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-c3a75813d0b24864aa4f7cd526efd6aa
ord-0838bc27829a48ddb77a3ea2f05dfa4b
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(F)c1>>CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1F
FC1=C(C=CC(=C1)F)NS(=O)(=O)C1CCCC=C1C(=O)OCC.FC1=C(C=CC(=C1)F)CS>>FC1=C(CSC2CCCC=C2C(=O)OCC)C=CC(=C1)F
O=S(=O)(Nc1ccc(F)cc1F)[CH:11]1[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][CH2:8][CH2:9][CH2:10]1.[SH:12][CH2:13][c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][c:20]1[F:21]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[CH:7][CH2:8][CH2:9][CH2:10][CH:11]1[S:12][CH2:13][c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][c:20]1[F:21]
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(F)c1
CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1F
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
e004b55701497d7f887b0985a65eca3bb4adb702fb3d6e33c5b8a4e402b31ab3
cfa39748e584de8627741a4eb08a3e46f3d1f6ce86fafef224e3e259ec2309d6
C1=CC(SCc2ccccc2)CCC1
F-c1:c:c:c(-N-S(=O)(=O)-[CH;D3;+0:1]2-[C:2]-[C:3]-[C:4]-[C:5]=[C:6]-2-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10]):c(-F):c:1.[SH;D1;+0:11]-[C:12]-[c:13]>>[C:10]-[#8:9]-[C:7](=[O;D1;H0:8])-[C:6]1=[C:5]-[C:4]-[C:3]-[C:2]-[CH;D3;+0:1]-1-[S;H0;D2;+0:11]-[C:12]-[c:13]
45
[{"value": 45.0, "product": "FC1=C(CSC2CCCC=C2C(=O)OCC)C=CC(=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In the same manner as in Reference Example 1, ethyl 6-[N-(2,4-difluorophenyl)sulfamoyl]-1-cyclohexene-1-carboxylate (455 mg) and (2,4-difluorophenyl)-methanethiol (421 mg) were reacted to give ethyl 6-[(2,4-difluorobenzyl)sulfanyl]-1-cyclohexene-1-carboxylate (185 mg) as a colorless oil. Conditions: See reaction.notes....
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Aromatic halide.Aromatic halide.Aliphatic thiol
Monosulfide
c1ccccc1.C1=CCCCC1
C1=CCCCC1
C1=CCCCC1.c1ccccc1
HF
null
null
null
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(F)c1>>CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3feff6d5a39d4247b999e4775af002e6
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(Cl)c1>>CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1Cl
FC1=C(C=CC(=C1)F)NS(=O)(=O)C1CCCC=C1C(=O)OCC.ClC1=C(C=CC(=C1)F)CS>>ClC1=C(CSC2CCCC=C2C(=O)OCC)C=CC(=C1)F
O=S(=O)(Nc1ccc(F)cc1F)[CH:11]1[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[CH:7][CH2:8][CH2:9][CH2:10]1.[SH:12][CH2:13][c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][c:20]1[Cl:21]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[CH:7][CH2:8][CH2:9][CH2:10][CH:11]1[S:12][CH2:13][c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][c:20]1[Cl:21]
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(Cl)c1
CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1Cl
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
e004b55701497d7f887b0985a65eca3bb4adb702fb3d6e33c5b8a4e402b31ab3
cfa39748e584de8627741a4eb08a3e46f3d1f6ce86fafef224e3e259ec2309d6
C1=CC(SCc2ccccc2)CCC1
F-c1:c:c:c(-N-S(=O)(=O)-[CH;D3;+0:1]2-[C:2]-[C:3]-[C:4]-[C:5]=[C:6]-2-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10]):c(-F):c:1.[SH;D1;+0:11]-[C:12]-[c:13]>>[C:10]-[#8:9]-[C:7](=[O;D1;H0:8])-[C:6]1=[C:5]-[C:4]-[C:3]-[C:2]-[CH;D3;+0:1]-1-[S;H0;D2;+0:11]-[C:12]-[c:13]
78.6
[{"value": 78.6, "product": "ClC1=C(CSC2CCCC=C2C(=O)OCC)C=CC(=C1)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In the same manner as in Reference Example 1, ethyl 6-[N-(2,4-difluorophenyl)sulfamoyl]-1-cyclohexene-1-carboxylate (835 mg) and (2-chloro-4-fluorophenyl)-methanethiol (853 mg) were reacted to give ethyl 6-[(2-chloro-4-fluorobenzyl)sulfanyl]-1-cyclohexene-1-carboxylate (625 mg) as a colorless oil. Conditions: See react...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Aromatic halide.Aromatic halide.Aliphatic thiol
Monosulfide
c1ccccc1.C1=CCCCC1
C1=CCCCC1
C1=CCCCC1.c1ccccc1
HF
null
null
null
CCOC(=O)C1=CCCCC1S(=O)(=O)Nc1ccc(F)cc1F.Fc1ccc(CS)c(Cl)c1>>CCOC(=O)C1=CCCCC1SCc1ccc(F)cc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b62278c274db46dcb1e9e75703cc9117
CCOC(=O)C1=C(S)COCC1.O.[O-]B1OO1>>CCOC(=O)C1=C(S(=O)(=O)O)COCC1
B1(OO1)[O-].O.O.O.O.[Na+].SC1=C(CCOC1)C(=O)OCC>>C(C)OC(=O)C1=C(COCC1)S(=O)(=O)O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([SH:8])[CH2:12][O:13][CH2:14][CH2:15]1.[OH2:10].O1B([O-:9])[O:11]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([S:8](=[O:9])(=[O:10])[OH:11])[CH2:12][O:13][CH2:14][CH2:15]1
CCOC(=O)C1=C(S)COCC1.O.[O-]B1OO1
CCOC(=O)C1=C(S(=O)(=O)O)COCC1
null
null
C(C)(=O)O
Oxidation
OtherReaction
758743a35c9f016e87fe2fb3df23bd0cb8d344cfb036e3d974e04ecd9b5c862b
aff842b1e0544720c37b2e5de00aad8b4ddf1a80763bf6e57aac3b66d41b30f2
C1=CCOCC1
[#8:1]-[C:2]-[C:3](-[SH;D1;+0:4])=[C:5](-[C:6](-[#8:7])=[O;D1;H0:8])-[C:9].[O-;H0;D1:10]-B1-O-[O;H0;D2;+0:11]-1.[OH2;D0;+0:12]>>[#8:1]-[C:2]-[C:3](-[S;H0;D4;+0:4](=[O;H0;D1;+0:12])(=[O;H0;D1;+0:10])-[OH;D1;+0:11])=[C:5](-[C:6](-[#8:7])=[O;D1;H0:8])-[C:9]
219.9
[{"value": 219.9, "product": "C(C)OC(=O)C1=C(COCC1)S(=O)(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
Sodium perborate tetrahydrate (24.5 g) was added to acetic acid (130 ml) and the mixture was heated to 50–55° C. Thereto was added dropwise a solution of ethyl 5-sulfanyl-3,6-dihydro-2H-pyran-4-carboxylate (10.0 g) in acetic acid (30 ml) over 2 h. The mixture was stirred at 50–55° C. for 3 h, and the reaction mixture w...
10.6084/m9.figshare.5104873.v1
null
Peroxide
Sulfonic acid
B1OO1
null
C1=CCOCC1
HO-.B
C(C)(=O)O
null
3
CCOC(=O)C1=C(S)COCC1.O.[O-]B1OO1>C(C)(=O)O>CCOC(=O)C1=C(S(=O)(=O)O)COCC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-56f544069272408e88280cef3c65fcbf
CCOC(=O)C1=C(S(=O)(=O)O)COCC1.O=S(Cl)Cl>>CCOC(=O)C1=C(S(=O)(=O)Cl)COCC1
C(C)OC(=O)C1=C(COCC1)S(=O)(=O)O.S(=O)(Cl)Cl>>ClS(=O)(=O)C1=C(CCOC1)C(=O)OCC
O[S:8]([C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[CH2:15][CH2:14][O:13][CH2:12]1)(=[O:9])=[O:10].O=S(Cl)[Cl:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([S:8](=[O:9])(=[O:10])[Cl:11])[CH2:12][O:13][CH2:14][CH2:15]1
CCOC(=O)C1=C(S(=O)(=O)O)COCC1.O=S(Cl)Cl
CCOC(=O)C1=C(S(=O)(=O)Cl)COCC1
null
null
null
Functional Group Interconversion
OtherReaction
1d60417dbcce8291d459a7fb34824cf29ea6f69a30ac46aeb585ac8e7b69013e
4a93b4a9749514113cd3dffa44b64f21b1f88d26b8739299bcad711fe7a13a1b
C1=CCOCC1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[C:5](=[C:6](-[C:7](-[#8:8])=[O;D1;H0:9])-[C:10])-[C:11]-[#8:12]>>[#8:12]-[C:11]-[C:5](-[S;H0;D4;+0:2](-[Cl;H0;D1;+0:1])(=[O;D1;H0:3])=[O;D1;H0:4])=[C:6](-[C:7](-[#8:8])=[O;D1;H0:9])-[C:10]
null
[]
85
CELSIUS
3
HOUR
4-(Ethoxycarbonyl)-5,6-dihydro-2H-pyran-3-sulfonic acid (27.5 g) was dissolved in thionyl chloride (82.6 ml) and the mixture was stirred at room temperature →85° C. for 3 h. The reaction mixture was concentrated to dryness under reduced pressure and the residue was dissolved in ethyl acetate (100 ml). The obtained solu...
10.6084/m9.figshare.5104873.v1
null
Sulfonic acid
Sulfonyl halide
null
null
C1=CCOCC1
HCl
null
85
3
CCOC(=O)C1=C(S(=O)(=O)O)COCC1.O=S(Cl)Cl>>CCOC(=O)C1=C(S(=O)(=O)Cl)COCC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c2ba31c2284e4a64a1f0849c2bdeeb97
Cc1c(O)ccc(OCC(=O)c2ccccc2)c1C>>Cc1c(O)cc2c(-c3ccccc3)coc2c1C
OC1=C(C(=C(OCC(=O)C2=CC=CC=C2)C=C1)C)C.O>>CC1=C(C2=C(C(=CO2)C2=CC=CC=C2)C=C1O)C
O=[C:7]([c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[CH2:14][O:15][c:16]1[cH:6][cH:5][c:3]([OH:4])[c:2]([CH3:1])[c:17]1[CH3:18]>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][c:6]2[c:7](-[c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)[cH:14][o:15][c:16]2[c:17]1[CH3:18]
Cc1c(O)ccc(OCC(=O)c2ccccc2)c1C
Cc1c(O)cc2c(-c3ccccc3)coc2c1C
null
null
C=1(C(=CC=CC1)C)C
Aromatic Heterocycle Formation
OtherReaction
41440ef63bdcad0549de493ff63648d9e9e6255c65e521389e251312ab757f94
a162075685c9eb50256a00ee0ecfa14ba2a448fd0344b073a356637e7fa80d08
c1ccc(-c2coc3ccccc23)cc1
O=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[O;H0;D2;+0:3]-[c:4](:[c:5]):[cH;D2;+0:6]:[c:7]:[c:8])-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[c:13]:[c:12]:[c;H0;D3;+0:9](-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[o;H0;D2;+0:3]:[c:4](:[c:5]):[c;H0;D3;+0:6]:1:[c:7]:[c:8]):[c:10]:[c:11]
50
[{"value": 50.0, "product": "CC1=C(C2=C(C(=CO2)C2=CC=CC=C2)C=C1O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
150
CELSIUS
5
HOUR
A mixture of 2-(4-hydroxy-2,3-dimethyl-phenoxy)-1-phenyl-ethanone (1.2 g, 4.70 mmol) and polyphosphoric acid (ca. 100 mg) in xylene (10 mL) was stirred at 150° C. for 5 h. The mixture was poured into water, extracted with ethylacetate, washed and dried to give 6,7-dimethyl-3-phenyl-benzofuran-5-ol (560 mg) as a light b...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether
null
c1ccccc1
c1ccc2occc2c1
c1ccccc1.c1ccc2occc2c1
HO-
C=1(C(=CC=CC1)C)C
150
5
Cc1c(O)ccc(OCC(=O)c2ccccc2)c1C>C=1(C(=CC=CC1)C)C>Cc1c(O)cc2c(-c3ccccc3)coc2c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d619a21ed5a948189dcf96e79df7704d
CC(=O)Oc1cc(C(C)=O)c(O)c(C)c1C>>CC(=O)c1cc(O)c(C)c(C)c1O
O.OC1=C(C=C(C(=C1C)C)OC(C)=O)C(C)=O.C([O-])([O-])=O.[K+].[K+].Cl.O>>OC1=C(C=C(C(=C1C)C)O)C(C)=O
CC(=O)[O:7][c:6]1[cH:5][c:4]([C:2]([CH3:1])=[O:3])[c:12]([OH:13])[c:10]([CH3:11])[c:8]1[CH3:9]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]([OH:7])[c:8]([CH3:9])[c:10]([CH3:11])[c:12]1[OH:13]
CC(=O)Oc1cc(C(C)=O)c(O)c(C)c1C
CC(=O)c1cc(O)c(C)c(C)c1O
null
null
CO
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
db7d50f1ad65e3456617ab9bc6ab5b9ede0e069a6dd971d117a653e2a40b05de
efe1c37482b229370967d04d1a68db10ee663983a92b84fa0f009f5bb178597f
c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
86.3
[{"value": 86.3, "product": "OC1=C(C=C(C(=C1C)C)O)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
The phenylethanone of Step 2 (500 mg) was dissolved in MeOH (20 mL), and potassium carbonate (1 eq.) was added followed by water (1 mL). The mixture was stirred at room temperature for 1 h, and then was poured into water. The solution was acidified with HCl and a precipitate was formed. The precipitate was collected an...
10.6084/m9.figshare.5104873.v1
null
Ester
Aromatic alcohol
null
null
c1ccccc1
HO-
CO
null
1
CC(=O)Oc1cc(C(C)=O)c(O)c(C)c1C>CO>CC(=O)c1cc(O)c(C)c(C)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0dedfd9308af4bb791ec2fa3e6564c11
C1=COCCC1.CC(=O)c1cc(O)c(C)c(C)c1O>>CC(=O)c1cc(OC2CCCCO2)c(C)c(C)c1O
OC1=C(C=C(C(=C1C)C)O)C(C)=O.O1CCCC=C1.C1(=CC=C(C=C1)S(=O)(=O)[O-])C.[NH+]1=CC=CC=C1>>OC1=C(C=C(C(=C1C)C)OC1OCCCC1)C(C)=O
[CH:8]1=[CH:9][CH2:10][CH2:11][CH2:12][O:13]1.[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]([OH:7])[c:14]([CH3:15])[c:16]([CH3:17])[c:18]1[OH:19]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]([O:7][CH:8]2[CH2:9][CH2:10][CH2:11][CH2:12][O:13]2)[c:14]([CH3:15])[c:16]([CH3:17])[c:18]1[OH:19]
C1=COCCC1.CC(=O)c1cc(O)c(C)c(C)c1O
CC(=O)c1cc(OC2CCCCO2)c(C)c(C)c1O
null
null
ClCCl
Heteroatom Alkylation and Arylation
oxa-Michael addition
1c7c788bec8addec628516b12629525fab255984248a4af23c71106a7726e25d
da6d2e768f263ce18da31b53a21ee41abe25d00717257e942f83f912a04f86d8
c1ccc(OC2CCCCO2)cc1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1):[c:10]
null
[]
null
null
4
HOUR
1-(2,5-Dihydroxy-3,4-dimethyl-phenyl)-ethanone of Step 3 (275 mg) was dissolved in dichloromethane (20 mL) and 3,4-dihydro-2H-pyran (0.2 mL) was added followed by pyridinium p-toluenesulfonate (PPTS) (30 mg). The mixture was stirred at room temperature for 4 h. The mixture was dried over MgSO4 and purified on silica ge...
10.6084/m9.figshare.5104873.v1
null
Ether.Aromatic alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
c1ccccc1.C1CCOCC1
null
ClCCl
null
4
C1=COCCC1.CC(=O)c1cc(O)c(C)c(C)c1O>ClCCl>CC(=O)c1cc(OC2CCCCO2)c(C)c(C)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6cf1ac37f0c3467b85144d07fc359468
CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1>>CC(=O)c1cc2cc(O)c(C)c(C)c2o1
OC1=C(C=O)C=C(C(=C1C)C)O.CC1=C(C2=C(C=C(O2)C(C)=O)C=C1OC1OCCCC1)C.O>>OC=1C(=C(C2=C(C=C(O2)C(C)=O)C1)C)C
C1CCC([O:9][c:8]2[cH:7][c:6]3[cH:5][c:4]([C:2]([CH3:1])=[O:3])[o:15][c:14]3[c:12]([CH3:13])[c:10]2[CH3:11])OC1>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][c:6]2[cH:7][c:8]([OH:9])[c:10]([CH3:11])[c:12]([CH3:13])[c:14]2[o:15]1
CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1
CC(=O)c1cc2cc(O)c(C)c(C)c2o1
null
Cl
CO
Reduction
OtherReaction
b5ceb9e953399e2a3f2f3d503c3846f04ccb158d8f8d4f3b209561e13fedc821
3165f563067f8d27bb50b0da034e3e854d1ead7f745de7cf575f7ca4cf677789
c1ccc2occc2c1
[c:1]:[c:2](-[O;H0;D2;+0:3]-C1-C-C-C-C-O-1):[c:4]>>[OH;D1;+0:3]-[c:2](:[c:1]):[c:4]
62.9
[{"value": 62.9, "product": "OC=1C(=C(C2=C(C=C(O2)C(C)=O)C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 1-[6,7-dimethyl-5-(tetrahydro-pyran-2-yloxy)-benzofuran-2-yl]-ethanone (1.1 g) (prepared from 2,5-dihydroxy-3,4-dimethyl-benzaldehyde following the procedure of Steps 3, 4 and 5 of Example 13) and conc. HCl (10 drops) in MeOH (20 mL) was stirred at room temperature for 2 h. Water was poured into the mixtur...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol
C1CCOCC1
null
c1ccc2occc2c1
HO-
Cl.CO
null
2
CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1>Cl.CO>CC(=O)c1cc2cc(O)c(C)c(C)c2o1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3d4f7692cf52494abd0a18c6db39fe8c
BrBr.CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1>>CC(=O)c1oc2c(C)c(C)c(O)cc2c1Br
CC1=C(C2=C(C=C(O2)C(C)=O)C=C1OC1OCCCC1)C.BrBr>>BrC1=C(OC2=C1C=C(C(=C2C)C)O)C(C)=O
Br[Br:16].C1CCC([O:12][c:11]2[c:9]([CH3:10])[c:7]([CH3:8])[c:6]3[o:5][c:4]([C:2]([CH3:1])=[O:3])[cH:15][c:14]3[cH:13]2)OC1>>[CH3:1][C:2](=[O:3])[c:4]1[o:5][c:6]2[c:7]([CH3:8])[c:9]([CH3:10])[c:11]([OH:12])[cH:13][c:14]2[c:15]1[Br:16]
BrBr.CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1
CC(=O)c1oc2c(C)c(C)c(O)cc2c1Br
null
null
C(Cl)(Cl)Cl
Functional Group Interconversion
OtherReaction
2c6f0975c32686d0299e1e32358c3adcdf96823c5abe80aa310f5798e47d19f7
ff4dd98a50e7cd80a36487c4e40275cd61e3a78460a3a8623820553c89f26f44
c1ccc2occc2c1
Br-[Br;H0;D1;+0:1].[C;D1;H3:2]-[C:3](=[O;D1;H0:4])-[c:5]1:[#8;a:6]:[c:7]2:[c:8]:[c:9]:[c:10](-[O;H0;D2;+0:11]-C3-C-C-C-C-O-3):[c:12]:[c:13]:2:[cH;D2;+0:14]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:14]1:[c:13]2:[c:12]:[c:10](-[OH;D1;+0:11]):[c:9]:[c:8]:[c:7]:2:[#8;a:6]:[c:5]:1-[C:3](-[C;D1;H3:2])=[O;D1;H0:4]
null
[]
null
null
1
HOUR
To a solution of 1-[6,7-dimethyl-5-(tetrahydro-pyran-2-yloxy)-benzofuran-2-yl]-ethanone (200 mg) in chloroform (20 mL) was added bromine (120 mg). After 1 h, the solution was washed with water and dried over MgSO4 and concentrated. The residue was purified by silica gel column eluting with 10% hexane in DCM to give 1-(...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic halide.Aromatic alcohol
C1CCOCC1.c1ccc2occc2c1
c1ccc2occc2c1
c1ccc2occc2c1
HBr
C(Cl)(Cl)Cl
null
1
BrBr.CC(=O)c1cc2cc(OC3CCCCO3)c(C)c(C)c2o1>C(Cl)(Cl)Cl>CC(=O)c1oc2c(C)c(C)c(O)cc2c1Br
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f20c4532687d4372ba7b7e28df96a7db
BrBr.CC(=O)Oc1cc2cc(C(C)=O)oc2c(C)c1C>>CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C
C(C)(=O)OC=1C(=C(C2=C(C=C(O2)C(C)=O)C1)C)C.BrBr.BrBr>>BrCC(=O)C=1OC2=C(C1)C=C(C(=C2C)C)OC(C)=O
Br[Br:13].[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7]2[cH:8][c:9]([C:10](=[O:11])[CH3:12])[o:14][c:15]2[c:16]([CH3:17])[c:18]1[CH3:19]>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7]2[cH:8][c:9]([C:10](=[O:11])[CH2:12][Br:13])[o:14][c:15]2[c:16]([CH3:17])[c:18]1[CH3:19]
BrBr.CC(=O)Oc1cc2cc(C(C)=O)oc2c(C)c1C
CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C
null
null
C(Cl)(Cl)Cl
Functional Group Interconversion
Bromination
97ca6720945af5a02c450d33ec56e946521050f9771c27f9cfcb85f3477593f6
cb3e14519230141aa015a4cf9c960def3e60f01997e61621f62506924bfa15de
c1ccc2occc2c1
Br-[Br;H0;D1;+0:1].[#8;a:2]:[c:3]-[C:4](-[CH3;D1;+0:5])=[O;D1;H0:6]>>[#8;a:2]:[c:3]-[C:4](=[O;D1;H0:6])-[CH2;D2;+0:5]-[Br;H0;D1;+0:1]
83.6
[{"value": 83.6, "product": "BrCC(=O)C=1OC2=C(C1)C=C(C(=C2C)C)OC(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
70
CELSIUS
10
MINUTE
1-(5-Acetoxy-6,7-dimethyl-benzofuran-2-yl)-ethanone (83 mg) (prepared from 1-(5-hydroxy-6,7-dimethyl-benzofuran-2-yl)-ethanone from Example 14 with acetanhydride and pyridine), was dissolved in chloroform (10 mL). Bromine (50 mg) was added and the solution was stirred at 70° C. for 10 min. When the color of bromine dis...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary halide
null
null
c1ccc2occc2c1
HBr
C(Cl)(Cl)Cl
70
0.166667
BrBr.CC(=O)Oc1cc2cc(C(C)=O)oc2c(C)c1C>C(Cl)(Cl)Cl>CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b060b3d71c424ba2bba7ef8e1ba232ce
C1COCCN1.CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C>>CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C
BrCC(=O)C=1OC2=C(C1)C=C(C(=C2C)C)OC(C)=O.N1CCOCC1.C([O-])([O-])=O.[K+].[K+]>>CC1=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C=C1OC(C)=O)C
[NH:13]1[CH2:14][CH2:15][O:16][CH2:17][CH2:18]1.Br[CH2:12][C:10]([c:9]1[cH:8][c:7]2[cH:6][c:5]([O:4][C:2]([CH3:1])=[O:3])[c:23]([CH3:24])[c:21]([CH3:22])[c:20]2[o:19]1)=[O:11]>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7]2[cH:8][c:9]([C:10](=[O:11])[CH2:12][N:13]3[CH2:14][CH2:15][O:16][CH2:17][CH2:18]3)[o:19][c:20]2[c:21...
C1COCCN1.CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
505036e350a62516c632060eeae05d8239108a346b706af40653d2560d91da48
98b92c1800516dd6f2e7ad31e751bba9f02d8a8062f38a8945939bbe90ecca84
O=C(CN1CCOCC1)c1cc2ccccc2o1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]:[#8;a:5].[#8:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[#8;a:5]:[c:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#8:6]-[C:11]-[C:10]-1
89.8
[{"value": 89.8, "product": "CC1=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C=C1OC(C)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-bromo-1-(5-acetoxy-6,7-dimethyl-benzofuran-2-yl)-ethanone (47 mg) from Example 16, morpholine (15 mg), and potassium carbonate (25 mg) in acetone (10 mL) was stirred at room temperature for 30 min. It was then evaporated to dryness, and the residue was purified by silica gel column eluting with 5% MeOH ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Secondary amine
Ketone.Tertiary amine
C1COCCN1
C1COCC[NH]1
c1ccc2occc2c1.C1COCC[NH]1
HBr
CC(=O)C
null
null
C1COCCN1.CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C>CC(=O)C>CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4b842ae5328c45729c573b6344de6cb9
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C>>Cc1c(O)cc2cc(C(=O)CN3CCOCC3)oc2c1C
CC1=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C=C1OC(C)=O)C.C([O-])(O)=O.[Na+]>>OC=1C(=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C1)C)C
CC(=O)[O:4][c:3]1[c:2]([CH3:1])[c:20]([CH3:21])[c:19]2[c:6]([cH:5]1)[cH:7][c:8]([C:9](=[O:10])[CH2:11][N:12]1[CH2:13][CH2:14][O:15][CH2:16][CH2:17]1)[o:18]2>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][c:6]2[cH:7][c:8]([C:9](=[O:10])[CH2:11][N:12]3[CH2:13][CH2:14][O:15][CH2:16][CH2:17]3)[o:18][c:19]2[c:20]1[CH3:21]
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C
Cc1c(O)cc2cc(C(=O)CN3CCOCC3)oc2c1C
null
null
CO
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
db7d50f1ad65e3456617ab9bc6ab5b9ede0e069a6dd971d117a653e2a40b05de
efe1c37482b229370967d04d1a68db10ee663983a92b84fa0f009f5bb178597f
O=C(CN1CCOCC1)c1cc2ccccc2o1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
54.8
[{"value": 54.8, "product": "OC=1C(=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A solution of acetic acid 6,7-dimethyl-2-(2-morpholin-4-yl-acetyl)-benzofuran-5-yl ester (23 mg), prepared as in Example 17, in MeOH (10 mL) was stirred while sodium bicarbonate (10 mg) was added. Then the mixture was stirred at RT overnight, followed by evaporation to dryness. The residue was purified by silica gel co...
10.6084/m9.figshare.5104873.v1
null
Ester
Aromatic alcohol
null
null
c1ccc2occc2c1.C1COCC[NH]1
HO-
CO
null
8
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C>CO>Cc1c(O)cc2cc(C(=O)CN3CCOCC3)oc2c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8069000183dc4965a4d2ca5ec8fc21cf
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C>>Cc1c(O)cc2cc(C(O)CN3CCOCC3)oc2c1C
[BH4-].[Na+].CC1=C(C2=C(C=C(O2)C(CN2CCOCC2)=O)C=C1OC(C)=O)C.O>>OC(CN1CCOCC1)C=1OC2=C(C1)C=C(C(=C2C)C)O
CC(=O)[O:4][c:3]1[c:2]([CH3:1])[c:20]([CH3:21])[c:19]2[c:6]([cH:5]1)[cH:7][c:8]([C:9](=[O:10])[CH2:11][N:12]1[CH2:13][CH2:14][O:15][CH2:16][CH2:17]1)[o:18]2>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][c:6]2[cH:7][c:8]([CH:9]([OH:10])[CH2:11][N:12]3[CH2:13][CH2:14][O:15][CH2:16][CH2:17]3)[o:18][c:19]2[c:20]1[CH3:21]
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C
Cc1c(O)cc2cc(C(O)CN3CCOCC3)oc2c1C
null
null
CO
Reduction
OtherReaction
ba270c4e4c66c0ca4c384010b56cde71211c1d0a42b18d125d377e517b054cad
0ceccbeb1a171407aae4661a0628d0d4c1bc76338bade38dd330e39814e68322
c1ccc2oc(CCN3CCOCC3)cc2c1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]-[C:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9](:[c:10]):[#8;a:11]:[c:12]>>[#7:5]-[C:6]-[CH;D3;+0:7](-[OH;D1;+0:8])-[c:9](:[c:10]):[#8;a:11]:[c:12].[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
68.2
[{"value": 68.2, "product": "OC(CN1CCOCC1)C=1OC2=C(C1)C=C(C(=C2C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
A solution of acetic acid 6,7-dimethyl-2-(2-morpholin-4-yl-acetyl)-benzofuran-5-yl ester (35 mg), prepared as in Example 17, in MeOH (10 mL) was stirred while NaBH4 (40 mg) was added, and the mixture was stirred at room temperature for an additional 4 h. The mixture was poured into water, and extracted with ethylacetat...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Secondary alcohol.Aromatic alcohol
null
null
c1ccc2occc2c1.C1COCC[NH]1
Other
CO
null
4
CC(=O)Oc1cc2cc(C(=O)CN3CCOCC3)oc2c(C)c1C>CO>Cc1c(O)cc2cc(C(O)CN3CCOCC3)oc2c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e0bcad1b034343be927c12c829b6cd8e
CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C.CNC(C)O>>Cc1c(O)cc2cc(C3(O)CN(C)CCO3)oc2c1C
O.BrCC(=O)C=1OC2=C(C1)C=C(C(=C2C)C)OC(C)=O.CNC(C)O.C([O-])([O-])=O.[K+].[K+]>>OC=1C(=C(C2=C(C=C(O2)C2(CN(CCO2)C)O)C1)C)C
CC(=O)[O:4][c:3]1[c:2]([CH3:1])[c:19]([CH3:20])[c:18]2[c:6]([cH:5]1)[cH:7][c:8]([C:9](=[O:10])[CH2:11]Br)[o:17]2.[NH:12]([CH3:13])[CH:14]([CH3:15])[OH:16]>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][c:6]2[cH:7][c:8]([C:9]3([OH:10])[CH2:11][N:12]([CH3:13])[CH2:14][CH2:15][O:16]3)[o:17][c:18]2[c:19]1[CH3:20]
CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C.CNC(C)O
Cc1c(O)cc2cc(C3(O)CN(C)CCO3)oc2c1C
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
702b157a86a56e76aa494318df7090c3c53371fc4fa7e2c29c8f72ab027fdc87
7e3331757dd2f750754139bc304381506c0f2b6dafa5e616dfc0c9fb97b7c4df
c1ccc2oc(C3CNCCO3)cc2c1
Br-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[#8;a:6]:[c:7].C-C(=O)-[O;H0;D2;+0:8]-[c:9](:[c:10]):[c:11].[C;D1;H3:12]-[NH;D2;+0:13]-[CH;D3;+0:14](-[CH3;D1;+0:15])-[OH;D1;+0:16]>>[C;D1;H3:12]-[N;H0;D3;+0:13]1-[CH2;D2;+0:1]-[C;H0;D4;+0:2](-[OH;D1;+0:3])(-[c:4](:[c:5]):[#8;a:6]:[c:7])-[O;H0;D2;+0:16]-[CH...
78.2
[{"value": 78.2, "product": "OC=1C(=C(C2=C(C=C(O2)C2(CN(CCO2)C)O)C1)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A mixture of 2-bromo-1-(5-acetoxy-6,7-dimethyl-benzofuran-2-yl)-ethanone (30 mg), methylaminoethanol (7 mg), and potassium carbonate (20 mg) in acetone (10 mL) was stirred at RT for 1 h. The mixture was poured into water and extracted with ethylacetate. The organic layer was dried and evaporated followed by purificatio...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone.Ester.Secondary alcohol.Secondary amine
Ether.Tertiary alcohol.Aromatic alcohol.Tertiary amine
null
C1COCC[NH]1
c1ccc2occc2c1.C1COCC[NH]1
HBr
CC(=O)C
null
1
CC(=O)Oc1cc2cc(C(=O)CBr)oc2c(C)c1C.CNC(C)O>CC(=O)C>Cc1c(O)cc2cc(C3(O)CN(C)CCO3)oc2c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7de22d0f2eb54aa7921a13c19744900f
C1=COCCC1.Cc1c(O)cc(C=O)c(O)c1C>>Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C
OC1=C(C=O)C=C(C(=C1C)C)O.O1CCCC=C1.O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>OC1=C(C=O)C=C(C(=C1C)C)OC1OCCCC1
[CH:5]1=[CH:6][CH2:7][CH2:8][CH2:9][O:10]1.[CH3:1][c:2]1[c:3]([OH:4])[cH:11][c:12]([CH:13]=[O:14])[c:15]([OH:16])[c:17]1[CH3:18]>>[CH3:1][c:2]1[c:3]([O:4][CH:5]2[CH2:6][CH2:7][CH2:8][CH2:9][O:10]2)[cH:11][c:12]([CH:13]=[O:14])[c:15]([OH:16])[c:17]1[CH3:18]
C1=COCCC1.Cc1c(O)cc(C=O)c(O)c1C
Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C
null
null
ClCCl
Heteroatom Alkylation and Arylation
oxa-Michael addition
1c7c788bec8addec628516b12629525fab255984248a4af23c71106a7726e25d
da6d2e768f263ce18da31b53a21ee41abe25d00717257e942f83f912a04f86d8
c1ccc(OC2CCCCO2)cc1
[#8:1]1-[C:2]-[C:3]-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-1.[OH;D1;+0:7]-[c:8](:[c:9]):[c:10]>>[c:9]:[c:8](-[O;H0;D2;+0:7]-[CH;D3;+0:6]1-[#8:1]-[C:2]-[C:3]-[C:4]-[CH2;D2;+0:5]-1):[c:10]
49.8
[{"value": 49.8, "product": "OC1=C(C=O)C=C(C(=C1C)C)OC1OCCCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2,5-Dihydroxy-3,4-dimethyl-benzaldehyde (2.0 g) was dissolved in dichloromethane (50 mL) and 3,4-dihydro-2H-pyran (1.5 g) was added followed by addition of p-toluenesulfonic acid monohydrate (200 mg). The solution was stirred at room temperature for 1 hour and quenched by adding sodium bicarbonate solution (1 mL). Then...
10.6084/m9.figshare.5104873.v1
null
Ether.Aromatic alcohol
Ether.Ether
C1=COCCC1
C1CCOCC1
c1ccccc1.C1CCOCC1
null
ClCCl
null
1
C1=COCCC1.Cc1c(O)cc(C=O)c(O)c1C>ClCCl>Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4343c0c6effe4c3a9e64392e14908cdb
COC(=O)CBr.Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C>>COC(=O)COc1c(C=O)cc(OC2CCCCO2)c(C)c1C
O.OC1=C(C=O)C=C(C(=C1C)C)OC1OCCCC1.BrCC(=O)OC.C([O-])([O-])=O.[K+].[K+]>>COC(COC1=C(C(=C(C=C1C=O)OC1OCCCC1)C)C)=O
Br[CH2:5][C:3]([O:2][CH3:1])=[O:4].[OH:6][c:7]1[c:8]([CH:9]=[O:10])[cH:11][c:12]([O:13][CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][O:19]2)[c:20]([CH3:21])[c:22]1[CH3:23]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][O:6][c:7]1[c:8]([CH:9]=[O:10])[cH:11][c:12]([O:13][CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][O:19]2)[c:20]([CH3:21])[c:22...
COC(=O)CBr.Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C
COC(=O)COc1c(C=O)cc(OC2CCCCO2)c(C)c1C
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
50d675b335c583a6ce22e1164b27a78b18b9ca447d45137820c344bcb6369217
0865de4e1853c59ac25437e36fd18b03329566cb9eff4b4f0ce70d5714692fd3
c1ccc(OC2CCCCO2)cc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C;D1;H3:5].[O;D1;H0:6]=[C:7]-[c:8]:[c:9](-[OH;D1;+0:10]):[c:11]>>[C;D1;H3:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[O;H0;D2;+0:10]-[c:9](:[c:11]):[c:8]-[C:7]=[O;D1;H0:6]
51.8
[{"value": 51.8, "product": "COC(COC1=C(C(=C(C=C1C=O)OC1OCCCC1)C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A mixture of 2-hydroxy-3,4-dimethyl-5-(tetrahydro-pyran-2-yloxy)-benzaldehyde (150 mg) from Step 1, methyl bromoacetate (180 mg) and potassium carbonate (200 mg) in DMF (10 mL) was stirred at room temperature for 2 hours. Then the solution was poured into water and extracted with ethylacetate. The ethyl acetate was was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Aromatic alcohol
Ester.Ether
null
null
c1ccccc1.C1CCOCC1
HBr
CN(C)C=O
null
2
COC(=O)CBr.Cc1c(OC2CCCCO2)cc(C=O)c(O)c1C>CN(C)C=O>COC(=O)COc1c(C=O)cc(OC2CCCCO2)c(C)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-85a2f5e267c84706804a0fc80444029f
COC(=O)c1cc2cc(O)c(C)c(C)c2o1>>Cc1c(O)cc2cc(CO)oc2c1C
COC(=O)C=1OC2=C(C1)C=C(C(=C2C)C)O.[H-].[Al+3].[Li+].[H-].[H-].[H-].O>>OCC=1OC2=C(C1)C=C(C(=C2C)C)O
CO[C:9]([c:8]1[cH:7][c:6]2[cH:5][c:3]([OH:4])[c:2]([CH3:1])[c:13]([CH3:14])[c:12]2[o:11]1)=[O:10]>>[CH3:1][c:2]1[c:3]([OH:4])[cH:5][c:6]2[cH:7][c:8]([CH2:9][OH:10])[o:11][c:12]2[c:13]1[CH3:14]
COC(=O)c1cc2cc(O)c(C)c(C)c2o1
Cc1c(O)cc2cc(CO)oc2c1C
null
null
C1CCOC1
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc2occc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c:3](:[c:4]):[#8;a:5]:[c:6]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[c:3](:[c:4]):[#8;a:5]:[c:6]
44.1
[{"value": 44.1, "product": "OCC=1OC2=C(C1)C=C(C(=C2C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
5-Hydroxy-6,7-dimethyl-benzofuran-2-carboxylic acid methyl ester (231 mg) prepared as in Example 2, was dissolved in THF and lithium aluminum hydride (93 mg) was added. The mixture was stirred at room temperature for 4 h. Then the solution was poured into water and extracted with ethylacetate. The ethyl acetate was was...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccc2occc2c1
Other
C1CCOC1
null
4
COC(=O)c1cc2cc(O)c(C)c(C)c2o1>C1CCOC1>Cc1c(O)cc2cc(CO)oc2c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e258e6a24542474ba0381f930f986120
CC(C)N(C(C)C)P(N)(=O)Cl.O=P([O-])(OCc1ccccc1)OCc1ccccc1>>CCOP(=O)(C#N)OCC
[O-]P([O-])(=O)OP(=O)([O-])[O-].P(OC(C)(C)C)(OC(C)(C)C)[O-].C(C1=CC=CC=C1)OP(=O)(OCC1=CC=CC=C1)[O-].C(C)(C)N(P(=O)(N)Cl)C(C)C>>C(C)OP(OCC)(=O)C#N
CC(N(P(=O)(Cl)[NH2:7])[CH:9]([CH3:1])[CH3:10])[CH3:6].[O-][P:4]([O:3][CH2:2]c1ccccc1)(=[O:5])[O:8]Cc1ccccc1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([C:6]#[N:7])[O:8][CH2:9][CH3:10]
CC(C)N(C(C)C)P(N)(=O)Cl.O=P([O-])(OCc1ccccc1)OCc1ccccc1
CCOP(=O)(C#N)OCC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
44945b48395c0ab715d6891c1001b38acdb76a09553e58c9b624fd3237cd5516
690ee693a3915ef015ee0ffe4e5bdd5a8963af32bdddfda193db21e9d178f8b9
null
C-C(-[CH3;D1;+0:1])-N(-[CH;D3;+0:2](-[C;D1;H3:3])-[CH3;D1;+0:4])-P(-Cl)(=O)-[NH2;D1;+0:5].[O-]-[P;H0;D4;+0:6](=[O;D1;H0:7])(-[#8:8]-[CH2;D2;+0:9]-c1:c:c:c:c:c:1)-[O;H0;D2;+0:10]-C-c1:c:c:c:c:c:1>>[C;D1;H3:3]-[CH2;D2;+0:2]-[O;H0;D2;+0:10]-[P;H0;D4;+0:6](=[O;D1;H0:7])(-[#8:8]-[CH2;D2;+0:9]-[CH3;D1;+0:4])-[C;H0;D2;+0:1]#[...
null
[]
null
null
null
null
In order to try different protecting groups on the phosphate, several other methods of phosphorylation were attempted. These included the use of alkylamidophosphines, which have been shown to readily phosphorylate alcohols and phenols in high yield. For example, di-tert-butyloxy (N,N-diisopropylamido)phosphine, prepare...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Tertiary amine
Nitrile
c1ccccc1.c1ccccc1
null
null
HCl
null
null
null
CC(C)N(C(C)C)P(N)(=O)Cl.O=P([O-])(OCc1ccccc1)OCc1ccccc1>>CCOP(=O)(C#N)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-553c413765554627bebc5f8dec940306
COc1ccc(C=O)c(OC)c1OC>>COc1ccc(C=O)c(O)c1O
Cl.B(Cl)(Cl)Cl.C([O-])(O)=O.[Na+].COC1=C(C=O)C=CC(=C1OC)OC.B(Cl)(Cl)Cl>>OC1=C(C=O)C=CC(=C1O)OC
C[O:10][c:9]1[c:6]([CH:7]=[O:8])[cH:5][cH:4][c:3]([O:2][CH3:1])[c:11]1[O:12]C>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]=[O:8])[c:9]([OH:10])[c:11]1[OH:12]
COc1ccc(C=O)c(OC)c1OC
COc1ccc(C=O)c(O)c1O
null
null
ClCCl.CCCCCC.C(C)(=O)OCC
Deprotection
OtherReaction
a0f05885bbc65ae2846cad0ac34029941211b2ef3a426958b0c8aa83bb16fe86
9df751cd682ad9d54ed75d7313aaead6a019c5d37ede15c4672866d319b900ff
c1ccccc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]-[C:4]=[O;D1;H0:5]):[c:6](-[O;H0;D2;+0:7]-C):[c:8]>>[O;D1;H0:5]=[C:4]-[c:3]:[c:2](-[OH;D1;+0:1]):[c:6](-[OH;D1;+0:7]):[c:8]
null
[]
null
null
2
HOUR
An anhydrous dichloromethane (500 mL) solution of 2,3,4-trimethoxy-benzaldehyde (6a, 19.6 g, 100 mmol) under argon at ambient temperature was stirred for 10 min and boron trichloride (100 mL, 100 mmol, 1 eq, 1.0 M soln in dichloromethane) was added. After 2 hours, the second equivalent of boron trichloride (100 mL, 100...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
null
null
c1ccccc1
Other
ClCCl.CCCCCC.C(C)(=O)OCC
null
2
COc1ccc(C=O)c(OC)c1OC>ClCCl.CCCCCC.C(C)(=O)OCC>COc1ccc(C=O)c(O)c1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f9af51249e6348399a70185518c0bc2d
CCCCCC1=CCCC1=O.COC(=O)CC(=O)OC>>CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC
C(CCCC)C=1C(CCC1)=O.C(CC(=O)OC)(=O)OC.C[O-].[Na+]>>C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6]1=[CH:11][CH2:10][CH2:9][C:7]1=[O:8].[CH2:12]([C:13](=[O:14])[O:15][CH3:16])[C:17](=[O:18])[O:19][CH3:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH:12]([C:13](=[O:14])[O:15][CH3:16])[C:17](=[O:18])[O:19][CH3:20]
CCCCCC1=CCCC1=O.COC(=O)CC(=O)OC
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC
null
null
null
C-C Coupling
OtherReaction
fd506cf634d55bf99e34f898f8d1975a1f72a9379fefd16d2e5845f9cf3c8814
898e66379ea5c9946b068a7796ddcf4c38fd80e0571f55d1ac4ead7978c7ea75
O=C1CCCC1
[C;D1;H3:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C;D1;H3:9].[C:10]-[C:11]-[C;H0;D3;+0:12]1=[CH;D2;+0:13]-[C:14]-[C:15]-[C:16]-1=[O;D1;H0:17]>>[C:10]-[C:11]-[CH;D3;+0:12]1-[C:16](=[O;D1;H0:17])-[C:15]-[C:14]-[CH;D3;+0:13]-1-[CH;D3;+0:5](-[C:3](=[O;D1;H0:4])-[#8:2]-[C;D1;H3:1])-[C:6](=[O;D...
93.8
[{"value": 93.8, "product": "C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
2
HOUR
The reaction product was refined to obtain 95 g (0.6 mol) of 2-pentyl-2-cyclopentenone. Moreover, 95 g (0.6 mol) of 2-pentyl-2-cyclopentenone was dropped to a solution, prepared by dissolving 118 g (0.9 mol) of dimethyl malonate in 38 g of methanol anhydride in a nitrogen atmosphere, cooling the mixture to 0° C. and ad...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Ester
Ketone.Ester.Ester
C1=CCCC1
C1CCCC1
C1CCCC1
null
null
0
2
CCCCCC1=CCCC1=O.COC(=O)CC(=O)OC>>CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7b77438f2ab34e7bb8042f94df2cf5a7
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O>>CCCCCC1C(=O)CCC1CC(=O)OC
C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)CC(=O)O>>C(CCCC)C1C(CCC1=O)CC(=O)OC
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)O[CH3:16].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH2:12][C:13](=[O:14])[OH:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH2:12][C:13](=[O:14])[O:15][CH3:16]
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O
CCCCCC1C(=O)CCC1CC(=O)OC
null
null
O
Heteroatom Alkylation and Arylation
O-methylation
584c206b70fd291cdfaa6a3fc8fb3b571f5864638d82543702ab3d931c144f86
43fdfffe15a01c77924b1c923a99c979d5ae5cf13440224e510e701641bf99be
O=C1CCCC1
C-C-C-C-C-C1-C(-C(-C(=O)-O-C)-C(=O)-O-[CH3;D1;+0:1])-C-C-C-1=O.[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
97.4
[{"value": 97.3, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.4, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A 1 L four-neck flask equipped with a stirrer, a supply unit, a thermometer and a rectifier was charged with 600 g of raw material containing 545 g (1.92 mol) of dimethyl 2-pentyl-3-oxo-cyclopentylmalonate produced in the same manner as in Production Example 1 and the raw material was heated to 180° C. with stirring un...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Ester.Ester
Ester
C1CCCC1
null
C1CCCC1
HO-
O
null
16
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O>O>CCCCCC1C(=O)CCC1CC(=O)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-adb75d18fb8c449a94b5109ee5f32ae9
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC>>CCCCCC1C(=O)CCC1CC(=O)OC
C(CCCC)C1C(CCC1=O)CC(=O)O.C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC>>C(CCCC)C1C(CCC1=O)CC(=O)OC
COC(=O)[CH:12]([CH:11]1[CH:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[C:7](=[O:8])[CH2:9][CH2:10]1)[C:13](=[O:14])[O:15][CH3:16]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH2:12][C:13](=[O:14])[O:15][CH3:16]
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC
CCCCCC1C(=O)CCC1CC(=O)OC
null
null
O
Reduction
Decarboxylation
33f176f6ce02426b2726e71e3c19f64673952a2b50dd48518b89a08efe25965b
b45711df98eaf2a3f54e3027da3f1b57580ab2f6d54e9ac2a56731961e64969a
O=C1CCCC1
C-O-C(=O)-[CH;D3;+0:1](-[C:2](-[C:3])-[C:4]-[C:5]=[O;D1;H0:6])-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10]>>[C:3]-[C:2](-[CH2;D2;+0:1]-[C:7](=[O;D1;H0:8])-[#8:9]-[C;D1;H3:10])-[C:4]-[C:5]=[O;D1;H0:6]
90.8
[{"value": 90.7, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.8, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
9
HOUR
The same 1 L four-neck flask that was used in Example 1 was charged with 600 g of raw material containing 557 g (1.96 mol) of dimethyl 2-pentyl-3-oxo-cyclopentylmalonate produced in the same manner as in Production Example 1 and the raw material was heated to 180° C. with stirring under normal pressure. Then, the suppl...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Ester
null
null
C1CCCC1
HO-
O
null
9
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC>O>CCCCCC1C(=O)CCC1CC(=O)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-442cb6effe204e93a42b49768d720102
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O>>CCCCCC1C(=O)CCC1CC(=O)OC
C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)C(C(=O)OC)C(=O)OC.C(CCCC)C1C(CCC1=O)CC(=O)O>>C(CCCC)C1C(CCC1=O)CC(=O)OC
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)O[CH3:16].[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH2:12][C:13](=[O:14])[OH:15]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]1[C:7](=[O:8])[CH2:9][CH2:10][CH:11]1[CH2:12][C:13](=[O:14])[O:15][CH3:16]
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O
CCCCCC1C(=O)CCC1CC(=O)OC
null
null
O
Heteroatom Alkylation and Arylation
O-methylation
584c206b70fd291cdfaa6a3fc8fb3b571f5864638d82543702ab3d931c144f86
43fdfffe15a01c77924b1c923a99c979d5ae5cf13440224e510e701641bf99be
O=C1CCCC1
C-C-C-C-C-C1-C(-C(-C(=O)-O-C)-C(=O)-O-[CH3;D1;+0:1])-C-C-C-1=O.[C:2]-[C:3](=[O;D1;H0:4])-[OH;D1;+0:5]>>[C:2]-[C:3](=[O;D1;H0:4])-[O;H0;D2;+0:5]-[CH3;D1;+0:1]
96
[{"value": 96.0, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.9, "product": "C(CCCC)C1C(CCC1=O)CC(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
The same 1 L four-neck flask that was used in Example 1 was charged with 600 g of raw material containing 550 g (1.94 mol) of dimethyl 2-pentyl-3-oxo-cyclopentylmalonate produced in the same manner as in Production Example 1 and the raw material was heated to 215° C. with stirring under normal pressure. Then, the suppl...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ketone.Ester.Ester
Ester
C1CCCC1
null
C1CCCC1
HO-
O
null
4
CCCCCC1C(=O)CCC1C(C(=O)OC)C(=O)OC.CCCCCC1C(=O)CCC1CC(=O)O>O>CCCCCC1C(=O)CCC1CC(=O)OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8793196be2554b07b1b776d773339178
CCCCCCCC(=O)Cl.CCO[Si](CCCS)(OCC)OCC>>CCCCCCCC(=O)SCCC[Si](OCC)(OCC)OCC
C(CCCCCCC)(=O)Cl.N#N.SCCC[Si](OCC)(OCC)OCC.[SiH4]>>C(CCCCCCC)(=O)SCCC[Si](OCC)(OCC)OCC
Cl[C:8]([CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:9].[SH:10][CH2:11][CH2:12][CH2:13][Si:14]([O:15][CH2:16][CH3:17])([O:18][CH2:19][CH3:20])[O:21][CH2:22][CH3:23]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][C:8](=[O:9])[S:10][CH2:11][CH2:12][CH2:13][Si:14]([O:15][CH2:16][CH3:17])([O:18][CH2:19][CH3:20...
CCCCCCCC(=O)Cl.CCO[Si](CCCS)(OCC)OCC
CCCCCCCC(=O)SCCC[Si](OCC)(OCC)OCC
null
null
CCCCCC.C(C)N(CC)CC
Acylation
thioether_nucl_sub
774e8f449f87493fdbd93fdbbfef7c7bc086966dfce8806abcb487630046ef59
cf70b55890699bc889b230d5ae9783daf8be8d20d1ad4c06197ffaf659088f4e
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6]-[SH;D1;+0:7]>>[C:5]-[C:6]-[S;H0;D2;+0:7]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
87
[{"value": 87.0, "product": "C(CCCCCCC)(=O)SCCC[Si](OCC)(OCC)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.8, "product": "C(CCCCCCC)(=O)SCCC[Si](OCC)(OCC)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Into a 12-liter, three-necked round bottom flask equipped with mechanical stirrer, addition funnel, thermocouple, heating mantle, N2 inlet, and temperature controller were charged 1,021 grams of 3-mercaptopropyltriethoxysilane (SILQUEST® A-1891 silane from OSi Specialties, Inc., a subsidiary of Crompton Corp. of Greenw...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aliphatic thiol
Carbo-thioester
null
null
null
HCl
CCCCCC.C(C)N(CC)CC
null
null
CCCCCCCC(=O)Cl.CCO[Si](CCCS)(OCC)OCC>CCCCCC.C(C)N(CC)CC>CCCCCCCC(=O)SCCC[Si](OCC)(OCC)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a2cdc9ab8298469c92bf748bc8239564
CCO[Si](CCCCl)(OCC)OCC.O=C(O)Cc1cccs1>>CCO[Si](CCCSC(C)=O)(OCC)OCC
S1C(=CC=C1)CC(=O)O.[O-]CC.[Na+].ClCCC[Si](OCC)(OCC)OCC>>C(C)(=O)SCCC[Si](OCC)(OCC)OCC
Cl[CH2:7][CH2:6][CH2:5][Si:4]([O:3][CH2:2][CH3:1])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17].O[C:9]([CH2:10]c1ccc[s:8]1)=[O:11]>>[CH3:1][CH2:2][O:3][Si:4]([CH2:5][CH2:6][CH2:7][S:8][C:9]([CH3:10])=[O:11])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17]
CCO[Si](CCCCl)(OCC)OCC.O=C(O)Cc1cccs1
CCO[Si](CCCSC(C)=O)(OCC)OCC
null
null
S1C(=CC=C1)C(=O)O.C(C)O
Acylation
OtherReaction
63c844c1ec474495593d771b062be3364adf503c0822f2fd1bfb69f229709474
dfe9fe1a6355f40a3f716cb9a21cc73ccd389fac1a8bf4766414c46a9aa66845
null
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].O-[C;H0;D3;+0:4](=[O;D1;H0:5])-[CH2;D2;+0:6]-c1:[s;H0;D2;+0:7]:c:c:c:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:7]-[C;H0;D3;+0:4](-[CH3;D1;+0:6])=[O;D1;H0:5]
78
[{"value": 78.0, "product": "C(C)(=O)SCCC[Si](OCC)(OCC)OCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
This example illustrates the preparation of a thiocarboxylate alkoxysilane from a salt of a thiolcarboxylic acid using as a solvent the alcohol corresponding to the silane alkoxy group. Into a 250 ml, three-neck round bottomed flask equipped with magnetic stir bar, temperature probe/controller, heating mantle, addition...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Carbo-thioester
c1ccsc1
null
null
HCl
S1C(=CC=C1)C(=O)O.C(C)O
null
null
CCO[Si](CCCCl)(OCC)OCC.O=C(O)Cc1cccs1>S1C(=CC=C1)C(=O)O.C(C)O>CCO[Si](CCCSC(C)=O)(OCC)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e50976b1d03a405c8b69ff3c747f0580
CCO[Si](CCl)(OCC)OCC.O=C(O)Cc1cccs1>>CCO[Si](CSC(C)=O)(OCC)OCC
N#N.S1C(=CC=C1)CC(=O)O.ClC[Si](OCC)(OCC)OCC.S1C(=CC=C1)C(=O)O.[O-]CC.[Na+]>>C(C)(=O)SC[Si](OCC)(OCC)OCC
Cl[CH2:5][Si:4]([O:3][CH2:2][CH3:1])([O:10][CH2:11][CH3:12])[O:13][CH2:14][CH3:15].O[C:7]([CH2:8]c1ccc[s:6]1)=[O:9]>>[CH3:1][CH2:2][O:3][Si:4]([CH2:5][S:6][C:7]([CH3:8])=[O:9])([O:10][CH2:11][CH3:12])[O:13][CH2:14][CH3:15]
CCO[Si](CCl)(OCC)OCC.O=C(O)Cc1cccs1
CCO[Si](CSC(C)=O)(OCC)OCC
null
null
COCCOCCOC
Acylation
OtherReaction
63c844c1ec474495593d771b062be3364adf503c0822f2fd1bfb69f229709474
dfe9fe1a6355f40a3f716cb9a21cc73ccd389fac1a8bf4766414c46a9aa66845
null
Cl-[CH2;D2;+0:1]-[#14:2](-[#8:3]-[C:4]-[C;D1;H3:5])(-[#8:6]-[C:7]-[C;D1;H3:8])-[#8:9]-[C:10]-[C;D1;H3:11].O-[C;H0;D3;+0:12](=[O;D1;H0:13])-[CH2;D2;+0:14]-c1:[s;H0;D2;+0:15]:c:c:c:1>>[C;D1;H3:5]-[C:4]-[#8:3]-[#14:2](-[#8:6]-[C:7]-[C;D1;H3:8])(-[#8:9]-[C:10]-[C;D1;H3:11])-[CH2;D2;+0:1]-[S;H0;D2;+0:15]-[C;H0;D3;+0:12](-[C...
55
[{"value": 55.0, "product": "C(C)(=O)SC[Si](OCC)(OCC)OCC", "details": "PERCENTYIELD", "is_desired": false}]
8
CELSIUS
null
null
This example illustrates the preparation of a thiocarboxylate alkoxysilane from a salt of a thiolcarboxylic acid using a nonprotic solvent. 88 grams of powdered sodium ethoxide and 600 ml diglyme were charged into a one-liter, three-neck round-bottomed flask equipped with magnetic stir bar, temperature probe/controller...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Carbo-thioester
c1ccsc1
null
null
HCl
COCCOCCOC
8
null
CCO[Si](CCl)(OCC)OCC.O=C(O)Cc1cccs1>COCCOCCOC>CCO[Si](CSC(C)=O)(OCC)OCC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-eda0b50d30a844b4a41d341f4fdb9a14
O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)[O-])c(O)c2O.O=S(=O)(O)Cl>>O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)Cl)c(O)c2O
ClS(=O)(=O)O.[Na+].OC=1C(=CC=2C(C3=CC=CC=C3C(C2C1O)=O)=O)S(=O)(=O)[O-]>>OC=1C(=CC=2C(C3=CC=CC=C3C(C2C1O)=O)=O)S(=O)(=O)Cl
[O-][S:15]([c:14]1[cH:13][c:12]2[c:11]([c:21]([OH:22])[c:19]1[OH:20])[C:9](=[O:10])[c:8]1[c:3]([cH:4][cH:5][cH:6][cH:7]1)[C:2]2=[O:1])(=[O:16])=[O:17].O=S(=O)(O)[Cl:18]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[c:11]2[c:12]1[cH:13][c:14]([S:15](=[O:16])(=[O:17])[Cl:18])[c:19]([OH:20])[c:21]2[OH:22...
O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)[O-])c(O)c2O.O=S(=O)(O)Cl
O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)Cl)c(O)c2O
null
null
null
Functional Group Interconversion
OtherReaction
1d60417dbcce8291d459a7fb34824cf29ea6f69a30ac46aeb585ac8e7b69013e
4a93b4a9749514113cd3dffa44b64f21b1f88d26b8739299bcad711fe7a13a1b
O=C1c2ccccc2C(=O)c2ccccc21
O-S(=O)(=O)-[Cl;H0;D1;+0:1].[O-]-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]1:[c:6]:[c:7](:[c:8](:[c:9](-[O;D1;H1:10]):[c:11]:1-[O;D1;H1:12])-[C:13](=[O;D1;H0:14])-[c:15])-[C:16]=[O;D1;H0:17]>>[Cl;H0;D1;+0:1]-[S;H0;D4;+0:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]1:[c:6]:[c:7](:[c:8](:[c:9](-[O;D1;H1:10]):[c:11]:1-[O;D1;...
66
[{"value": 66.0, "product": "OC=1C(=CC=2C(C3=CC=CC=C3C(C2C1O)=O)=O)S(=O)(=O)Cl", "details": "PERCENTYIELD", "is_desired": false}]
90
CELSIUS
null
null
3,4-dihydroxy-9,10-dioxo-2-anthracenesulfonic acid sodium salt (1.4 g, 3.9 mmoles) was combined with 30 mL of chlorosulfonic acid and heated to 90° C. for 5 hours, after which the solution was cooled to 0° C. and poured into 100 g of ice. After the ice melted the solution was extracted with CH2Cl2 (3×100 mL), methylene...
10.6084/m9.figshare.5104873.v1
null
Sulfonic acid
Sulfonyl halide
null
null
c1ccc2c(c1)Cc1ccccc1C2
HO-
null
90
null
O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)[O-])c(O)c2O.O=S(=O)(O)Cl>>O=C1c2ccccc2C(=O)c2c1cc(S(=O)(=O)Cl)c(O)c2O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b6db5d76b7944ff18a499f9e72331b8a
CC(C)=CCCl.Cc1cccc(C)c1O>>CC(C)=CCC1(C)CCC=C(C)C1=O
C(C=C(C)C)Cl.[H-].[Na+].CC1=C(C(=CC=C1)C)O.CO>>CC=1C(C(CCC1)(CC=C(C)C)C)=O
Cl[CH2:5][CH:4]=[C:2]([CH3:1])[CH3:3].[c:6]1([CH3:7])[cH:8][cH:9][cH:10][c:11]([CH3:12])[c:13]1[OH:14]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:13]1=[O:14]
CC(C)=CCCl.Cc1cccc(C)c1O
CC(C)=CCC1(C)CCC=C(C)C1=O
null
[Pd]
C1(=CC=CC=C1)C
Acylation
OtherReaction
6fffa0d222ffb075bcbc34d9c48f49de1c39007f8ab248d00542f709b46ecf62
42da64ec40e29427a46e8ef6b6ff47f2a7e2f11a2072895485933fd72aabade3
O=C1C=CCCC1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3](-[C;D1;H3:4])-[C;D1;H3:5].[C;D1;H3:6]-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+0:11](-[C;D1;H3:12]):[c;H0;D3;+0:13]:1-[OH;D1;+0:14]>>[C;D1;H3:6]-[C;H0;D3;+0:7]1=[CH;D2;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[C;H0;D4;+0:11](-[C;D1;H3:12])(-[CH2;D2;+0:1]-[C:2]=[C:3](-[C;D...
null
[]
50
CELSIUS
45
MINUTE
Sodium hydride (60%, 85 g, 2.13 mol) was added portionwise to a solution of 2,6-dimethylphenol (250 g, 2.05 mol) in 2 L of toluene at 10-15° C. The resulting suspension was stirred for 45 min. The mixture was cooled to 50° C., and prenyl chloride (262 g, 2.13 mol, 85%) was added during 1.5 h keeping the temperature at ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ketone
c1ccccc1
C1=CCCCC1
C1=CCCCC1
Other
[Pd].C1(=CC=CC=C1)C
50
0.75
CC(C)=CCCl.Cc1cccc(C)c1O>[Pd].C1(=CC=CC=C1)C>CC(C)=CCC1(C)CCC=C(C)C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-00827ff276b54f969f5cbc888a5ba452
CC(C)=CCC1(C)CCC=C(C)C1=O>>CC(C)=CCC1(C)CCC2CC2(C)C1=O
CC=1C(C(CCC1)(CC=C(C)C)C)=O.[H-].[Na+].[I-].C[S+](=O)(C)C.[H][H]>>CC12C(C(CCC2C1)(CC=C(C)C)C)=O
[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:12]([CH3:13])[C:14]1=[O:15]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]2[CH2:11][C:12]2([CH3:13])[C:14]1=[O:15]
CC(C)=CCC1(C)CCC=C(C)C1=O
CC(C)=CCC1(C)CCC2CC2(C)C1=O
null
null
O.CS(=O)C
C-C Coupling
OtherReaction
6383c24477e07121e04e7644483ae404183a2aa5a3feed555f1b575b70ffe352
6c72a64362b644ff7380f8d0c7bdda962edffb1f22535d7f0916fcd367b6b992
O=C1CCCC2CC12
[C;D1;H3:1]-[C;H0;D3;+0:2]1=[CH;D2;+0:3]-[C:4]-[C:5]-[C:6]-[C:7]-1=[O;D1;H0:8]>>[C;D1;H3:1]-[C;H0;D4;+0:2]12-[C:9]-[CH;D3;+0:3]-1-[C:4]-[C:5]-[C:6]-[C:7]-2=[O;D1;H0:8]
83
[{"value": 83.0, "product": "CC12C(C(CCC2C1)(CC=C(C)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Sodium hydride (60%, 2.11 g, 52.8 mmol) was added to a suspension of trimethylsulfoxonium iodide (11.6 g, 52.8 mmol) in 60 ml of dimethyl sulfoxide. The mixture was stirred for 30 min until hydrogen evolution stopped. 2,6-Dimethyl-6-(3-methyl-but-2-enyl)-cyclohex-2-enone was added and the mixture was stirred over night...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=CCCCC1
C1CCC2CC2C1
C1CCC2CC2C1
Other
O.CS(=O)C
null
null
CC(C)=CCC1(C)CCC=C(C)C1=O>O.CS(=O)C>CC(C)=CCC1(C)CCC2CC2(C)C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f9f153e8525b4067966b861eb0782cb3
CC(C)=CCC1(C)CCC=C(C)C1=O.CI>>CC(C)=CCC1(C)CC=CC(C)(C)C1=O
CC=1C(C(CCC1)(CC=C(C)C)C)=O.[Li+].CC(C)[N-]C(C)C.CI>>CC1(C(C(CC=C1)(CC=C(C)C)C)=O)C
[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:14]1=[O:15].I[CH3:13]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH:9]=[CH:10][C:11]([CH3:12])([CH3:13])[C:14]1=[O:15]
CC(C)=CCC1(C)CCC=C(C)C1=O.CI
CC(C)=CCC1(C)CC=CC(C)(C)C1=O
null
null
CC(C)(C)OC.C1CCOC1
C-C Coupling
OtherReaction
a5ed2f3bda8728aa6eb383f8aa7578c4b8c5323291d56fb502a1a0736d1e049b
6c72a64362b644ff7380f8d0c7bdda962edffb1f22535d7f0916fcd367b6b992
O=C1CC=CCC1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[C;H0;D3;+0:3]1=[CH;D2;+0:4]-[CH2;D2;+0:5]-[C:6]-[C:7]-[C:8]-1=[O;D1;H0:9]>>[C;D1;H3:2]-[C;H0;D4;+0:3]1(-[CH3;D1;+0:1])-[CH;D2;+0:4]=[CH;D2;+0:5]-[C:6]-[C:7]-[C:8]-1=[O;D1;H0:9]
null
[]
-78
CELSIUS
1
HOUR
2,6-Dimethyl-6-(3-methyl-but-2-enyl)-cyclohex-2-enone (5.00 g, 26 mmol) was added to a solution of LDA (prepared from diisopropylamine (3.15 g, 31.2 mmol) and n-BuLi (1.6M in hexane, 19.5 ml, 31.2 mmol)) in THF (50 ml) at −78° C. The mixture was stirred for 1 h at −78° C. Methyl iodide (5.54 g, 39 mmol) was added and t...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=CCCCC1
C1=CCCCC1
C1=CCCCC1
HI
CC(C)(C)OC.C1CCOC1
-78
1
CC(C)=CCC1(C)CCC=C(C)C1=O.CI>CC(C)(C)OC.C1CCOC1>CC(C)=CCC1(C)CC=CC(C)(C)C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f340efd2e2d0433dbd255d55b8ae8bf5
CC(C)=CCC1(C)CCC=C(C)C1=O>>CC(C)=CCC1(C)CCCC(C)C1=O
CC=1C(C(CCC1)(CC=C(C)C)C)=O.[O-]S(=O)S(=O)[O-].[Na+].[Na+]>>CC1(C(C(CCC1)C)=O)CC=C(C)C
[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:13]1=[O:14]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH2:10][CH:11]([CH3:12])[C:13]1=[O:14]
CC(C)=CCC1(C)CCC=C(C)C1=O
CC(C)=CCC1(C)CCCC(C)C1=O
null
null
null
Reduction
Hydrogenation (double to single)
36c089d27e46ae7bb4df3563f4ed1e4684984208b1f092ae42b91f9c5627fd64
0e0db21233797ec1d2a9464a1f32cef94e53e6a41f96d680fa1307067bbf01f2
O=C1CCCCC1
[C;D1;H3:1]-[C;H0;D3;+0:2]1=[CH;D2;+0:3]-[C:4]-[C:5]-[C:6]-[C:7]-1=[O;D1;H0:8]>>[C;D1;H3:1]-[CH;D3;+0:2]1-[CH2;D2;+0:3]-[C:4]-[C:5]-[C:6]-[C:7]-1=[O;D1;H0:8]
null
[]
null
null
null
null
This compound was prepared as a mixture of 2 isomers by reduction of 2,6-dimethyl-6-(3-methyl-but-2-enyl)-cyclohex-2-enone with Na2S2O4. 1H-NMR (400 MHz, CDCl3): 5.15-5.12, 4.94-4.89 (2m, 1H, 2′-H), 2.69-1.26 (m, 9H), 1.70, 1.68 (2s, 3H, 3′-CH3), 1.61, 1.60 (2s, 3H, 4′-H), 1.47, 0.98 (2s, 3H, 6-CH3), 1.00, 0.99 (2d, J=...
10.6084/m9.figshare.5104873.v1
null
Ketone
Ketone
C1=CCCCC1
C1CCCCC1
C1CCCCC1
null
null
null
null
CC(C)=CCC1(C)CCC=C(C)C1=O>>CC(C)=CCC1(C)CCCC(C)C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6dd357ae782d47b2bc25946eb45b099c
CC(C)=CCC1(C)CCC=C(C)C1=O>>CC(C)=CCC1(C)CCC=C(C)C1(C)O
CC=1C(C(CCC1)(CC=C(C)C)C)=O.C[Mg]Cl>>CC1(C(=CCCC1(CC=C(C)C)C)C)O
[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:13]1=[O:15]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:13]1([CH3:14])[OH:15]
CC(C)=CCC1(C)CCC=C(C)C1=O
CC(C)=CCC1(C)CCC=C(C)C1(C)O
null
null
C1(=CC=CC=C1)C.C1CCOC1
Miscellaneous
OtherReaction
82f307c2771f24472352179bfdcbd50ca1b6a8d7cf7b2748b565724a523407a8
8811b4d793f7cfa9f0f1f47a008648edabb54f371f76dfa680dd5b2e1564c6c5
C1=CCCCC1
[C:1]=[C:2]-[C:3]-[C:4]1(-[C;D1;H3:5])-[C:6]-[C:7]-[C:8]=[C:9](-[C;D1;H3:10])-[C;H0;D3;+0:11]-1=[O;H0;D1;+0:12]>>[C:1]=[C:2]-[C:3]-[C:4]1(-[C;D1;H3:5])-[C:6]-[C:7]-[C:8]=[C:9](-[C;D1;H3:10])-[C;H0;D4;+0:11]-1(-[C;D1;H3:13])-[OH;D1;+0:12]
78
[{"value": 78.0, "product": "CC1(C(=CCCC1(CC=C(C)C)C)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.0, "product": "CC1(C(=CCCC1(CC=C(C)C)C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
15
CELSIUS
45
MINUTE
2,6-Dimethyl-6-(3-methyl-but-2-enyl)-cyclohexenone (245 g, 1.28 mol) was added dropwise to a solution of methyl magnesium chloride (105 g, 1.41 mol) in THF (400 ml) and toluene (1.5 L) at room temperature. The temperature rose to 50° C. The mixture was stirred for additional 45 min, was then cooled to 15° C. and poured...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
C1=CCCCC1
C1=CCCCC1
C1=CCCCC1
Other
C1(=CC=CC=C1)C.C1CCOC1
15
0.75
CC(C)=CCC1(C)CCC=C(C)C1=O>C1(=CC=CC=C1)C.C1CCOC1>CC(C)=CCC1(C)CCC=C(C)C1(C)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-dd44bcdd9c8945a98b0da8058f632e23
CC(C)=CCC1(C)CCC=C(C)C1(C)O.CI>>COC1(C)C(C)=CCCC1(C)CC=C(C)C
CI.CC1(C(=CCCC1(CC=C(C)C)C)C)O.[Li]CCCC>>COC1(C(CCC=C1C)(CC=C(C)C)C)C
[OH:2][C:3]1([CH3:4])[C:5]([CH3:6])=[CH:7][CH2:8][CH2:9][C:10]1([CH3:11])[CH2:12][CH:13]=[C:14]([CH3:15])[CH3:16].I[CH3:1]>>[CH3:1][O:2][C:3]1([CH3:4])[C:5]([CH3:6])=[CH:7][CH2:8][CH2:9][C:10]1([CH3:11])[CH2:12][CH:13]=[C:14]([CH3:15])[CH3:16]
CC(C)=CCC1(C)CCC=C(C)C1(C)O.CI
COC1(C)C(C)=CCCC1(C)CC=C(C)C
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
cd10a9010f842ab825b304bd2965f17f9c39c4c64e5fc6cd91306ae51817de0d
9271b713ded6954f3329c61a211042ac37c82b3aff1b62cb455035e69339dd27
C1=CCCCC1
I-[CH3;D1;+0:1].[C:2]-[C:3](-[C;D1;H3:4])(-[OH;D1;+0:5])-[C:6](-[C;D1;H3:7])=[C:8]-[C:9]>>[C:2]-[C:3](-[C;D1;H3:4])(-[O;H0;D2;+0:5]-[CH3;D1;+0:1])-[C:6](-[C;D1;H3:7])=[C:8]-[C:9]
93.7
[{"value": 93.0, "product": "COC1(C(CCC=C1C)(CC=C(C)C)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.7, "product": "COC1(C(CCC=C1C)(CC=C(C)C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 1,2,6-trimethyl-6-(3-methyl-but-2-enyl)-cyclohex-2-enol (5.00 g, 24.0 mmol) in THF (80 ml) was added n-BuLi (1.6M in hexane, 16.5 ml, 26.4 mmol) at 0° C. After the mixture was stirred for 30 min, methyl iodide (5.18 g, 36.5 mmol) was added. The mixture was stirred at room temperature over night and the...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
C1=CCCCC1
HI
C1CCOC1
null
0.5
CC(C)=CCC1(C)CCC=C(C)C1(C)O.CI>C1CCOC1>COC1(C)C(C)=CCCC1(C)CC=C(C)C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8a4703e3c2844eb2a6fea95691c7e22c
CC(C)=CCC1(C)CCC=C(C)C1=O>>CC(C)=CCC1(C)CCC=C(C)C1O
CC=1C(C(CCC1)(CC=C(C)C)C)=O.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>CC=1C(C(CCC1)(CC=C(C)C)C)O
[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[C:13]1=[O:14]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH2:8][CH2:9][CH:10]=[C:11]([CH3:12])[CH:13]1[OH:14]
CC(C)=CCC1(C)CCC=C(C)C1=O
CC(C)=CCC1(C)CCC=C(C)C1O
null
null
C(C)OCC
Reduction
Reduction of ketone to secondary alcohol
363d5f69f20636c0e94be5dd25ac73c01a81378640b68ce139612b5190f90ea7
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
C1=CCCCC1
[C:1]=[C:2]-[C:3]-[C:4]1(-[C;D1;H3:5])-[C:6]-[C:7]-[C:8]=[C:9](-[C;D1;H3:10])-[C;H0;D3;+0:11]-1=[O;H0;D1;+0:12]>>[C:1]=[C:2]-[C:3]-[C:4]1(-[C;D1;H3:5])-[C:6]-[C:7]-[C:8]=[C:9](-[C;D1;H3:10])-[CH;D3;+0:11]-1-[OH;D1;+0:12]
98
[{"value": 98.0, "product": "CC=1C(C(CCC1)(CC=C(C)C)C)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 97.4, "product": "CC=1C(C(CCC1)(CC=C(C)C)C)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
2,6-Dimethyl-6-(3-methyl-but-2-enyl)-cyclohex-2-enone (5.00 g, 26.04 mmol) was added dropwise to a suspension of lithium aluminium hydride (0.73 g, 18.2 mmol) in diethyl ether at 0° C. The mixture was stirred at room temperature for 1 h. The resulting suspension was quenched with water, aqueous sodium hydroxide solutio...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
C1=CCCCC1
C1=CCCCC1
C1=CCCCC1
null
C(C)OCC
null
1
CC(C)=CCC1(C)CCC=C(C)C1=O>C(C)OCC>CC(C)=CCC1(C)CCC=C(C)C1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f7d02303c56544f8ad2d461477c161c2
CC(C)=CCCl.Cc1cccc(C)c1O>>CC(C)=CCC1(C)C=CC=C(C)C1=O
CC1=C(C(=CC=C1)C)O.[OH-].[K+].C(C=C(C)C)Cl>>CC=1C(C(C=CC1)(CC=C(C)C)C)=O
Cl[CH2:5][CH:4]=[C:2]([CH3:1])[CH3:3].[c:6]1([CH3:7])[cH:8][cH:9][cH:10][c:11]([CH3:12])[c:13]1[OH:14]>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][C:6]1([CH3:7])[CH:8]=[CH:9][CH:10]=[C:11]([CH3:12])[C:13]1=[O:14]
CC(C)=CCCl.Cc1cccc(C)c1O
CC(C)=CCC1(C)C=CC=C(C)C1=O
null
null
C1=CC=CC=C1
Acylation
OtherReaction
88fb5000ae461b24cd74d7407af653ba3d3fc4b2d1217911456ffd00ec357618
b4f30537787923ba4feee7b56623cd7e4096609819c2bebbb8bd88243f26f603
O=C1C=CC=CC1
Cl-[CH2;D2;+0:1]-[C:2]=[C:3](-[C;D1;H3:4])-[C;D1;H3:5].[C;D1;H3:6]-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[c;H0;D3;+0:11](-[C;D1;H3:12]):[c;H0;D3;+0:13]:1-[OH;D1;+0:14]>>[C;D1;H3:6]-[C;H0;D3;+0:7]1=[CH;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:10]-[C;H0;D4;+0:11](-[C;D1;H3:12])(-[CH2;D2;+0:1]-[C:2]=[C:3](-[C;D1;...
null
[]
0
CELSIUS
3
HOUR
A mixture of 2,6-dimethylphenol (5.00 g, 41.0 mmol), powdered KOH (85%, 1.5 eq., 4.05 g, 61.5 mmol), prenyl chloride (85%, 1.2 eq., 6.05 g, 49.2 mmol) and (NBu4)HSO4 (50 mg) in benzene (50 ml) was stirred at 0° C. for 3 h. The green suspension was then poured on ice and extracted with pentane. The organic phase was was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ketone.Conjugated diene
c1ccccc1
C1=CCCC=C1
C1=CCCC=C1
HCl
C1=CC=CC=C1
0
3
CC(C)=CCCl.Cc1cccc(C)c1O>C1=CC=CC=C1>CC(C)=CCC1(C)C=CC=C(C)C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-265cf475ddee42328a84105d9d35affc
CC(C)(C#N)c1ccccc1.O>>CC(C)(C=O)c1ccccc1
Cl.O.CC(C#N)(C)C1=CC=CC=C1.[H-].C(C(C)C)[Al+]CC(C)C>>CC(C=O)(C)C1=CC=CC=C1
N#[C:4][C:2]([CH3:1])([CH3:3])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1.[OH2:5]>>[CH3:1][C:2]([CH3:3])([CH:4]=[O:5])[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1
CC(C)(C#N)c1ccccc1.O
CC(C)(C=O)c1ccccc1
null
null
CCCCCC
Heteroatom Alkylation and Arylation
OtherReaction
26082e4725cd2a7c1eb6362fc44981286c2087c015aba2f1b570103659ffb41e
e783d65987caa6ceae095ff666413e4c8d25ead96c003eb4f99d66fc68c0b0bb
c1ccccc1
N#[C;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[c:5].[OH2;D0;+0:6]>>[C;D1;H3:3]-[C:2](-[C;D1;H3:4])(-[c:5])-[CH;D2;+0:1]=[O;H0;D1;+0:6]
92.8
[{"value": 92.8, "product": "CC(C=O)(C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
To a solution of 2-methyl-2-phenylpropanenitrile (290 g, 2.00 mol) in hexane (2000 mL) at 0° C. under N2 is added diisobutylaluminum hydride (DIBAL-H) (2600 mL, 1M in hexane) over a period of 80 minutes. The reaction mixture is stirred at 6–14° C. for 15 minutes, then allowed to warm to room temperature and stirred for...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Aldehyde
null
null
c1ccccc1
Other
CCCCCC
null
0.25
CC(C)(C#N)c1ccccc1.O>CCCCCC>CC(C)(C=O)c1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-dba42e243a1e4925a377154a69991339
CC(C)(C=O)c1ccccc1.CN.[C-]#N>>CNC(C#N)C(C)(C)c1ccccc1
[C-]#N.[K+].Cl.CN.CC(C=O)(C)C1=CC=CC=C1>>CC(C(C#N)NC)(C)C1=CC=CC=C1
O=[CH:3][C:6]([CH3:7])([CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1.[CH3:1][NH2:2].[C-:4]#[N:5]>>[CH3:1][NH:2][CH:3]([C:4]#[N:5])[C:6]([CH3:7])([CH3:8])[c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
CC(C)(C=O)c1ccccc1.CN.[C-]#N
CNC(C#N)C(C)(C)c1ccccc1
null
null
O.CO
Heteroatom Alkylation and Arylation
OtherReaction
67834ce29ee7faed9c771a892a45df3a078cc52972b167e999c188543c3ef065
8743950731596ea1e685ccc6d45d1ba830801fe94588e1dd93bbf1291f95e93b
c1ccccc1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[c:5].[C-;H0;D1:6]#[N;D1;H0:7].[C;D1;H3:8]-[NH2;D1;+0:9]>>[C;D1;H3:8]-[NH;D2;+0:9]-[CH;D3;+0:1](-[C;H0;D2;+0:6]#[N;D1;H0:7])-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[c:5]
95
[{"value": 95.0, "product": "CC(C(C#N)NC)(C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
25
HOUR
To a solution of potassium cyanide (103 g, 1.56 mol) and methylamine hydrochloride (106 g, 1.56 mol) in water (1000 mL) is added a solution of 2-methyl-2-phenylpropanal (222 g, 1.50 mol) in methanol (1000 mL) over a period of 30 minutes. An ice-water bath is used occasionally to maintain the reaction temperature betwee...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Nitrile.Secondary amine
null
null
c1ccccc1
HO-
O.CO
null
25
CC(C)(C=O)c1ccccc1.CN.[C-]#N>O.CO>CNC(C#N)C(C)(C)c1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-02dcb73ac3424272a81fdd4037603a1a
CC(C)(C=O)c1ccccc1.Cc1ccc([S@@](N)=O)cc1>>Cc1ccc([S@](=O)N=CC(C)(C)c2ccccc2)cc1
CC1(OC1C1=CC=CC=C1)C.CC(C=O)(C)C1=CC=CC=C1.C1(=CC=C(C=C1)[S@](=O)N)C>>CC(C=N[S@@](=O)C1=CC=C(C=C1)C)(C)C1=CC=CC=C1
O=[CH:9][C:10]([CH3:11])([CH3:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1.[CH3:1][c:2]1[cH:3][cH:4][c:5]([S@:6](=[O:7])[NH2:8])[cH:19][cH:20]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([S@:6](=[O:7])[N:8]=[CH:9][C:10]([CH3:11])([CH3:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:19][cH:20]1
CC(C)(C=O)c1ccccc1.Cc1ccc([S@@](N)=O)cc1
Cc1ccc([S@](=O)N=CC(C)(C)c2ccccc2)cc1
null
[O-]CC.[Ti+4].[O-]CC.[O-]CC.[O-]CC.FC1=C(C(=C(C(=C1B(C1=C(C(=C(C(=C1F)F)F)F)F)C1=C(C(=C(C(=C1F)F)F)F)F)F)F)F)F
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
54882f986dad145756472fc79464161665827db6af7b3780cb2b83c72b495424
3d6c7b6a0f29252ce5dcda36fa3ef05efc366c421f47850a88ae430c686fc79d
O=[S@](N=CCc1ccccc1)c1ccccc1
O=[CH;D2;+0:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[c:5].[NH2;D1;+0:6]-[#16:7](=[O;D1;H0:8])-[c:9]>>[C;D1;H3:3]-[C:2](-[C;D1;H3:4])(-[c:5])-[CH;D2;+0:1]=[N;H0;D2;+0:6]-[#16:7](=[O;D1;H0:8])-[c:9]
81
[{"value": 81.0, "product": "CC(C=N[S@@](=O)C1=CC=C(C=C1)C)(C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
25
CELSIUS
19
HOUR
To a stirred solution of 2.5 g of 2,2-dimethyl-3-phenyloxirane (16 mmol) in 85 mL of anhydrous benzene is added 0.415 g (0.362 mmol, 5 mol %) of tris(pentafluorophenyl) borane. The light yellow solution is stirred at 25° C. for 19 hours. The reaction mixture containing the 2-methyl-2-phenylpropanal is then treated with...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
null
null
null
c1ccccc1.c1ccccc1
HO-
[O-]CC.[Ti+4].[O-]CC.[O-]CC.[O-]CC.FC1=C(C(=C(C(=C1B(C1=C(C(=C(C(=C1F)F)F)F)F)C1=C(C(=C(C(=C1F)F)F)F)F)F)F)F)F.C1=CC=CC=C1
25
19
CC(C)(C=O)c1ccccc1.Cc1ccc([S@@](N)=O)cc1>[O-]CC.[Ti+4].[O-]CC.[O-]CC.[O-]CC.FC1=C(C(=C(C(=C1B(C1=C(C(=C(C(=C1F)F)F)F)F)C1=C(C(=C(C(=C1F)F)F)F)F)F)F)F)F.C1=CC=CC=C1>Cc1ccc([S@](=O)N=CC(C)(C)c2ccccc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-26e67c3358a347cdbaf3b4613a22bfa4
CC(C)(C(=O)O)c1ccccc1.COc1ccc(CN)cc1OC>>COc1ccc(CNC(=O)C(C)(C)c2ccccc2)cc1OC
COC=1C=C(CN)C=CC1OC.CC(C(=O)O)(C)C1=CC=CC=C1.C(C)(C)N(C(C)C)CC.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1N=CC=C2)OC(=[N+](C)C)N(C)C>>COC=1C=C(CNC(C(C)(C)C2=CC=CC=C2)=O)C=CC1OC
O[C:9](=[O:10])[C:11]([CH3:12])([CH3:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][NH2:8])[cH:20][c:21]1[O:22][CH3:23]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][NH:8][C:9](=[O:10])[C:11]([CH3:12])([CH3:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[cH:20][c:21]1[O:22][...
CC(C)(C(=O)O)c1ccccc1.COc1ccc(CN)cc1OC
COc1ccc(CNC(=O)C(C)(C)c2ccccc2)cc1OC
null
null
CN(C)C=O.CCOC(=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Cc1ccccc1)NCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[c:6].[NH2;D1;+0:7]-[C:8]-[c:9]>>[C;D1;H3:4]-[C:3](-[C;D1;H3:5])(-[c:6])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:8]-[c:9]
95
[{"value": 95.0, "product": "COC=1C=C(CNC(C(C)(C)C2=CC=CC=C2)=O)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 94.9, "product": "COC=1C=C(CNC(C(C)(C)C2=CC=CC=C2)=O)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 2-methyl-2-phenylpropionic acid (3.28 g, 20 mmol) in DMF (50 ml) was treated sequentially with N,N-diisopropylethylamine (8.09 g, 80 mmol), O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate (HATU) (7.60 g, 20 mmol) then 3,4-dimethoxybenzylamine (3.34 g, 20 mmol) and then stirred ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CN(C)C=O.CCOC(=O)C
null
null
CC(C)(C(=O)O)c1ccccc1.COc1ccc(CN)cc1OC>CN(C)C=O.CCOC(=O)C>COc1ccc(CNC(=O)C(C)(C)c2ccccc2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f446c5c1f2ca4b21879adc68a053ceb4
CO.COc1ccc(C#N)cc1Br>>CONCc1cccc(Br)c1
CO.BrC=1C=C(C#N)C=CC1OC.B.C1CCOC1>>BrC=1C=C(CNOC)C=CC1
[CH3:1][OH:2].CO[c:8]1[cH:7][cH:6][c:5]([C:4]#[N:3])[cH:11][c:9]1[Br:10]>>[CH3:1][O:2][NH:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][c:9]([Br:10])[cH:11]1
CO.COc1ccc(C#N)cc1Br
CONCc1cccc(Br)c1
null
null
C1CCOC1
Miscellaneous
OtherReaction
06e3b738e36a3fb3b92f84d0fa24f3a2fe570200e0b8cfa7863114ff98d06671
44d286b4cdb5308a16d5fd2584ba1c21eb94ef264b5d325ba52275eb8bc4678b
c1ccccc1
C-O-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4](-[C;H0;D2;+0:5]#[N;H0;D1;+0:6]):[c:7]:[c:8]:1-[Br;D1;H0:9].[C;D1;H3:10]-[OH;D1;+0:11]>>[Br;D1;H0:9]-[c:8]1:[c:7]:[c:4](-[CH2;D2;+0:5]-[NH;D2;+0:6]-[O;H0;D2;+0:11]-[C;D1;H3:10]):[c:3]:[c:2]:[cH;D2;+0:1]:1
64
[{"value": 64.0, "product": "BrC=1C=C(CNOC)C=CC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A stirring solution of 3-bromo-4-methoxy-benzonitrile (1.00 g, 4.7 mmol) in THF (30 ml) was treated drop-wise with borane-THF (14.2 ml, 1M solution in THF, 14.2 mmol). The mixture was heated at reflux, under argon for 5 h. To the cooled reaction mixture was cautiously added MeOH (20 ml). The volatiles were removed in v...
10.6084/m9.figshare.5104873.v1
null
Ether.Nitrile.Methanol
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1
Other
C1CCOC1
null
null
CO.COc1ccc(C#N)cc1Br>C1CCOC1>CONCc1cccc(Br)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-271befcf31bf4de5be010ffc3ee4aa19
COc1ccc(C=O)cc1OC.C[C@H](N)Cc1ccccc1>>COc1ccc(CN[C@@H](C)Cc2ccccc2)cc1OC
C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+].COC=1C=C(C=O)C=CC1OC.S(=O)(=O)(O)O.C[C@@H](CC1=CC=CC=C1)N.C(C)N(CC)CC>>COC=1C=C(CN[C@H](CC2=CC=CC=C2)C)C=CC1OC
O=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:19]([O:20][CH3:21])[cH:18]1.[NH2:8][C@@H:9]([CH3:10])[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][NH:8][C@@H:9]([CH3:10])[CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][c:19]1[O:20][CH3:21]
COc1ccc(C=O)cc1OC.C[C@H](N)Cc1ccccc1
COc1ccc(CN[C@@H](C)Cc2ccccc2)cc1OC
null
null
ClCCCl
Heteroatom Alkylation and Arylation
Reductive amination with aldehyde
422be648aea52bce28ccc8fb32ec3178aaa47bbd624f063874619362f075b5f2
7915721a3e395aed85e3c40dc4d725c571a931ac517c6a0da16f2a2b0bb5eac7
c1ccc(CCNCc2ccccc2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](-[C;D1;H3:7])-[NH2;D1;+0:8]>>[C:5]-[C:6](-[C;D1;H3:7])-[NH;D2;+0:8]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
67
[{"value": 67.0, "product": "COC=1C=C(CN[C@H](CC2=CC=CC=C2)C)C=CC1OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.7, "product": "COC=1C=C(CN[C@H](CC2=CC=CC=C2)C)C=CC1OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A solution of 3,4-dimethoxybenzaldehyde (1.06 g, 6.4 mmol), (S)-1-methyl-2-phenylethylamine sulfate (1.18 g, 6.4 mmol) and triethylamine (0.89 ml, 6.4 mmol) in 1,2-dichloroethane (50 ml) was stirred at room temperature under argon for 15 min. Sodium triacetoxyborohydride (2.97 g, 14 mmol) was added over 5 min. then sti...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
Other
ClCCCl
null
16
COc1ccc(C=O)cc1OC.C[C@H](N)Cc1ccccc1>ClCCCl>COc1ccc(CN[C@@H](C)Cc2ccccc2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-87b5f8a346014a829528bbadfc81e446
COc1ccc(CCN[C@@H](C)Cc2ccccc2)cc1OC.O=C(Cl)c1cccc(Br)c1>>COc1ccc(CCN(C(=O)c2cccc(Br)c2)[C@@H](C)Cc2ccccc2)cc1OC
BrC=1C=C(C(=O)Cl)C=CC1.COC=1C=C(C=CC1OC)CCN[C@H](CC1=CC=CC=C1)C>>BrC=1C=C(C(=O)N([C@H](CC2=CC=CC=C2)C)CCC2=CC(=C(C=C2)OC)OC)C=CC1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][NH:9][C@@H:19]([CH3:20])[CH2:21][c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[cH:28][c:29]1[O:30][CH3:31].Cl[C:10](=[O:11])[c:12]1[cH:13][cH:14][cH:15][c:16]([Br:17])[cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][N:9]([C:10](=[O:11])[c:12]2[cH:13][cH:14][c...
COc1ccc(CCN[C@@H](C)Cc2ccccc2)cc1OC.O=C(Cl)c1cccc(Br)c1
COc1ccc(CCN(C(=O)c2cccc(Br)c2)[C@@H](C)Cc2ccccc2)cc1OC
null
null
null
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N(CCc1ccccc1)CCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7](-[C;D1;H3:8])-[NH;D2;+0:9]-[C:10]-[C:11]>>[C:6]-[C:7](-[C;D1;H3:8])-[N;H0;D3;+0:9](-[C:10]-[C:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
The title compound was prepared from 3-bromobenzoyl chloride and (S)-[2-(3,4 dimethoxyphenyl)ethyl]-(1-methyl-2-phenylethyl)amine D8 according to a procedure similar to that for Example 76. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccccc1.c1ccccc1
HCl
null
null
null
COc1ccc(CCN[C@@H](C)Cc2ccccc2)cc1OC.O=C(Cl)c1cccc(Br)c1>>COc1ccc(CCN(C(=O)c2cccc(Br)c2)[C@@H](C)Cc2ccccc2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1b6c9c55b1b4432a92c1ab271f086e9c
COc1ccc(CCNC[C@H](C)c2ccccc2)cc1OC.O=C(Cl)c1ccc2c(c1)OCO2>>COc1ccc(CCN(C[C@H](C)c2ccccc2)C(=O)c2ccc3c(c2)OCO3)cc1OC
O1COC2=C1C=CC(=C2)C(=O)Cl.COC=1C=C(C=CC1OC)CCNC[C@H](C)C1=CC=CC=C1>>COC=1C=C(C=CC1OC)CCN(C(=O)C1=CC2=C(OCO2)C=C1)C[C@H](C)C1=CC=CC=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][NH:9][CH2:10][C@H:11]([CH3:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[cH:30][c:31]1[O:32][CH3:33].Cl[C:19](=[O:20])[c:21]1[cH:22][cH:23][c:24]2[c:25]([cH:26]1)[O:27][CH2:28][O:29]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][N:9]([CH2:10][C@H:11]([CH3:12]...
COc1ccc(CCNC[C@H](C)c2ccccc2)cc1OC.O=C(Cl)c1ccc2c(c1)OCO2
COc1ccc(CCN(C[C@H](C)c2ccccc2)C(=O)c2ccc3c(c2)OCO3)cc1OC
null
null
C(C)N(CC)CC
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccc2c(c1)OCO2)N(CCc1ccccc1)CCc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C:10])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
74.5
[{"value": 68.0, "product": "COC=1C=C(C=CC1OC)CCN(C(=O)C1=CC2=C(OCO2)C=C1)C[C@H](C)C1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.5, "product": "COC=1C=C(C=CC1OC)CCN(C(=O)C1=CC2=C(OCO2)C=C1)C[C@H](C)C1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
72
HOUR
A stirring solution of benzo[1,3]dioxole-5-carbonyl chloride (151 mg, 0.82 mmol) in MDC (5 ml) was treated with a pre-mixed solution of (R)-[2-(3,4-dimethoxy-phenyl)-ethyl]-(2-phenyl-propyl)-amine (D12, 245 mg, 0.75 mmol) and triethylamine (0.17 ml) in MDC (2 ml). After stirring under argon at room temperature for 72 h...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccccc1.c1ccc2c(c1)OCO2
HCl
C(C)N(CC)CC
null
72
COc1ccc(CCNC[C@H](C)c2ccccc2)cc1OC.O=C(Cl)c1ccc2c(c1)OCO2>C(C)N(CC)CC>COc1ccc(CCN(C[C@H](C)c2ccccc2)C(=O)c2ccc3c(c2)OCO3)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-198625e865c349d6bf36a744738e8613
C1C2CC3CC1CC(C2)C3.O=CO.O=S(=O)(O)O>>O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
C12CC3CC(CC(C1)C3)C2.OC12CC3(CC(CC(C1)C3)C2)O.ClCCCl.S(O)(O)(=O)=O.C(=O)O>>OC12CC3(CC(CC(C1)C3)C2)O.C12(CC3(CC(CC(C1)C3)C2)C(=O)O)C(=O)O
[CH:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9]1)[CH2:10][CH:11]([CH2:15]3)[CH2:16]2.[CH:12](=[O:13])[OH:14].O=S(=O)([OH:1])[OH:3]>>[O:1]=[C:2]([OH:3])[C:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9]1)[CH2:10][C:11]([C:12](=[O:13])[OH:14])([CH2:15]3)[CH2:16]2
C1C2CC3CC1CC(C2)C3.O=CO.O=S(=O)(O)O
O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
null
null
null
Acylation
OtherReaction
3e8c4b9d86edd07c04e618791abcbd8dbe11208be45d91e4f36d3bce3521dc9a
05b1e9e4110bc86f2bd7cbdf6b80dcc179cd6fe787ce74ddba60fa77e8ec4cfa
C1C2CC3CC1CC(C2)C3
O=S(=O)(-[OH;D1;+0:1])-[OH;D1;+0:2].[C:3]1-[C:4]-[C:5]-[CH;D3;+0:6]2-[C:7]-[CH;D3;+0:8]-1-[C:9]-[C:10]-[C:11]-2.[O;D1;H0:12]=[CH;D2;+0:13]-[O;D1;H1:14]>>[O;D1;H0:12]=[C;H0;D3;+0:13](-[O;D1;H1:14])-[C;H0;D4;+0:8]12-[C:3]-[C:4]-[C:5]-[C;H0;D4;+0:6](-[C:15](=[O;H0;D1;+0:1])-[OH;D1;+0:2])(-[C:7]-1)-[C:11]-[C:10]-[C:9]-2
null
[]
null
null
null
null
The synthesis of 2-methacryloyloxy-2-(3-(2-hydroxy-2-propyl)1-1-adamantyl)propane was performed by the following method. First, according to the method described in Japanese Patent Application Laid-open No. 2002-167342, 1000 g of 1,3-dihydroxyadamantane was synthesized from adamantane. Next, a four-necked flask equippe...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Carboxylic acid.Carboxylic acid
C1C2CC3CC1CC(C2)C3
C1C2CC3CC1CC(C2)C3
C1C2CC3CC1CC(C2)C3
HO-
null
null
null
C1C2CC3CC1CC(C2)C3.O=CO.O=S(=O)(O)O>>O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-946f03b2dca0420599ed66931098e182
C=C(C)C(=O)OC(C)(C)C12CC3CC(C1)CC(C(C)(C)OC(=O)C(=C)C)(C3)C2>>O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
C(C(=C)C)(=O)OC(C)(C)C12CC3(CC(CC(C1)C3)C2)C(C)(C)OC(C(=C)C)=O.C12CC3CC(CC(C1)C3)C2.OC12CC3(CC(CC(C1)C3)C2)O.S(O)(O)(=O)=O>>OC12CC3(CC(CC(C1)C3)C2)O.C12(CC3(CC(CC(C1)C3)C2)C(=O)O)C(=O)O
C=C(C)C(=[O:13])[O:14]C(C)(C)[C:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9]1)[CH2:10][C:11]([C:12](C)(C)[O:3][C:2](C(=C)C)=[O:1])([CH2:15]3)[CH2:16]2>>[O:1]=[C:2]([OH:3])[C:4]12[CH2:5][CH:6]3[CH2:7][CH:8]([CH2:9]1)[CH2:10][C:11]([C:12](=[O:13])[OH:14])([CH2:15]3)[CH2:16]2
C=C(C)C(=O)OC(C)(C)C12CC3CC(C1)CC(C(C)(C)OC(=O)C(=C)C)(C3)C2
O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
null
null
C(=O)O.ClCCCl
Miscellaneous
OtherReaction
9351ea7ce4c16b15d2a92bf25854d47b2fdd561705737f42f9bde07f336c30fd
f23d9e9523698ee811d52b830189892076b3f889e1772926d6055086cb6cc8cf
C1C2CC3CC1CC(C2)C3
C-C(=C)-C(=[O;H0;D1;+0:1])-[O;H0;D2;+0:2]-C(-C)(-C)-[C;H0;D4;+0:3]12-[C:4]-[C:5](-[C;H0;D4;+0:6](-C)(-C)-[O;H0;D2;+0:7]-[C;H0;D3;+0:8](=[O;D1;H0:9])-C(-C)=C)(-[C:10]-[C:11]-[C:12]-1)-[C:13]-[C:14]-[C:15]-2>>[O;D1;H0:9]=[C;H0;D3;+0:8](-[OH;D1;+0:7])-[C;H0;D4;+0:3]12-[C:4]-[C:5](-[C;H0;D3;+0:6](=[O;H0;D1;+0:1])-[OH;D1;+0...
null
[]
null
null
null
null
The synthesis of 2-methacryloyloxy-2-(3-(2-methacryloyloxy-2-propyl)-1-adamantyl)propane was performed by the following method. First, according to the method described in Japanese Patent Application Laid-open No. 2002-167342, 100 g of 1,3-dihydroxyadamantane was synthesized from adamantane. Next, a four-necked flask e...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester.Vinyl.Vinyl
Carboxylic acid.Carboxylic acid
C1C2CC3CC1CC(C2)C3
C1C2CC3CC1CC(C2)C3
C1C2CC3CC1CC(C2)C3
Other
C(=O)O.ClCCCl
null
null
C=C(C)C(=O)OC(C)(C)C12CC3CC(C1)CC(C(C)(C)OC(=O)C(=C)C)(C3)C2>C(=O)O.ClCCCl>O=C(O)C12CC3CC(C1)CC(C(=O)O)(C3)C2
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e661ecaad28b4a00931ae197f0f3c7ff
CC(C)(C#N)N=NC(C)(C)C#N.c1ccc2c(c1)CCN2>>CC(C)N1CCc2ccccc21
N1CCC2=CC=CC=C12.[SnH](CCCC)(CCCC)CCCC.CC(C)(C#N)N=NC(C)(C)C#N>>C(C)(C)N1CCC2=CC=CC=C12
CC(C)(C#N)N=N[C:1](C)([C:2]#N)[CH3:3].[NH:4]1[CH2:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]21>>[CH3:1][CH:2]([CH3:3])[N:4]1[CH2:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]21
CC(C)(C#N)N=NC(C)(C)C#N.c1ccc2c(c1)CCN2
CC(C)N1CCc2ccccc21
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
6f8aa694c1fea69721deedda2030a76837f3663aafe54b379ef0fdc23d0471db
d99cc8e2c462a957cfb2c9c6cb463a002ac6cab2ca5969133dc779eb1a3a9348
c1ccc2c(c1)CCN2
C-C(-C)(-C#N)-N=N-[C;H0;D4;+0:1](-C)(-[CH3;D1;+0:2])-[C;H0;D2;+0:3]#N.[c:4]:[c:5]1:[c:6]-[C:7]-[C:8]-[NH;D2;+0:9]-1>>[CH3;D1;+0:1]-[CH;D3;+0:3](-[CH3;D1;+0:2])-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[c:6]:[c:5]-1:[c:4]
null
[]
null
null
null
null
A three-hour addition of nBu3SnH (154 μL, 573 μmol) and AIBN (34 mg, 208 μmol) solution in benzene (1 mL) to a refluxing solution of the unpurified ketimine (125 mg, 521 μmol) in benzene (50 mL) delivered, after flash chromatography (30% CH2Cl2/Hexanes) 0.024 g (30%) of the desired indoline as a colorless oil. Rƒ=0.1 (...
10.6084/m9.figshare.5104873.v1
null
Diazene.Nitrile.Nitrile.Secondary amine
Tertiary amine
c1ccc2c(c1)CCN2
c1ccc2c(c1)CC[NH]2
c1ccc2c(c1)CC[NH]2
Other
C1=CC=CC=C1
null
null
CC(C)(C#N)N=NC(C)(C)C#N.c1ccc2c(c1)CCN2>C1=CC=CC=C1>CC(C)N1CCc2ccccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4a68867ef8f04e06881a1c8b1485ab02
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.Clc1nccc(Oc2ccnc(Cl)n2)n1>>C=Cc1nccc(Oc2ccnc(C=C)n2)n1
ClC1=NC=CC(=N1)OC1=NC(=NC=C1)Cl.C(=C)[Sn](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)C>>C(=C)C1=NC=CC(=N1)OC1=NC(=NC=C1)C=C
CCC[CH2][Sn]([CH2]CCC)([CH2]C[CH2:14][CH3:15])[CH:2]=[CH2:1].Cl[c:3]1[n:4][cH:5][cH:6][c:7]([O:8][c:9]2[cH:10][cH:11][n:12][c:13](Cl)[n:16]2)[n:17]1>>[CH2:1]=[CH:2][c:3]1[n:4][cH:5][cH:6][c:7]([O:8][c:9]2[cH:10][cH:11][n:12][c:13]([CH:14]=[CH2:15])[n:16]2)[n:17]1
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.Clc1nccc(Oc2ccnc(Cl)n2)n1
C=Cc1nccc(Oc2ccnc(C=C)n2)n1
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
CCOC(=O)C
C-C Coupling
OtherReaction
09a9788678a16cc7a2710b39b4c5c6e4dce07f7dedb3ec29fb75bec0bcda3989
20a56244d59ecb15ab496f5cdf3a085b565f2b94a0e0464d13b172a4e17b1d21
c1cc(Oc2ccncn2)ncn1
C-C-C-[CH2]-[Sn](-[CH2]-C-C-C)(-[CH2]-C-[CH2;D2;+0:1]-[CH3;D1;+0:2])-[CH;D2;+0:3]=[C;D1;H2:4].Cl-[c;H0;D3;+0:5](:[#7;a:6]:[c:7]):[#7;a:8]:[c:9].Cl-[c;H0;D3;+0:10](:[#7;a:11]:[c:12]):[#7;a:13]:[c:14]>>[C;D1;H2:4]=[CH;D2;+0:3]-[c;H0;D3;+0:10](:[#7;a:11]:[c:12]):[#7;a:13]:[c:14].[CH2;D1;+0:2]=[CH;D2;+0:1]-[c;H0;D3;+0:5](:...
61
[{"value": 61.0, "product": "C(=C)C1=NC=CC(=N1)OC1=NC(=NC=C1)C=C", "details": "PERCENTYIELD", "is_desired": false}]
115
CELSIUS
null
null
The 2-chloropyrimidinyl ether intermediate (500 mg, 0.896 mmol) (see Example 1), vinyltributyltin (600 mg, 1.89 mmol), BHT (20 mg), and (PPh3)4Pd (50 mg, 0.045 mmol) were suspended in degassed toluene (10 mL) under argon and heated to 115° C. for 3 h. The reaction mixture was cooled, diluted with EtOAc (100 mL), washed...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Vinyl.Tin
Vinyl.Vinyl
c1cncnc1.c1cncnc1
c1cncnc1.c1cncnc1
c1cncnc1.c1cncnc1
HCl.Sn
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.CCOC(=O)C
115
null
C=[CH][Sn]([CH2]CCC)([CH2]CCC)[CH2]CCC.Clc1nccc(Oc2ccnc(Cl)n2)n1>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.CCOC(=O)C>C=Cc1nccc(Oc2ccnc(C=C)n2)n1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-171ce8970ab944cf9a8e13b2499c8ab9
C1COCCN1.Cc1cc(Cl)ccn1>>Clc1ccnc(CN2CCOCC2)c1
CC1=NC=CC(=C1)Cl.C1CC(=O)N(C1=O)Br.N1CCOCC1.C(=O)([O-])[O-].[K+].[K+]>>O1CCN(CC1)CC1=NC=CC(=C1)Cl
[NH:8]1[CH2:9][CH2:10][O:11][CH2:12][CH2:13]1.[Cl:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH3:7])[cH:14]1>>[Cl:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][O:11][CH2:12][CH2:13]2)[cH:14]1
C1COCCN1.Cc1cc(Cl)ccn1
Clc1ccnc(CN2CCOCC2)c1
null
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O
CCOC(=O)C.CN(C)C=O.C(Cl)(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
a82e7b369befc31fcac88f7fe646a76e64499f9d60ba9b1ff71c1adbcf448387
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(CN2CCOCC2)nc1
[#8:1]1-[C:2]-[C:3]-[NH;D2;+0:4]-[C:5]-[C:6]-1.[CH3;D1;+0:7]-[c:8](:[c:9]):[#7;a:10]:[c:11]>>[c:9]:[c:8](-[CH2;D2;+0:7]-[N;H0;D3;+0:4]1-[C:5]-[C:6]-[#8:1]-[C:2]-[C:3]-1):[#7;a:10]:[c:11]
null
[]
null
null
8
HOUR
A mixture of the 2-methyl-4-chloropyridine (1.00 g, 7.84 mmol), NBS (1.42 g, 8.00 mmol) and benzoyl peroxide (˜10 mg) in 10 mL of CCl4 was heated at reflux for 5 h. After cooling down, the reaction mixture was filtered and filtrate was concentrated to give the crude products mixture, which was dissolved in DMF and trea...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
C1COCCN1
C1COCC[NH]1
c1ccncc1.C1COCC[NH]1
null
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.CCOC(=O)C.CN(C)C=O.C(Cl)(Cl)(Cl)Cl
null
8
C1COCCN1.Cc1cc(Cl)ccn1>C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.CCOC(=O)C.CN(C)C=O.C(Cl)(Cl)(Cl)Cl>Clc1ccnc(CN2CCOCC2)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2646942418ce43359f515379ea575146
BrCc1ccccc1.CN(C)C=O>>c1ccc(COCc2ccccc2)cc1
C(C1=CC=CC=C1)Br.[H-].[Na+].CN(C)C=O>>C(C1=CC=CC=C1)OCC1=CC=CC=C1
Br[CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1.N([CH3:1])([CH:5]=[O:6])[CH3:15]>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][O:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[cH:14][cH:15]1
BrCc1ccccc1.CN(C)C=O
c1ccc(COCc2ccccc2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
571bca16a08ddaad6e3abed2f99b04fbb2bbe07d2c42b4008d772773a112e55e
204900b68d487b245252094c4ccbed5a9df699c5195177b38ee4d7a1438c290c
c1ccc(COCc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-N(-[CH3;D1;+0:6])-[CH;D2;+0:7]=[O;H0;D1;+0:8]>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[CH2;D2;+0:7]-[c:9]1:[c:10]:[cH;D2;+0:5]:[cH;D2;+0:6]:[c:11]:[c:12]:1):[c:4]
null
[]
null
null
3
HOUR
To a solution of the above alcohol (430 mg, 3.0 mmol) in DMF (10 mL) was added NaH (144 mg of a 60% dispersion in mineral oil, 3.60 mmol) and the mixture was then cooled in an ice bath. Benzyl bromide (437 uL, 3.60 mmol) was then added and the mixture was stirred at room temperature for 3 h. After normal aqueous work-u...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary amide
Ether
null
c1ccccc1
c1ccccc1.c1ccccc1
Br-
null
null
3
BrCc1ccccc1.CN(C)C=O>>c1ccc(COCc2ccccc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d793debe87e84fa9bb83bfe2b15e1506
CNC(=O)c1cc(Oc2cccc3cc(C(=O)Nc4cc(C(C)(C)C)cc(NS(C)(=O)=O)c4OC)n(C)c23)ccn1>>CCOCC.c1ccc2[nH]ccc2c1
[O-]P(=O)([O-])[O-].[K+].[K+].[K+].C(C)(C)(C)C=1C=C(C(=C(C1)NC(=O)C=1N(C2=C(C=CC=C2C1)OC1=CC(=NC=C1)C(NC)=O)C)OC)NS(=O)(=O)C>>N1C=CC2=CC=CC=C12.CCOCC
Cn1c([C:11](=O)[NH:10][c:9]2[cH:8][c:7]([C:6](C)(C)C)[cH:14][c:12](NS(C)(=O)=O)[c:13]2O[CH3:1])cc2ccc[c:4](Oc3ccnc(C(=O)N[CH3:2])c3)[c:5]21>>[CH3:1][CH2:2][O:3][CH2:4][CH3:5].[cH:6]1[cH:7][cH:8][c:9]2[nH:10][cH:11][cH:12][c:13]2[cH:14]1
CNC(=O)c1cc(Oc2cccc3cc(C(=O)Nc4cc(C(C)(C)C)cc(NS(C)(=O)=O)c4OC)n(C)c23)ccn1
CCOCC.c1ccc2[nH]ccc2c1
null
CC(=O)[O-].CC(=O)[O-].[Pd+2]
null
Reduction
OtherReaction
03faa860ef6b466af806e2bc83289cb1f8d4c2ed6d035c283d235098f562adcf
c4bcc1a8ff503468e268147b10e897f21d3383088aede53a5f9aadc76751a156
c1ccc2[nH]ccc2c1
C-n1:[c;H0;D3;+0:1]2:[c;H0;D3;+0:2](-O-c3:c:c:n:c(-C(=O)-N-[CH3;D1;+0:3]):c:3):c:c:c:c:2:c:c:1-[C;H0;D3;+0:4](=O)-[NH;D2;+0:5]-[c:6]1:[c:7]:[c;H0;D3;+0:8](-[C;H0;D4;+0:9](-C)(-C)-C):[cH;D2;+0:10]:[c;H0;D3;+0:11](-N-S(-C)(=O)=O):[c;H0;D3;+0:12]:1-O-[CH3;D1;+0:13]>>[CH3;D1;+0:13]-[CH2;D2;+0:3]-[#8:14]-[CH2;D2;+0:2]-[CH3;...
61
[{"value": 61.0, "product": "N1C=CC2=CC=CC=C12.CCOCC", "details": "PERCENTYIELD", "is_desired": false}]
100
CELSIUS
6
HOUR
A Schlenk tube was charged with Pd(OAc)2 (16 mg, 0.07 mmol), K3PO4 (525 mg, 2.40 mmol), di-t-butylbiphenylphosphine (42 mg, 0.14 mmol) and the 7-hydroxyindole ester (see Example 6) (307 mg, 1.4 mmol), and capped with a septum and purged with argon. A solution of the benzyl ether from above (270 mg, 1.16 mmol) in 3 mL o...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Ether.Ether.Secondary amide.Secondary amide
Ether
c1ccccc1.c1cccc2cc[nH]c12.c1ccncc1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
HO-
CC(=O)[O-].CC(=O)[O-].[Pd+2]
100
6
CNC(=O)c1cc(Oc2cccc3cc(C(=O)Nc4cc(C(C)(C)C)cc(NS(C)(=O)=O)c4OC)n(C)c23)ccn1>CC(=O)[O-].CC(=O)[O-].[Pd+2]>CCOCC.c1ccc2[nH]ccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-65517cb8e3c04b42a5dcdb707311818a
CN(C)C(On1nnc2cccnc21)=[N+](C)C.CN(C)C=O.COc1c(N)cc(C(C)(C)C)cc1NS(C)(=O)=O.O=C(O)c1cc2ccccc2[nH]1.On1nnc2cccnc21>>COc1c(NC(=O)c2cc3cccc(Oc4ccnc(CN(C)C)c4)c3n2C)cc(C(C)(C)C)cc1NS(C)(=O)=O
N1C(=CC2=CC=CC=C12)C(=O)O.CCN(C(C)C)C(C)C.CN(C)C=O.CN(C)C(=[N+](C)C)ON1C2=C(C=CC=N2)N=N1.F[P-](F)(F)(F)(F)F.C1=CC2=C(N=C1)N(N=N2)O.NC=1C(=C(C=C(C1)C(C)(C)C)NS(=O)(=O)C)OC>>C(C)(C)(C)C=1C=C(C(=C(C1)NC(=O)C=1N(C2=C(C=CC=C2C1)OC1=CC(=NC=C1)CN(C)C)C)OC)NS(=O)(=O)C
CN(C(On1nnc2cccnc21)=[N+](C)C)[CH3:28].O=[CH:21][N:22]([CH3:23])[CH3:24].[CH3:1][O:2][c:3]1[c:4]([NH2:5])[cH:29][c:30]([C:31]([CH3:32])([CH3:33])[CH3:34])[cH:35][c:36]1[NH:37][S:38]([CH3:39])(=[O:40])=[O:41].O[C:6](=[O:7])[c:8]1[cH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:26]2[nH:27]1.n1n[c:25]2[cH:16][cH:17][cH:18][n:1...
CN(C)C(On1nnc2cccnc21)=[N+](C)C.CN(C)C=O.COc1c(N)cc(C(C)(C)C)cc1NS(C)(=O)=O.O=C(O)c1cc2ccccc2[nH]1.On1nnc2cccnc21
COc1c(NC(=O)c2cc3cccc(Oc4ccnc(CN(C)C)c4)c3n2C)cc(C(C)(C)C)cc1NS(C)(=O)=O
null
null
CCOC(=O)C
Acylation
OtherReaction
d48d9fe12e9c882a2b0abbe0a4725b562d0bb32b760c5865247e93ffe3888a2f
a85f7c688100a96cb1a549bfbfc45d8593b2dbb406198a553b98eabaa1a2d9e2
O=C(Nc1ccccc1)c1cc2cccc(Oc3ccncc3)c2[nH]1
C-N(-[CH3;D1;+0:1])-C(-O-n1:n:n:c2:c:c:c:n:c:2:1)=[N+](-C)-C.O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4]1:[c:5]:[c:6]:[c:7](:[cH;D2;+0:8]:[c:9]:[c:10]):[nH;D2;+0:11]:1.O=[CH;D2;+0:12]-[#7:13](-[C;D1;H3:14])-[C;D1;H3:15].[NH2;D1;+0:16]-[c:17](:[c:18]):[c:19].[OH;D1;+0:20]-n1:n:n:[c;H0;D3;+0:21]2:[cH;D2;+0:22]:[c:23]:[c:24]:[#7...
null
[]
null
null
5
MINUTE
To a solution of the indole carboxylic acid (360 mg, 0.93 mmol) in 4 mL of DMF was added Hunig's base (418 uL, 2.4 mmol). After 5 min, HATU (439 mg, 1.12 mmol) and HOAt (12 mg, 0.09 mmol) were added and then N-(3-amino-5-tert-butyl-2-methoxy-phenyl)-methanesulfonamide (253 mg, 0.93 mmol). The mixture was stirred overni...
10.6084/m9.figshare.5104873.v1
null
Amidinium.Carboxylic acid.Tertiary amide.Primary amine
Ether.Secondary amide
c1cnc2[nH]nnc2c1.c1ccc2[nH]ccc2c1.c1cnc2nn[nH]c2c1
c1cc2ccccc2[nH]1.c1ccncc1
c1ccccc1.c1cc2ccccc2[nH]1.c1ccncc1
HO-
CCOC(=O)C
null
0.083333
CN(C)C(On1nnc2cccnc21)=[N+](C)C.CN(C)C=O.COc1c(N)cc(C(C)(C)C)cc1NS(C)(=O)=O.O=C(O)c1cc2ccccc2[nH]1.On1nnc2cccnc21>CCOC(=O)C>COc1c(NC(=O)c2cc3cccc(Oc4ccnc(CN(C)C)c4)c3n2C)cc(C(C)(C)C)cc1NS(C)(=O)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-666ad5959a9b4ddc926a44f4999e78fe
COc1cccc([N+](=O)[O-])c1[N+](=O)[O-]>>COc1cccc(N)c1N
O.O.[Sn](Cl)Cl.[N+](=O)([O-])C=1C(=C(C=CC1)OC)[N+](=O)[O-].[OH-].[Na+]>>NC=1C(=C(C=CC1)OC)N
O=[N+:8]([O-])[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:9]1[N+:10](=O)[O-]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([NH2:8])[c:9]1[NH2:10]
COc1cccc([N+](=O)[O-])c1[N+](=O)[O-]
COc1cccc(N)c1N
null
null
CCOC(=O)C
Reduction
OtherReaction
6748a51a25102225412593c5a930e43f5a8904a80803177de025a6f83c59d65e
a303b0dfb15cc6bade463acf71681cf3ba7580b599dfa4d28d8caac83d08cd17
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4](-[N+;H0;D3:5](=O)-[O-]):[c:6]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4](-[NH2;D1;+0:5]):[c:6]
71.1
[{"value": 52.0, "product": "NC=1C(=C(C=CC1)OC)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.1, "product": "NC=1C(=C(C=CC1)OC)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Tin(II)chloride dihydrate (11.9 g, 52.6 mmol) was added to a solution of the above dinitroanisole (2.21 g, 8.76 mmol) in EtOAc (30 mL). The mixture was heated to reflux for 0.25 h upon which the solution became red in color. The solution was cooled to room temperature and poured onto aqueous 2.0 M NaOH. The aqueous pha...
10.6084/m9.figshare.5104873.v1
null
Nitro group.Nitro group
Primary amine.Primary amine
null
null
c1ccccc1
Other
CCOC(=O)C
null
null
COc1cccc([N+](=O)[O-])c1[N+](=O)[O-]>CCOC(=O)C>COc1cccc(N)c1N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e5746b5c34054a009e87e1018a304f9f
COC(OC)c1cc(Cl)ccn1>>O=C(O)c1cc2ccccc2[nH]1
ClC1=CC(=NC=C1)C(OC)OC.O[Li].O.C1CCOC1.CO>>N1C(=CC2=CC=CC=C12)C(=O)O
C[O:3][CH:2]([O:1][CH3:8])[c:4]1[cH:5][c:6](Cl)[cH:7][cH:11][n:12]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[nH:12]1
COC(OC)c1cc(Cl)ccn1
O=C(O)c1cc2ccccc2[nH]1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
4758d7ba060182abc70ff60394fdbf25716cfffb54c039c464771dd27dd9a5f4
5dfe87e64357b461f30fd7c81794ec7e48f7637c7ac9c03e71e87d3737bdb306
c1ccc2[nH]ccc2c1
C-[O;H0;D2;+0:1]-[CH;D3;+0:2](-[O;H0;D2;+0:3]-[CH3;D1;+0:4])-[c:5]1:[c:6]:[c;H0;D3;+0:7](-Cl):[cH;D2;+0:8]:[cH;D2;+0:9]:[n;H0;D2;+0:10]:1>>[O;H0;D1;+0:3]=[C;H0;D3;+0:2](-[OH;D1;+0:1])-[c:5]1:[c:6]:[c;H0;D3;+0:7]2:[cH;D2;+0:8]:[cH;D2;+0:4]:[c:11]:[c:12]:[c;H0;D3;+0:9]:2:[nH;D2;+0:10]:1
90.5
[{"value": 90.5, "product": "N1C(=CC2=CC=CC=C12)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a solution of the above ether (770 mg, 2.1 mmol) in THF/MeOH (25 mL/10 mL) was added LiOH.H2O (218.1 mg, 2.50 eq) dissolved in 3 mL of water. The clear reaction solution was stirred at room temperature for 5 h, then concentrated in vacuo. The residual aqueous solution was diluted with water (15 mL), and extracted wi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ether.Ether
Carboxylic acid
c1ccncc1
c1ccc2[nH]ccc2c1
c1ccc2[nH]ccc2c1
null
O
null
5
COC(OC)c1cc(Cl)ccn1>O>O=C(O)c1cc2ccccc2[nH]1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1bf0f83c98cd47049c28a4312f33317e
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>>Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
C(C)(C)(C)[Si](O[C@H]1C[C@@H](O[C@@]1(CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C(NCC1=CC=CC=C1)NCC1=CC=CC=C1)N1C(=O)NC(=O)C(C)=C1)(C)C.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.CO>>C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO
CC(C)(C)[Si](C)(C)[O:8][C@H:7]1[CH2:6][C@H:5]([n:4]2[cH:3][c:2]([CH3:1])[c:33](=[O:34])[nH:32][c:30]2=[O:31])[O:29][C@@:9]1([CH2:10][O:11][Si](c1ccccc1)(c1ccccc1)C(C)(C)C)[CH:12]([NH:13][CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1)[NH:21][CH2:22][c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1>>[CH3:1][c:2]1[cH:3][n:...
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
null
null
O1CCCC1
Deprotection
OtherReaction
bd7040a39ad85a2c3bfd998d34ac16e7127d9c4e33a1400049e3f4e51e3ba999
48f3bf6b592ef26d22b6b1cdf6554655672438fd529e8208760ff43315f27aa1
O=c1ccn([C@H]2CCC(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[C:4](-[C:5]-[O;H0;D2;+0:6]-[Si](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-C(-C)(-C)-C)-[#8:7]>>[#8:7]-[C:4](-[C:5]-[OH;D1;+0:6])-[C:2](-[OH;D1;+0:1])-[C:3]
100
[{"value": 100.0, "product": "C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.9, "product": "C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired"...
null
null
3
HOUR
3′-O-[(tertbutyl)dimethylsilyl]-5′-O-[(tertbutyl)diphenylsilyl]-4′-C-(1,1′-diphenylmethylaminomethyl)thymidine (2) (1.2 g, 1.5 mmol) was dissolved in tetrahydrofuran (50 mL) at ambient temperature. A solution of tetrabutylammonium fluoride in tetrahydrofuran (4.5 mL) was then added to the solution. The resulting mixtur...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.Silyl protective group
Primary alcohol.Secondary alcohol
c1ccccc1.c1ccccc1
null
c1cncnc1.C1CCOC1.c1ccccc1.c1ccccc1
Other
O1CCCC1
null
3
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>O1CCCC1>Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-dc05bdb0f53e4ab480962f2ffcda9a1e
Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>>Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O
C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO.C(C)(=O)O>>NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO
c1ccc(CN[CH:10]([C@@:9]2([CH2:12][OH:13])[C@@H:7]([OH:8])[CH2:6][C@H:5]([n:4]3[cH:3][c:2]([CH3:1])[c:18](=[O:19])[nH:17][c:15]3=[O:16])[O:14]2)[NH:11]Cc2ccccc2)cc1>>[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@@:9]([CH2:10][NH2:11])([CH2:12][OH:13])[O:14]2)[c:15](=[O:16])[nH:17][c:18]1=[O:19]
Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O
null
[Pd]
C(C)O
Deprotection
OtherReaction
ebcb62b0cee28ac375043d4efcc15ae372e32a8afec9cbfdfea9a3d36c8b53ff
979bea025e86b23768e3b6416c2b4011b3ba1bc8928a29b90e7c5e231c2241bc
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
[C:1]-[C:2](-[CH;D3;+0:3](-N-C-c1:c:c:c:c:c:1)-[NH;D2;+0:4]-C-c1:c:c:c:c:c:1)(-[C:5])-[#8:6]-[C:7]>>[C:1]-[C:2](-[CH2;D2;+0:3]-[NH2;D1;+0:4])(-[C:5])-[#8:6]-[C:7]
null
[]
null
null
null
null
4′-C-(1,1′-diphenylmethylaminomethyl)thymidine (3) (0.65 g, 1.5 mmol) was dissolved in absolute ethanol (50 mL). Cyctohexene (12 mL), glacial acetic acid (5 mL) and 5%-palladium on charcoal (0.6 g) were added and the mixture heated under reflux with stirring. The solution was heated for 5 hours and then allowed to cool...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Secondary amine
Primary amine
c1ccccc1.c1ccccc1
null
c1cncnc1.C1CCOC1
Other
[Pd].C(C)O
null
null
Cc1cn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>[Pd].C(C)O>Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4786a30f4102434ba01e0ca25365f301
Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O.O=C(O)CNC(=O)C(F)(F)F>>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
C(C)(C)N(CC)C(C)C.FC(C(=O)NCC(=O)O)(F)F.NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO>>FC(C(=O)NCC(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO)(F)F
[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@:9]([CH2:10][OH:11])([CH2:12][NH2:13])[O:24]2)[c:25](=[O:26])[nH:27][c:28]1=[O:29].O[C:14](=[O:15])[CH2:16][NH:17][C:18](=[O:19])[C:20]([F:21])([F:22])[F:23]>>[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@:9]([CH2:10][OH:11])([CH2:12][NH:13][C:14](=[...
Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O.O=C(O)CNC(=O)C(F)(F)F
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5]=[O;D1;H0:6].[#8:7]-[C:8]-[C:9]-[NH2;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5]=[O;D1;H0:6]
null
[]
null
null
null
null
4′-C-Aminomethylthymidine (4) (0.14 mmol) was dissolved in anhydrous N,N-dimethylformamide (1 mL). N-Trifluoroacetylglycine (0.036 g, 0.21 mmol) and O-(N-succimidyl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate [TSTU] (0.085, 0.28 mmol) were then added and the solution stirred at ambient temperature. Diisopropylethyl...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1cncnc1.C1CCOC1
HO-
CN(C=O)C
null
null
Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O.O=C(O)CNC(=O)C(F)(F)F>CN(C=O)C>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2a2225e84c354943a777719f4cd032d4
CCOC(=O)C(F)(F)F.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O>>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO.C(C)N(CC)CC.FC(C(=O)OCC)(F)F>>FC(C(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO)(F)F
CCO[C:14](=[O:15])[C:16]([F:17])([F:18])[F:19].[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@:9]([CH2:10][OH:11])([CH2:12][NH2:13])[O:20]2)[c:21](=[O:22])[nH:23][c:24]1=[O:25]>>[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@:9]([CH2:10][OH:11])([CH2:12][NH:13][C:14](=[O:15])[C:16]([F:17])([F:18])...
CCOC(=O)C(F)(F)F.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
null
null
CO
Acylation
Aminolysis of esters
04c54ce22aa9bc0cea0de3d900446bcab51cf02bebeb606fa788a47dcd0e37ff
4335147c9ad02004b7c12428d7eac0b2e7e0e2017adc471d01c387239de8017d
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6].[#8:7]-[C:8]-[C:9]-[NH2;D1;+0:10]>>[#8:7]-[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[F;D1;H0:6]
66
[{"value": 66.0, "product": "FC(C(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
4′-C-Aminomethylthymidine (4) (1.5 mmol) was dissolved in methanol (10 mL) and triethylamine (1.5 mL) at ambient temperature. The solution was then treated with neat ethyl trifluoroacetate (1 mL) and the resulting solution stirred for 18 hours at ambient temperature with exclusion of moisture. The solvents and reagents...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Secondary amide
null
null
c1cncnc1.C1CCOC1
HO-
CO
null
18
CCOC(=O)C(F)(F)F.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O>CO>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8cd46d3c7d05431fb2c0c7f3a7ae3da7
Cc1cn([C@H]2C[C@H](O)[C@@](CNC(=O)C(F)(F)F)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O>>Cc1cn([C@H]2C[C@H](O)[C@@](CN)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
P(O)(=O)(OP(=O)(O)OP(=O)(O)O)OC[C@@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CNC(C(F)(F)F)=O>>P(O)(=O)(OP(=O)(O)OP(=O)(O)O)OC[C@@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CN
O=C(C(F)(F)F)[NH:11][CH2:10][C@@:9]1([CH2:12][O:13][P:14](=[O:15])([OH:16])[O:17][P:18](=[O:19])([OH:20])[O:21][P:22](=[O:23])([OH:24])[OH:25])[C@@H:7]([OH:8])[CH2:6][C@H:5]([n:4]2[cH:3][c:2]([CH3:1])[c:30](=[O:31])[nH:29][c:27]2=[O:28])[O:26]1>>[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@@:9]([CH2:10][NH...
Cc1cn([C@H]2C[C@H](O)[C@@](CNC(=O)C(F)(F)F)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
Cc1cn([C@H]2C[C@H](O)[C@@](CN)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
null
null
N
Reduction
Hydrogenolysis of amides/imides/carbamates
44b36597c7daf0608965c52c8db8a9220c21d9447ce54e0af375898475f3493f
caaeb83af2cb178156ae90fe7f610a106cd4bb5397d23f56d37a7fe11e2668ed
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3]-[#8:4]>>[#8:4]-[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
18
HOUR
4′-C-(N-trifluoroacetylaminomethyl)thymidine triphosphate (8) was dissolved in concentrated aqueous ammonia solution and allowed to stand for 18 hours at ambient temperature. The solution was then lyophilised to give the title compound (9) as a white powder. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Secondary amide
Primary amine
null
null
c1cncnc1.C1CCOC1
Other
N
null
18
Cc1cn([C@H]2C[C@H](O)[C@@](CNC(=O)C(F)(F)F)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O>N>Cc1cn([C@H]2C[C@H](O)[C@@](CN)(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8d5e97497e1d41aab531e4ebb94a2526
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>>CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1
C(C)(C)(C)[Si](O[C@H]1C[C@@H](O[C@@]1(CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C(NCC1=CC=CC=C1)NCC1=CC=CC=C1)N1C(=O)NC(=O)C(C)=C1)(C)C.C(C1=CC=CC=C1)(C1=CC=CC=C1)N.C(C)(=O)O.[BH3-]C#N.[Na+]>>C(C)(C)(C)[Si](O[C@H]1C[C@@H](O[C@@]1(CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C(NCC1=CC=CC=C1)NCC1=CC=CC=C1)N1C(=O)NC(=O)C=C1)(C...
C[c:14]1[cH:13][n:12]([C@H:11]2[CH2:10][C@H:9]([O:8][Si:5]([C:2]([CH3:1])([CH3:3])[CH3:4])([CH3:6])[CH3:7])[C@:21]([CH2:22][O:23][Si:24]([c:25]3[cH:26][cH:27][cH:28][cH:29][cH:30]3)([c:31]3[cH:32][cH:33][cH:34][cH:35][cH:36]3)[C:37]([CH3:38])([CH3:39])[CH3:40])([CH:41]([NH:42][CH2:43][c:44]3[cH:45][cH:46][cH:47][cH:48]...
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O
CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1
null
null
C(C)#N
Miscellaneous
OtherReaction
e2b428145bb25f1063aa09bb03912d37079cb743b4732df627cc55fd0c4649a9
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=c1ccn([C@H]2CC[C@](CO[SiH](c3ccccc3)c3ccccc3)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
C-[c;H0;D3;+0:1]1:[c:2]:[#7;a:3](-[C:4]-[#8:5]):[c:6]:[#7;a:7]:[c:8]:1=[O;D1;H0:9]>>[#8:5]-[C:4]-[#7;a:3]1:[c:2]:[cH;D2;+0:1]:[c:8](=[O;D1;H0:9]):[#7;a:7]:[c:6]:1
69
[{"value": 69.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
3′-O-[(tertbutyl)dimethylsilyl]-5′-O-[(tertbutyl)diphenylsilyl]-4′-C-formyl-2-deoxyuridine (10) (Yang et al; Tetrahedron Letters 1992, 33, 37–40.) (0.15 g, 0.25 mmol) was treated with Ph2CHNH2 (0.07 g, 0.37 mmol, 0.064 mL), glacial acetic acid (0.015 g, 0.26 mmol, 0.015 mL) and NaBH3CN (0.023 g, 0.37 mmol) in acetonitr...
10.6084/m9.figshare.5104873.v1
null
null
null
c1cncnc1
c1ccncn1
C1CCOC1.c1ccncn1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)#N
null
null
Cc1cn([C@H]2C[C@H](O[Si](C)(C)C(C)(C)C)[C@](CO[Si](c3ccccc3)(c3ccccc3)C(C)(C)C)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]c1=O>C(C)#N>CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8c5835ed9058457aa9bbc2561f7d57c9
CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1>>O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
C(C)(C)(C)[Si](O[C@H]1C[C@@H](O[C@@]1(CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C(NCC1=CC=CC=C1)NCC1=CC=CC=C1)N1C(=O)NC(=O)C=C1)(C)C.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO>>C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)C...
CC(C)(C)[Si](C)(C)[O:9][C@H:8]1[CH2:7][C@H:6]([n:5]2[cH:4][cH:3][c:2](=[O:1])[nH:33][c:31]2=[O:32])[O:30][C@@:10]1([CH2:11][O:12][Si](c1ccccc1)(c1ccccc1)C(C)(C)C)[CH:13]([NH:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[NH:22][CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1>>[O:1]=[c:2]1[cH:3][cH:4][n:5]([...
CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1
O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
null
null
O1CCCC1
Deprotection
OtherReaction
bd7040a39ad85a2c3bfd998d34ac16e7127d9c4e33a1400049e3f4e51e3ba999
48f3bf6b592ef26d22b6b1cdf6554655672438fd529e8208760ff43315f27aa1
O=c1ccn([C@H]2CCC(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2](-[C:3])-[C:4](-[C:5]-[O;H0;D2;+0:6]-[Si](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-C(-C)(-C)-C)-[#8:7]>>[#8:7]-[C:4](-[C:5]-[OH;D1;+0:6])-[C:2](-[OH;D1;+0:1])-[C:3]
78
[{"value": 78.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
3′-O-[(tertbutyl)dimethylsilyl]-5′-O-[(tertbutyl)diphenylsilyl]-4′-C-(1,1′-diphenylmethylaminomethyl)-2′-deoxyuridine (11) (0.13 g, 0.16 mmol) was treated with tetrabutylammonium fluoride solution (0.45 mL) in tetrahydrofuran (5 mL) according to the procedure used for the preparation of compound (3). The title compound...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.Silyl protective group
Primary alcohol.Secondary alcohol
c1ccccc1.c1ccccc1
null
c1ccncn1.C1CCOC1.c1ccccc1.c1ccccc1
Other
O1CCCC1
null
null
CC(C)(C)[Si](C)(C)O[C@H]1C[C@H](n2ccc(=O)[nH]c2=O)O[C@@]1(CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C)C(NCc1ccccc1)NCc1ccccc1>O1CCCC1>O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5d943e80966940b7bc9cb935cb92d36f
O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1>>NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
C1(=CC=CC=C1)CNC(NCC1=CC=CC=C1)[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO.C1=CCCCC1.C(C)(=O)O.NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO>>NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO
c1ccc(CN[CH:2]([NH:1]Cc2ccccc2)[C@:3]2([CH2:4][OH:5])[O:6][C@@H:7]([n:8]3[cH:9][cH:10][c:11](=[O:12])[nH:13][c:14]3=[O:15])[CH2:16][C@@H:17]2[OH:18])cc1>>[NH2:1][CH2:2][C@:3]1([CH2:4][OH:5])[O:6][C@@H:7]([n:8]2[cH:9][cH:10][c:11](=[O:12])[nH:13][c:14]2=[O:15])[CH2:16][C@@H:17]1[OH:18]
O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1
NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
null
[Pd]
C(C)O
Deprotection
OtherReaction
ebcb62b0cee28ac375043d4efcc15ae372e32a8afec9cbfdfea9a3d36c8b53ff
979bea025e86b23768e3b6416c2b4011b3ba1bc8928a29b90e7c5e231c2241bc
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
[C:1]-[C:2](-[C:3])(-[CH;D3;+0:4](-N-C-c1:c:c:c:c:c:1)-[NH;D2;+0:5]-C-c1:c:c:c:c:c:1)-[#8:6]-[C:7]>>[C:1]-[C:2](-[C:3])(-[CH2;D2;+0:4]-[NH2;D1;+0:5])-[#8:6]-[C:7]
101.7
[{"value": 100.0, "product": "NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 101.7, "product": "NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4′-C-(1,1′-diphenylmethylaminomethyl)-2′-deoxyuridine (12) (0.056 g, 0.13 mmol) was treated with cyclohexene (1 mL), glacial acetic acid 0.5 mL) and 5% palladium on charcoal (0.06 g) in ethanol (5 mL) according to the procedure used for the preparation of compound (4). The crude product was purified by dissolving in wa...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Secondary amine
Primary amine
c1ccccc1.c1ccccc1
null
C1CCOC1.c1ccncn1
Other
[Pd].C(C)O
null
null
O=c1ccn([C@H]2C[C@H](O)[C@](CO)(C(NCc3ccccc3)NCc3ccccc3)O2)c(=O)[nH]1>[Pd].C(C)O>NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8ed602aad6f84b358ab5d4461855826e
CC(=O)Oc1c(F)c(F)c(F)c(F)c1F.NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O>>CC(=O)NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO.C(C)(=O)OC1=C(C(=C(C(=C1F)F)F)F)F>>C(C)(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C=C1)O)CO
Fc1c(F)c(F)c(O[C:2]([CH3:1])=[O:3])c(F)c1F.[NH2:4][CH2:5][C@:6]1([CH2:7][OH:8])[O:9][C@@H:10]([n:11]2[cH:12][cH:13][c:14](=[O:15])[nH:16][c:17]2=[O:18])[CH2:19][C@@H:20]1[OH:21]>>[CH3:1][C:2](=[O:3])[NH:4][CH2:5][C@:6]1([CH2:7][OH:8])[O:9][C@@H:10]([n:11]2[cH:12][cH:13][c:14](=[O:15])[nH:16][c:17]2=[O:18])[CH2:19][C@@H...
CC(=O)Oc1c(F)c(F)c(F)c(F)c1F.NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
CC(=O)NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
null
null
CN(C=O)C
Acylation
Aminolysis of esters
bee80c17ba750e5b878660daaf03b34b83cc65c10d42a24fde7726a66e741f89
f21fd5f8c88779686ca0dcd2a6ec464a4e9cd0b9a76d99bbd673ae535081dde3
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
F-c1:c(-F):c(-F):c(-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]):c(-F):c:1-F.[#8:4]-[C:5]-[C:6]-[NH2;D1;+0:7]>>[#8:4]-[C:5]-[C:6]-[NH;D2;+0:7]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
82
[{"value": 82.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
4′-C-Aminomethyl-2′-deoxyuridine (13) (0.034 g, 0.13 mmol) was dissolved in anhydrous N,N-dimethylformamide (0.5 mL) at ambient temperature. Excess pentafluorophenyl acetate (0.88 g, 0.39 mmol) was then added directly to the reaction mixture as a solid. The resulting solution was stirred for 18 hours at ambient tempera...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide.Aromatic halide.Ester.Primary amine
Secondary amide
c1ccccc1
null
C1CCOC1.c1ccncn1
HF
CN(C=O)C
null
18
CC(=O)Oc1c(F)c(F)c(F)c(F)c1F.NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O>CN(C=O)C>CC(=O)NC[C@]1(CO)O[C@@H](n2ccc(=O)[nH]c2=O)C[C@@H]1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fb8b2ce4648d484bbd1870054f1bc6c7
CC(=O)NCC(=O)O.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O>>CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
C(C)(C)N(CC)C(C)C.NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO.C(C)(=O)NCC(=O)O.[B-](F)(F)(F)F.CN(C)C(=[N+](C)C)ON1C(=O)CCC1=O>>C(C)(=O)NCC(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO
O[C:6]([CH2:5][NH:4][C:2]([CH3:1])=[O:3])=[O:7].[NH2:8][CH2:9][C@:10]1([CH2:11][OH:12])[O:13][C@@H:14]([n:15]2[cH:16][c:17]([CH3:18])[c:19](=[O:20])[nH:21][c:22]2=[O:23])[CH2:24][C@@H:25]1[OH:26]>>[CH3:1][C:2](=[O:3])[NH:4][CH2:5][C:6](=[O:7])[NH:8][CH2:9][C@:10]1([CH2:11][OH:12])[O:13][C@@H:14]([n:15]2[cH:16][c:17]([C...
CC(=O)NCC(=O)O.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O
CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
null
null
CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5](-[C;D1;H3:6])=[O;D1;H0:7].[#8:8]-[C:9]-[C:10]-[NH2;D1;+0:11]>>[#8:8]-[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[#7:4]-[C:5](-[C;D1;H3:6])=[O;D1;H0:7]
null
[]
null
null
18
HOUR
4′-C-(Aminomethyl)thymidine (4) (0.025 g, 0.1 mmol), N-acetylglycine (0.023 g, 0.2 mmol) and TSTU (0.09 g, 0.3 mmol) were dissolved in anhydrous N,N-dimethylformamide (1 mL) at ambient temperature. Diisopropylethylamine (0.065 g, 0.5 mmol, 0.087 mL) was then added and the reaction mixture stirred for 18 hours at ambien...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
C1CCOC1.c1cncnc1
HO-
CN(C=O)C
null
18
CC(=O)NCC(=O)O.Cc1cn([C@H]2C[C@H](O)[C@@](CN)(CO)O2)c(=O)[nH]c1=O>CN(C=O)C>CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c9949be2671b4e299f745542bda2d702
CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O.CC(C)C[C@H](NC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)O>>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)[C@H](CC(C)C)NC(=O)OCC3c4ccccc4-c4ccccc43)O2)c(=O)[nH]c1=O
[B-](F)(F)(F)F.CN(C)C(=[N+](C)C)ON1C(=O)CCC1=O.C(C)(=O)NCC(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO.NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO.C(C)(C)N(CC)C(C)C.C1=CC=CC=2C3=CC=CC=C3C(C12)COC(=O)N[C@@H](CC(C)C)C(=O)O>>C1=CC=CC=2C3=CC=CC=C3C(C12)COC(=O)N[C@@H](CC(C)C)C(=O)NC[C@]1([C@H](C[C@@H](O1)N1...
CC(=O)NCC(=O)[NH:13][CH2:12][C@@:9]1([CH2:10][OH:11])[C@@H:7]([OH:8])[CH2:6][C@H:5]([n:4]2[cH:3][c:2]([CH3:1])[c:43](=[O:44])[nH:42][c:40]2=[O:41])[O:39]1.O[C:14](=[O:15])[C@H:16]([CH2:17][CH:18]([CH3:19])[CH3:20])[NH:21][C:22](=[O:23])[O:24][CH2:25][CH:26]1[c:27]2[cH:28][cH:29][cH:30][cH:31][c:32]2-[c:33]2[cH:34][cH:3...
CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O.CC(C)C[C@H](NC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)O
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)[C@H](CC(C)C)NC(=O)OCC3c4ccccc4-c4ccccc43)O2)c(=O)[nH]c1=O
null
null
CN(C)C=O
Acylation
OtherReaction
4665d7eb1e059fa98b3f12c5adcb8b6eb803a667ac153193dd3326828285173d
bbb043cea476a895a106a81a54aecbe1570485968aab284509e3f5f3d74caae2
O=C(CNC(=O)OCC1c2ccccc2-c2ccccc21)NCC1CC[C@H](n2ccc(=O)[nH]c2=O)O1
C-C(=O)-N-C-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3]-[#8:4].O-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:7](-[C:8])-[#7:9]-[C:10]=[O;D1;H0:11]>>[#8:4]-[C:3]-[C:2]-[NH;D2;+0:1]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[C:7](-[C:8])-[#7:9]-[C:10]=[O;D1;H0:11]
null
[]
null
null
null
null
4′-C-(Aminomethyl)thymidine (4) (0.025 g, 0.1 mmol), N-(9-fluorenylmethyloxycarbonyl)leucine (0.071 g, 0.2 mmol), TSTU (0.09 g, 0.3 mmol) and diisopropylethylamine (0.065 g, 0.5 mmol, 0.087 mL) were combined in DMF (1 mL) according to the procedure used to prepare compound (19). The title compound (20) was obtained as ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amide.Secondary amide
Secondary amide
null
null
c1cncnc1.C1CCOC1.c1ccc2c(c1)Cc1ccccc12
HO-
CN(C)C=O
null
null
CC(=O)NCC(=O)NC[C@]1(CO)O[C@@H](n2cc(C)c(=O)[nH]c2=O)C[C@@H]1O.CC(C)C[C@H](NC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)O>CN(C)C=O>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)[C@H](CC(C)C)NC(=O)OCC3c4ccccc4-c4ccccc43)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e281f1e4429247d3adca645f05b2dcea
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O>>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CN)O2)c(=O)[nH]c1=O
FC(C(=O)NCC(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO)(F)F>>NCC(=O)NC[C@]1([C@H](C[C@@H](O1)N1C(=O)NC(=O)C(C)=C1)O)CO
O=C(C(F)(F)F)[NH:17][CH2:16][C:14]([NH:13][CH2:12][C@@:9]1([CH2:10][OH:11])[C@@H:7]([OH:8])[CH2:6][C@H:5]([n:4]2[cH:3][c:2]([CH3:1])[c:22](=[O:23])[nH:21][c:19]2=[O:20])[O:18]1)=[O:15]>>[CH3:1][c:2]1[cH:3][n:4]([C@H:5]2[CH2:6][C@H:7]([OH:8])[C@:9]([CH2:10][OH:11])([CH2:12][NH:13][C:14](=[O:15])[CH2:16][NH2:17])[O:18]2)...
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CN)O2)c(=O)[nH]c1=O
null
null
N
Reduction
Hydrogenolysis of amides/imides/carbamates
44b36597c7daf0608965c52c8db8a9220c21d9447ce54e0af375898475f3493f
caaeb83af2cb178156ae90fe7f610a106cd4bb5397d23f56d37a7fe11e2668ed
O=c1ccn([C@H]2CCCO2)c(=O)[nH]1
F-C(-F)(-F)-C(=O)-[NH;D2;+0:1]-[C:2]-[C:3](=[O;D1;H0:4])-[#7:5]-[C:6]>>[C:6]-[#7:5]-[C:3](=[O;D1;H0:4])-[C:2]-[NH2;D1;+0:1]
67
[{"value": 67.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
4′-C-(N-trifluoroacetylglycylaminomethyl)thymidine (5) (17 mg, 0.4 mmol) was dissolved in concentrated aqueous ammonia solution (1 mL) and allowed to stand overnight at ambient temperature. The reaction mixture was then lyophilised to give the title compound (22) as a colourless resin (0.0088 g, 67%). δH(300 MHz, D2O) ...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Secondary amide
Primary amine
null
null
c1cncnc1.C1CCOC1
Other
N
null
8
Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CNC(=O)C(F)(F)F)O2)c(=O)[nH]c1=O>N>Cc1cn([C@H]2C[C@H](O)[C@](CO)(CNC(=O)CN)O2)c(=O)[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ef2f3557d9a44dbeaeb9c3c384b3664e
NCCc1c[nH]cn1.O=[N+]([O-])c1ccc(F)cc1>>O=[N+]([O-])c1ccc(NCCc2cnc[nH]2)cc1
CS(=O)C.C(C)N(CC)CC.Cl.Cl.NCCC1=CNC=N1.FC1=CC=C(C=C1)[N+](=O)[O-]>>[N+](=O)([O-])C1=CC=C(C=C1)NCCC1=CN=CN1
[NH2:8][CH2:9][CH2:10][c:11]1[cH:12][nH:13][cH:14][n:15]1.F[c:7]1[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:17][cH:16]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][CH2:9][CH2:10][c:11]2[cH:12][n:13][cH:14][nH:15]2)[cH:16][cH:17]1
NCCc1c[nH]cn1.O=[N+]([O-])c1ccc(F)cc1
O=[N+]([O-])c1ccc(NCCc2cnc[nH]2)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(NCCc2cnc[nH]2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[NH2;D1;+0:6]-[C:7]-[C:8]-[c:9]1:[c:10]:[nH;D2;+0:11]:[c:12]:[n;H0;D2;+0:13]:1>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[NH;D2;+0:6]-[C:7]-[C:8]-[c:9]1:[c:10]:[n;H0;D2;+0:11]:[c:12]:[nH;D2;+0:13]:1):[c:4]:[c:5]
89.6
[{"value": 89.6, "product": "[N+](=O)([O-])C1=CC=C(C=C1)NCCC1=CN=CN1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
10
HOUR
100 ml of DMSO were introduced into a 500 ml three-necked flask and treated with 30.9 g of triethylamine, 18.4 g of histamine dihydrochloride and 14.4 g of 1-fluoro-4-nitrobenzene. The mixture was stirred at 80° C. for 10 h, treated with 20 ml of water and stirred at 80° C. for a further 3 h. Following this, the mixtur...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1c[nH]cn1
HF
O
80
10
NCCc1c[nH]cn1.O=[N+]([O-])c1ccc(F)cc1>O>O=[N+]([O-])c1ccc(NCCc2cnc[nH]2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2f1ef429b3c44887b59ac94f97264e8c
NCCCn1ccnc1.O=[N+]([O-])c1ccc(F)cc1>>O=[N+]([O-])c1ccc(NCCCn2ccnc2)cc1
NCCCN1C=NC=C1.FC1=CC=C(C=C1)[N+](=O)[O-].CS(=O)C>>[N+](=O)([O-])C1=CC=C(C=C1)NCCCN1C=NC=C1
[NH2:8][CH2:9][CH2:10][CH2:11][n:12]1[cH:13][cH:14][n:15][cH:16]1.F[c:7]1[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:18][cH:17]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][CH2:9][CH2:10][CH2:11][n:12]2[cH:13][cH:14][n:15][cH:16]2)[cH:17][cH:18]1
NCCCn1ccnc1.O=[N+]([O-])c1ccc(F)cc1
O=[N+]([O-])c1ccc(NCCCn2ccnc2)cc1
null
null
C(C)N(CC)CC
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(NCCCn2ccnc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
111.4
[{"value": 111.4, "product": "[N+](=O)([O-])C1=CC=C(C=C1)NCCCN1C=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
12
HOUR
100 ml of DMSO were introduced into a 500 ml three-necked flask and treated with 10.3 g of triethylamine, 12.8 g of 1-(3-aminopropyl)imidazole and 14.4 g of 1-fluoro-4-nitrobenzene. The mixture was stirred at 80° C. for 12 h, cooled to room temperature and subsequently poured onto 1 l of ice. A sample of the resulting ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1c[nH]cn1
HF
C(C)N(CC)CC
80
12
NCCCn1ccnc1.O=[N+]([O-])c1ccc(F)cc1>C(C)N(CC)CC>O=[N+]([O-])c1ccc(NCCCn2ccnc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6c83fa214378440c89210958526a08e4
Cc1cc(F)ccc1[N+](=O)[O-].NCCCn1ccnc1>>Cc1cc(NCCCn2ccnc2)ccc1[N+](=O)[O-]
N(CCO)(CCO)CCO.NCCCN1C=NC=C1.FC=1C=CC(=C(C1)C)[N+](=O)[O-]>>[N+](=O)([O-])C1=C(C=C(C=C1)NCCCN1C=NC=C1)C
F[c:4]1[cH:3][c:2]([CH3:1])[c:16]([N+:17](=[O:18])[O-:19])[cH:15][cH:14]1.[NH2:5][CH2:6][CH2:7][CH2:8][n:9]1[cH:10][cH:11][n:12][cH:13]1>>[CH3:1][c:2]1[cH:3][c:4]([NH:5][CH2:6][CH2:7][CH2:8][n:9]2[cH:10][cH:11][n:12][cH:13]2)[cH:14][cH:15][c:16]1[N+:17](=[O:18])[O-:19]
Cc1cc(F)ccc1[N+](=O)[O-].NCCCn1ccnc1
Cc1cc(NCCCn2ccnc2)ccc1[N+](=O)[O-]
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation primary amine
da9dae6a655c4bd18887b692f91621e77027436294d6e1fc7be7295afb364796
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(NCCCn2ccnc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH2;D1;+0:8]>>[C:6]-[C:7]-[NH;D2;+0:8]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
80
CELSIUS
17
HOUR
150 ml of dimethyl sulfoxide were introduced into a 500 ml three-necked flask and treated with 22.6 g of triethanolamine (99% strength), 28.7 g of 1-(3-amino-propyl)imidazole (98% strength) and 24.2 g of 5-fluoro-2-nitrotoluene (96% strength). The mixture was stirred at 80° C. for 17 h. Following this, the batch was co...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1c[nH]cn1
HF
CS(=O)C
80
17
Cc1cc(F)ccc1[N+](=O)[O-].NCCCn1ccnc1>CS(=O)C>Cc1cc(NCCCn2ccnc2)ccc1[N+](=O)[O-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-00e902becac84755aca74d9f42cf30fb
CCO>>CCO.O.OCC(O)CO
C(C)O.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO>>C(C)O.O.OCC(O)CO.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO
[CH3:26][CH2:27][OH:28]>>[CH3:26][CH2:27][OH:28].[OH2:29].[OH:30][CH2:31][CH:32]([OH:33])[CH2:34][OH:35]
CCO
CCO.O.OCC(O)CO
null
null
O.OCC(O)CO
Miscellaneous
OtherReaction
a244f833733718b07f52109095aa98cd5943ebccc6e7556166190ea2fb1e9527
3886f50ccf014aba7d974a7f782a7e63fb3f50b880ebcf5701bc7ab1c8a8ad31
null
null
null
[]
null
null
null
null
95% ethanol (USP) was diluted with water (USP), glycerin (USP), and glycerol monooleate (Eastman Chemical, Kingsport N.Y.) to provide a final solution at ethanol/water/glycerin/glycerol monooleate percent ratios of 35/59/5/1, respectively. Oxybutynin free base was then dissolved into the above solution to a concentrati...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol.Primary alcohol.Secondary alcohol
null
null
null
Other
O.OCC(O)CO
null
null
CCO>O.OCC(O)CO>CCO.O.OCC(O)CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-88fa344a52a84607aa162aa511c4c43b
CCO>>CCO.O.OCC(O)CO
C(C)O.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO>>C(C)O.O.OCC(O)CO.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO
[CH3:26][CH2:27][OH:28]>>[CH3:26][CH2:27][OH:28].[OH2:29].[OH:30][CH2:31][CH:32]([OH:33])[CH2:34][OH:35]
CCO
CCO.O.OCC(O)CO
null
null
O.OCC(O)CO
Miscellaneous
OtherReaction
a244f833733718b07f52109095aa98cd5943ebccc6e7556166190ea2fb1e9527
3886f50ccf014aba7d974a7f782a7e63fb3f50b880ebcf5701bc7ab1c8a8ad31
null
null
null
[]
null
null
null
null
95% ethanol (USP) was diluted with water (USP), glycerin (USP), and glycerol monooleate (Eastman Chemical, Kingsport N.Y.) to provide a final solution at ethanol/water/glycerin/glycerol monooleate percent ratios of 35/59/5/1, respectively. Oxybutynin free base was then dissolved into the above solution to a concentrati...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol.Primary alcohol.Secondary alcohol
null
null
null
Other
O.OCC(O)CO
null
null
CCO>O.OCC(O)CO>CCO.O.OCC(O)CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f07d33de0b8549108bb55562f9fdb65a
CCO>>CCO.O.OCC(O)CO
C(C)O.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO>>C(C)O.O.OCC(O)CO.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO
[CH3:26][CH2:27][OH:28]>>[CH3:26][CH2:27][OH:28].[OH2:29].[OH:30][CH2:31][CH:32]([OH:33])[CH2:34][OH:35]
CCO
CCO.O.OCC(O)CO
null
null
O.OCC(O)CO
Miscellaneous
OtherReaction
a244f833733718b07f52109095aa98cd5943ebccc6e7556166190ea2fb1e9527
3886f50ccf014aba7d974a7f782a7e63fb3f50b880ebcf5701bc7ab1c8a8ad31
null
null
null
[]
null
null
null
null
95% ethanol (USP) was diluted with water (USP), glycerin (USP), and glycerol monooleate (Eastman Chemical, Kingsport NY) to provide a final solution at ethanol/water/glycerin/glycerol monooleate percent ratios of 35/59/5/1, respectively. Oxybutynin free base was then dissolved into the above solution to a concentration...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol.Primary alcohol.Secondary alcohol
null
null
null
Other
O.OCC(O)CO
null
null
CCO>O.OCC(O)CO>CCO.O.OCC(O)CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-761efd575dc141deb57881de7b02e7ad
CCO>>CCO.O.OCC(O)CO
C(C)O.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO>>C(C)O.O.OCC(O)CO.C(CCCCCCC\C=C/CCCCCCCC)(=O)OCC(O)CO
[CH3:26][CH2:27][OH:28]>>[CH3:26][CH2:27][OH:28].[OH2:29].[OH:30][CH2:31][CH:32]([OH:33])[CH2:34][OH:35]
CCO
CCO.O.OCC(O)CO
null
null
O.OCC(O)CO
Miscellaneous
OtherReaction
a244f833733718b07f52109095aa98cd5943ebccc6e7556166190ea2fb1e9527
3886f50ccf014aba7d974a7f782a7e63fb3f50b880ebcf5701bc7ab1c8a8ad31
null
null
null
[]
null
null
null
null
95% ethanol (USP) was diluted with water (USP), glycerin (USP), and glycerol monooleate (Eastman Chemical, Kingsport N.Y.) to provide a final solution at ethanol/water/glycerin/glycerol monooleate percent ratios of 35/59/5/1, respectively. Oxybutynin free base was then dissolved into the above solution to a concentrati...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol.Primary alcohol.Secondary alcohol
null
null
null
Other
O.OCC(O)CO
null
null
CCO>O.OCC(O)CO>CCO.O.OCC(O)CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-278ccc5998f54f15ac9cb0e5406b4b9d
CCOc1ccc(C2CCC3(CC2)OCCO3)c(F)c1F>>CCOc1ccc(C2CCC(=O)CC2)c(F)c1F
C1COC2(CCC(CC2)C2=C(C(=C(C=C2)OCC)F)F)O1.C(=O)O>>FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=O
C1C[O:12][C:11]2(O1)[CH2:10][CH2:9][CH:8]([c:7]1[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:17]([F:18])[c:15]1[F:16])[CH2:14][CH2:13]2>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH:8]2[CH2:9][CH2:10][C:11](=[O:12])[CH2:13][CH2:14]2)[c:15]([F:16])[c:17]1[F:18]
CCOc1ccc(C2CCC3(CC2)OCCO3)c(F)c1F
CCOc1ccc(C2CCC(=O)CC2)c(F)c1F
null
null
C1(=CC=CC=C1)C
Miscellaneous
Ketal hydrolysis to ketone
7165849453c1f3f22c37497ec202aa2a6a319b018b3ae9fffa16fa9182ebd128
547697208447432e865290cf95eed8e4fcddc12f59856b7ddbf24dc1accb1210
O=C1CCC(c2ccccc2)CC1
[C:1]-[C:2]-[C;H0;D4;+0:3]1(-O-C-C-[O;H0;D2;+0:4]-1)-[C:5]-[C:6]>>[C:1]-[C:2]-[C;H0;D3;+0:3](=[O;H0;D1;+0:4])-[C:5]-[C:6]
100
[{"value": 100.0, "product": "FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Crude 4-(2,3-difluoro-4-ethoxyphenyl)-cyclohexanone monoethylene acetal (50.3 mmol) obtained in Step 1 was dissolved in 200 ml of toluene, 87% formic acid (503 mmol) was added, and the solution was heated to reflux for 4 hours. The reaction solution was washed twice with 100 ml of a saturated aqueous solution of sodium...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ketone
C1CCC2(CC1)OCCO2
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
C1(=CC=CC=C1)C
null
null
CCOc1ccc(C2CCC3(CC2)OCCO3)c(F)c1F>C1(=CC=CC=C1)C>CCOc1ccc(C2CCC(=O)CC2)c(F)c1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4ff8dfbed6ca40f0b866cec334ac483f
CCOc1ccc(C2CCC(=O)CC2)c(F)c1F.c1ccc([P+](CCC2OCCCO2)(c2ccccc2)c2ccccc2)cc1>>CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F
CC(C)(C)[O-].[K+].[Br-].O1C(OCCC1)CC[P+](C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1.FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=O>>FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=CCC1OCCCO1
O=[C:11]1[CH2:10][CH2:9][CH:8]([c:7]2[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:24]([F:25])[c:22]2[F:23])[CH2:21][CH2:20]1.c1ccc([P+](c2ccccc2)(c2ccccc2)[CH2:12][CH2:13][CH:14]2[O:15][CH2:16][CH2:17][CH2:18][O:19]2)cc1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH:8]2[CH2:9][CH2:10][C:11](=[CH:12][CH2:13][CH:14]3[O:15]...
CCOc1ccc(C2CCC(=O)CC2)c(F)c1F.c1ccc([P+](CCC2OCCCO2)(c2ccccc2)c2ccccc2)cc1
CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F
null
null
C1CCOC1
C-C Coupling
Wittig with Phosphonium
4ace91bfe286d7308b684482c14d0e07094c3e16f8d78c7715341add0f69a6d3
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
C(CC1OCCCO1)=C1CCC(c2ccccc2)CC1
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5].[#8:6]-[C:7](-[C:8]-[CH2;D2;+0:9]-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1)-[#8:10]>>[#8:6]-[C:7](-[C:8]-[CH;D2;+0:9]=[C;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5])-[#8:10]
73.4
[{"value": 73.4, "product": "FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=CCC1OCCCO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-30
CELSIUS
1
HOUR
A mixture of 2-(1,3-dioxane-2-yl)-ethyltriphenyl phosphonium bromide (60.4 mmol) and 30 ml of THF was cooled down to −30° C. by use of a refrigerant under a nitrogen flow. To this mixture, t-BuOK (60.4 mmol) was added, and the mixture was stirred for one hour. A solution of the crude 4-(2,3-difluoro-4-ethoxyphenyl)-cyc...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
C1CCCCC1.c1ccccc1.c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1.C1COCOC1
HO-
C1CCOC1
-30
1
CCOc1ccc(C2CCC(=O)CC2)c(F)c1F.c1ccc([P+](CCC2OCCCO2)(c2ccccc2)c2ccccc2)cc1>C1CCOC1>CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ce76130bc77244d494327549fffb2ce1
CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F>>CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F
FC1=C(C=CC(=C1F)OCC)C1CCC(CC1)=CCC1OCCCO1>>FC1=C(C=CC(=C1F)OCC)[C@@H]1CC[C@H](CC1)CCC1OCCCO1
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([CH:8]2[CH2:9][CH2:10][C:11](=[CH:12][CH2:13][CH:14]3[O:15][CH2:16][CH2:17][CH2:18][O:19]3)[CH2:20][CH2:21]2)[c:22]([F:23])[c:24]1[F:25]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C@H:8]2[CH2:9][CH2:10][C@H:11]([CH2:12][CH2:13][CH:14]3[O:15][CH2:16][CH2:17][CH2:18][O:19]3)[C...
CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F
CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F
null
[Pd]
C1(=CC=CC=C1)C.C(C)O
Reduction
Hydrogenation (double to single)
da8a9b0fabf153e7390d0529375b4e7b6b9340230ccf509d4c3ece1ac615e7d0
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccc([C@H]2CC[C@H](CCC3OCCCO3)CC2)cc1
[#8:1]-[C:2](-[C:3]-[CH;D2;+0:4]=[C;H0;D3;+0:5](-[C:6]-[C:7])-[C:8]-[C:9])-[#8:10]>>[#8:1]-[C:2](-[C:3]-[CH2;D2;+0:4]-[C@H;D3;+0:5](-[C:6]-[C:7])-[C:8]-[C:9])-[#8:10]
100
[{"value": 100.0, "product": "FC1=C(C=CC(=C1F)OCC)[C@@H]1CC[C@H](CC1)CCC1OCCCO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
The 2-(2-(4-(2,3-difluoro-4-ethoxyphenyl)cyclohexylidene)-ethyl)-1,3-dioxane (36.9 mmol) obtained by the reaction of Step 3 was dissolved in 100 ml of a mixed solvent of toluene/ethanol (1/1), 4.0 g of 5-wt %-palladium/carbon catalyst was added, and the solution was stirred for 7 hours at room temperature under a hydro...
10.6084/m9.figshare.5104873.v1
null
null
null
C1CCCCC1
C1CCCCC1
c1ccccc1.C1CCCCC1.C1COCOC1
null
[Pd].C1(=CC=CC=C1)C.C(C)O
null
7
CCOc1ccc(C2CCC(=CCC3OCCCO3)CC2)c(F)c1F>[Pd].C1(=CC=CC=C1)C.C(C)O>CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c5d2a3c98a094bf9b2875bcfff8c573c
CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F>>CCOc1ccc([C@@H]2CC[C@@H](CCC=O)CC2)c(F)c1F
FC1=C(C=CC(=C1F)OCC)[C@@H]1CC[C@H](CC1)CCC1OCCCO1.C(=O)O>>FC1=C(C=CC(=C1F)OCC)[C@@H]1CC[C@H](CC1)CCC=O
C1CO[CH:14]([CH2:13][CH2:12][C@H:11]2[CH2:10][CH2:9][C@H:8]([c:7]3[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[c:20]([F:21])[c:18]3[F:19])[CH2:17][CH2:16]2)[O:15]C1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]([C@H:8]2[CH2:9][CH2:10][C@H:11]([CH2:12][CH2:13][CH:14]=[O:15])[CH2:16][CH2:17]2)[c:18]([F:19])[c:20]1[F:21]
CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F
CCOc1ccc([C@@H]2CC[C@@H](CCC=O)CC2)c(F)c1F
null
null
C1(=CC=CC=C1)C
Miscellaneous
Acetal hydrolysis to aldehyde
c0e8259a4c04433c939fe17907d7eafe1c52bcb535318030bf0e1cb6f82c0712
84d5a69453aa750f462aa94a6bf2116fc17c5d88a9619aaa9eefb74b0c09848d
c1ccc(C2CCCCC2)cc1
[C:1]-[C:2]-[CH;D3;+0:3]1-O-C-C-C-[O;H0;D2;+0:4]-1>>[C:1]-[C:2]-[CH;D2;+0:3]=[O;H0;D1;+0:4]
100
[{"value": 100.0, "product": "FC1=C(C=CC(=C1F)OCC)[C@@H]1CC[C@H](CC1)CCC=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The 2-(2-(trans-4-(2,3-difluoro-4-ethoxyphenyl)-cyclohexyl)-ethyl)-1,3-dioxane (19.8 mmol) obtained by the reaction of Step 4 was dissolved in 100 ml of toluene, 87% formic acid (198 mmol) was added, and the solution was heated to reflux for 4 hours. The reaction solution was twice washed with 50 ml of a saturated aque...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aldehyde
C1COCOC1
null
c1ccccc1.C1CCCCC1
HO-
C1(=CC=CC=C1)C
null
null
CCOc1ccc([C@@H]2CC[C@@H](CCC3OCCCO3)CC2)c(F)c1F>C1(=CC=CC=C1)C>CCOc1ccc([C@@H]2CC[C@@H](CCC=O)CC2)c(F)c1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e406312d98c049aa96999117a8c91f3e
C=CC=O>>C=CC=O
CN(C(C=C)=O)C.C(=O)C=C.N(=NC(C#N)(C)C)C(C#N)(C)C>>CN(C(C=C)=O)C.C(=O)C=C
[CH2:8]=[CH:9][CH:10]=[O:11]>>[CH2:8]=[CH:9][CH:10]=[O:11]
C=CC=O
C=CC=O
null
null
O1CCCC1
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
To tetrahydrofuran (300 g) were added N,N-dimethylacrylamide (70 g), acrolein (30 g) and AIBN (2,2′-azobisisobutyronitrile) (5 g). The resulting mixture was reacted at 66° C. for 8 hours. After reaction, the resulting mixture was precipitated in ether, filtered, and dehydrated, thereby obtaining poly(N,N-dimethylacryla...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O1CCCC1
null
null
C=CC=O>O1CCCC1>C=CC=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-12928a2eaec7459589ce187d1ee9646a
C=C(C)C(=O)OCCO>>C=C(C)C(=O)OCCO
COC(C(=C)C)=O.OCCOC(C(=C)C)=O.C(C=C)(=O)O.CC(C)(C#N)N=NC(C)(C)C#N>>COC(C(=C)C)=O.OCCOC(C(=C)C)=O.C(C=C)(=O)O
[CH2:8]=[C:9]([CH3:10])[C:11](=[O:12])[O:13][CH2:14][CH2:15][OH:16]>>[CH2:8]=[C:9]([CH3:10])[C:11](=[O:12])[O:13][CH2:14][CH2:15][OH:16]
C=C(C)C(=O)OCCO
C=C(C)C(=O)OCCO
null
null
CC(=O)CC.O1CCCC1
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
To tetrahydrofuran (250 g) and methylethylketone (250 g) were added methylmethacrylate (40 g), 2-hydroxyethylmethacrylate (30 g), acrylic acid (30 g) and AIBN (2.5 g). The resulting mixture was reacted at 66° C. for 8 hours. After reaction, the resulting mixture was precipitated in ether, filtered, and dehydrated, ther...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CC(=O)CC.O1CCCC1
null
null
C=C(C)C(=O)OCCO>CC(=O)CC.O1CCCC1>C=C(C)C(=O)OCCO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-750d8ab497db4ebeb91e5d10a9695c1b
C=CC(OC)OC.C=CC=O.COCC(C)OC(C)=O>>C=C(C)C(=O)OC.C=C(C)C(=O)OCCO.C=CC(=O)O
CC(COC)OC(=O)C.COC(C=C)OC.C(=O)C=C>>COC(C(=C)C)=O.OCCOC(C(=C)C)=O.C(C=C)(=O)O
[CH3:14][O:20][CH:19]([O:16][CH3:15])[CH:18]=[CH2:17].[CH:9](=[CH2:10])[CH:11]=[O:12].[CH2:1]([CH:2]([CH3:3])[O:21][C:4](=[O:5])[CH3:8])[O:6][CH3:7]>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH3:7].[CH2:8]=[C:9]([CH3:10])[C:11](=[O:12])[O:13][CH2:14][CH2:15][OH:16].[CH2:17]=[CH:18][C:19](=[O:20])[OH:21]
C=CC(OC)OC.C=CC=O.COCC(C)OC(C)=O
C=C(C)C(=O)OC.C=C(C)C(=O)OCCO.C=CC(=O)O
null
null
null
Acylation
OtherReaction
65460a54a1bf21ae503da0fb81f9b603fc6db58af8e7bac21de01b6e814263bf
4394e8022841beefad133ac77e7c756c74cc3fec5db8914262dd1070a955fcc5
null
[C;D1;H2:1]=[C:2]-[CH;D3;+0:3](-[O;H0;D2;+0:4]-[CH3;D1;+0:5])-[O;H0;D2;+0:6]-[CH3;D1;+0:7].[C;D1;H3:8]-[CH;D3;+0:9](-[CH2;D2;+0:10]-[O;H0;D2;+0:11]-[C;D1;H3:12])-[O;H0;D2;+0:13]-[C;H0;D3;+0:14](-[CH3;D1;+0:15])=[O;D1;H0:16].[CH2;D1;+0:17]=[CH;D2;+0:18]-[CH;D2;+0:19]=[O;D1;H0:20]>>[C;D1;H2:1]=[C:2]-[C;H0;D3;+0:3](=[O;H0...
null
[]
null
null
null
null
To propyleneglycolmethyletheracetate (PGMEA) (130 g) as an organic solvent were added poly(N,N-dimethylacryladmide/3,3-dimethoxypropene/acrolein) (3 g) obtained from Example 1, poly(methylmethacrylate/2-hydroxyethylmethacrylate/acrylic acid) (7 g) obtained from Example 2 and triphenylsulfonium triflate (0.05 g) as a ph...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester.Ether.Ether.Ether.Vinyl
Carboxylic acid.Ester.Ester.Primary alcohol.Vinyl.Vinyl
null
null
null
Other
null
null
null
C=CC(OC)OC.C=CC=O.COCC(C)OC(C)=O>>C=C(C)C(=O)OC.C=C(C)C(=O)OCCO.C=CC(=O)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-156955290ae845ef8c4c29c66f5866ca
C=C(C)C(=O)O.CC(C)=O.O=C1OC(=O)[C@@H]2CCCC[C@H]12>>C=C(C)C(=O)OCCOC(=O)C1CCCCC1C(=O)O
CC(=O)C.[C@@H]12[C@@H](CCCC1)C(=O)OC2=O.C(C(=C)C)(=O)O>>C(C(=C)C)(=O)OCCOC(=O)C1C(CCCC1)C(=O)O
[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[OH:6].C[C:8]([CH3:7])=[O:9].[C:10]1(=[O:11])[C@H:12]2[CH2:13][CH2:14][CH2:15][CH2:16][C@H:17]2[C:18](=[O:19])[O:20]1>>[CH2:1]=[C:2]([CH3:3])[C:4](=[O:5])[O:6][CH2:7][CH2:8][O:9][C:10](=[O:11])[CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH:17]1[C:18](=[O:19])[OH:20]
C=C(C)C(=O)O.CC(C)=O.O=C1OC(=O)[C@@H]2CCCC[C@H]12
C=C(C)C(=O)OCCOC(=O)C1CCCCC1C(=O)O
null
null
O
Protection
OtherReaction
88e33a1da3a3458d2b82b80e9b8e6d156e5642270cb078fa99f672050dfa2a85
d08edf875d3a4b403a08ae8fd0cf1342df8502dc704b991940af7ae29f106b2d
C1CCCCC1
C-[C;H0;D3;+0:1](-[CH3;D1;+0:2])=[O;H0;D1;+0:3].[C;D1;H2:4]=[C:5](-[C;D1;H3:6])-[C:7](=[O;D1;H0:8])-[OH;D1;+0:9].[O;D1;H0:10]=[C;H0;D3;+0:11]1-[O;H0;D2;+0:12]-[C:13](=[O;D1;H0:14])-[C@@H;D3;+0:15]2-[C:16]-[C:17]-[C:18]-[C:19]-[C@H;D3;+0:20]-1-2>>[C;D1;H2:4]=[C:5](-[C;D1;H3:6])-[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-[CH2;D2...
null
[]
null
null
1
HOUR
Into acetone (1,000 ml) were dissolved cis-1,2-cyclohexane dicarboxylic anhydride (308.3 g), methacrylic acid (2-hydroxyethyl) (273.3 g) and 4-(dimethylamine) pyridine (4.9 g), and heated for 5 hours under reflux. After acetone had been distilled off under reduced pressure, 1N hydrochloric acid (500 ml) and ethyl aceta...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Carboxylic acid.Ketone
Carboxylic acid.Ester.Ester
C1CC[C@H]2COC[C@H]2C1
null
C1CCCCC1
Other
O
null
1
C=C(C)C(=O)O.CC(C)=O.O=C1OC(=O)[C@@H]2CCCC[C@H]12>O>C=C(C)C(=O)OCCOC(=O)C1CCCCC1C(=O)O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-02c0ddb3dd46487290cbe5ee3bbd5d63
OC[C@@H](O)[C@@H](O)[C@@H](O)CO.OC[C@H](O)C(O)[C@@H](O)CO.O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O>>OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
C([C@H]([C@H]([C@H]([C@H](CO)O)O)O)O)O.C([C@H]([C@@H]([C@@H]([C@H](CO)O)O)O)O)O.OC[C@@H](O)[C@H](O)[C@@H](O)[C@@H](O)CO.C([C@H](O)[C@H](O)[C@H](O)CO)O.C([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)O.C([C@H](O)[C@@H](O)[C@H](O)[C@@H](O)CO)O.[C@@H]1([C@@H]([C@@H]([C@@H]([C@H]([C@@H]1O)O)O)O)O)O.C...
O[C@H:5]([C@@H:3]([CH2:2][OH:1])[OH:4])[C@@H:18]([OH:19])[CH2:20][OH:21].OC([C@@H](O)[CH2:10][OH:11])[C@@H](O)[CH2:22][OH:23].O[C@H]1[C@H:7]([OH:6])[C@H:16]([OH:17])[C@H:14]([OH:15])[C@@H:12]([OH:13])[C@@H:9]1[OH:8]>>[OH:1][CH2:2][C@@H:3]([OH:4])[C@@H:5]([O:6][C@H:7]1[O:8][C@H:9]([CH2:10][OH:11])[C@@H:12]([OH:13])[C@H:...
OC[C@@H](O)[C@@H](O)[C@@H](O)CO.OC[C@H](O)C(O)[C@@H](O)CO.O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O
OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
34e0a3f88b2f57ed7c4bec6476031bf118be09afc16e8b39b989f686f1540b33
7e797b6b8c0c9bab05d231d06fdd9e03052e7f7b88ca619d2e7f6dd67bfb2df8
C1CCOCC1
O-C(-[C@@H](-O)-[CH2;D2;+0:1]-[O;D1;H1:2])-[C@@H](-O)-[CH2;D2;+0:3]-[O;D1;H1:4].O-[C@@H]1-[C@H;D3;+0:5](-[OH;D1;+0:6])-[C:7](-[O;D1;H1:8])-[C:9]-[C:10](-[O;D1;H1:11])-[C@H;D3;+0:12]-1-[OH;D1;+0:13].O-[C@H;D3;+0:14](-[C:15](-[O;D1;H1:16])-[CH2;D2;+0:17]-[O;D1;H1:18])-[C:19](-[C:20])-[O;D1;H1:21]>>[C:20]-[C:19](-[O;D1;H1...
null
[]
null
null
null
null
Examples of the sugar alcohols are D, L-arabitol, ribitol, xylitol, D, L-sorbitol, D, L-mannitol, D, L-iditol, D, L-talitol, meso-inositol, dulcitol, and allodulcitol. Further, maltitol obtained by subjecting disaccharides to hydrogenation and reductants (e.g., reduced starch syrup) obtained by subjecting oligosacchari...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
Ether.Ether.Primary alcohol.Primary alcohol.Secondary alcohol
C1CCCCC1
C1CCOCC1
C1CCOCC1
HO-
null
null
null
OC[C@@H](O)[C@@H](O)[C@@H](O)CO.OC[C@H](O)C(O)[C@@H](O)CO.O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]1O>>OC[C@@H](O)[C@@H](O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)[C@H](O)[C@@H](O)CO
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-02e7e21623fd4748b28d74da50786052
Nc1ccc2nc(O)c(O)nc2c1>>[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1
Cl.NC=1C=C2N=C(C(=NC2=CC1)O)O.[N-]=[N+]=[N-].[Na+].N(=O)[O-].[Na+]>>N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1)O)O
[NH2:3][c:4]1[cH:5][cH:6][c:7]2[n:8][c:9]([OH:10])[c:11]([OH:12])[n:13][c:14]2[cH:15]1>>[N-:1]=[N+:2]=[N:3][c:4]1[cH:5][cH:6][c:7]2[n:8][c:9]([OH:10])[c:11]([OH:12])[n:13][c:14]2[cH:15]1
Nc1ccc2nc(O)c(O)nc2c1
[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1
null
null
O.OS(=O)(=O)O
Miscellaneous
Amine to azide
874c0cf1984ab0c3156493e6524e4a76434860bf4d8c4f6115608f4b54932f2a
0dcf06f7cec37f2f50b2497bf88be0f43ce4890a2df8b6f4eb18df3f7b6a2a7d
c1ccc2nccnc2c1
[#7;a:1]:[c:2]:[c:3]:[c:4](-[NH2;D1;+0:5]):[c:6]>>[#7;a:1]:[c:2]:[c:3]:[c:4](-[N;H0;D2;+0:5]=[#7;+:7]=[N;-;D1;H0:8]):[c:6]
67
[{"value": 67.0, "product": "N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1)O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.8, "product": "N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1)O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
15
MINUTE
A solution of 5 g (23.5 mmol) 6-amino-2,3-dihydroxyquinoxaline hydrochloride in 250 ml 0.5 N H2SO4 is cooled to 0° C. and then a solution of 1.65 g (24 mmol) NaNO2 in 50 ml water is added. After stirring at 0° C. for 15 min., a solution of 1.5 g (24 mmol) NaN3 in 100 ml water is added. Stirring at 0° C. for 45 min. giv...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Azide
null
null
c1ccc2nccnc2c1
Other
O.OS(=O)(=O)O
0
0.25
Nc1ccc2nc(O)c(O)nc2c1>O.OS(=O)(=O)O>[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a942e4fd4c9b4307850ab5026494e834
O=[N+]([O-])O.[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1>>[N-]=[N+]=Nc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1)O)O.[N+](=O)(O)[O-]>>N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O
O[N+:16](=[O:17])[O-:18].[N-:1]=[N+:2]=[N:3][c:15]1[cH:4][cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14]1>>[N-:1]=[N+:2]=[N:3][c:4]1[cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14][c:15]1[N+:16](=[O:17])[O-:18]
O=[N+]([O-])O.[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1
[N-]=[N+]=Nc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
null
null
C(C)(=O)O
Functional Group Addition
Aromatic nitration with HNO3
37bdfc0ed0dc9f813368bd3bc7c72a93dce8c81565853939e7b462c53f39d02d
5a3824aa005ce892a6e1c787f983b0d27b16b43391fc0c52a724f93c6266a8aa
c1ccc2nccnc2c1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[N;-;D1;H0:4]=[#7;+:5]=[N;H0;D2;+0:6]-[c;H0;D3;+0:7]1:[c:8]:[c:9]2:[#7;a:10]:[c:11]:[c:12]:[#7;a:13]:[c:14]:2:[c:15]:[cH;D2;+0:16]:1>>[N;-;D1;H0:4]=[#7;+:5]=[N;H0;D2;+0:6]-[c;H0;D3;+0:16]1:[c:15]:[c:14]2:[#7;a:13]:[c:12]:[c:11]:[#7;a:10]:[c:9]:2:[c:8]:[c;H0;D3;+0:7]:1-[N+;H0;D...
78
[{"value": 78.0, "product": "N(=[N+]=[N-])C=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O", "details": "PERCENTYIELD", "is_desired": false}]
24
CELSIUS
4
HOUR
2 g 6-azido-2,3-dihydroxyquinoxaline is suspended in 100 ml glacial acetic acid. To the suspension is added 16 ml fuming nitric acid at 24° C. The mixture is stirred at 24° C. for 4 h giving a precipitate of 1.9 g (78%) 6-azido-2,3-dihydroxy-7-nitroquinoxaline. IR: a peak at 2120 cm−1. NMR: two singlets (7.0 and 7.7 pp...
10.6084/m9.figshare.5104873.v1
null
Azide.Nitrate
Azide.Nitro group
c1ccc2nccnc2c1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
HO-
C(C)(=O)O
24
4
O=[N+]([O-])O.[N-]=[N+]=Nc1ccc2nc(O)c(O)nc2c1>C(C)(=O)O>[N-]=[N+]=Nc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-13df26d266a64ad88e30ef4d4128c856
Oc1nc2ccc(C(F)(F)F)cc2nc1O>>O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1C(F)(F)F
OC1=NC2=CC=C(C=C2N=C1O)C(F)(F)F.[N+](=O)([O-])[O-].[K+].Cl>>OC1=NC2=CC(=C(C=C2N=C1O)[N+](=O)[O-])C(F)(F)F
[cH:4]1[cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14][c:15]1[C:16]([F:17])([F:18])[F:19]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14][c:15]1[C:16]([F:17])([F:18])[F:19]
Oc1nc2ccc(C(F)(F)F)cc2nc1O
O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1C(F)(F)F
null
null
[OH-].[Na+].OS(=O)(=O)O
Functional Group Addition
OtherReaction
5bb74314601b8a07868b6724521bd2147502d00fa9938aa4b54a5783d20f96b8
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccc2nccnc2c1
[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[c:5]1:[c:6]:[c:7]2:[#7;a:8]:[c:9]:[c:10]:[#7;a:11]:[c:12]:2:[c:13]:[cH;D2;+0:14]:1>>[F;D1;H0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[c:5]1:[c:6]:[c:7]2:[#7;a:8]:[c:9]:[c:10]:[#7;a:11]:[c:12]:2:[c:13]:[c;H0;D3;+0:14]:1-[#7;+:15](-[O;-;D1;H0:16])=[O;D1;H0:17]
72
[{"value": 72.0, "product": "OC1=NC2=CC(=C(C=C2N=C1O)[N+](=O)[O-])C(F)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 71.0, "product": "OC1=NC2=CC(=C(C=C2N=C1O)[N+](=O)[O-])C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
24
CELSIUS
3
HOUR
A solution of 1 g (4.4 mmol) 2,3-dihydroxy-6-trifluoromethylquinoxaline in 10 ml concentrated H2SO4 is cooled to 0° C. and 438 mg (4.4 mmol) KNO3 is added. The mixture is stirred at 0° C. for 0.5 h and at 24° C. for 3 h. The reaction mixture is poured into ice-water to give 1.02 g crude product. The crude product is di...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccc2nccnc2c1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
Other
[OH-].[Na+].OS(=O)(=O)O
24
3
Oc1nc2ccc(C(F)(F)F)cc2nc1O>[OH-].[Na+].OS(=O)(=O)O>O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1C(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d389543dfca3403984fc379dfada1957
Oc1nc2ccc(Cl)cc2nc1O>>O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Cl
[N+](=O)([O-])[O-].[K+].ClC=1C=C2N=C(C(=NC2=CC1)O)O>>ClC=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O
[cH:4]1[cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14][c:15]1[Cl:16]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]2[n:7][c:8]([OH:9])[c:10]([OH:11])[n:12][c:13]2[cH:14][c:15]1[Cl:16]
Oc1nc2ccc(Cl)cc2nc1O
O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Cl
null
null
S(O)(O)(=O)=O
Functional Group Addition
OtherReaction
5bb74314601b8a07868b6724521bd2147502d00fa9938aa4b54a5783d20f96b8
22f3183026a2d99c91ec0c53f0059a15c8421016bd62c8ab45281362b96dc686
c1ccc2nccnc2c1
[Cl;D1;H0:1]-[c:2]1:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[cH;D2;+0:11]:1>>[Cl;D1;H0:1]-[c:2]1:[c:3]:[c:4]2:[#7;a:5]:[c:6]:[c:7]:[#7;a:8]:[c:9]:2:[c:10]:[c;H0;D3;+0:11]:1-[#7;+:12](-[O;-;D1;H0:13])=[O;D1;H0:14]
88
[{"value": 88.0, "product": "ClC=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.8, "product": "ClC=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
Finely powdered potassium nitrate (1.01 g, 10 mmol) is added during 5 min. to a stirred solution of 6-chloro-2,3-dihydroxyquinoxaline (1.97 g, 10 mmol) in 50 ml of concentrated sulfuric acid at 0° C. After 1 h, the ice bath was removed and stirring continued for 2.5 h at room temperature. The mixture is poured into 200...
10.6084/m9.figshare.5104873.v1
null
null
Nitro group
c1ccc2nccnc2c1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
Other
S(O)(O)(=O)=O
null
1
Oc1nc2ccc(Cl)cc2nc1O>S(O)(O)(=O)=O>O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2b9757f8dd5e40beb81d93fb78750d32
C#C[Si](C)(C)C.O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Br>>C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
BrC=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O.C[Si](C)(C)C#C>>OC1=NC2=CC(=C(C=C2N=C1O)C#C[Si](C)(C)C)[N+](=O)[O-]
[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[CH:6].Br[c:7]1[cH:8][c:9]2[n:10][c:11]([OH:12])[c:13]([OH:14])[n:15][c:16]2[cH:17][c:18]1[N+:19](=[O:20])[O-:21]>>[CH3:1][Si:2]([CH3:3])([CH3:4])[C:5]#[C:6][c:7]1[cH:8][c:9]2[n:10][c:11]([OH:12])[c:13]([OH:14])[n:15][c:16]2[cH:17][c:18]1[N+:19](=[O:20])[O-:21]
C#C[Si](C)(C)C.O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Br
C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
null
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1
C(C)N(CC)CC.CN(C=O)C.C(C)(=O)OCC
C-C Coupling
Sonogashira alkyne_aryl halide
8917c76131fd1d6c0f73ddeb3eada5a190521ccd8222fe1834ae40371801b863
305eca0fd2975da49e7f69e4edfb9dc1cbce82513954bc5a73be3289e70e5f76
c1ccc2nccnc2c1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]2:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:2:[c:9]:[c:10]:1-[#7;+:11].[C;D1;H3:12]-[#14:13](-[C;D1;H3:14])(-[C;D1;H3:15])-[C:16]#[CH;D1;+0:17]>>[#7;+:11]-[c:10]1:[c:9]:[c:8]2:[#7;a:7]:[c:6]:[c:5]:[#7;a:4]:[c:3]:2:[c:2]:[c;H0;D3;+0:1]:1-[C;H0;D2;+0:17]#[C:16]-[#14:13](-[C;D1;H3:12])(-[C;D1;H3:14...
70
[{"value": 70.0, "product": "OC1=NC2=CC(=C(C=C2N=C1O)C#C[Si](C)(C)C)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.4, "product": "OC1=NC2=CC(=C(C=C2N=C1O)C#C[Si](C)(C)C)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 500 mg (1.9 mmol) 6-bromo-2,3-dihydroxy-7-nitroquinoxaline (supra) in 10 ml dry dimethylformamide and 20 ml dry triethylamine is added to 4 mg palladium(II)acetate, 8 mg triphenylphosphine and 600 μl (4.3 mmol) trimethylsilylacetylene. The mixture is refluxed for 2.5 h under nitrogen. After cooling to room...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Alkyne
Alkyne
c1ccc2nccnc2c1
c1ccc2nccnc2c1
c1ccc2nccnc2c1
HBr
C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC.CN(C=O)C.C(C)(=O)OCC
null
null
C#C[Si](C)(C)C.O=[N+]([O-])c1cc2nc(O)c(O)nc2cc1Br>C(C)(=O)[O-].[Pd+2].C(C)(=O)[O-].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(C)N(CC)CC.CN(C=O)C.C(C)(=O)OCC>C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0ece84acd02d486896ae7513d4434d3f
C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]>>C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
OC1=NC2=CC(=C(C=C2N=C1O)C#C[Si](C)(C)C)[N+](=O)[O-].C([O-])([O-])=O.[K+].[K+]>>C(#C)C=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O
C[Si](C)(C)[C:1]#[C:2][c:3]1[cH:4][c:5]2[n:6][c:7]([OH:8])[c:9]([OH:10])[n:11][c:12]2[cH:13][c:14]1[N+:15](=[O:16])[O-:17]>>[CH:1]#[C:2][c:3]1[cH:4][c:5]2[n:6][c:7]([OH:8])[c:9]([OH:10])[n:11][c:12]2[cH:13][c:14]1[N+:15](=[O:16])[O-:17]
C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
null
null
CO
Deprotection
TMS deprotection from alkyne
e85676bb81da384790c9c858d44f182cdd01e3a79f77f7a239fe38487234cb96
56d526d7c9cb1bd7bee4940e216a9b1dd4597fd025a186b8d6e4675d8f4db26b
c1ccc2nccnc2c1
C-[Si](-C)(-C)-[C;H0;D2;+0:1]#[C:2]-[c:3]>>[CH;D1;+0:1]#[C:2]-[c:3]
88
[{"value": 88.0, "product": "C(#C)C=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 87.4, "product": "C(#C)C=1C=C2N=C(C(=NC2=CC1[N+](=O)[O-])O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 300 mg (0.99 mmol) 2,3-dihydroxy-6-trimethylsilylethynyl-7-nitroquinoxaline in 10 ml methanol is added to 200 mg (1.45 mmol) potassium carbonate and then stirred at room temperature for 1 h. The reaction mixture is evaporated in vacuo and 4N hydrochloric acid is added to pH 6. The precipitated product is ...
10.6084/m9.figshare.5104873.v1
null
Alkyne.Silyl protective group
Alkyne
null
null
c1ccc2nccnc2c1
Other
CO
null
1
C[Si](C)(C)C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]>CO>C#Cc1cc2nc(O)c(O)nc2cc1[N+](=O)[O-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-47f59773229d4319a93d7c9cf0becb3a
C=CCC(O)CC=C.O=C(Cl)CCCCBr>>C=CCCC(C=C)OC(=O)CCCCBr
BrCCCCC(=O)Cl.C=CCC(CC=C)O.C(C)N(CC)CC>>BrCCCCC(=O)OC(CCC=C)C=C
[CH2:1]=[CH:7][CH2:6][CH:5]([CH2:4][CH:3]=[CH2:2])[OH:8].Cl[C:9](=[O:10])[CH2:11][CH2:12][CH2:13][CH2:14][Br:15]>>[CH2:1]=[CH:2][CH2:3][CH2:4][CH:5]([CH:6]=[CH2:7])[O:8][C:9](=[O:10])[CH2:11][CH2:12][CH2:13][CH2:14][Br:15]
C=CCC(O)CC=C.O=C(Cl)CCCCBr
C=CCCC(C=C)OC(=O)CCCCBr
null
null
C(Cl)Cl
Acylation
OtherReaction
eaf7edf95fe1ca81729982649f7a94da84a6028e14bdb80377c73dbda364ed1b
a4c1c928193a4ebe64c0ee17bff0acb7a23b182e790a7ce7aa444a685a0a6aef
null
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[CH2;D1;+0:5]=[CH;D2;+0:6]-[CH2;D2;+0:7]-[C:8](-[OH;D1;+0:9])-[C:10]-[CH;D2;+0:11]=[CH2;D1;+0:12]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8](-[C:10]-[CH2;D2;+0:11]-[CH;D2;+0:12]=[CH2;D1;+0:5])-[CH;D2;+0:7]=[CH2;D1;+0:6]
48
[{"value": 48.0, "product": "BrCCCCC(=O)OC(CCC=C)C=C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.5, "product": "BrCCCCC(=O)OC(CCC=C)C=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
5-Bromopentanoyl chloride (3.0 g, 0.015 mol) was added dropwise to 1,6-heptadien-4-ol (1.5 g, 0.013 mol) and triethylamine (1.4 g, 0.014 mol) in DCM (25 cm3). The mixture was stirred for 2 h and washed with dilute hydrochloric acid (20%, 50 cm3), saturated aqueous potassium carbonate solution (50 cm3), water (50 cm3) t...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary alcohol.Allyl.Allyl
Ester.Allyl.Vinyl
null
null
null
HCl
C(Cl)Cl
null
2
C=CCC(O)CC=C.O=C(Cl)CCCCBr>C(Cl)Cl>C=CCCC(C=C)OC(=O)CCCCBr
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0a04d58b441a458d8c93e6b0ec9022dc
C=CCN(CC=C)CCCCCCCCO.Cc1ccc(S(=O)(=O)Cl)cc1>>C=CCN(CC=C)CCCCCCCCOS(=O)(=O)c1ccc(C)cc1
O.C1(=CC=C(C=C1)S(=O)(=O)Cl)C.C(C=C)N(CCCCCCCCO)CC=C.N1=CC=CC=C1>>C(C=C)N(CCCCCCCCOS(=O)(=O)C1=CC=C(C=C1)C)CC=C
[CH2:1]=[CH:2][CH2:3][N:4]([CH2:5][CH:6]=[CH2:7])[CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][OH:16].Cl[S:17](=[O:18])(=[O:19])[c:20]1[cH:21][cH:22][c:23]([CH3:24])[cH:25][cH:26]1>>[CH2:1]=[CH:2][CH2:3][N:4]([CH2:5][CH:6]=[CH2:7])[CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][O:16][S:1...
C=CCN(CC=C)CCCCCCCCO.Cc1ccc(S(=O)(=O)Cl)cc1
C=CCN(CC=C)CCCCCCCCOS(=O)(=O)c1ccc(C)cc1
null
null
C(Cl)(Cl)Cl
Acylation
Formation of Sulfonic Esters
d05d91207659f8fa672c205a316a670adfe2b92492fc9adad2ee3f241e574fb9
a7748b0f3b0eba3868d0cf03ae67721db046202accaaea9cadb4edbc96ec8768
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
40.1
[{"value": 40.0, "product": "C(C=C)N(CCCCCCCCOS(=O)(=O)C1=CC=C(C=C1)C)CC=C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.1, "product": "C(C=C)N(CCCCCCCCOS(=O)(=O)C1=CC=C(C=C1)C)CC=C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
4-Toluene-sulphonyl chloride (12.5 g, 0.066 mol) was added slowly to a stirred solution of 8-diallylaminooctan-1-ol (10.0 g, 0.044 mol) and pyridine (7.0 g, 0.088 mol) in chloroform (100 cm3) at 0° C. After 24 h, water (100 cm3) was added and the solution washed with dilute hydrochloric acid (20%, 100 cm3), sodium carb...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Primary alcohol.Sulfonyl halide
Tosylate
null
null
c1ccccc1
HCl
C(Cl)(Cl)Cl
null
24
C=CCN(CC=C)CCCCCCCCO.Cc1ccc(S(=O)(=O)Cl)cc1>C(Cl)(Cl)Cl>C=CCN(CC=C)CCCCCCCCOS(=O)(=O)c1ccc(C)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9baa63cbb81b4f17809fed9662aa572c
CCBr.c1ccc2c(c1)Cc1ccccc1-2>>CCC1c2ccccc2-c2ccccc21
Cl.C(CCC)[Li].C1=CC=CC=2C3=CC=CC=C3CC12.BrCC>>C(C)C1C2=CC=CC=C2C=2C=CC=CC12
Br[CH2:2][CH3:1].[CH2:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2-[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]21>>[CH3:1][CH2:2][CH:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2-[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]21
CCBr.c1ccc2c(c1)Cc1ccccc1-2
CCC1c2ccccc2-c2ccccc21
null
null
O.C1CCOC1
C-C Coupling
OtherReaction
2ec7afc7a563c192c7d2e68bbaec52523c841fcdc0b50693c5649c4cfbd5acf0
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
c1ccc2c(c1)Cc1ccccc1-2
Br-[CH2;D2;+0:1]-[C;D1;H3:2].[c:3]:[c:4]1:[c:5]-[c:6]:[c:7](:[c:8])-[CH2;D2;+0:9]-1>>[C;D1;H3:2]-[CH2;D2;+0:1]-[CH;D3;+0:9]1-[c:4](:[c:3]):[c:5]-[c:6]:[c:7]-1:[c:8]
null
[]
-75
CELSIUS
1
HOUR
A solution of n-butyllithium (79.52 cm3, 0.2168 mol, 2.5M in hexane) was added slowly to a solution of fluorene (30.00 g, 0.1807 mol) in THF (300 cm3) at −70° C. The solution was stirred for 1 hour at −75° C. and 1-bromoethane (17.59 cm3, 0.2349 mol) was added slowly. The solution was allowed to warm to room temperatur...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2c(c1)Cc1ccccc12
c1ccc2c(c1)Cc1ccccc12
c1ccc2c(c1)Cc1ccccc12
HBr
O.C1CCOC1
-75
1
CCBr.c1ccc2c(c1)Cc1ccccc1-2>O.C1CCOC1>CCC1c2ccccc2-c2ccccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a3d1dca7d64040ff9adba958a4a4f430
CCBr.CCC1c2ccccc2-c2ccccc21>>CCC1(CC)c2ccccc2-c2ccccc21
Cl.C(CCC)[Li].C(C)C1C2=CC=CC=C2C=2C=CC=CC12.BrCC>>C(C)C1(C2=CC=CC=C2C=2C=CC=CC12)CC
Br[CH2:2][CH3:1].[CH:3]1([CH2:4][CH3:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2-[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]21>>[CH3:1][CH2:2][C:3]1([CH2:4][CH3:5])[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2-[c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]21
CCBr.CCC1c2ccccc2-c2ccccc21
CCC1(CC)c2ccccc2-c2ccccc21
null
null
O.C1CCOC1
C-C Coupling
OtherReaction
2ec7afc7a563c192c7d2e68bbaec52523c841fcdc0b50693c5649c4cfbd5acf0
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
c1ccc2c(c1)Cc1ccccc1-2
Br-[CH2;D2;+0:1]-[C;D1;H3:2].[C;D1;H3:3]-[C:4]-[CH;D3;+0:5]1-[c:6](:[c:7]):[c:8]-[c:9]:[c:10]-1:[c:11]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:5]1(-[C:4]-[C;D1;H3:3])-[c:6](:[c:7]):[c:8]-[c:9]:[c:10]-1:[c:11]
68
[{"value": 68.0, "product": "C(C)C1(C2=CC=CC=C2C=2C=CC=CC12)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.0, "product": "C(C)C1(C2=CC=CC=C2C=2C=CC=CC12)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-75
CELSIUS
1
HOUR
A solution of n-butyllithium (77.34 cm3, 0.1934 mol, 2.5M in hexane) was added slowly to a solution of 9-ethylfluorene (25.00 g, 0.1289 mol) in THF (250 cm3) at −70° C. The solution was stirred for 1 hour at −75° C. and 1-bromoethane (17.59 cm3, 0.1934 mol) was added slowly. The solution was allowed to warm to room tem...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccc2c(c1)Cc1ccccc12
c1ccc2c(c1)Cc1ccccc12
c1ccc2c(c1)Cc1ccccc12
HBr
O.C1CCOC1
-75
1
CCBr.CCC1c2ccccc2-c2ccccc21>O.C1CCOC1>CCC1(CC)c2ccccc2-c2ccccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6ad25c02e6ed4dac9bd0fc0cd79b7aae
CCCCCCCCBr.Oc1ccc(-c2ccc(Br)cc2)cc1>>CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1
BrC1=CC=C(C=C1)C1=CC=C(C=C1)O.BrCCCCCCCC.C([O-])([O-])=O.[K+].[K+]>>BrC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC
Br[CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1].[OH:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]2)[cH:21][cH:22]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]2)[cH:21][cH:22]1
CCCCCCCCBr.Oc1ccc(-c2ccc(Br)cc2)cc1
CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1
null
null
CC(CC)=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(-c2ccccc2)cc1
Br-[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]
66
[{"value": 66.0, "product": "BrC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.2, "product": "BrC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-bromo-4′-hydroxybiphenyl (50.00 g, 0.2008 mol), 1-bromooctane (50.38 g, 0.2610 mol), potassium carbonate (47.11 g, 0.3414 mol) and butanone (500 cm3) was heated under reflux overnight. The cooled mixture was filtered and the solvent removed on a rotary evaporator. The crude solid was recrystallised from ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccccc1
HBr
CC(CC)=O
null
null
CCCCCCCCBr.Oc1ccc(-c2ccc(Br)cc2)cc1>CC(CC)=O>CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ec27e8507aed4b5fb3044aa9e9651662
CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1>>CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1
BrC1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC.B(OC)(OC)OC.Cl>>C(CCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)B(O)O
Br[c:17]1[cH:16][cH:15][c:14](-[c:13]2[cH:12][cH:11][c:10]([O:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:24][cH:23]2)[cH:22][cH:21]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13](-[c:14]2[cH:15][cH:16][c:17]([B:18]([OH:19])[OH:20])[cH:21][cH:22]2)[cH:23][c...
CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1
CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1
null
null
CCCCCC.C1CCOC1
Functional Group Interconversion
Preparation of boronic acids without boronic ether
ea18136a2a812ba75d88f0154de74a11e900f53593099ed5cfbdc7bb208ca0bd
3c67ef5cce82b121a680ae296eb1f6d78abe8f9494b62ca3b872477b7553bcfd
c1ccc(-c2ccccc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[O;D1;H1:6]-[#5:7](-[O;D1;H1:8])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
73
[{"value": 73.0, "product": "C(CCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)B(O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.5, "product": "C(CCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)B(O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
1
HOUR
A solution of n-butylithium (50.97 cm3, 0.1274 mol, 2.5M in hexane) was added dropwise to a cooled (−78° C.) stirred solution of 4-bromo-4′-octyloxybiphenyl (40.00 g, 0.1108 mol) in THF (400 cm3). After 1 h, trimethyl borate (23.05 g, 0.2216 mol) was added dropwise to the reaction mixture maintaining a temperature of −...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Boronic acid
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Br-
CCCCCC.C1CCOC1
-78
1
CCCCCCCCOc1ccc(-c2ccc(Br)cc2)cc1>CCCCCC.C1CCOC1>CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e45de571a67c4461b310445d255b6fe5
CCC1(CC)c2cc(Br)ccc2-c2ccc(Br)cc21.CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1.COCCOC>>CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCCCC)cc6)cc5)ccc3-4)cc2)cc1
BrC1=CC=2C(C3=CC(=CC=C3C2C=C1)Br)(CC)CC.C(CCCCCCC)OC1=CC=C(C=C1)C1=CC=C(C=C1)B(O)O.C([O-])([O-])=O.[Na+].[Na+].COCCOC>>C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)CC
Br[c:18]1[cH:19][cH:20][c:21]2[c:22]([cH:23]1)[C:24]([CH2:25][CH3:33])([CH2:27][CH3:28])[c:29]1[cH:30][c:31](Br)[cH:53][cH:54][c:55]1-2.OB(O)[c:17]1[cH:16][cH:15][c:14](-[c:13]2[cH:12][cH:11][c:10]([O:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:59][cH:58]2)[cH:57][cH:56]1.O([CH2:26][CH2:49][O:40][CH3...
CCC1(CC)c2cc(Br)ccc2-c2ccc(Br)cc21.CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1.COCCOC
CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCCCC)cc6)cc5)ccc3-4)cc2)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
Aromatic Heterocycle Formation
OtherReaction
a7eb521df5414e3505fc0f7fadecba333485ca367552f4fca79f10fe1c5ef724
17a93ecb1d3a04979b265b277453639fdd52f96192a54e63bd73e5cfb4be6f7c
c1ccc(-c2ccc(-c3ccc4c(c3)Cc3cc(-c5ccc(-c6ccccc6)cc5)ccc3-4)cc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]-[C:6](-[C:7])(-[CH2;D2;+0:8]-[CH3;D1;+0:9])-[c:10]:[c:11]:[c;H0;D3;+0:12](-Br):[c:13]:[c:14].O-B(-O)-[c;H0;D3;+0:15](:[c:16]:[c:17]):[c:18]:[c:19].[CH3;D1;+0:20]-[O;H0;D2;+0:21]-[CH2;D2;+0:22]-[CH2;D2;+0:23]-O-[CH3;D1;+0:24]>>[C:7]-[C:6](-[CH2;D2;+0:8]-[CH3;D1;+0:23])(-[c:5]:...
65
[{"value": 65.0, "product": "C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Tetrakis(triphenylphosphine)palladium(0) (0.70 g, 0.0006 mol) was added to a stirred solution of 2,7-dibromo-9,9-diethylfluorene (4) (2.33 g, 0.0061 mol), 4-octyloxybiphenyl-4′-yl boronic acid (5.00 g, 0.0153 mol), 20% sodium carbonate solution (100 cm3) and 1,2-dimethoxyethane (150 cm3). The reaction mixture was heate...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Ether.Ether.Boronic acid
Ether
c1ccc2c(c1)Cc1ccccc12.c1ccccc1
c1ccccc1.c1ccc2c(c1)Cc1ccccc12.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2c(c1)Cc1ccccc12.c1ccccc1.c1ccccc1
Br-.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
null
null
CCC1(CC)c2cc(Br)ccc2-c2ccc(Br)cc21.CCCCCCCCOc1ccc(-c2ccc(B(O)O)cc2)cc1.COCCOC>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>CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCC...
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-01ec93ef06ae422da47bd4a3dd215994
CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCCCC)cc6)cc5)ccc3-4)cc2)cc1>>CCC1(CC)c2cc(-c3ccc(-c4ccc(O)cc4)cc3)ccc2-c2ccc(-c3ccc(-c4ccc(O)cc4)cc3)cc21
B(Br)(Br)Br.C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)C1=CC=C(C=C1)C1=CC=C(C=C1)OCCCCCCCC)CC>>C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)O)C1=CC=C(C=C1)C1=CC=C(C=C1)O)CC
CCCCCCCC[O:17][c:16]1[cH:15][cH:34][c:33](-[c:32]2[cH:31][cH:30][c:29](-[c:28]3[cH:27][cH:26][c:25]4[c:43]([cH:42]3)[C:3]([CH2:2][CH3:1])([CH2:4][CH3:5])[c:6]3[cH:7][c:8](-[c:9]5[cH:10][cH:11][c:12](-[c:13]6[cH:14][cH:35][c:36]([O:37]CCCCCCCC)[cH:38][cH:19]6)[cH:20][cH:21]5)[cH:22][cH:23][c:24]3-4)[cH:41][cH:40]2)[cH:3...
CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCCCC)cc6)cc5)ccc3-4)cc2)cc1
CCC1(CC)c2cc(-c3ccc(-c4ccc(O)cc4)cc3)ccc2-c2ccc(-c3ccc(-c4ccc(O)cc4)cc3)cc21
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
b6f69d716d502b64d6179a2edef13b917c16c52b1906f6d68ae629bc33b79b9d
736e5be0c4313f69ce19fa28727a9da18e7a37db0f912ae36fd9ca7a66469bc3
c1ccc(-c2ccc(-c3ccc4c(c3)Cc3cc(-c5ccc(-c6ccccc6)cc5)ccc3-4)cc2)cc1
C-C-C-C-C-C-C-C-[O;H0;D2;+0:1]-[c:2]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[c:5](-[c:6]):[cH;D2;+0:7]:[cH;D2;+0:8]:1.C-C-C-C-C-C-C-C-[O;H0;D2;+0:9]-[c:10]1:[cH;D2;+0:11]:[cH;D2;+0:12]:[c:13](-[c:14]):[cH;D2;+0:15]:[cH;D2;+0:16]:1>>[OH;D1;+0:1]-[c:2]1:[cH;D2;+0:3]:[cH;D2;+0:12]:[c:13](-[c:14]):[cH;D2;+0:15]:[cH;D2;+0:8]:1.[OH;D1;+...
40.2
[{"value": 40.0, "product": "C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)O)C1=CC=C(C=C1)C1=CC=C(C=C1)O)CC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 40.2, "product": "C(C)C1(C2=CC(=CC=C2C=2C=CC(=CC12)C1=CC=C(C=C1)C1=CC=C(C=C1)O)C1=CC=C(C=C1)C1=CC=C(C=C1)O)CC", "details": "CALCULATEDPERC...
0
CELSIUS
8
HOUR
Boron tribromide (99.9%, 1.05 cm3, 0.0111 mol) in DCM (10 ml) was added dropwise to a cooled (0° C.) stirred solution of 9,9-diethyl-2,7-bis(4-octyloxybiphenyl-4′-yl)fluorene (2.90 g, 0.0037 mol) in DCM (100 cm3). The reaction mixture was stirred at room temperature overnight, then poured onto an ice/water mixture (50 ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Aromatic alcohol.Aromatic alcohol
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccc2c(c1)Cc1ccccc12.c1ccccc1.c1ccccc1
Other
C(Cl)Cl
0
8
CCCCCCCCOc1ccc(-c2ccc(-c3ccc4c(c3)C(CC)(CC)c3cc(-c5ccc(-c6ccc(OCCCCCCCC)cc6)cc5)ccc3-4)cc2)cc1>C(Cl)Cl>CCC1(CC)c2cc(-c3ccc(-c4ccc(O)cc4)cc3)ccc2-c2ccc(-c3ccc(-c4ccc(O)cc4)cc3)cc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-cd38cd31acaa413aa640bf639ad33f0a
CC(C)=CCC[C@H](C)CCBr.Oc1ccc(Br)cc1>>CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1
BrC1=CC=C(C=C1)O.C(C[C@@H](C)CCC=C(C)C)Br.C([O-])([O-])=O.[K+].[K+]>>BrC1=CC=C(C=C1)OCC[C@H](CCC=C(C)C)C
Br[CH2:10][CH2:9][C@H:7]([CH2:6][CH2:5][CH:4]=[C:2]([CH3:1])[CH3:3])[CH3:8].[OH:11][c:12]1[cH:13][cH:14][c:15]([Br:16])[cH:17][cH:18]1>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][CH2:6][C@H:7]([CH3:8])[CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]([Br:16])[cH:17][cH:18]1
CC(C)=CCC[C@H](C)CCBr.Oc1ccc(Br)cc1
CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1
null
null
CC(CC)=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
Br-[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]
590.9
[{"value": 68.2, "product": "BrC1=CC=C(C=C1)OCC[C@H](CCC=C(C)C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 590.9, "product": "BrC1=CC=C(C=C1)OCC[C@H](CCC=C(C)C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 4-bromophenol (34.6 g, 0.20 mol), (S)-(+)-citronellyl bromide (50 g, 0.023 mol) and potassium carbonate (45 g, 0.33 mol) in butanone (500 cm3) was heated under reflux overnight. The cooled reaction mixture was filtered and the filtrate concentrated under reduced pressure. The crude product was purified by ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HBr
CC(CC)=O
null
null
CC(C)=CCC[C@H](C)CCBr.Oc1ccc(Br)cc1>CC(CC)=O>CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d0bf40c95fe842e4ad5746ef10d8c610
CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1>>CC(C)=CCC[C@H](C)CCOc1ccc(B(O)O)cc1
B(OC)(OC)OC.BrC1=CC=C(C=C1)OCC[C@H](CCC=C(C)C)C.Cl>>C[C@H](CCOC1=CC=C(C=C1)B(O)O)CCC=C(C)C
Br[c:15]1[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:9][C@H:7]([CH2:6][CH2:5][CH:4]=[C:2]([CH3:1])[CH3:3])[CH3:8])[cH:20][cH:19]1>>[CH3:1][C:2]([CH3:3])=[CH:4][CH2:5][CH2:6][C@H:7]([CH3:8])[CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]([B:16]([OH:17])[OH:18])[cH:19][cH:20]1
CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1
CC(C)=CCC[C@H](C)CCOc1ccc(B(O)O)cc1
null
null
O1CCCC1
Functional Group Interconversion
Preparation of boronic acids without boronic ether
ea18136a2a812ba75d88f0154de74a11e900f53593099ed5cfbdc7bb208ca0bd
3c67ef5cce82b121a680ae296eb1f6d78abe8f9494b62ca3b872477b7553bcfd
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]>>[O;D1;H1:6]-[#5:7](-[O;D1;H1:8])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
67
[{"value": 65.0, "product": "C[C@H](CCOC1=CC=C(C=C1)B(O)O)CCC=C(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.0, "product": "C[C@H](CCOC1=CC=C(C=C1)B(O)O)CCC=C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
null
null
2.5M n-Butylithium in hexanes (49.3 cm3, 0.12 mol) was added dropwise to a cooled (−78° C.) solution of 1-bromo-4-[(S)-3,7-dimethyloct-6-enyloxy]benzene (35 g, 0.11 mol) in tetrahydrofuran (350 cm3). The resultant solution was stirred at this temperature for 1 h and then trimethyl borate (23.8 g, 0.23 mol) was added dr...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Boronic acid
c1ccccc1
c1ccccc1
c1ccccc1
Br-
O1CCCC1
-78
null
CC(C)=CCC[C@H](C)CCOc1ccc(Br)cc1>O1CCCC1>CC(C)=CCC[C@H](C)CCOc1ccc(B(O)O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1fe3f07cdc4946e3899738f226f57903
CC(=O)O.CO[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1>>CC(=O)O[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
S(O)(O)(=O)=O.CO[C@H]1[C@H](OC(C2=CC=CC=C2)=O)[C@H](OC(C2=CC=CC=C2)=O)C(O1)(COC(C1=CC=CC=C1)=O)COC(C1=CC=CC=C1)=O.C(C)(=O)O>>C(C)(=O)O[C@H]1[C@H](OC(C2=CC=CC=C2)=O)[C@H](OC(C2=CC=CC=C2)=O)C(O1)(COC(C1=CC=CC=C1)=O)COC(C1=CC=CC=C1)=O
[CH3:1][C:2](=[O:3])[OH:4].CO[C@@H:5]1[O:6][C:7]([CH2:8][O:9][C:10](=[O:11])[c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)([CH2:18][O:19][C:20](=[O:21])[c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)[C@@H:28]([O:29][C:30](=[O:31])[c:32]2[cH:33][cH:34][cH:35][cH:36][cH:37]2)[C@H:38]1[O:39][C:40](=[O:41])[c:42]1[cH:43][cH:44]...
CC(=O)O.CO[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
CC(=O)O[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
null
null
O.C(C)(=O)OC(C)=O.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
OtherReaction
f97cf69d0b7f69a19fc4ee79e45dfa20e2de9ec7fbaa3c85f72b970a508cfd4f
f1d0c21bce3f84df8e09e027f5fecc48c78a31aaf69561ba0dce25419b3c823e
O=C(OCC1(COC(=O)c2ccccc2)OC[C@H](OC(=O)c2ccccc2)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
C-O-[C@@H;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1-[#8:6]-[C:7]=[O;D1;H0:8].[C;D1;H3:9]-[C:10](=[O;D1;H0:11])-[OH;D1;+0:12]>>[C;D1;H3:9]-[C:10](=[O;D1;H0:11])-[O;H0;D2;+0:12]-[C@@H;D3;+0:1]1-[#8:2]-[C:3]-[C:4]-[C:5]-1-[#8:6]-[C:7]=[O;D1;H0:8]
null
[]
25
CELSIUS
15
HOUR
Sulfuric acid (97%, 75 mL) was added to a solution of 1-O-methyl-2,3,5-tri-O-benzoyl-4-C-(benzoyloxymethyl)-β-D-ribofuranose (1.7 g, 2.8 mmoles) in a mixture of acetic acid (6.7 mL) and acetic anhydride (0.67 mL) at 0° C. The reaction mixture was stirred at 25° C. for 15 h and diluted with ethyl acetate (50 mL) and wat...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Ether
Ester
C1CCOC1
C1CCOC1
C1CCOC1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
O.C(C)(=O)OC(C)=O.C(C)(=O)OCC
25
15
CC(=O)O.CO[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1>O.C(C)(=O)OC(C)=O.C(C)(=O)OCC>CC(=O)O[C@@H]1OC(COC(=O)c2ccccc2)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d337e890f4ac46aea5a533793e1357af
CC(=O)O.CO[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1>>CC(=O)O[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
S(O)(O)(=O)=O.C(C1=CC=CC=C1)(=O)O[C@H]1[C@H](OC)O[C@@]([C@H]1OC(C1=CC=CC=C1)=O)(COC(C1=CC=CC=C1)=O)C.C(C)(=O)O>>C(C)(=O)O[C@H]1[C@H](OC(C2=CC=CC=C2)=O)[C@H](OC(C2=CC=CC=C2)=O)[C@](O1)(COC(C1=CC=CC=C1)=O)C
O[C:2]([CH3:1])=[O:3].C[O:4][C@@H:5]1[O:6][C@:7]([CH3:8])([CH2:9][O:10][C:11](=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[C@@H:19]([O:20][C:21](=[O:22])[c:23]2[cH:24][cH:25][cH:26][cH:27][cH:28]2)[C@H:29]1[O:30][C:31](=[O:32])[c:33]1[cH:34][cH:35][cH:36][cH:37][cH:38]1>>[CH3:1][C:2](=[O:3])[O:4][C@@H:5]1[O:6][...
CC(=O)O.CO[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
CC(=O)O[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
null
null
C(C)(=O)OC(C)=O.[Cl-].[Na+].O.C(C)(=O)OCC
Acylation
OtherReaction
d7652b37cfea6f861e95f72916116d0fb1ed41637e20224471cfc7dab29585ba
5d96d8cabdf7480c9ca6f9372e2eba1f4c54ba44bff87c469521888d79df5495
O=C(OCC1OC[C@H](OC(=O)c2ccccc2)[C@@H]1OC(=O)c1ccccc1)c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])-[#8:4]-[C:5].O-[C;H0;D3;+0:6](-[C;D1;H3:7])=[O;D1;H0:8]>>[C:3]-[C:2](-[O;H0;D2;+0:1]-[C;H0;D3;+0:6](-[C;D1;H3:7])=[O;D1;H0:8])-[#8:4]-[C:5]
56
[{"value": 56.0, "product": "C(C)(=O)O[C@H]1[C@H](OC(C2=CC=CC=C2)=O)[C@H](OC(C2=CC=CC=C2)=O)[C@](O1)(COC(C1=CC=CC=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
25
CELSIUS
16
HOUR
Concentrated sulfuric acid (97%, 99 mL) was added to a solution of 2,3,5-tri-O-benzoyl-1-O-methyl-4-C-methyl-β-D-ribofuranose (1.8 g, 3.6 mmoles) in a mixture of acetic acid (9.0 mL) and acetic anhydride (0.90 mL) at 0° C. The reaction mixture was stirred at 25° C. for 16 h and diluted with ethyl acetate (50 mL) and br...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether
Ester
null
null
C1CCOC1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
C(C)(=O)OC(C)=O.[Cl-].[Na+].O.C(C)(=O)OCC
25
16
CC(=O)O.CO[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1>C(C)(=O)OC(C)=O.[Cl-].[Na+].O.C(C)(=O)OCC>CC(=O)O[C@@H]1O[C@](C)(COC(=O)c2ccccc2)[C@@H](OC(=O)c2ccccc2)[C@H]1OC(=O)c1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-379b0ec7c95d4c418e88f52f69f88941
Nc1ncnc2c1c(=O)ccn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>>c1cnc2ncncc2c1
NC=1C2=C(N=CN1)N(C=CC2=O)[C@H]2[C@H](O)[C@H](O)[C@H](O2)CO.Cl[Si](O[Si](C(C)C)(C(C)C)Cl)(C(C)C)C(C)C.O>>N1=CN=CC2=C1N=CC=C2
N[c:8]1[n:7][cH:6][n:5][c:4]2[n:3]([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)[cH:2][cH:1][c:10](=O)[c:9]21>>[cH:1]1[cH:2][n:3][c:4]2[n:5][cH:6][n:7][cH:8][c:9]2[cH:10]1
Nc1ncnc2c1c(=O)ccn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O
c1cnc2ncncc2c1
null
null
N1=CC=CC=C1
Reduction
OtherReaction
183772bfc4c94fd9be16c7dc4d9cbfc8516c790e592c9b5261f5b9663a8d090d
52812dd970894bd2b93cad2e096e0c03648dd649df9f4a3211853c4ae28652a7
c1cnc2ncncc2c1
N-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5]2:[c:6]:1:[c;H0;D3;+0:7](=O):[c:8]:[c:9]:[n;H0;D3;+0:10]:2-[C@H]1-O-[C@H](-C-O)-[C@@H](-O)-[C@@H]-1-O>>[#7;a:4]1:[c:3]:[#7;a:2]:[cH;D2;+0:1]:[c:6]2:[cH;D2;+0:7]:[c:8]:[c:9]:[n;H0;D2;+0:10]:[c:5]:1:2
null
[]
null
null
20
HOUR
A reaction mixture of 4-amino-5-oxo-8-(β-D-ribofuranosyl)pyrido[2,3-d]pyrimidine (1.8 g, 6.20 mmol) and 1,3-dichloro-1,1,3,3-tetraisopropyldisiloxane (2.15 mL, 6.73 mmol) in anhydrous pyridine (25 mL) was stirred at room temperature for 20 h and cooled with ice. Water (0.5 mL) was added, and the mixture stirred at ambi...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary alcohol.Secondary alcohol.Secondary alcohol.Primary amine
null
C1CCOC1.c1cnc2ncncc2c1
c1cnc2ncncc2c1
c1cnc2ncncc2c1
HO-
N1=CC=CC=C1
null
20
Nc1ncnc2c1c(=O)ccn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O>N1=CC=CC=C1>c1cnc2ncncc2c1