C#N)N=NC(C)(C)C#N.C(Cl)(Cl)(Cl)Cl>ClCc1ccc(-c2ccccn2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-20c040d52e9041069b9315065b0b9dc3
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C=C2CC2)cc1
CC1=C(C(=NN1)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)CC1=CC=C(C=C1)C=C1CC1.C[O-].[Na+]>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C=C1CC1)C
CC(=O)[O:11][CH2:10][C@H:9]1[O:8][C@@H:7]([O:6][c:5]2[n:4][nH:3][c:2]([CH3:1])[c:18]2[CH2:19][c:20]2[cH:21][cH:22][c:23]([CH:24]=[C:25]3[CH2:26][CH2:27]3)[cH:28][cH:29]2)[C@H:16]([O:17]C(C)=O)[C@@H:14]([O:15]C(C)=O)[C@@H:12]1[O:13]C(C)=O>>[CH3:1][c:2]1[nH:3][n:4][c:5]([O:6][C@@H:7]2[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C=C2CC2)cc1
null
null
CO
Reduction
OtherReaction
f25a9a23a5ab89548ff4c6a5183e7d00920a9005d871a82164b8da27dcb3ee4f
613f6029949a010495656f96609cb4885878fc82e324c8aa3a03bf565e6d5cf2
C(=C1CC1)c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C(-C)=O)-[C:8](-[O;H0;D2;+0:9]-C(-C)=O)-[C:10]-1-[O;H0;D2;+0:11]-C(-C)=O>>[OH;D1;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[OH;D1;+0:7])-[C:8](-[OH;D1;+0:9])-[C:10]-1-[OH;D1;+0:11]
99.2
[{"value": 99.2, "product": "[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C=C1CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A solution of 5-methyl-4-{[4-(cyclopropylidenemethyl)phenyl]methyl}-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.010 g) in methanol (2 mL) was added sodium methoxide (28% methanol solution, 0.0020 mL), and the mixture was stirred at room temperature for 30 minutes. The reaction mixture was concentrat...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
c1cn[nH]c1.C1CCOCC1.c1ccccc1.C1CC1
HO-
CO
null
0.5
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C=C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>CO>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C=C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-712420777a354dadae1bb00c8c7fe75a
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1
CC1=C(C(=NN1)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)CC1=CC=C(C=C1)C1CC1.[OH-].[Na+]>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C1CC1)C
CC(=O)[O:11][CH2:10][C@H:9]1[O:8][C@@H:7]([O:6][c:5]2[n:4][nH:3][c:2]([CH3:1])[c:18]2[CH2:19][c:20]2[cH:21][cH:22][c:23]([CH:24]3[CH2:25][CH2:26]3)[cH:27][cH:28]2)[C@H:16]([O:17]C(C)=O)[C@@H:14]([O:15]C(C)=O)[C@@H:12]1[O:13]C(C)=O>>[CH3:1][c:2]1[nH:3][n:4][c:5]([O:6][C@@H:7]2[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:1...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1
null
null
C(C)O
Reduction
OtherReaction
f25a9a23a5ab89548ff4c6a5183e7d00920a9005d871a82164b8da27dcb3ee4f
613f6029949a010495656f96609cb4885878fc82e324c8aa3a03bf565e6d5cf2
c1cc(C2CC2)ccc1Cc1c[nH]nc1O[C@H]1CCCCO1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C(-C)=O)-[C:8](-[O;H0;D2;+0:9]-C(-C)=O)-[C:10]-1-[O;H0;D2;+0:11]-C(-C)=O>>[OH;D1;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[OH;D1;+0:7])-[C:8](-[OH;D1;+0:9])-[C:10]-1-[OH;D1;+0:11]
88.9
[{"value": 88.9, "product": "[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C1CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 5-methyl-4-[(4-cyclopropylphenyl)methyl]-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.14 g) in ethanol (8.4 mL) was added 2 mol/L aqueous sodium hydroxide solution (0.63 mL), and the mixture was stirred at room temperature for 30 minutes. The solvent was removed under reduced pressur...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
c1cn[nH]c1.C1CCOCC1.c1ccccc1.C1CC1
HO-
C(C)O
null
0.5
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(C3CC3)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>C(C)O>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-f73b9914b2544aef8093298d9c350683
CC(C)I.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1>>Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C(C)C
O.[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C1CC1)C.C([O-])([O-])=O.[Cs+].[Cs+].IC(C)C>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NN(C(=C1CC1=CC=C(C=C1)C1CC1)C)C(C)C
I[CH:29]([CH3:30])[CH3:31].[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([CH:9]3[CH2:10][CH2:11]3)[cH:12][cH:13]2)[c:14]([O:15][C@@H:16]2[O:17][C@H:18]([CH2:19][OH:20])[C@@H:21]([OH:22])[C@H:23]([OH:24])[C@H:25]2[OH:26])[n:27][nH:28]1>>[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([CH:9]3[CH2:10][CH2:11]3)[cH:1...
CC(C)I.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1
Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C(C)C
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
16e7264339c5da2b038fe36dfca9cfcc21c80f0292d644875f157fe8da0791e0
3456c966f3f7e7d410f206842ab08ae4d1cfab4368ca2a0de7a6ad251462e6f4
c1cc(C2CC2)ccc1Cc1c[nH]nc1O[C@H]1CCCCO1
I-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3].[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[nH;D2;+0:9]:1>>[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[n;H0;D3;+0:9]:1-[CH;D3;+0:1](-[C;D1;H3:2])-[C;D1;H3:3]
null
[]
null
null
35
MINUTE
To a suspension of 3-(β-D-glucopyranosyloxy)-5-methyl-4-[(4-cyclopropylphenyl)methyl]-1H-pyrazole (56 mg) and cesium carbonate (23 mg) in N,N-dimethylformamide (1.5 mL) was added 2-iodopropane (0.043 mL) at 80° C., and the mixture was stirred for 35 minutes. To the reaction mixture was added water, and the mixture was ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1ccccc1.C1CC1.C1CCOCC1
HI
CN(C=O)C
null
0.583333
CC(C)I.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1>CN(C=O)C>Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-26f326e36a904d5e9f2369e5f379ac90
Cc1[nH][nH]c(=O)c1Cc1ccc(-c2ccccn2)cc1>>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(-c2ccccn2)cc1
CC1=C(C(NN1)=O)CC1=CC=C(C=C1)C1=NC=CC=C1.CC1=C(C(=NN1)O[C@H]1[C@](O)([C@@](O)([C@](O)([C@H](O1)C(O)C(C)=O)C(C)=O)C(C)=O)C(C)=O)CC1=CC=C(C=C1)C1=NC=CC=C1>>CC1=C(C(=NN1)O[C@H]1[C@](O)([C@@](O)([C@](O)([C@H](O1)C(O)C(C)=O)C(C)=O)C(C)=O)C(C)=O)CC1=CC=C(C=C1)C1=NC=CC=C1.[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=...
[CH3:44][c:45]1[nH:46][nH:47][c:48](=[O:49])[c:61]1[CH2:62][c:63]1[cH:64][cH:65][c:66](-[c:67]2[cH:68][cH:69][cH:70][cH:71][n:72]2)[cH:73][cH:74]1>>[CH3:44][c:45]1[nH:46][n:47][c:48]([O:49][C@@H:50]2[O:51][C@H:52]([CH2:53][OH:54])[C@@H:55]([OH:56])[C@H:57]([OH:58])[C@H:59]2[OH:60])[c:61]1[CH2:62][c:63]1[cH:64][cH:65][c...
Cc1[nH][nH]c(=O)c1Cc1ccc(-c2ccccn2)cc1
Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(-c2ccccn2)cc1
null
null
null
Functional Group Interconversion
OtherReaction
ead1fc6f6adf9c6d299f2cfdd5a28b72dce9daf92747912a06341759e2e7b8cd
6f24b6011ab4070dd247a50f72b747bca7d9d29ae512b8f5758535ae9ced16bd
c1ccc(-c2ccc(Cc3c[nH]nc3O[C@H]3CCCCO3)cc2)nc1
[C:1]-[c:2]1:[c:3](-[C;D1;H3:4]):[#7;a:5]:[nH;D2;+0:6]:[c;H0;D3;+0:7]:1=[O;H0;D1;+0:8]>>[#8:9]-[C:10](-[O;H0;D2;+0:8]-[c;H0;D3;+0:7]1:[n;H0;D2;+0:6]:[#7;a:5]:[c:3](-[C;D1;H3:4]):[c:2]:1-[C:1])-[C:11]
null
[]
null
null
null
null
5-Methyl-4-{[4-(pyridin-2-yl)phenyl]methyl}-3-(2,3,4,6-tetraacetyl-β-D-glucopyranosyloxy)-1H-pyrazole was prepared in a similar manner to that described in Example 4 using 5-methyl-4-{[4-(pyridin-2-yl)phenyl]methyl}-1,2-dihydro-3H-pyrazol-3-one instead of 5-methyl-4-[(4-cyclopropylphenyl)methyl]-1,2-dihydro-3H-pyrazol-...
10.6084/m9.figshare.5104873.v1
null
null
Ether.Ether.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
c1cn[nH]c1
c1cn[nH]c1.C1CCOCC1
c1cn[nH]c1.C1CCOCC1.c1ccccc1.c1ccncc1
Other
null
null
null
Cc1[nH][nH]c(=O)c1Cc1ccc(-c2ccccn2)cc1>>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(-c2ccccn2)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e1891c54274e463798b044aadeb68576
CC(=O)OCCBr.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1>>Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CCO
[OH-].[Na+].[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)C1CC1)C.C([O-])([O-])=O.[Cs+].[Cs+].C(C)(=O)OCCBr>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NN(C(=C1CC1=CC=C(C=C1)C1CC1)C)CCO
CC(=O)[O:31][CH2:30][CH2:29]Br.[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([CH:9]3[CH2:10][CH2:11]3)[cH:12][cH:13]2)[c:14]([O:15][C@@H:16]2[O:17][C@H:18]([CH2:19][OH:20])[C@@H:21]([OH:22])[C@H:23]([OH:24])[C@H:25]2[OH:26])[n:27][nH:28]1>>[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([CH:9]3[CH2:10][CH2:11]3)[...
CC(=O)OCCBr.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1
Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CCO
null
null
CO.O.CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
d852c722c2aca2b7d389659753689a45a4758ac8a419d359b535bfc85cb51b90
54abde2d478ff296b6bbfd081f08f62192a65526240f7099e8b16537b3165ae6
c1cc(C2CC2)ccc1Cc1c[nH]nc1O[C@H]1CCCCO1
Br-[CH2;D2;+0:1]-[C:2]-[O;H0;D2;+0:3]-C(-C)=O.[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[nH;D2;+0:9]:1>>[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[n;H0;D3;+0:9]:1-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3]
null
[]
null
null
2
HOUR
To a suspension of 3-(β-D-glucopyranosyloxy)-5-methyl-4-[(4-cyclopropylphenyl)methyl]-1H-pyrazole (33 mg) and cesium carbonate (138 mg) in N,N-dimethylformamide (1 mL) was added 2-bromoethyl acetate (0.035 mL) at 40° C., and the mixture was stirred for 2 hours. To the reaction mixture was added water, and the mixture w...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Primary alcohol
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1ccccc1.C1CC1.C1CCOCC1
HBr
CO.O.CN(C=O)C
null
2
CC(=O)OCCBr.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(C2CC2)cc1>CO.O.CN(C=O)C>Cc1c(Cc2ccc(C3CC3)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CCO
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-109fe8804b6a4af0845004d8cdb6b4e7
BrCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>>CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1
[OH-].[Na+].C(C)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.C([O-])([O-])=O.[Cs+].[Cs+].C(C1=CC=CC=C1)OCCBr>>C(C1=CC=CC=C1)OCCN1N=C(C(=C1C)CC1=CC=C(C=C1)CC)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
Br[CH2:24][CH2:25][O:26][CH2:27][c:28]1[cH:29][cH:30][cH:31][cH:32][cH:33]1.CC(=O)[O:15][CH2:14][C@H:13]1[O:12][C@@H:11]([O:10][c:9]2[c:8]([CH2:7][c:6]3[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:37][cH:36]3)[c:34]([CH3:35])[nH:23][n:22]2)[C@H:20]([O:21]C(C)=O)[C@@H:18]([O:19]C(C)=O)[C@@H:16]1[O:17]C(C)=O>>[CH3:1][CH2:2][c:3]...
BrCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1
CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1
null
null
CO.O.C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
6ee0687f8babb1e9e5cf5916e44ac5b5c459bb6a896b3332ada71047bcded01e
d801f850e0a060636a41be97e2f9380e4486de67ba2f3b00fe109c16997b93ef
c1ccc(COCCn2cc(Cc3ccccc3)c(O[C@H]3CCCCO3)n2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[#8:3].C-C(=O)-[O;H0;D2;+0:4]-[C:5]-[C:6]1-[#8:7]-[C:8]-[C:9](-[O;H0;D2;+0:10]-C(-C)=O)-[C:11](-[O;H0;D2;+0:12]-C(-C)=O)-[C:13]-1-[O;H0;D2;+0:14]-C(-C)=O.[C;D1;H3:15]-[c:16]1:[c:17]:[c:18]:[#7;a:19]:[nH;D2;+0:20]:1>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:20]1:[#7;a:19]:[c:18]:[c:17]:[c:16]:1-[C;D...
null
[]
80
CELSIUS
30
MINUTE
To a suspension of 4-[(4-ethylphenyl)methyl]-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.030 g) and cesium carbonate (0.091 g) in acetonitrile (0.4 mL) was added benzyl(2-bromoethyl)ether (0.035 mL), and the mixture was stirred at 80° C. for 30 minutes. After cooling to room temperature, th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
c1cn[nH]c1
c1cn[nH]c1
c1ccccc1.C1CCOCC1.c1cn[nH]c1.c1ccccc1
HBr
CO.O.C(C)#N
80
0.5
BrCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>CO.O.C(C)#N>CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8b516180d4e44f6ab2a17607b71443c4
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2sccc2C)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1
CC1=C(C(=NN1)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O)CC=1SC=CC1C.C[O-].[Na+].C(C)O>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)SC)C
CC(=O)[O:15][CH2:14][C@H:13]1[O:12][C@@H:11]([O:10][c:9]2[c:8]([CH2:7][c:6]3[s:2][cH:3][cH:4][c:5]3[CH3:26])[c:24]([CH3:25])[nH:23][n:22]2)[C@H:20]([O:21]C(C)=O)[C@@H:18]([O:19]C(C)=O)[C@@H:16]1[O:17]C(C)=O>>[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c:9]([O:10][C@@H:11]3[O:12][C@H:13]([CH2:14][OH:15])[C@@H:16](...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2sccc2C)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1
null
null
null
Miscellaneous
OtherReaction
0cdfed43039c68caaeff6b35e038f2ba97c89e0158bda5e1b4b95f9551247d29
1c2f9a866c22d324ca04dd42d041706cd3480ef8d7d753c19b41d48590c4c482
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C(-C)=O)-[C:8](-[O;H0;D2;+0:9]-C(-C)=O)-[C:10]-1-[O;H0;D2;+0:11]-C(-C)=O.[CH3;D1;+0:12]-[c;H0;D3;+0:13]1:[c:14]:[cH;D2;+0:15]:[s;H0;D2;+0:16]:[c;H0;D3;+0:17]:1-[C:18]-[c:19]1:[c:20]:[#7;a:21]:[#7;a:22]:[c:23]:1>>[C;D1;H3:24]-[S;H0;D2;+0:16]-[c;H0;D3...
null
[]
null
null
1
HOUR
To a solution of 5-methyl-4-[(methylthiophenyl)methyl]-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.42 g) in ethanol (5 mL) was added sodium methoxide (28% methanol solution, 0.042 mL), and the mixture was stirred at room temperature for 1 hour. The reaction mixture was concentrated under reduced pre...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Monosulfide
c1ccsc1
c1ccccc1
c1ccccc1.C1CCOCC1.c1cn[nH]c1
HO-
null
null
1
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2sccc2C)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-565d90381b814599892f25d706657501
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(OC(C)C)cc1>>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
C(C)(C)OC1=CC=C(C=C1)CC=1C(NNC1C)=O.CC(=O)OC[C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)Br)OC(=O)C)OC(=O)C)OC(=O)C>>C(C)(C)OC1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O
Br[C@H:8]1[O:7][C@H:6]([CH2:5][O:4][C:2]([CH3:1])=[O:3])[C@@H:37]([O:38][C:39]([CH3:40])=[O:41])[C@H:32]([O:33][C:34]([CH3:35])=[O:36])[C@H:27]1[O:28][C:29]([CH3:30])=[O:31].[O:9]=[c:10]1[nH:11][nH:12][c:13]([CH3:14])[c:15]1[CH2:16][c:17]1[cH:18][cH:19][c:20]([O:21][CH:22]([CH3:23])[CH3:24])[cH:25][cH:26]1>>[CH3:1][C:2...
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(OC(C)C)cc1
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
null
C([O-])([O-])=O.[Ag+2]
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
49b04419fad6ce95036469eff0b0bfaaabc2fb3bd31dcfbbcd47a76a3bff025b
5cef8b32be1a1b6849554821131ec7ae3bfda59406cde9d9abe4b3a7d689dd3d
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
Br-[C@@H;D3;+0:1](-[#8:2]-[C:3])-[C:4](-[#8:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8])-[C:9].[C:10]-[c:11]1:[c:12](-[C;D1;H3:13]):[#7;a:14]:[nH;D2;+0:15]:[c;H0;D3;+0:16]:1=[O;H0;D1;+0:17]>>[C:10]-[c:11]1:[c:12](-[C;D1;H3:13]):[#7;a:14]:[n;H0;D2;+0:15]:[c;H0;D3;+0:16]:1-[O;H0;D2;+0:17]-[C@H;D3;+0:1](-[#8:2]-[C:3])-[C:4](-[#8:5...
39
[{"value": 39.0, "product": "C(C)(C)OC1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
8
HOUR
To a suspension of 4-[(4-isopropoxyphenyl)methyl]-5-methyl-1,2-dihydro-3H-pyrazol-3-one (46 mg), acetobromo-α-D-glucose (99 mg) and 4A molecular sieves in tetrahydrofuran (3 mL) was added silver carbonate (66 mg), and the mixture was stirred at 65° C. overnight under light shielding. The reaction mixture was purified b...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ether
Ether.Ether
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1
C1CCOCC1.c1cn[nH]c1.c1ccccc1
HBr
C([O-])([O-])=O.[Ag+2].O1CCCC1
65
8
CC(=O)OC[C@H]1O[C@H](Br)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O.Cc1[nH][nH]c(=O)c1Cc1ccc(OC(C)C)cc1>C([O-])([O-])=O.[Ag+2].O1CCCC1>CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-65c85569dca248bba77632215a4e4b48
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1
C(C)(C)OC1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.[OH-].[Na+]>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)OC(C)C)C
CC(=O)[O:11][CH2:10][C@H:9]1[O:8][C@@H:7]([O:6][c:5]2[n:4][nH:3][c:2]([CH3:1])[c:18]2[CH2:19][c:20]2[cH:21][cH:22][c:23]([O:24][CH:25]([CH3:26])[CH3:27])[cH:28][cH:29]2)[C@H:16]([O:17]C(C)=O)[C@@H:14]([O:15]C(C)=O)[C@@H:12]1[O:13]C(C)=O>>[CH3:1][c:2]1[nH:3][n:4][c:5]([O:6][C@@H:7]2[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]...
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O
Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1
null
null
C(C)O
Reduction
OtherReaction
f25a9a23a5ab89548ff4c6a5183e7d00920a9005d871a82164b8da27dcb3ee4f
613f6029949a010495656f96609cb4885878fc82e324c8aa3a03bf565e6d5cf2
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C(-C)=O)-[C:8](-[O;H0;D2;+0:9]-C(-C)=O)-[C:10]-1-[O;H0;D2;+0:11]-C(-C)=O>>[OH;D1;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[OH;D1;+0:7])-[C:8](-[OH;D1;+0:9])-[C:10]-1-[OH;D1;+0:11]
90.3
[{"value": 90.3, "product": "[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)OC(C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 4-[(4-isopropoxyphenyl)methyl]-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (61 mg) in ethanol (3 mL) was added 1 mol/L aqueous sodium hydroxide solution (0.53 mL), and the mixture was stirred at room temperature for 2 hours. The solvent was removed under reduced pressure, and ...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ester.Ester
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
c1cn[nH]c1.C1CCOCC1.c1ccccc1
HO-
C(C)O
null
2
CC(=O)OC[C@H]1O[C@@H](Oc2n[nH]c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@@H]1OC(C)=O>C(C)O>Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-061bca7ca0d24355a6d61c73b9464cfc
CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1>>Cc1ccnn1CCO
C(C1=CC=CC=C1)OCCN1N=C(C(=C1C)CC1=CC=C(C=C1)CC)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO>>OCCN1N=CC=C1C
CCc1ccc(C[c:3]2[c:2]([CH3:1])[n:6]([CH2:7][CH2:8][O:9]Cc3ccccc3)[n:5][c:4]2O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)cc1>>[CH3:1][c:2]1[cH:3][cH:4][n:5][n:6]1[CH2:7][CH2:8][OH:9]
CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1
Cc1ccnn1CCO
null
[C].[Pd]
C(C)O
Reduction
OtherReaction
360868ba954e0c04c8c98a7bc724315b8b64f892bc0d297f40f854fdbe539055
f2e1056b76894f3ffea8a99e38b24ab137cec9a13a66d2264741f4b40927f61c
c1cn[nH]c1
C-C-c1:c:c:c(-C-[c;H0;D3;+0:1]2:[c:2](-[C;D1;H3:3]):[#7;a:4](-[C:5]-[C:6]-[O;H0;D2;+0:7]-C-c3:c:c:c:c:c:3):[#7;a:8]:[c;H0;D3;+0:9]:2-O-[C@H]2-O-[C@H](-C-O)-[C@@H](-O)-[C@H](-O)-[C@@H]-2-O):c:c:1>>[C;D1;H3:3]-[c:2]1:[cH;D2;+0:1]:[cH;D2;+0:9]:[#7;a:8]:[#7;a:4]:1-[C:5]-[C:6]-[OH;D1;+0:7]
372.5
[{"value": 372.5, "product": "OCCN1N=CC=C1C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 1-(2-benzyloxyethyl)-4-[(4-ethylphenyl)methyl]-3-(β-D-glucopyranosyloxy)-5-methyl-1H-pyrazole (0.012 g) in ethanol (2 mL) was added a catalytic amount of 10% palladium-carbon powder, and the mixture was stirred at room temperature under a hydrogen atmosphere for 30 minutes. Insoluble materials were rem...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
Primary alcohol
c1ccccc1.c1cn[nH]c1.c1ccccc1.C1CCOCC1
c1cc[nH]n1
c1cc[nH]n1
HO-
[C].[Pd].C(C)O
null
0.5
CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCOCc3ccccc3)c2C)cc1>[C].[Pd].C(C)O>Cc1ccnn1CCO
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9a0224bc18ff4dde8591bc36f4b1149a
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1.OCCCBr>>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
O.[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)SC)C.C([O-])([O-])=O.[Cs+].[Cs+].BrCCCO>>[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NN(C(=C1CC1=CC=C(C=C1)SC)C)CCCO
[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c:9]([O:10][C@@H:11]3[O:12][C@H:13]([CH2:14][OH:15])[C@@H:16]([OH:17])[C@H:18]([OH:19])[C@H:20]3[OH:21])[n:22][nH:23][c:28]2[CH3:29])[cH:30][cH:31]1.Br[CH2:24][CH2:25][CH2:26][OH:27]>>[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c:9]([O:10][C@@H:11]3[O:12][C@H:13](...
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1.OCCCBr
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
31849359320dc3760d1a762ce95f120a544970fcb32b476aacf584ef81779a29
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[nH;D2;+0:9]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:9]1:[#7;a:8]:[c:7]:[c:6]:[c:5]:1-[C;D1;H3:4]
null
[]
40
CELSIUS
8
HOUR
To a suspension of 3-(β-D-glucopyranosyloxy)-5-methyl-4-[(4-methylthiophenyl)methyl]-1H-pyrazole (0.020 g) and cesium carbonate (0.11 g) in N,N-dimethylformamide (0.5 mL) was added 3-bromopropanol (0.022 mL), and the mixture was stirred at 40° C. overnight. To the reaction mixture was added water, and the mixture was p...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1ccccc1.C1CCOCC1.c1cn[nH]c1
HBr
CN(C=O)C
40
8
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1.OCCCBr>CN(C=O)C>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-aa90f8b214a24555af3b5a9a4cc0ed66
C=CCI.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>>C=CCn1nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c(Cc2ccc(CC)cc2)c1C
[OH-].[Na+].C(C)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.C([O-])([O-])=O.[Cs+].[Cs+].C(C=C)I>>C(C=C)N1N=C(C(=C1C)CC1=CC=C(C=C1)CC)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
I[CH2:3][CH:2]=[CH2:1].CC(=O)[O:12][CH2:11][C@H:10]1[O:9][C@@H:8]([O:7][c:6]2[n:5][nH:4][c:29]([CH3:30])[c:19]2[CH2:20][c:21]2[cH:22][cH:23][c:24]([CH2:25][CH3:26])[cH:27][cH:28]2)[C@H:17]([O:18]C(C)=O)[C@@H:15]([O:16]C(C)=O)[C@@H:13]1[O:14]C(C)=O>>[CH2:1]=[CH:2][CH2:3][n:4]1[n:5][c:6]([O:7][C@@H:8]2[O:9][C@H:10]([CH2:...
C=CCI.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1
C=CCn1nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c(Cc2ccc(CC)cc2)c1C
null
null
CO.O.C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
86f197887924543584440aec8dd5852a59f1ca6af42669d4366a4869dc0f7b92
f126eb1e2efac33fff492856e1c02e35fd2d9ad264b3d1e1e904df355a9609c4
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[C:3]1-[#8:4]-[C:5]-[C:6](-[O;H0;D2;+0:7]-C(-C)=O)-[C:8](-[O;H0;D2;+0:9]-C(-C)=O)-[C:10]-1-[O;H0;D2;+0:11]-C(-C)=O.[C;D1;H3:12]-[c:13]1:[c:14]:[c:15]:[#7;a:16]:[nH;D2;+0:17]:1.I-[CH2;D2;+0:18]-[C:19]=[C;D1;H2:20]>>[C;D1;H2:20]=[C:19]-[CH2;D2;+0:18]-[n;H0;D3;+0:17]1:[#7;a:16]:[c:15]:[c:14]:[...
null
[]
null
null
1
HOUR
To a suspension of 4-[(4-ethylphenyl)methyl]-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.030 g) and cesium carbonate (0.036 g) in acetonitrile (0.4 mL) was added allyl iodide (0.010 mL), and the mixture was stirred at room temperature for 1 hour. To the reaction mixture were added methanol ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester.Ester.Ester.Allyl
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Allyl
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.C1CCOCC1.c1ccccc1
HI
CO.O.C(C)#N
null
1
C=CCI.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>CO.O.C(C)#N>C=CCn1nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c(Cc2ccc(CC)cc2)c1C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-18c5dd7d2c2244d79595acf160ae3565
BrCC1CC1.CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1>>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CC3CC3)c2C)cc1
[I-].[Na+].[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)SC)C.C([O-])([O-])=O.[Cs+].[Cs+].BrCC1CC1>>C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)SC)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
Br[CH2:24][CH:25]1[CH2:26][CH2:27]1.[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c:9]([O:10][C@@H:11]3[O:12][C@H:13]([CH2:14][OH:15])[C@@H:16]([OH:17])[C@H:18]([OH:19])[C@H:20]3[OH:21])[n:22][nH:23][c:28]2[CH3:29])[cH:30][cH:31]1>>[CH3:1][S:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c:9]([O:10][C@@H:11]3[O:12][C@H:13...
BrCC1CC1.CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1
CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CC3CC3)c2C)cc1
null
null
O.CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
31849359320dc3760d1a762ce95f120a544970fcb32b476aacf584ef81779a29
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cc2cn(CC3CC3)nc2O[C@H]2CCCCO2)cc1
Br-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1.[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[nH;D2;+0:10]:1>>[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[n;H0;D3;+0:10]:1-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1
null
[]
null
null
null
null
To a solution of 3-(β-D-glucopyranosyloxy)-5-methyl-4-[(4-methylthiophenyl)methyl]-1H-pyrazole (0.081 g) in N,N-dimethylformamide (1 mL) were added cesium carbonate (0.40 g), bromomethylcyclopropane (0.099 mL) and a catalytic amount of sodium iodide, and the mixture was stirred at room temperature for 7 days. Water was...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1ccccc1.C1CCOCC1.c1cn[nH]c1.C1CC1
HBr
O.CN(C=O)C
null
null
BrCC1CC1.CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)n[nH]c2C)cc1>O.CN(C=O)C>CSc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CC3CC3)c2C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b269f573691d4ca6aca44037f3491647
BrCCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>>CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
[OH-].[Na+].C(C)C1=CC=C(C=C1)CC=1C(=NNC1C)O[C@H]1[C@H](OC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H](O1)COC(C)=O.C([O-])([O-])=O.[Cs+].[Cs+].C(C1=CC=CC=C1)OCCCBr>>C(C)C1=CC=C(C=C1)CC=1C(=NN(C1C)CCCO)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
Br[CH2:24][CH2:25][CH2:26][O:27]Cc1ccccc1.CC(=O)[O:15][CH2:14][C@H:13]1[O:12][C@@H:11]([O:10][c:9]2[c:8]([CH2:7][c:6]3[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:31][cH:30]3)[c:28]([CH3:29])[nH:23][n:22]2)[C@H:20]([O:21]C(C)=O)[C@@H:18]([O:19]C(C)=O)[C@@H:16]1[O:17]C(C)=O>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][c:8]2[c...
BrCCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1
CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
null
null
CO.O.C(C)#N
Heteroatom Alkylation and Arylation
OtherReaction
9ab42c90d847e96b9b80d52bf0ff6ac70490bebeda01adde8871f99f9e0d96de
e25864d4e27a8101363e96bf37d311b351fc70dd354922080edad2faae228b3e
c1ccc(Cc2c[nH]nc2O[C@H]2CCCCO2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1.C-C(=O)-[O;H0;D2;+0:5]-[C:6]-[C:7]1-[#8:8]-[C:9]-[C:10](-[O;H0;D2;+0:11]-C(-C)=O)-[C:12](-[O;H0;D2;+0:13]-C(-C)=O)-[C:14]-1-[O;H0;D2;+0:15]-C(-C)=O.[C;D1;H3:16]-[c:17]1:[c:18]:[c:19]:[#7;a:20]:[nH;D2;+0:21]:1>>[C;D1;H3:16]-[c:17]1:[c:18]:[c:19]:[#7;a:20]:[n;H...
null
[]
80
CELSIUS
30
MINUTE
To a suspension of 4-[(4-ethylphenyl)methyl]-5-methyl-3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-1H-pyrazole (0.030 g) and cesium carbonate (0.091 g) in acetonitrile (0.4 mL) was added benzyl(3-bromopropyl)ether (0.039 mL), and the mixture was stirred at 80° C. for 30 minutes. To the reaction mixture were added m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Ester.Ester.Ester.Ether
Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
c1ccccc1.c1cn[nH]c1
c1cn[nH]c1
c1ccccc1.C1CCOCC1.c1cn[nH]c1
HBr
CO.O.C(C)#N
80
0.5
BrCCCOCc1ccccc1.CCc1ccc(Cc2c(O[C@@H]3O[C@H](COC(C)=O)[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]3OC(C)=O)n[nH]c2C)cc1>CO.O.C(C)#N>CCc1ccc(Cc2c(O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)nn(CCCO)c2C)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0f63970ca7eb460d85e9a8fe0683d4ce
BrCC1CC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1>>Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1
O.[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)OC(C)C)C.[I-].[Na+].BrCC1CC1>>C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
Br[CH2:30][CH:31]1[CH2:32][CH2:33]1.[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([O:9][CH:10]([CH3:11])[CH3:12])[cH:13][cH:14]2)[c:15]([O:16][C@@H:17]2[O:18][C@H:19]([CH2:20][OH:21])[C@@H:22]([OH:23])[C@H:24]([OH:25])[C@H:26]2[OH:27])[n:28][nH:29]1>>[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([O:9][CH:10]([C...
BrCC1CC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1
Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
31849359320dc3760d1a762ce95f120a544970fcb32b476aacf584ef81779a29
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
c1ccc(Cc2cn(CC3CC3)nc2O[C@H]2CCCCO2)cc1
Br-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1.[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[nH;D2;+0:10]:1>>[C;D1;H3:5]-[c:6]1:[c:7]:[c:8]:[#7;a:9]:[n;H0;D3;+0:10]:1-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1
60
[{"value": 60.0, "product": "C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
DAY
To a suspension of 3-(β-D-glucopyranosyloxy)-4-[(4-isopropoxyphenyl)methyl]-5-methyl-1H-pyrazole (0.050 g) cesium carbonate (0.20 g) and a catalytic amount of sodium iodide in N,N-dimethylformamide (1 mL) was added bromomethylcyclopropane (0.050 g) at 50° C., and the mixture was stirred for 3 days. Water was added to t...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1ccccc1.C1CCOCC1.C1CC1
HBr
CN(C=O)C
null
72
BrCC1CC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1>CN(C=O)C>Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c3d1338347874e4b9770a415431dc81b
BrC1CCCC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1>>Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C1CCCC1
O.[C@@H]1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)OC1=NNC(=C1CC1=CC=C(C=C1)OC(C)C)C.C([O-])([O-])=O.[Cs+].[Cs+].C1(CCCC1)Br>>C1(CCCC1)N1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO
Br[CH:30]1[CH2:31][CH2:32][CH2:33][CH2:34]1.[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([O:9][CH:10]([CH3:11])[CH3:12])[cH:13][cH:14]2)[c:15]([O:16][C@@H:17]2[O:18][C@H:19]([CH2:20][OH:21])[C@@H:22]([OH:23])[C@H:24]([OH:25])[C@H:26]2[OH:27])[n:28][nH:29]1>>[CH3:1][c:2]1[c:3]([CH2:4][c:5]2[cH:6][cH:7][c:8]([O:9][C...
BrC1CCCC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1
Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C1CCCC1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
b6d603a26a93a1070dbd9cb4e26fba0f00d31dc341b43ea3961a58bc9ca18137
3456c966f3f7e7d410f206842ab08ae4d1cfab4368ca2a0de7a6ad251462e6f4
c1ccc(Cc2cn(C3CCCC3)nc2O[C@H]2CCCCO2)cc1
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1.[C;D1;H3:6]-[c:7]1:[c:8]:[c:9]:[#7;a:10]:[nH;D2;+0:11]:1>>[C;D1;H3:6]-[c:7]1:[c:8]:[c:9]:[#7;a:10]:[n;H0;D3;+0:11]:1-[CH;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1
58.3
[{"value": 58.3, "product": "C1(CCCC1)N1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a suspension of 3-(β-D-glucopyranosyloxy)-4-[(4-isopropoxyphenyl)methyl]-5-methyl-1H-pyrazole (0.050 g) and cesium carbonate (0.20 g) in N,N-dimethylformamide (1 mL) was added cyclopentyl bromide (0.055 g) at 80° C., and the mixture was stirred for 30 minutes. After cooling to room temperature, water was added to th...
10.6084/m9.figshare.5104873.v1
null
Secondary halide
null
C1CCCC1.c1cn[nH]c1
c1cn[nH]c1.C1CCCC1
c1cn[nH]c1.c1ccccc1.C1CCOCC1.C1CCCC1
HBr
CN(C=O)C
null
0.5
BrC1CCCC1.Cc1[nH]nc(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)c1Cc1ccc(OC(C)C)cc1>CN(C=O)C>Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1C1CCCC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2d65b92df53145f896e32cc79fe50f43
CCC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1>>CCC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
O.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.O.C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO.C(CC)(=O)Cl>>C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)COC(CC)=O
Cl[C:3]([CH2:2][CH3:1])=[O:4].[OH:5][CH2:6][C@H:7]1[O:8][C@@H:9]([O:10][c:11]2[n:12][n:13]([CH2:14][CH:15]3[CH2:16][CH2:17]3)[c:18]([CH3:19])[c:20]2[CH2:21][c:22]2[cH:23][cH:24][c:25]([O:26][CH:27]([CH3:28])[CH3:29])[cH:30][cH:31]2)[C@H:32]([OH:33])[C@@H:34]([OH:35])[C@@H:36]1[OH:37]>>[CH3:1][CH2:2][C:3](=[O:4])[O:5][C...
CCC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1
CCC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
null
null
CC1=NC(=CC(=C1)C)C
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
c1ccc(Cc2cn(CC3CC3)nc2O[C@H]2CCCCO2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C;D1;H3:4].[#8:5]-[C:6]-[C:7]-[OH;D1;+0:8]>>[#8:5]-[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C;D1;H3:4]
405.5
[{"value": 405.5, "product": "C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)COC(CC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 1-(cyclopropylmethyl)-3-(β-D-glucopyranosyloxy)-4-[(4-isopropoxyphenyl)methyl]-5-methyl-1H-pyrazole (0.40 g) in 2,4,6-trimethylpyridine (1.5 mL) was added propionyl chloride (0.0088 g) at 0° C., and the mixture was stirred for 3 hours. Citric acid monohydrate (3.3 g) and water were added to the reactio...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
C1CCOCC1.c1cn[nH]c1.C1CC1.c1ccccc1
HCl
CC1=NC(=CC(=C1)C)C
null
3
CCC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1>CC1=NC(=CC(=C1)C)C>CCC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a263acd080c74398b09f94a2fc949eda
CCOC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1>>CCOC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
O.C(CC(O)(C(=O)O)CC(=O)O)(=O)O.O.C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO.ClC(=O)OCC>>C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)COC(=O)OCC
Cl[C:4]([O:3][CH2:2][CH3:1])=[O:5].[OH:6][CH2:7][C@H:8]1[O:9][C@@H:10]([O:11][c:12]2[n:13][n:14]([CH2:15][CH:16]3[CH2:17][CH2:18]3)[c:19]([CH3:20])[c:21]2[CH2:22][c:23]2[cH:24][cH:25][c:26]([O:27][CH:28]([CH3:29])[CH3:30])[cH:31][cH:32]2)[C@H:33]([OH:34])[C@@H:35]([OH:36])[C@@H:37]1[OH:38]>>[CH3:1][CH2:2][O:3][C:4](=[O...
CCOC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1
CCOC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
null
null
CC1=NC(=CC(=C1)C)C
Acylation
Schotten-Baumann to ester
ab2604cac7a0887c37303ad0fec59fb6a84cf40820c840730a9f7f5636dcc83e
7ed0ec8c4c25c8af523f531911c9dd0a60119de4cab841f882ce9a65c39be54c
c1ccc(Cc2cn(CC3CC3)nc2O[C@H]2CCCCO2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6]-[C:7]-[OH;D1;+0:8]>>[#8:5]-[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4]
74.4
[{"value": 74.4, "product": "C1(CC1)CN1N=C(C(=C1C)CC1=CC=C(C=C1)OC(C)C)O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O1)COC(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a solution of 1-(cyclopropylmethyl)-3-(β-D-glucopyranosyloxy)-4-[(4-isopropoxyphenyl)methyl]-5-methyl-1H-pyrazole (0.050 g) in 2,4,6-trimethylpyridine (1 mL) was added ethyl chloroformate (0.035 g), and the mixture was stirred at room temperature overnight. Citric acid monohydrate (3.3 g) and water were added to the...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Primary alcohol
Carbonic Ester
null
null
C1CCOCC1.c1cn[nH]c1.C1CC1.c1ccccc1
HCl
CC1=NC(=CC(=C1)C)C
null
8
CCOC(=O)Cl.Cc1c(Cc2ccc(OC(C)C)cc2)c(O[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)nn1CC1CC1>CC1=NC(=CC(=C1)C)C>CCOC(=O)OC[C@H]1O[C@@H](Oc2nn(CC3CC3)c(C)c2Cc2ccc(OC(C)C)cc2)[C@H](O)[C@@H](O)[C@@H]1O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c7f6d570e3cd42f6a92e57cb911288ae
CC[C@@H](C(N)=O)N1CCC(COS(C)(=O)=O)CC1=O.[I-]>>CC[C@@H](C(N)=O)N1CCC(CI)CC1=O
[I-].[Na+].CS(=O)(=O)OCC1CC(N(CC1)[C@@H](CC)C(=O)N)=O.[I-].[Na+]>>ICC1CC(N(CC1)[C@H](C(=O)N)CC)=O
CS(=O)(=O)O[CH2:11][CH:10]1[CH2:9][CH2:8][N:7]([C@@H:3]([CH2:2][CH3:1])[C:4]([NH2:5])=[O:6])[C:14](=[O:15])[CH2:13]1.[I-:12]>>[CH3:1][CH2:2][C@@H:3]([C:4]([NH2:5])=[O:6])[N:7]1[CH2:8][CH2:9][CH:10]([CH2:11][I:12])[CH2:13][C:14]1=[O:15]
CC[C@@H](C(N)=O)N1CCC(COS(C)(=O)=O)CC1=O.[I-]
CC[C@@H](C(N)=O)N1CCC(CI)CC1=O
null
null
C1CCOC1
Functional Group Interconversion
OtherReaction
119410ad0456baafba3b2935b12d3e44977c506a6dd8cacdd3e4fe37abe9db9f
ddf832dd4937bef392b42ed4281006ae20524cc7fc61b350edeb12d7b5bf783f
O=C1CCCCN1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2](-[C:3])-[C:4]-[C:5](=[O;D1;H0:6])-[#7:7].[I-;H0;D0:8]>>[#7:7]-[C:5](=[O;D1;H0:6])-[C:4]-[C:2](-[CH2;D2;+0:1]-[I;H0;D1;+0:8])-[C:3]
65,636,364
[{"value": 66.0, "product": "ICC1CC(N(CC1)[C@H](C(=O)N)CC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65636364.0, "product": "ICC1CC(N(CC1)[C@H](C(=O)N)CC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
5
HOUR
In a 150 ml three necked flask fitted with magnetic stirrer and reflux condenser, under inert atmosphere, 6.88 g (23.5 nmoles) of {1-[(1S)-1-(aminocarbonyl)propyl]-6-oxo-3-piperidinyl}methyl methanesulfonate 24 were dissolved in 86 ml of THF. 3.9 g (25.9 mmoles, 1.1 eq) of sodium iodide were added in one portion and th...
10.6084/m9.figshare.5104873.v1
null
Mesylate
Primary halide
null
null
C1CC[NH]CC1
MsOH.HO-
C1CCOC1
0
5
CC[C@@H](C(N)=O)N1CCC(COS(C)(=O)=O)CC1=O.[I-]>C1CCOC1>CC[C@@H](C(N)=O)N1CCC(CI)CC1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1eef3dbcfb0c48a58fb44f859aa4293d
CCOC(=O)C(Br)CC.O=C1CCC(c2ccccc2)CN1>>CCOC(=O)C(CC)N1CC(c2ccccc2)CCC1=O
BrC(C(=O)OCC)CC.CC(C)([O-])C.[K+].C(C)(=O)OCC.C1(=CC=CC=C1)C1CCC(NC1)=O>>O=C1N(CC(CC1)C1=CC=CC=C1)C(C(=O)OCC)CC
Br[CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:7][CH3:8].[NH:9]1[CH2:10][CH:11]([c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19][C:20]1=[O:21]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]([CH2:7][CH3:8])[N:9]1[CH2:10][CH:11]([c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[CH2:18][CH2:19][C:20]1=[O:21]
CCOC(=O)C(Br)CC.O=C1CCC(c2ccccc2)CN1
CCOC(=O)C(CC)N1CC(c2ccccc2)CCC1=O
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
bd0f600bacc94ea43dea015f98985d948c00d421c78f487c2d3e740688f9c6bb
29b3e231b1d2708086b87ea5e8bddd4b64f3d7251e67b4cc4f6db43e63a60af6
O=C1CCC(c2ccccc2)CN1
Br-[CH;D3;+0:1](-[C:2]-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7].[C:8]-[C:9]-[NH;D2;+0:10]-[C:11](=[O;D1;H0:12])-[C:13]>>[C:8]-[C:9]-[N;H0;D3;+0:10](-[CH;D3;+0:1](-[C:2]-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7])-[C:11](=[O;D1;H0:12])-[C:13]
70.4
[{"value": 70.4, "product": "O=C1N(CC(CC1)C1=CC=CC=C1)C(C(=O)OCC)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 19.1, "product": "O=C1N(CC(CC1)C1=CC=CC=C1)C(C(=O)OCC)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
30
MINUTE
In a 1 l three necked flask fitted with reflux condenser, magnetic stirrer and dropping funnel under inert atmosphere, 9.8 g (87 mmoles) of potassium t-butoxide were suspended in 600 ml of dry toluene. 11.8 g (67 mmoles) of 5-phenyl-2-piperidinone 25 were added, and the mixture stirred for 30 min. 17 g (87 mmoles) of e...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CCNCC1
C1CC[NH]CC1
C1CC[NH]CC1.c1ccccc1
HBr
C1(=CC=CC=C1)C
70
0.5
CCOC(=O)C(Br)CC.O=C1CCC(c2ccccc2)CN1>C1(=CC=CC=C1)C>CCOC(=O)C(CC)N1CC(c2ccccc2)CCC1=O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-98c17061ed0941a5ba5bcf3a6530bf66
CCOC(=O)C1CCC(=O)CC1>>CCOC(=O)C1CCNC(=O)CC1
CS(=O)(=O)O.O=C1CCC(CC1)C(=O)OCC.C([O-])(O)=O.[Na+].[N-]=[N+]=[N-].[Na+]>>O=C1CCC(CCN1)C(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][CH2:8][C:10](=[O:11])[CH2:12][CH2:13]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][CH2:8][NH:9][C:10](=[O:11])[CH2:12][CH2:13]1
CCOC(=O)C1CCC(=O)CC1
CCOC(=O)C1CCNC(=O)CC1
null
null
C(Cl)(Cl)Cl
Functional Group Addition
Schmidt ketone amide
bd03f575cc59664fd68bc4dea65aaf5b902271d018d65d5bd3b85398a36f8d70
2eb609f54422c0279557c5451dffbcf43fa7dc53a915eee10665042f34f6a171
O=C1CCCCCN1
[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[C:5]-[C:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[CH2;D2;+0:9]-[C:10]-1>>[#8:1]-[C:2](=[O;D1;H0:3])-[C:4]1-[C:5]-[C:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[#7:11]-[CH2;D2;+0:9]-[C:10]-1
70
[{"value": 70.0, "product": "O=C1CCC(CCN1)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.0, "product": "O=C1CCC(CCN1)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
10
CELSIUS
null
null
In a 250 ml three necked flask fitted with reflux condenser, magnetic stirrer and dropping funnel under inert atmosphere, 5.6 ml (5.98 g, 34 mmoles, 1 eq) of ethyl 4-oxocyclohexanecarboxylate 27 were dissolved in 50 ml of CHCl3. 6.65 g (102 mmole, 3 eq) of sodium azide were added, followed by 22.1 ml (32.8 g, 341 mmole...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary amide
C1CCCCC1
C1CCCNCC1
C1CCCNCC1
Other
C(Cl)(Cl)Cl
10
null
CCOC(=O)C1CCC(=O)CC1>C(Cl)(Cl)Cl>CCOC(=O)C1CCNC(=O)CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-82f8dd09f130443ab0aefbeeb0485fd7
CCC(Br)C(=O)OC(C)(C)C.CCOC(=O)C1CCNC(=O)CC1>>CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1
[H-].[Na+].O=C1CCC(CCN1)C(=O)OCC.BrC(C(=O)OC(C)(C)C)CC>>C(C)(C)(C)OC(=O)C(CC)N1CCC(CCC1=O)C(=O)OCC
Br[CH:12]([CH2:13][CH3:14])[C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20])[CH3:21].[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][CH2:8][C:9](=[O:10])[NH:11][CH2:22][CH2:23]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][CH2:8][C:9](=[O:10])[N:11]([CH:12]([CH2:13][CH3:14])[C:15](=[O:16])[O:17][C:18]([CH3:19])([CH3:20...
CCC(Br)C(=O)OC(C)(C)C.CCOC(=O)C1CCNC(=O)CC1
CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1
null
null
C(C)#N
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
7e2d047380fda5ccab9522d1ecd6114ed9ac7870607d92d33de993ebbcc7e977
29b3e231b1d2708086b87ea5e8bddd4b64f3d7251e67b4cc4f6db43e63a60af6
O=C1CCCCCN1
Br-[CH;D3;+0:1](-[C:2]-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C;D1;H3:10].[C:11]-[C:12]-[NH;D2;+0:13]-[C:14](=[O;D1;H0:15])-[C:16]>>[C:11]-[C:12]-[N;H0;D3;+0:13](-[CH;D3;+0:1](-[C:2]-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7](-[C;D1;H3:8])(-[C;D1;H3:9])-[C;D1;H3:10])-[C:14](=[O;D1...
94.4
[{"value": 69.0, "product": "C(C)(C)(C)OC(=O)C(CC)N1CCC(CCC1=O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.4, "product": "C(C)(C)(C)OC(=O)C(CC)N1CCC(CCC1=O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
In a 150 ml three necked flask fitted with reflux condenser, magnetic stirrer and dropping funnel under inert atmosphere, 5.09 g (27.5 mmoles, 1 eq) of ethyl 7-oxo-4-azepanecarboxylate 28 and 12.27 g (55 mmoles, 2 eq) of tert-butyl 2-bromobutanoate were dissolved in 70 ml of acetonitrile. The temperature was raised to ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester.Secondary amide
Ester.Tertiary amide
C1CCCNCC1
C1CCC[NH]CC1
C1CCC[NH]CC1
HBr
C(C)#N
50
null
CCC(Br)C(=O)OC(C)(C)C.CCOC(=O)C1CCNC(=O)CC1>C(C)#N>CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-645ca911aca9427b9ef5667e682c5d11
CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1>>CCOC(=O)C1CCC(=O)N(C(CC)C(=O)O)CC1
C(C)(C)(C)OC(=O)C(CC)N1CCC(CCC1=O)C(=O)OCC.FC(C(=O)O)(F)F>>C(C)OC(=O)C1CCC(N(CC1)C(C(=O)O)CC)=O
CC(C)(C)[O:17][C:15]([CH:12]([N:11]1[C:9](=[O:10])[CH2:8][CH2:7][CH:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:19][CH2:18]1)[CH2:13][CH3:14])=[O:16]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH:6]1[CH2:7][CH2:8][C:9](=[O:10])[N:11]([CH:12]([CH2:13][CH3:14])[C:15](=[O:16])[OH:17])[CH2:18][CH2:19]1
CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1
CCOC(=O)C1CCC(=O)N(C(CC)C(=O)O)CC1
null
null
C(Cl)Cl
Deprotection
Deprotection of carboxylic acid
152e5537e48c95b4a3e767536b0f9f68d1308e5f484070828ab5ed951805157a
7f019d4cfe9b3036d0a2d3a3209aa0e1fcb05418ebee15a4be5e125d315d5f01
O=C1CCCCCN1
C-C(-C)(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
0
CELSIUS
24
HOUR
In a 25 ml three necked flask fitted with magnetic stirrer and dropping funnel under inert atmosphere, 1 g (3.1 mmoles) of pure ethyl 1-[1-(tert-butoxycarbonyl)propyl]-7-oxo-4-azepanecarboxylate 29 was dissolved in 5 ml of CH2Cl2. The mixture was cooled down to 0° C., 5 ml of trifluoroacetic acid was added. The mixture...
10.6084/m9.figshare.5104873.v1
null
Ester.Boc
Carboxylic acid
null
null
C1CCC[NH]CC1
Other
C(Cl)Cl
0
24
CCOC(=O)C1CCC(=O)N(C(CC)C(=O)OC(C)(C)C)CC1>C(Cl)Cl>CCOC(=O)C1CCC(=O)N(C(CC)C(=O)O)CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a657f347ef0e49a29c12131dbb390714
C=CC(=O)Cl.Cc1cccc(C(=O)NC(C)C)c1N>>C=CC(=O)Nc1c(C)cccc1C(=O)NC(C)C
CN(C)C1=NC=CC=C1.NC1=C(C(=O)NC(C)C)C=CC=C1C.C(C)N(CC)CC.C(C=C)(=O)Cl.C(C=C)(=O)Cl>>CC=1C(=C(C(=O)NC(C)C)C=CC1)NC(C=C)=O
Cl[C:3]([CH:2]=[CH2:1])=[O:4].[NH2:5][c:6]1[c:7]([CH3:8])[cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[NH:15][CH:16]([CH3:17])[CH3:18]>>[CH2:1]=[CH:2][C:3](=[O:4])[NH:5][c:6]1[c:7]([CH3:8])[cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[NH:15][CH:16]([CH3:17])[CH3:18]
C=CC(=O)Cl.Cc1cccc(C(=O)NC(C)C)c1N
C=CC(=O)Nc1c(C)cccc1C(=O)NC(C)C
null
null
ClCCl.Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[#7:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](-[NH2;D1;+0:10]):[c:11]>>[#7:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4]):[c:11]
52.4
[{"value": 52.4, "product": "CC=1C(=C(C(=O)NC(C)C)C=CC1)NC(C=C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
8
HOUR
To a solution of the title compound of Step B (0.93 g, 4.8 mmol) in dichloromethane (10 mL) was added triethylamine (0.876 mL, 6.2 mmol) and the mixture was cooled to 0° C. Acryloyl chloride (0.433 mL, 5.3 mmol) was then added and the mixture was warmed to ambient temperature and stirred overnight. Dimethylaminopyridin...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
ClCCl.Cl
0
8
C=CC(=O)Cl.Cc1cccc(C(=O)NC(C)C)c1N>ClCCl.Cl>C=CC(=O)Nc1c(C)cccc1C(=O)NC(C)C
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a1a53def4c664a96999097c0e8311779
COC(=O)C=O.NNc1ccccc1Cl>>COC(=O)/C=N/Nc1ccccc1Cl
C(C=O)(=O)OC.Cl.ClC1=C(C=CC=C1)NN>>ClC1=C(C=CC=C1)N\N=C\C(=O)OC
O=[CH:5][C:3]([O:2][CH3:1])=[O:4].[NH2:6][NH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[Cl:14]>>[CH3:1][O:2][C:3](=[O:4])/[CH:5]=[N:6]/[NH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[Cl:14]
COC(=O)C=O.NNc1ccccc1Cl
COC(=O)/C=N/Nc1ccccc1Cl
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
c78be09cf200f3a07b02946ce0bbc22b647e9aaae7494d0480373904a4f330a9
c3cbc07b90655a7aa9777b584274a03a2ec0cff34c5b5edc214a16916fe29f1c
c1ccccc1
O=[CH;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[NH2;D1;+0:6]-[#7:7]-[c:8]>>[C;D1;H3:5]-[#8:4]-[C:2](=[O;D1;H0:3])/[CH;D2;+0:1]=[N;H0;D2;+0:6]/[#7:7]-[c:8]
null
[]
null
null
null
null
To a solution of methyl glyoxylate (6.8 g, 77 mmol) in methanol (150 mL) was added 2-chlorophenylhydrazine hydrochloride (12.5 g, 77 mmol) and the mixture was heated at reflux overnight, cooled and concentrated. The residue was re-dissolved in toluene and concentrated to give the title compound of Step A. Conditions: S...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Aldehyde
Hydrazone
null
null
c1ccccc1
HO-
CO
null
null
COC(=O)C=O.NNc1ccccc1Cl>CO>COC(=O)/C=N/Nc1ccccc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a30fcfbaca0f4f4f879d97038b13ac03
COC(=O)/C=N/Nc1ccccc1Cl.O=C1CCC(=O)N1Br>>COC(=O)/C(Br)=N/Nc1ccccc1Cl
ClC1=C(C=CC=C1)N\N=C\C(=O)OC.BrN1C(CCC1=O)=O>>Br\C(\C(=O)OC)=N/NC1=C(C=CC=C1)Cl
[CH3:1][O:2][C:3](=[O:4])/[CH:5]=[N:7]/[NH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[Cl:15].O=C1CCC(=O)N1[Br:6]>>[CH3:1][O:2][C:3](=[O:4])/[C:5]([Br:6])=[N:7]/[NH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][c:14]1[Cl:15]
COC(=O)/C=N/Nc1ccccc1Cl.O=C1CCC(=O)N1Br
COC(=O)/C(Br)=N/Nc1ccccc1Cl
null
null
O1CCCC1
Functional Group Interconversion
Bromination
a7c00719e839face56bb6216cdade7363196489e7c6b7cc1c5406f7f68c2c5a7
68cd054524e636d74778502f9e7f5c5bef9bcf9a0813a8a4bfdcfd2b317bdb5c
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[C;D1;H3:2]-[#8:3]-[C:4](=[O;D1;H0:5])/[CH;D2;+0:6]=[#7:7]/[#7:8]-[c:9]>>[Br;H0;D1;+0:1]/[C;H0;D3;+0:6](=[#7:7]\[#7:8]-[c:9])-[C:4](=[O;D1;H0:5])-[#8:3]-[C;D1;H3:2]
71.3
[{"value": 71.3, "product": "Br\\C(\\C(=O)OC)=N/NC1=C(C=CC=C1)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of the title compound of Step A (16.5 g, 77 mmol) in tetrahydrofuran (150 mL) was added N-bromosuccinimide (13.7 g, 77 mmol) and the mixture was stirred at ambient temperature for 2 hours. The mixture was concentrated and extracted with hexane and the hexane solution was concentrated to give the title com...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ester.Tertiary amide.Tertiary amide
Hydrazone.Alkenyl halide
C1CCNC1
null
c1ccccc1
HO-
O1CCCC1
null
2
COC(=O)/C=N/Nc1ccccc1Cl.O=C1CCC(=O)N1Br>O1CCCC1>COC(=O)/C(Br)=N/Nc1ccccc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b62c82ce4a9f497c902d1d7f12e1a2c2
CC(c1ccccc1)n1ccnc1.O=C1CCN(Cc2ccccc2)CC1>>OC1(c2nccn2CCc2ccccc2)CCN(Cc2ccccc2)CC1
C1(=CC=CC=C1)CN1CCC(CC1)=O.C1(=CC=CC=C1)C(C)N1C=NC=C1.C(CCC)[Li].CCCCCC>>C1(=CC=CC=C1)CCN1C(=NC=C1)C1(CCN(CC1)CC1=CC=CC=C1)O
[cH:3]1[n:4][cH:5][cH:6][n:7]1[CH:8]([CH3:9])[c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1.[O:1]=[C:2]1[CH2:16][CH2:17][N:18]([CH2:19][c:20]2[cH:21][cH:22][cH:23][cH:24][cH:25]2)[CH2:26][CH2:27]1>>[OH:1][C:2]1([c:3]2[n:4][cH:5][cH:6][n:7]2[CH2:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)[CH2:16][CH2:17][N:18]([C...
CC(c1ccccc1)n1ccnc1.O=C1CCN(Cc2ccccc2)CC1
OC1(c2nccn2CCc2ccccc2)CCN(Cc2ccccc2)CC1
null
null
C1CCOC1.O
C-C Coupling
OtherReaction
104c0d12140db71c4a07a78a0bc19d9e90210ce156ef7bb9b397b7f586769b88
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1ccc(CCn2ccnc2C2CCN(Cc3ccccc3)CC2)cc1
[CH3;D1;+0:1]-[CH;D3;+0:2](-[#7;a:3]1:[c:4]:[c:5]:[#7;a:6]:[cH;D2;+0:7]:1)-[c;H0;D3;+0:8](:[c:9]:[c:10]):[c:11]:[c:12].[O;H0;D1;+0:13]=[C;H0;D3;+0:14]1-[C:15]-[C:16]-[#7:17]-[C:18]-[C:19]-1>>[OH;D1;+0:13]-[C;H0;D4;+0:14]1(-[c;H0;D3;+0:7]2:[#7;a:6]:[c:5]:[c:4]:[#7;a:3]:2-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[c;H0;D3;+0:8](:[c:9]...
75
[{"value": 75.0, "product": "C1(=CC=CC=C1)CCN1C(=NC=C1)C1(CCN(CC1)CC1=CC=CC=C1)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 75.0, "product": "C1(=CC=CC=C1)CCN1C(=NC=C1)C1(CCN(CC1)CC1=CC=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-70
CELSIUS
null
null
A mixture of DIPA (1.4 mol) in THF (3000 ml) was stirred at −70° C. under N2 flow. Butyllithium 2.5 M/hexane (1.3 mol) was added portionwise at a temperature below −40° C. The mixture was stirred at −70° C. for 15 min. 1-phenylethyl-1H-imidazole (1 mol) dissolved in THF was added dropwise at a temperature below −55° C....
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1c[nH]cn1.c1ccccc1.C1CC[NH]CC1
c1ncc[nH]1.c1ccccc1.C1CC[NH]CC1
c1ncc[nH]1.c1ccccc1.C1CC[NH]CC1.c1ccccc1
null
C1CCOC1.O
-70
null
CC(c1ccccc1)n1ccnc1.O=C1CCN(Cc2ccccc2)CC1>C1CCOC1.O>OC1(c2nccn2CCc2ccccc2)CCN(Cc2ccccc2)CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-36dcda66a7bc4f35af86da77d22e3518
OC1(c2nccn2Cc2ccccc2)CCN(Cc2ccccc2)CC1.[Cl-].[Cl-]>>Cl.Cl.c1ccc(CN2CCC3(CC2)c2ccccc2Cn2ccnc23)cc1
[OH-].[Na+].C1(=CC=CC=C1)CN1CCC(CC1)(O)C=1N(C=CN1)CC1=CC=CC=C1.[Al+3].[Cl-].[Cl-].[Cl-].[Al+3].[Cl-].[Cl-].[Cl-]>>Cl.Cl.C1(=CC=CC=C1)CN1CCC2(CC1)C=1N(CC=3C=CC=CC32)C=CN1
O[C:11]1([c:25]2[n:21]([CH2:20][c:19]3[cH:14][cH:15][cH:16][cH:17][cH:18]3)[cH:22][cH:23][n:24]2)[CH2:10][CH2:9][N:8]([CH2:7][c:6]2[cH:5][cH:4][cH:3][cH:27][cH:26]2)[CH2:13][CH2:12]1.[Cl-:2].[Cl-:1]>>[ClH:1].[ClH:2].[cH:3]1[cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][C:11]3([CH2:12][CH2:13]2)[c:14]2[cH:15][cH:16][cH:...
OC1(c2nccn2Cc2ccccc2)CCN(Cc2ccccc2)CC1.[Cl-].[Cl-]
Cl.Cl.c1ccc(CN2CCC3(CC2)c2ccccc2Cn2ccnc23)cc1
null
null
null
C-C Coupling
OtherReaction
57f4cf808426353a6122d5db873756c3882c9b4bca5ffeb055984b6b79f55f16
80806390361076ffee90cd775b1e87663148d08d65f5b27bdd06ebc36de07186
c1ccc(CN2CCC3(CC2)c2ccccc2Cn2ccnc23)cc1
O-[C;H0;D4;+0:1]1(-[c:2]2:[#7;a:3]:[c:4]:[c:5]:[#7;a:6]:2-[C:7]-[c:8](:[c:9]):[cH;D2;+0:10]:[c:11]:[c:12])-[C:13]-[C:14]-[#7:15]-[C:16]-[C:17]-1.[Cl-;H0;D0:18].[Cl-;H0;D0:19]>>[ClH;D0;+0:19].[ClH;D0;+0:18].[c:12]:[c:11]:[c;H0;D3;+0:10]1:[c:8](:[c:9])-[C:7]-[#7;a:6]2:[c:5]:[c:4]:[#7;a:3]:[c:2]:2-[C;H0;D4;+0:1]-12-[C:13]...
1.8
[{"value": 1.8, "product": "Cl.Cl.C1(=CC=CC=C1)CN1CCC2(CC1)C=1N(CC=3C=CC=CC32)C=CN1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
1
HOUR
1-(phenylmethyl)-4-[1-(phenylmethyl)-1H-imidazol-2-yl]-4-piperidinol (0.124 mol) and AlCl3 (0.31 mol) were stirred in a melt at 120° C. for 1 h. The mixture was cooled, AlCl3 (0.31 mol) was added and the mixture was stirred at 120° C. for 1 h. The mixture was poured into ice, alkalized with NaOH 50% and extracted with ...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
null
c1ccccc1.C1CC[NH]CC1
c1ccc2c(c1)Cn1ccnc1C21CC[NH]CC1
c1ccccc1.c1ccc2c(c1)Cn1ccnc1C21CC[NH]CC1
Other
null
120
1
OC1(c2nccn2Cc2ccccc2)CCN(Cc2ccccc2)CC1.[Cl-].[Cl-]>>Cl.Cl.c1ccc(CN2CCC3(CC2)c2ccccc2Cn2ccnc23)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-208c125703734caba2a9259dcaadb6cc
CN1CCC(C(=O)Cl)(c2ccccc2)CC1.NCc1ccccc1>>CN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1
CN1CCC(CC1)(C(=O)Cl)C1=CC=CC=C1.C1(=CC=CC=C1)CN.C(C)N(CC)CC.C(=O)([O-])[O-].[K+].[K+]>>CN1CCC(CC1)(C(=O)NCC1=CC=CC=C1)C1=CC=CC=C1
Cl[C:6]([C:5]1([c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[CH2:4][CH2:3][N:2]([CH3:1])[CH2:23][CH2:22]1)=[O:7].[NH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1>>[CH3:1][N:2]1[CH2:3][CH2:4][C:5]([C:6](=[O:7])[NH:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][cH:15]2)([c:16]2[cH:17][cH:18][cH:19][cH:20][cH:21]2)[...
CN1CCC(C(=O)Cl)(c2ccccc2)CC1.NCc1ccccc1
CN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1
null
null
O.C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCc1ccccc1)C1(c2ccccc2)CCNCC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[c:4])(-[C:5])-[C:6].[NH2;D1;+0:7]-[C:8]-[c:9]>>[C:5]-[C:3](-[c:4])(-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:8]-[c:9])-[C:6]
95.3
[{"value": 95.0, "product": "CN1CCC(CC1)(C(=O)NCC1=CC=CC=C1)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.3, "product": "CN1CCC(CC1)(C(=O)NCC1=CC=CC=C1)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
1-Methyl-4-phenyl-4-piperidinecarbonyl chloride (0.49 mol) was added portionwise at room temperature to a stirring mixture of benzenemethanamine (0.49 mol) and triethyl amine (1.223 mol) in CH2Cl2 (2500 ml). The mixture was stirred at room temperature for 1 hour. K2CO3 (150 g) and H2O were added. The mixture was stirre...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
C1CC[NH]CC1.c1ccccc1.c1ccccc1
HCl
O.C(Cl)Cl
null
1
CN1CCC(C(=O)Cl)(c2ccccc2)CC1.NCc1ccccc1>O.C(Cl)Cl>CN1CCC(C(=O)NCc2ccccc2)(c2ccccc2)CC1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-696b82fd9a0a4806818870df0e9948e3
CN(C)C=O.c1ccc(CCCCn2ccnc2)cc1>>NC(=O)c1nccn1CCCCc1ccccc1
[NH4+].[Cl-].CN(C=O)C.C(CCC)[Li].CCCCCC.C1(=CC=CC=C1)CCCCN1C=NC=C1>>C1(=CC=CC=C1)CCCCN1C(=NC=C1)C(=O)N
C[N:1](C)[CH:2]=[O:3].[cH:4]1[n:5][cH:6][cH:7][n:8]1[CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[NH2:1][C:2](=[O:3])[c:4]1[n:5][cH:6][cH:7][n:8]1[CH2:9][CH2:10][CH2:11][CH2:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
CN(C)C=O.c1ccc(CCCCn2ccnc2)cc1
NC(=O)c1nccn1CCCCc1ccccc1
null
null
C1CCOC1
C-C Coupling
OtherReaction
7f57a7521d1baa0851e1141ce1cea38ee563de57b44f5f72d186fcb0ae1b20dd
2b96b5a9b8a7ea9a2f788a30832f4ff1c689451b5a72ad75fa45cd01ef4810db
c1ccc(CCCCn2ccnc2)cc1
C-[N;H0;D3;+0:1](-C)-[CH;D2;+0:2]=[O;D1;H0:3].[C:4]-[#7;a:5]1:[c:6]:[c:7]:[#7;a:8]:[cH;D2;+0:9]:1>>[C:4]-[#7;a:5]1:[c:6]:[c:7]:[#7;a:8]:[c;H0;D3;+0:9]:1-[C;H0;D3;+0:2](-[NH2;D1;+0:1])=[O;D1;H0:3]
null
[]
-78
CELSIUS
null
null
Reaction under N2 atmosphere. A mixture of DIPA (0.455 mol) in THF (500 ml) was stirred at −78° C. Butyllithium, 2.5M/hexane (0.390 mol) was added dropwise at −40° C. The mixture was stirred for 15 min, then re-cooled to −78° C. A solution of 1-(4-phenylbutyl)-1H-imidazole, prepared according to the procedure described...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Primary amide
c1c[nH]cn1
c1ncc[nH]1
c1ncc[nH]1.c1ccccc1
Other
C1CCOC1
-78
null
CN(C)C=O.c1ccc(CCCCn2ccnc2)cc1>C1CCOC1>NC(=O)c1nccn1CCCCc1ccccc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-ebdb6c09cb774332a0a1cecc00fe64cd
CN(C)C=O.Oc1cc2c(cc1O)Cn1ccnc1C2>>COc1cc2c(cc1OC)Cn1ccnc1C2
O.N=1C=CN2CC=3C=C(C(=CC3CC21)O)O.C(=O)([O-])[O-].[K+].[K+].CN(C)C=O>>COC=1C(=CC=2CC=3N(CC2C1)C=CN3)OC
CN([CH:1]=O)[CH3:10].[OH:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:8]1[OH:9])[CH2:11][n:12]1[cH:13][cH:14][n:15][c:16]1[CH2:17]2>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([cH:7][c:8]1[O:9][CH3:10])[CH2:11][n:12]1[cH:13][cH:14][n:15][c:16]1[CH2:17]2
CN(C)C=O.Oc1cc2c(cc1O)Cn1ccnc1C2
COc1cc2c(cc1OC)Cn1ccnc1C2
null
[Cl-].C1(=CC=CC=C1)[N+](C)(C)C
null
Heteroatom Alkylation and Arylation
OtherReaction
05add0336860651e77560062fbde59de7637be14641b2137a48bb7a130e673d5
70540f8b47d0cb308c47727b03916eb5873a3febfc3e6645bdd3176ffa63991d
c1ccc2c(c1)Cc1nccn1C2
C-N(-[CH3;D1;+0:1])-[CH;D2;+0:2]=O.[OH;D1;+0:3]-[c:4](:[c:5]):[c:6](-[OH;D1;+0:7]):[c:8]>>[CH3;D1;+0:1]-[O;H0;D2;+0:7]-[c:6](:[c:8]):[c:4](-[O;H0;D2;+0:3]-[CH3;D1;+0:2]):[c:5]
8.4
[{"value": 8.4, "product": "COC=1C(=CC=2CC=3N(CC2C1)C=CN3)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 5,10-dihydro-imidazo[1,2-b]-isoquinoline-7,8-diol, obtained according to the procedure described in Ex.No. A8 c, (0.155 mol), phenyltrimethylammonium chloride (0.31 mol) and K2CO3 (0.68 mol) in DMF (400 ml) was stirred at 90° C. for 20 hours, cooled, poured out into H2O and filtered over dicalite. The filt...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Aromatic alcohol.Aromatic alcohol
Ether.Ether
null
null
c1ccc2c(c1)Cc1nccn1C2
HO-
[Cl-].C1(=CC=CC=C1)[N+](C)(C)C
null
null
CN(C)C=O.Oc1cc2c(cc1O)Cn1ccnc1C2>[Cl-].C1(=CC=CC=C1)[N+](C)(C)C>COc1cc2c(cc1OC)Cn1ccnc1C2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-825838bf0675463188070eeb1a8507bd
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O>>C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O
CCCCCCCC(=O)C(C(=O)CCCCCCC)(C(=O)CCCCCCC)[NH3+].[Cl-].C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=O)CC[C@H]34>>O[C@@H]1[C@]2(C)[C@@H](CC1)[C@@H]1CC[C@@H]3CC(CC[C@@H]3[C@H]1CC2)=O
[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]3[C@@H:6]([CH2:7][CH2:8][C:9]4=[CH:10][C:11](=[O:12])[CH2:13][CH2:14][C@H:15]34)[C@@H:16]1[CH2:17][CH2:18][C@@H:19]2[OH:20]>>[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]3[C@@H:6]([CH2:7][CH2:8][C@@H:9]4[CH2:10][C:11](=[O:12])[CH2:13][CH2:14][C@H:15]34)[C@@H:16]1[CH2:17][CH2:18][C@@H:19]2[OH:...
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O
null
null
ClCCl.O
Reduction
Hydrogenation (double to single)
57601b680323e405817ba7605c71f4c533dd9299fe6c475cc1627ae4949cdd43
0e0db21233797ec1d2a9464a1f32cef94e53e6a41f96d680fa1307067bbf01f2
O=C1CC[C@H]2[C@H](CC[C@@H]3[C@@H]2CCC2CCC[C@H]23)C1
[C:1]-[C:2]1-[C:3]-[C:4]-[C:5](=[O;D1;H0:6])-[CH;D2;+0:7]=[C;H0;D3;+0:8]-1-[C:9]-[C:10]>>[C:1]-[C:2]1-[C:3]-[C:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-[C@H;D3;+0:8]-1-[C:9]-[C:10]
107
[{"value": 92.0, "product": "O[C@@H]1[C@]2(C)[C@@H](CC1)[C@@H]1CC[C@@H]3CC(CC[C@@H]3[C@H]1CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 107.0, "product": "O[C@@H]1[C@]2(C)[C@@H](CC1)[C@@H]1CC[C@@H]3CC(CC[C@@H]3[C@H]1CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of 19-nortestosterone (10.0 g, 35.5 mmol) in dichloromethane (100.0 ml) was mixed with the catalyst previously prepared from RhCl3.H2O (380 mg) and Aliquat-336® (800 mg) in water (10.0 ml) and dichloromethane (22.0 ml). The mixture was hydrogenated overnight at 20 psi. The product was washed twice with water...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=C2CC[C@H]3[C@@H]4CCC[C@@H]4CC[C@@H]3[C@H]2CCC1
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@H]2CCC[C@H]21
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@H]2CCC[C@H]21
null
ClCCl.O
null
8
C[C@]12CC[C@H]3[C@@H](CCC4=CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O>ClCCl.O>C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(=O)CC[C@@H]43)[C@@H]1CC[C@@H]2O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-faa2f348d6f5478eb5c5bd468fd5e72f
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC2=O.OCCO>>C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC21OCCO1
C(CO)O.C1(=CC=C(C=C1)S(=O)(=O)[O-])C.[NH+]1=CC=CC=C1.CCOC(=O)C.CCCCCC.OC1C[C@H]2CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@H]2CC1)=O>>C1COC2([C@]3(C)[C@@H](CC2)[C@@H]2CC[C@@H]4CC(CC[C@@H]4[C@H]2CC3)O)O1
[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]3[C@@H:6]([CH2:7][CH2:8][C@@H:9]4[CH2:10][CH:11]([OH:12])[CH2:13][CH2:14][C@H:15]34)[C@@H:16]1[CH2:17][CH2:18][C:19]2=[O:20].O[CH2:21][CH2:22][OH:23]>>[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]3[C@@H:6]([CH2:7][CH2:8][C@@H:9]4[CH2:10][CH:11]([OH:12])[CH2:13][CH2:14][C@H:15]34)[C@@H:16]1[CH...
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC2=O.OCCO
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC21OCCO1
null
null
CCOC(=O)C.C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
41ae5195ba47d3db987aa5d31e3b31b1e97aef93f007000a7df7639fc806d9f0
f8121a7732f8ef583111433d2b2d82886bf3a134c51dc6363d813c8cbf4e36f5
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CCC2[C@H]1CCC21OCCO1
O-[CH2;D2;+0:1]-[C:2]-[OH;D1;+0:3].[C:4]-[C:5]1(-[C;D1;H3:6])-[C:7]-[C:8]-[C:9]-[C;H0;D3;+0:10]-1=[O;H0;D1;+0:11]>>[C:4]-[C:5]1(-[C;D1;H3:6])-[C:7]-[C:8]-[C:9]-[C;H0;D4;+0:10]-12-[O;H0;D2;+0:11]-[CH2;D2;+0:1]-[C:2]-[O;H0;D2;+0:3]-2
94.8
[{"value": 94.5, "product": "C1COC2([C@]3(C)[C@@H](CC2)[C@@H]2CC[C@@H]4CC(CC[C@@H]4[C@H]2CC3)O)O1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.8, "product": "C1COC2([C@]3(C)[C@@H](CC2)[C@@H]2CC[C@@H]4CC(CC[C@@H]4[C@H]2CC3)O)O1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Compound 4(10 g, 36.2 mmol) was dissolved in dry benzene (150 ml) mixed with ethylene glycol (25 ml, 280 mmol) and pyridinium p-toluenesulfonate (1 g, 3.9 mmol) and refluxed using a Dean-stark separator overnight till no starting material was detected by TLC. The cold solution was diluted with EtOAc (100 ml), washed tw...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary alcohol.Primary alcohol
Ether.Ether
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@H]2CCC[C@H]21
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@@H]2[C@H]1CCC21OCCO1
C1CC[C@H]2[C@@H](C1)CC[C@@H]1[C@@H]2CC[C@@H]2[C@H]1CCC21OCCO1
HO-
CCOC(=O)C.C1=CC=CC=C1
null
8
C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC2=O.OCCO>CCOC(=O)C.C1=CC=CC=C1>C[C@]12CC[C@H]3[C@@H](CC[C@@H]4CC(O)CC[C@@H]43)[C@@H]1CCC21OCCO1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-347b46abced84de9bf8ce6a178260fd5
CCOC=C(C(=O)OCC)C(=O)OCC.CSC(=N)N>>CCOC(=O)c1cnc(SC)nc1O
[OH-].[Na+].CSC(=N)N.OS(=O)(=O)O.C(C)OC=C(C(=O)OCC)C(=O)OCC>>CSC1=NC=C(C(=N1)O)C(=O)OCC
CCO[CH:7]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:13](OCC)=[O:14].[NH2:8][C:9]([S:10][CH3:11])=[NH:12]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([S:10][CH3:11])[n:12][c:13]1[OH:14]
CCOC=C(C(=O)OCC)C(=O)OCC.CSC(=N)N
CCOC(=O)c1cnc(SC)nc1O
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
caf9cb78c7502ec533d5fe3b7a8a08e1fb6cf99301dd7b428451735db624aa4a
06f73c43becdfac6f63abd2370cc1e14a2a3568880484871cbc0fc9a1c48b1b0
c1cncnc1
C-C-O-[CH;D2;+0:1]=[C;H0;D3;+0:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-O-C-C.[C;D1;H3:9]-[#16:10]-[C;H0;D3;+0:11](-[NH2;D1;+0:12])=[NH;D1;+0:13]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[c;H0;D3;+0:2]1:[cH;D2;+0:1]:[n;H0;D2;+0:12]:[c;H0;D3;+0:11](-[#16:10]-[C;D1;H3:9]):[n;H0;D2;+0:13]:[c;H0;D3;+0...
61
[{"value": 61.0, "product": "CSC1=NC=C(C(=N1)O)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.7, "product": "CSC1=NC=C(C(=N1)O)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a 4N sodium hydroxide solution (200 mL) was added S-methylisothioureasulfate (55.6 g, 0.2 mol), and after stirring for 30 min, at room temperature a solution of diethyl ethoxymethylenemalonate (80.8 mL, 0.35 mol) in ethanol (100 mL) was dropwise added slowly over 1 h. After stirring for 18 h, the precipitated crysta...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Ether.Primary amine.Monosulfide
Ester.Aromatic alcohol.Monosulfide
null
c1cncnc1
c1cncnc1
HO-
C(C)O
null
18
CCOC=C(C(=O)OCC)C(=O)OCC.CSC(=N)N>C(C)O>CCOC(=O)c1cnc(SC)nc1O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b3ebf651e99d40be9d11ee0c8e9016bb
CCOC(=O)c1cnc(SC)nc1O.c1ccc2c(c1)CCN2>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O
N1CCC2=CC=CC=C12.CSC1=NC=C(C(=N1)O)C(=O)OCC>>OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12
CS[c:9]1[n:8][cH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[c:20]([OH:21])[n:19]1.[NH:10]1[CH2:11][CH2:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]21>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19][c:20]1[OH:21]
CCOC(=O)c1cnc(SC)nc1O.c1ccc2c(c1)CCN2
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
4505c639bebc45c428c7c95a2ea93278a0c93ae321cd06f8fa554f9f2513cd5d
f5aa33108984aad43441754644c214239e577e2035dc027b4aa13ab85821a21b
c1cnc(N2CCc3ccccc32)nc1
C-S-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5].[c:6]:[c:7]1:[c:8]-[C:9]-[C:10]-[NH;D2;+0:11]-1>>[c:6]:[c:7]1:[c:8]-[C:9]-[C:10]-[N;H0;D3;+0:11]-1-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[#7;a:4]:[c:5]
77.1
[{"value": 77.0, "product": "OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.1, "product": "OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of indoline (3.58 g, 30 mmol) in ethanol (50 mL) was added ethyl 2-methylthio-4-hydroxypyrimidine-5-carboxylate (5.35 g, 25 mmol) and the mixture was heated under reflux for 18 h. The reaction mixture was allowed to cool to room temperature and the precipitated crystals were collected by filtration. The c...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Monosulfide
Tertiary amine
c1cncnc1.c1ccc2c(c1)CCN2
c1cncnc1.c1ccc2c(c1)CC[NH]2
c1cncnc1.c1ccc2c(c1)CC[NH]2
Other
C(C)O
null
null
CCOC(=O)c1cnc(SC)nc1O.c1ccc2c(c1)CCN2>C(C)O>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-05fcf5b00c234f1c840e80e373f6affb
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.Fc1ccc(CBr)cc1>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(F)cc1
O.OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.C([O-])([O-])=O.[K+].[K+].FC1=CC=C(CBr)C=C1>>N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)F)C(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19][c:20]1[OH:21].Br[CH2:22][c:23]1[cH:24][cH:25][c:26]([F:27])[cH:28][cH:29]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c...
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.Fc1ccc(CBr)cc1
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(F)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccnc(N3CCc4ccccc43)n2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1-[OH;D1;+0:14]>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1-[O;H0;D2;+0:14]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
79.2
[{"value": 79.0, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)F)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.2, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)F)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
18
HOUR
To a solution of ethyl 4-hydroxy-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (7.1 g, 27.6 mmol) in N,N-dimethylformamide (100 ml) were added potassium carbonate (7.8 g, 60 mmol) and 4-fluorobenzylbromide (3.74 ml, 30 mmol) and the mixture was stirred at 80° C. for 18 h. The reaction mixture was allowed to coo...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1cncnc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HBr
CN(C=O)C
80
18
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.Fc1ccc(CBr)cc1>CN(C=O)C>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(F)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-4b9b0f31ba6b4ff9aace7ffd9d916a47
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.COc1ccc(CCl)cc1>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC)cc1
OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.C([O-])([O-])=O.[K+].[K+].[I-].[Na+].COC1=CC=C(CCl)C=C1>>N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC)C(=O)OCC
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19][c:20]1[OH:21].Cl[CH2:22][c:23]1[cH:24][cH:25][c:26]([O:27][CH3:28])[cH:29][cH:30]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][...
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.COc1ccc(CCl)cc1
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC)cc1
null
null
O.CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(COc2ccnc(N3CCc4ccccc43)n2)cc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1-[OH;D1;+0:14]>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]1:[c:9]:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1-[O;H0;D2;+0:14]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
78
[{"value": 78.0, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.5, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
18
HOUR
To a solution of ethyl 4-hydroxy-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (500 mg, 1.75 mmol) in N,N-dimethylformamide (10 mL) were added potassium carbonate (500 g, 4 mmol), sodium iodide (300 mg, 2 mmol) and 4-methoxybenzyl chloride (0.29 mL, 2 mmol), and the mixture was stirred at 80° C. for 18 h. The r...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1cncnc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HCl
O.CN(C=O)C
80
18
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.COc1ccc(CCl)cc1>O.CN(C=O)C>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-1b563b66a76d47b3b1470b157246b957
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.O=P(Cl)(Cl)Cl>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl
OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.P(=O)(Cl)(Cl)Cl>>ClC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12
O[c:20]1[c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19]1.O=P(Cl)(Cl)[Cl:21]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19][c:20]1[Cl:21]
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.O=P(Cl)(Cl)Cl
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl
null
null
null
Functional Group Interconversion
Alcohol to chloride_POCl3_ortho
c34cc3a735ba90a6ebc3a31af86c6a0085713d9dcab569055caa3b8d444bb07d
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1cnc(N2CCc3ccccc32)nc1
Cl-P(-Cl)(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4](-[#7:5]):[#7;a:6]:[c:7]:[c:8]:1-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12]>>[#7:5]-[c:4]1:[#7;a:3]:[c;H0;D3;+0:2](-[Cl;H0;D1;+0:1]):[c:8](-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12]):[c:7]:[#7;a:6]:1
477.4
[{"value": 100.0, "product": "ClC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 477.4, "product": "ClC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
15
HOUR
To ethyl 4-hydroxy-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (2.85 g, 10 mmol) was added phosphorus oxychloride (10 mL, 2 mmol) and the mixture was stirred at 120° C. for 15 h. The reaction mixture was concentrated under reduced pressure. The obtained residue was dissolved in ethyl acetate, washed with satu...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1cncnc1
c1cncnc1
c1cncnc1.c1ccc2c(c1)CC[NH]2
HCl
null
120
15
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.O=P(Cl)(Cl)Cl>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-47cbd00618f04a099dd5260bd5b784b4
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.OCc1ccc(OC(F)(F)F)cc1>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC(F)(F)F)cc1
O.ClC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.C([O-])([O-])=O.[K+].[K+].FC(OC1=CC=C(CO)C=C1)(F)F>>N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC(F)(F)F)C(=O)OCC
Cl[c:20]1[c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19]1.[OH:21][CH2:22][c:23]1[cH:24][cH:25][c:26]([O:27][C:28]([F:29])([F:30])[F:31])[cH:32][cH:33]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3...
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.OCc1ccc(OC(F)(F)F)cc1
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC(F)(F)F)cc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
a445000eb5ed501274d93689ad5b9d45095af02deca02b6b541c8a834890a276
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(COc2ccnc(N3CCc4ccccc43)n2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[#7:4]):[#7;a:5]:[c:6]:[c:7]:1-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11].[OH;D1;+0:12]-[C:13]-[c:14]>>[#7:4]-[c:3]1:[#7;a:2]:[c;H0;D3;+0:1](-[O;H0;D2;+0:12]-[C:13]-[c:14]):[c:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]):[c:6]:[#7;a:5]:1
53.2
[{"value": 53.0, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC(F)(F)F)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.2, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)OCC1=CC=C(C=C1)OC(F)(F)F)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
18
HOUR
To a solution of ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (520 mg, 1.72 mmol) in N,N-dimethylformamide (5 mL) was added potassium carbonate (829 mg, 6 mmol) and 4-(trifluoromethoxy)benzyl alcohol (384 mg, 2 mmol) and the mixture was stirred at 100° C. for 18 h. The reaction mixture was allow...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1cncnc1
c1cncnc1
c1cncnc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HCl
CN(C=O)C
100
18
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.OCc1ccc(OC(F)(F)F)cc1>CN(C=O)C>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1OCc1ccc(OC(F)(F)F)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-a61417b4a55b431fb3b5c4a7891ca0c1
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.NCc1ccc(F)cc1>>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1NCc1ccc(F)cc1
O.ClC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.C([O-])([O-])=O.[Na+].[Na+].FC1=CC=C(CN)C=C1>>N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)NCC1=CC=C(C=C1)F)C(=O)OCC
Cl[c:20]1[c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]32)[n:19]1.[NH2:21][CH2:22][c:23]1[cH:24][cH:25][c:26]([F:27])[cH:28][cH:29]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[CH2:11][CH2:12][c:13]3[cH:14][cH:15][cH:16][cH:17...
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.NCc1ccc(F)cc1
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1NCc1ccc(F)cc1
null
null
C(C)(C)O
Heteroatom Alkylation and Arylation
N-arylation (Buchwald-Hartwig/Ullmann-Goldberg)
c38b7155556ff28144ae37859ff6668b20d59da60c705d26b158542b6d8385da
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(CNc2ccnc(N3CCc4ccccc43)n2)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3](-[#7:4]):[#7;a:5]:[c:6]:[c:7]:1-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11].[NH2;D1;+0:12]-[C:13]-[c:14]>>[#7:4]-[c:3]1:[#7;a:2]:[c;H0;D3;+0:1](-[NH;D2;+0:12]-[C:13]-[c:14]):[c:7](-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]):[c:6]:[#7;a:5]:1
81.2
[{"value": 81.0, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)NCC1=CC=C(C=C1)F)C(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.2, "product": "N1(CCC2=CC=CC=C12)C1=NC=C(C(=N1)NCC1=CC=C(C=C1)F)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (607 mg, 2.0 mmol) in isopropanol (5 mL) were added sodium carbonate (424 mg, 4 mmol) and 4-fluorobenzylamine (313 mg, 4 mmol) and the mixture was heated under reflux for 18 h. The reaction mixture was allowed to cool to room temperat...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1cncnc1
c1cncnc1
c1cncnc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HCl
C(C)(C)O
null
null
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1Cl.NCc1ccc(F)cc1>C(C)(C)O>CCOC(=O)c1cnc(N2CCc3ccccc32)nc1NCc1ccc(F)cc1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-246db8c799c144b3969777dadbb12e19
COc1ccc2[nH]ccc2c1>>COc1ccc2c(c1)CCN2
COC=1C=C2C=CNC2=CC1.C(#N)[BH3-].[Na+]>>COC=1C=C2CCNC2=CC1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[cH:9][cH:10][nH:11]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][NH:11]2
COc1ccc2[nH]ccc2c1
COc1ccc2c(c1)CCN2
null
null
C(C)(=O)O
Reduction
OtherReaction
d7c64ff5bdeff25897e9ebfc8baf5f34c2f69037fd4e91a3394e3e20a554de0e
2b7f370a519e29b4dede190aa36b37f30822496e32f2c8bfa9736e631bde52e2
c1ccc2c(c1)CCN2
[c:1]:[c:2]1:[nH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[c:6]:1:[c:7]>>[c:1]:[c:2]1:[c:6](:[c:7])-[CH2;D2;+0:5]-[CH2;D2;+0:4]-[NH;D2;+0:3]-1
94
[{"value": 94.0, "product": "COC=1C=C2CCNC2=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.7, "product": "COC=1C=C2CCNC2=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of 5-methoxyindole (528 mg, 3.6 mmol) in acetic acid (5 mL) was added sodium cyanoborohydride (452 mg, 7.2 mmol) by small portions at room temperature and the mixture was stirred for 18 h in situ. The solvent was evaporated under reduced pressure and the obtained residue was dissolved in ethyl acetate. Th...
10.6084/m9.figshare.5104873.v1
null
null
Secondary amine
c1ccc2[nH]ccc2c1
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
null
C(C)(=O)O
null
18
COc1ccc2[nH]ccc2c1>C(C)(=O)O>COc1ccc2c(c1)CCN2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-44c45998a8b849329f98083d33b92282
O=C(O)C1Cc2ccccc2N1>>OCC1Cc2ccccc2N1
[H-].[Al+3].[Li+].[H-].[H-].[H-].N1C(CC2=CC=CC=C12)C(=O)O.C(C)O.Cl>>OCC1NC2=CC=CC=C2C1
O=[C:2]([OH:1])[CH:3]1[CH2:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[NH:11]1>>[OH:1][CH2:2][CH:3]1[CH2:4][c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[NH:11]1
O=C(O)C1Cc2ccccc2N1
OCC1Cc2ccccc2N1
null
null
O1CCCC1
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccc2c(c1)CCN2
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[C:3](-[C:4])-[#7:5]-[c:6]>>[C:4]-[C:3](-[CH2;D2;+0:1]-[O;D1;H1:2])-[#7:5]-[c:6]
64.3
[{"value": 64.0, "product": "OCC1NC2=CC=CC=C2C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 64.3, "product": "OCC1NC2=CC=CC=C2C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
18
HOUR
To a solution of (RS)-indoline-2-carboxylic acid (8.16 g, 50 mmol) in tetrahydrofuran (50 ml) was added under ice-cooling lithium aluminum hydride (5.7 g, 150 mmol) and the mixture was stirred at 60° C. for 18 h. The reaction mixture was stirred under ice-cooling and ethanol and 1N hydrochloric acid were added. The pre...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccc2c(c1)CCN2
Other
O1CCCC1
60
18
O=C(O)C1Cc2ccccc2N1>O1CCCC1>OCC1Cc2ccccc2N1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2d6bc2f5413f417781b69375e7336008
O=C(O)c1ccc2c(c1)CCO2>>OCc1ccc2c(c1)CCO2
[H-].[Al+3].[Li+].[H-].[H-].[H-].O1C2=C(CC1)C=C(C=C2)C(=O)O.CO.Cl>>O1C2=C(CC1)C=C(C=C2)CO
O=[C:2]([OH:1])[c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][O:11]2>>[OH:1][CH2:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][O:11]2
O=C(O)c1ccc2c(c1)CCO2
OCc1ccc2c(c1)CCO2
null
null
O1CCCC1
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccc2c(c1)CCO2
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[c:3](:[c:4]):[c:5]>>[O;D1;H1:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
100
[{"value": 100.0, "product": "O1C2=C(CC1)C=C(C=C2)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.9, "product": "O1C2=C(CC1)C=C(C=C2)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
1
HOUR
To a solution of 2,3-dihydrobenzo[b]furan-5-carboxylic acid (1.64 g, 10 mmol) in tetrahydrofuran (10 mL) was added under ice-cooling lithium aluminum hydride (949 mg, 25 mmol) and the mixture was stirred at 60° C. for 1 h. The reaction mixture was stirred under ice-cooling and methanol and 1N hydrochloric acid were add...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccc2c(c1)CCO2
Other
O1CCCC1
60
1
O=C(O)c1ccc2c(c1)CCO2>O1CCCC1>OCc1ccc2c(c1)CCO2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-481ec1a85eb24912b47c7efbb63a5f15
CS(=O)(=O)Cl.OCc1ccc2c(c1)CCO2>>ClCc1ccc2c(c1)CCO2
O1C2=C(CC1)C=C(C=C2)CO.C(C)N(CC)CC.CS(=O)(=O)Cl>>O1C2=C(CC1)C=C(C=C2)CCl
CS(=O)(=O)[Cl:1].O[CH2:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][O:11]2>>[Cl:1][CH2:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[CH2:9][CH2:10][O:11]2
CS(=O)(=O)Cl.OCc1ccc2c(c1)CCO2
ClCc1ccc2c(c1)CCO2
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_sulfonyl chloride
58d25ddf86b8daa38762ecb08ed922faa2d01716f69924f9b8413703fe1b3fc7
d5d71bad4297b1f4f93dd1d1d9cddf0bb6fadb3f4dca1f84369c4074a39097d6
c1ccc2c(c1)CCO2
C-S(=O)(=O)-[Cl;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
100
[{"value": 100.0, "product": "O1C2=C(CC1)C=C(C=C2)CCl", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.9, "product": "O1C2=C(CC1)C=C(C=C2)CCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of (2,3-dihydrobenzo[b]furan-5-yl)methanol (1.5 g, 10 mmol) in dichloromethane (10 mL) were added under ice-cooling triethylamine (1.67 mL, 12 mmol) and methanesulfonyl chloride (0.85 mL, 10 mmol) and the mixture was stirred at room temperature for 1 h. The solvent was evaporated under reduced pressure an...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Primary halide
null
null
c1ccc2c(c1)CCO2
HO-
ClCCl
null
1
CS(=O)(=O)Cl.OCc1ccc2c(c1)CCO2>ClCCl>ClCc1ccc2c(c1)CCO2
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-32baeeeecd374a7189596c7a144284aa
CI.CN(C)C=O.O=C(O)c1ccc(O)c(Cl)c1>>COC(=O)c1ccc(OC)c(Cl)c1
O.ClC=1C=C(C(=O)O)C=CC1O.C([O-])([O-])=O.[K+].[K+].CI.CN(C=O)C>>ClC=1C=C(C(=O)OC)C=CC1OC
I[CH3:1].CN(C=O)[CH3:10].[OH:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([OH:9])[c:11]([Cl:12])[cH:13]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]([O:9][CH3:10])[c:11]([Cl:12])[cH:13]1
CI.CN(C)C=O.O=C(O)c1ccc(O)c(Cl)c1
COC(=O)c1ccc(OC)c(Cl)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4e302a5c4b5749a27005cfac332d21a67cd4b03cabc4b79c56523042a9f3f68a
11e44eaefaffcf2f4bedaafd68334cfa44459302a483454fd2d2ec963968ffac
c1ccccc1
C-N(-[CH3;D1;+0:1])-C=O.I-[CH3;D1;+0:2].[O;D1;H0:3]=[C:4](-[OH;D1;+0:5])-[c:6].[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[CH3;D1;+0:2]-[O;H0;D2;+0:5]-[C:4](=[O;D1;H0:3])-[c:6].[CH3;D1;+0:1]-[O;H0;D2;+0:7]-[c:8](:[c:9]):[c:10]
100
[{"value": 100.0, "product": "ClC=1C=C(C(=O)OC)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}]
60
CELSIUS
2
HOUR
To a solution of 3-chloro-4-hydroxybenzoic acid (3.45 g, 20 mmol) in N,N-dimethylformamide (10 mL) were added potassium carbonate (6.9 g, 50 mmol) and methyl iodide (large excess) and the mixture was stirred at 60° C. for 2 h. Water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amide.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1
HI
null
60
2
CI.CN(C)C=O.O=C(O)c1ccc(O)c(Cl)c1>>COC(=O)c1ccc(OC)c(Cl)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-2bf43f8c975c483f9da765c710675886
COC(=O)c1ccc(OC)c(Cl)c1>>COc1ccc(CO)cc1Cl
ClC=1C=C(C(=O)OC)C=CC1OC.[H-].[Al+3].[Li+].[H-].[H-].[H-].Cl>>ClC=1C=C(CO)C=CC1OC
CO[C:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:10]([Cl:11])[cH:9]1)=[O:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[cH:9][c:10]1[Cl:11]
COC(=O)c1ccc(OC)c(Cl)c1
COc1ccc(CO)cc1Cl
null
null
O1CCCC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[c:5]
106.2
[{"value": 100.0, "product": "ClC=1C=C(CO)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 106.2, "product": "ClC=1C=C(CO)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of methyl 3-chloro-4-methoxybenzoate (1.2 g, 6 mmol) in tetrahydrofuran (10 ml) was added under ice-cooling lithium aluminum hydride (455 mg, 12 mmol) and the mixture was stirred at room temperature for 1 h. The reaction mixture was stirred under ice-cooling and 0.1N hydrochloric acid was added. The mixtu...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccccc1
Other
O1CCCC1
null
1
COC(=O)c1ccc(OC)c(Cl)c1>O1CCCC1>COc1ccc(CO)cc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-e4e85b88e8b940a682a714ca09b108c4
COc1ccc(CO)cc1Cl.CS(=O)(=O)Cl>>COc1ccc(CCl)cc1Cl
ClC=1C=C(CO)C=CC1OC.C(C)N(CC)CC.CS(=O)(=O)Cl>>ClC=1C=C(CCl)C=CC1OC
O[CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:10]([Cl:11])[cH:9]1.CS(=O)(=O)[Cl:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][Cl:8])[cH:9][c:10]1[Cl:11]
COc1ccc(CO)cc1Cl.CS(=O)(=O)Cl
COc1ccc(CCl)cc1Cl
null
null
O1CCCC1
Functional Group Interconversion
Alcohol to chloride_sulfonyl chloride
58d25ddf86b8daa38762ecb08ed922faa2d01716f69924f9b8413703fe1b3fc7
d5d71bad4297b1f4f93dd1d1d9cddf0bb6fadb3f4dca1f84369c4074a39097d6
c1ccccc1
C-S(=O)(=O)-[Cl;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
61.1
[{"value": 61.0, "product": "ClC=1C=C(CCl)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.1, "product": "ClC=1C=C(CCl)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of 3-chloro-4-methoxybenzyl alcohol (1.1 g, 6 mmol) in tetrahydrofuran (5 mL) were added under ice-cooling triethylamine (1.67 mL, 12 mmol) and methanesulfonyl chloride (0.51 ml, 6 mmol) and the mixture was stirred at room temperature for 18 h. The solvent was evaporated under reduced pressure and the obt...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Primary halide
null
null
c1ccccc1
HO-
O1CCCC1
null
18
COc1ccc(CO)cc1Cl.CS(=O)(=O)Cl>O1CCCC1>COc1ccc(CCl)cc1Cl
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-731e44cf7bd248f291c99babee57228d
COc1ccc(C=O)cc1F>>COc1ccc(CO)cc1F
FC=1C=C(C=O)C=CC1OC.[BH4-].[Na+]>>FC=1C=C(CO)C=CC1OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[cH:9][c:10]1[F:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[cH:9][c:10]1[F:11]
COc1ccc(C=O)cc1F
COc1ccc(CO)cc1F
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
100
[{"value": 100.0, "product": "FC=1C=C(CO)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.5, "product": "FC=1C=C(CO)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 3-fluoro-4-methoxybenzaldehyde (1 g, 6.5 mmol) in methanol (15 mL) was added under ice-cooling sodium borohydride (378 mg, 10 mmol) and the mixture was stirred at room temperature for 1 h. The solvent was evaporated under reduced pressure and the obtained residue was dissolved in ethyl acetate. The org...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1
null
CO
null
1
COc1ccc(C=O)cc1F>CO>COc1ccc(CO)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-c80cfa37516948f992096c6023c594af
COc1ccc(CO)cc1F.CS(=O)(=O)Cl>>COc1ccc(CCl)cc1F
FC=1C=C(CO)C=CC1OC.C(C)N(CC)CC.CS(=O)(=O)Cl>>FC=1C=C(CCl)C=CC1OC
O[CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:10]([F:11])[cH:9]1.CS(=O)(=O)[Cl:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][Cl:8])[cH:9][c:10]1[F:11]
COc1ccc(CO)cc1F.CS(=O)(=O)Cl
COc1ccc(CCl)cc1F
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_sulfonyl chloride
58d25ddf86b8daa38762ecb08ed922faa2d01716f69924f9b8413703fe1b3fc7
d5d71bad4297b1f4f93dd1d1d9cddf0bb6fadb3f4dca1f84369c4074a39097d6
c1ccccc1
C-S(=O)(=O)-[Cl;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
100
[{"value": 100.0, "product": "FC=1C=C(CCl)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.9, "product": "FC=1C=C(CCl)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 3-fluoro-4-methoxybenzyl alcohol (1 g, 6.5 mmol) in dichloromethane (10 mL) were added under ice-cooling triethylamine (1.8 mL, 13 mmol) and methanesulfonyl chloride (0.60 mL, 7 mmol) and the mixture was stirred at room temperature for 30 min. The solvent was evaporated under reduced pressure and the o...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Primary halide
null
null
c1ccccc1
HO-
ClCCl
null
0.5
COc1ccc(CO)cc1F.CS(=O)(=O)Cl>ClCCl>COc1ccc(CCl)cc1F
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-0c167f9a9f1b44cc9678a067bdab38e6
CI.O=Cc1ccc(O)cc1Cl>>COc1ccc(C=O)c(Cl)c1
O.ClC1=C(C=O)C=CC(=C1)O.C([O-])([O-])=O.[K+].[K+].CI>>ClC1=C(C=O)C=CC(=C1)OC
I[CH3:1].[OH:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[c:9]([Cl:10])[cH:11]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[c:9]([Cl:10])[cH:11]1
CI.O=Cc1ccc(O)cc1Cl
COc1ccc(C=O)c(Cl)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
b8b041187bac58376aae824630608e7deb49a01db3d652291f8b379c10d4e434
0f0966e3597a58033417ecee71659f4d0c082f95d46b1e52c95541e6e4a59086
c1ccccc1
I-[CH3;D1;+0:1].[OH;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
71
[{"value": 70.0, "product": "ClC1=C(C=O)C=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.0, "product": "ClC1=C(C=O)C=CC(=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of 2-chloro-4-hydroxybenzaldehyde (2 g, 12.8 mmol) in N,N-dimethylformamide (25 mL) were added potassium carbonate (3.46 g, 25 mmol) and methyl iodide (large excess) and the mixture was stirred at room temperature for 18 h. Water was added to the reaction mixture and the mixture was extracted with ethyl a...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Ether
null
null
c1ccccc1
HI
CN(C=O)C
null
18
CI.O=Cc1ccc(O)cc1Cl>CN(C=O)C>COc1ccc(C=O)c(Cl)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-8f16daff33a54d7dbea2b1c031fe1318
COc1ccc(C=O)c(Cl)c1>>COc1ccc(CO)c(Cl)c1
ClC1=C(C=O)C=CC(=C1)OC.[BH4-].[Na+]>>ClC1=C(CO)C=CC(=C1)OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[c:9]([Cl:10])[cH:11]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][OH:8])[c:9]([Cl:10])[cH:11]1
COc1ccc(C=O)c(Cl)c1
COc1ccc(CO)c(Cl)c1
null
null
CO
Reduction
Reduction of aldehydes and ketones to alcohols
e7895795cd3f75445716c94697823c5929dcd4b5344525875fe75d36bca2f9d7
21bb81d5469aaaca71ab12c186bea4016451717fad8780cf288858a7d8fbc55a
c1ccccc1
[O;H0;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[OH;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
97
[{"value": 97.0, "product": "ClC1=C(CO)C=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.6, "product": "ClC1=C(CO)C=CC(=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 2-chloro-4-methoxybenzaldehyde (1.55 g, 9 mmol) in methanol (20 mL) was added under ice-cooling sodium borohydride (378 mg, 10 mmol) and the mixture was stirred at room temperature for 30 min. The solvent was evaporated under reduced pressure and the obtained residue was dissolved in ethyl acetate. The...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Primary alcohol
null
null
c1ccccc1
null
CO
null
0.5
COc1ccc(C=O)c(Cl)c1>CO>COc1ccc(CO)c(Cl)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-b00621e1ea214c459e6cb56650daa47b
COc1ccc(CO)c(Cl)c1.CS(=O)(=O)Cl>>COc1ccc(CCl)c(Cl)c1
ClC1=C(CO)C=CC(=C1)OC.C(C)N(CC)CC.CS(=O)(=O)Cl>>ClC1=C(CCl)C=CC(=C1)OC
O[CH2:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:11][c:9]1[Cl:10].CS(=O)(=O)[Cl:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][Cl:8])[c:9]([Cl:10])[cH:11]1
COc1ccc(CO)c(Cl)c1.CS(=O)(=O)Cl
COc1ccc(CCl)c(Cl)c1
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_sulfonyl chloride
58d25ddf86b8daa38762ecb08ed922faa2d01716f69924f9b8413703fe1b3fc7
d5d71bad4297b1f4f93dd1d1d9cddf0bb6fadb3f4dca1f84369c4074a39097d6
c1ccccc1
C-S(=O)(=O)-[Cl;H0;D1;+0:1].O-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
61
[{"value": 61.0, "product": "ClC1=C(CCl)C=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.8, "product": "ClC1=C(CCl)C=CC(=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 2-chloro-4-methoxybenzyl alcohol (1.5 g, 8.7 mmol) in dichloromethane (10 mL) were added under ice-cooling triethylamine (2.4 mL, 17.4 mmol) and methanesulfonyl chloride (0.74 mL, 9.5 mmol) and the mixture was stirred at room temperature for 2 h. The solvent was evaporated under reduced pressure and th...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Primary halide
null
null
c1ccccc1
HO-
ClCCl
null
2
COc1ccc(CO)c(Cl)c1.CS(=O)(=O)Cl>ClCCl>COc1ccc(CCl)c(Cl)c1
ord_dataset-0387783899c642a8b7eb4ba379bcdf5d
ord-9d6f264348c148c5921ef355a3645ed6
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1O>>CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1OC(C)c1ccccc1
OC1=NC(=NC=C1C(=O)OCC)N1CCC2=CC=CC=C12.OC1=NC(=NC=C1C(=O)OCC)N1[C@@H](CC2=CC=CC=C12)C>>C[C@H]1N(C2=CC=CC=C2C1)C1=NC=C(C(=N1)OC(C)C1=CC=CC=C1)C(=O)OCC
CCOC(=O)c1cnc(N2[CH2:24][CH2:23][c:25]3[cH:26][cH:27][cH:28][cH:29][c:30]32)nc1O.[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[CH2:17][C@H:18]2[CH3:19])[n:20][c:21]1[OH:22]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][n:8][c:9]([N:10]2[c:11]3[cH:12][cH:13][cH:...
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1O
CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1OC(C)c1ccccc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
2724f80c2567a4f114f4a243ee529f50ccfc2f75653a37ba7ef63b9c8def247e
3d147d59f10970b97131a934c589965ca51508f13649cb58509581dd98eb4186
c1ccc(COc2ccnc(N3CCc4ccccc43)n2)cc1
C-C-O-C(=O)-c1:c:n:c(-N2-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c;H0;D3;+0:5]-2:[c:6]:[c:7]):n:c:1-O.[#8:8]-[C:9](=[O;D1;H0:10])-[c:11]1:[c:12]:[#7;a:13]:[c:14]:[#7;a:15]:[c:16]:1-[OH;D1;+0:17]>>[#8:8]-[C:9](=[O;D1;H0:10])-[c:11]1:[c:12]:[#7;a:13]:[c:14]:[#7;a:15]:[c:16]:1-[O;H0;D2;+0:17]-[CH;D3;+0:2](-[CH3;D1;+0:1...
null
[]
null
null
null
null
In the same manner as in Reference Example 3-1 using ethyl 4-hydroxy-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate and ethyl 4-hydroxy-2-[(R)-2-methyl-2,3-dihydro-1H-indol-1-yl]-5-pyrimidinecarboxylate as starting materials, compounds of Reference Examples 26 and 27 were synthesized. Conditions: See reaction.no...
10.6084/m9.figshare.5104873.v1
null
Ester.Aromatic alcohol.Aromatic alcohol.Tertiary amine
Ether
c1cncnc1.c1ccc2c(c1)CCN2
c1ccccc1
c1cncnc1.c1ccc2c(c1)CC[NH]2.c1ccccc1
HO-
null
null
null
CCOC(=O)c1cnc(N2CCc3ccccc32)nc1O.CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1O>>CCOC(=O)c1cnc(N2c3ccccc3C[C@H]2C)nc1OC(C)c1ccccc1