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-de7f9117544941b58fe05a3b6a6abcd9
O=C(Cl)C(=O)Cl.O=C(O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>>O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
FC1=CC=CC=2C=3C(=CNC12)C(N(N3)C3=CC=C(C(=O)O)C=C3)=O.C(C(=O)Cl)(=O)Cl.CN(C=O)C>>FC1=CC=CC=2C=3C(=CNC12)C(N(N3)C3=CC=C(C(=O)Cl)C=C3)=O
O=C(Cl)C(=O)[Cl:3].O[C:2](=[O:1])[c:4]1[cH:5][cH:6][c:7](-[n:8]2[n:9][c:10]3[c:11]4[cH:12][cH:13][cH:14][c:15]([F:16])[c:17]4[nH:18][cH:19][c:20]-3[c:21]2=[O:22])[cH:23][cH:24]1>>[O:1]=[C:2]([Cl:3])[c:4]1[cH:5][cH:6][c:7](-[n:8]2[n:9][c:10]3[c:11]4[cH:12][cH:13][cH:14][c:15]([F:16])[c:17]4[nH:18][cH:19][c:20]-3[c:21]2=...
O=C(Cl)C(=O)Cl.O=C(O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_Other
013cec2edeb273a7a148f349d36a52d99ff4e7bcf8eed78085df830088e387ac
aedb1f68dc5b7eb0583043e1125b741382b17974140a2f46554f0110e2ddc884
O=c1c2c[nH]c3ccccc3c-2nn1-c1ccccc1
Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
99
[{"value": 99.0, "product": "FC1=CC=CC=2C=3C(=CNC12)C(N(N3)C3=CC=C(C(=O)Cl)C=C3)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
45
CELSIUS
3
HOUR
To a suspension of finely ground 4-(6-Fluoro-3-oxo-3,5-dihydro-pyrazolo[4,3-c]quinolin-2-yl]-benzoic acid (1.1 g. 3.4 mmol) in dichloromethane (6 ml) was added oxalyl chloride (2.4 ml, 29 mmol) followed by a drop of dimethyl formamide. The mixture was stirred under nitrogen at 45° C. for 3 h. The solvent was removed in...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid
Acyl halide
null
null
c1ccccc1.c1ccc2c(c1)ncc1c[nH]nc12
HCl
ClCCl
45
3
O=C(Cl)C(=O)Cl.O=C(O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>ClCCl>O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d0a9987fba804406a5ad7e3620f944c8
CN(C)CCCN.O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>>CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1.Cl
FC1=CC=CC=2C=3C(=CNC12)C(N(N3)C3=CC=C(C(=O)Cl)C=C3)=O.CN(CCCN)C>>Cl.CN(CCCNC(C1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O)=O)C
[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH2:7].[C:8](=[O:9])([c:10]1[cH:11][cH:12][c:13](-[n:14]2[n:15][c:16]3[c:17]4[cH:18][cH:19][cH:20][c:21]([F:22])[c:23]4[nH:24][cH:25][c:26]-3[c:27]2=[O:28])[cH:29][cH:30]1)[Cl:31]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13](-[n:14]...
CN(C)CCCN.O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1.Cl
null
null
O1CCCC1
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=c1c2c[nH]c3ccccc3c-2nn1-c1ccccc1
[C:1]-[C:2]-[NH2;D1;+0:3].[Cl;H0;D1;+0:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c:7](:[c:8]):[c:9]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c:7](:[c:8]):[c:9].[ClH;D0;+0:4]
53
[{"value": 53.0, "product": "Cl.CN(CCCNC(C1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.6, "product": "Cl.CN(CCCNC(C1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
90
MINUTE
To a partial solution of 4-(6-Fluoro-3-oxo-3,5-dihydro-pyrazolo[4,3-c]quinolin-2-yl]-benzoyl chloride (0.1 g, 0.3 mmol) in tetrahydrofurane (5 ml) under nitrogen was added a solution of 3-dimethylamino-propyl amine (0.03 g, 0.3 mmol) in tetrahydrofurane. The mixture was stirred at rt for 90 minutes. The solvent was rem...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2c(c1)ncc1c[nH]nc12
null
O1CCCC1
null
1.5
CN(C)CCCN.O=C(Cl)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>O1CCCC1>CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1.Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8c9731bb3eec402c862e43f2dccd3054
CCOC(=O)COC#N.Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>>CCOC(=O)CNC(=O)Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
O.O(C#N)CC(=O)OCC.NC1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O.NC1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O.CN(C=O)C>>C(C)OC(CNC(=O)NC1=CC=C(C=C1)N1N=C2C(=CNC=3C(=CC=CC23)F)C1=O)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][O:9][C:8]#[N:7].[NH2:10][c:11]1[cH:12][cH:13][c:14](-[n:15]2[n:16][c:17]3[c:18]4[cH:19][cH:20][cH:21][c:22]([F:23])[c:24]4[nH:25][cH:26][c:27]-3[c:28]2=[O:29])[cH:30][cH:31]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][NH:7][C:8](=[O:9])[NH:10][c:11]1[cH:12][cH:13][c:14](-[n:15]2[n:...
CCOC(=O)COC#N.Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
CCOC(=O)CNC(=O)Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d3fa590c406383703a06396aa0a74d0ff12812878c20f7c6d1c9b72857232ec5
e0e6e17835ffb90ed25d1370bd81769d9371700d8697fc8bf30fa3f2251d1c16
O=c1c2c[nH]c3ccccc3c-2nn1-c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[O;H0;D2;+0:6]-[C;H0;D2;+0:7]#[N;H0;D1;+0:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[NH;D2;+0:8]-[C;H0;D3;+0:7](=[O;H0;D1;+0:6])-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12]
null
[]
null
null
16
HOUR
Ethyl cyanatoacetate (31 mg, 0.24 mmol) was added in one portion to a stirred solution of 2-(4-aminophenyl)-6-fluoro-2,5-dihydropyrazolo[4,3-c]quinolin-3-one (intermediate 2) (50 mg, 0.17 mmol) in N,N-dimethylformamide (2 ml) and the mixture stirred at room temperature for 16 h. Water (1 ml) was then added to the mixtu...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Nitrile.Primary amine
Ester.Urea
null
null
c1ccccc1.c1ccc2c(c1)ncc1c[nH]nc12
null
null
null
16
CCOC(=O)COC#N.Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1>>CCOC(=O)CNC(=O)Nc1ccc(-n2nc3c4cccc(F)c4[nH]cc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fd748a9264b7496b92cc25c146887dc5
COC(=O)C#N.O=C1CCSc2ccccc21>>COC(=O)C1CSc2ccccc2C1=O
S1CCC(C2=CC=CC=C12)=O.[Cl-].[NH4+].C[Si](C)(C)[N-][Si](C)(C)C.[Li+].CCCCCC.C(#N)C(=O)OC>>O=C1C(CSC2=CC=CC=C12)C(=O)OC
N#C[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][S:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][S:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[C:14]1=[O:15]
COC(=O)C#N.O=C1CCSc2ccccc21
COC(=O)C1CSc2ccccc2C1=O
null
null
O1CCCC1
C-C Coupling
OtherReaction
3f5e1dab2b9ef219d58e7426e20576645bbd1219860adff413bd963c90326325
ea62efa90ef3cfb13125a23e62e9e1787aa2a0b0ee48c8a61b3326a3bda24134
O=C1CCSc2ccccc21
N#C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[#16:9]-[c:10]:[c:11]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[#16:9]-[c:10]:[c:11]-[C:6]-1=[O;D1;H0:5]
42
[{"value": 42.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
60
MINUTE
Dry tetrahydrofuran (60 ml) was cooled under nitrogen atmosphere to −50 to −60° C. 1M Lithium bis(trimethylsily)amide solution in hexane (56 ml, 56 mmol) was added. The temperature was kept at −50 to −60° C. and thiochroman-4-one was added dropwise over 20 min. Stirring was continued at low temperature for 60 min. Meth...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Nitrile
Ketone.Ester
c1ccc2c(c1)CCCS2
c1ccc2c(c1)CCCS2
c1ccc2c(c1)CCCS2
Other
O1CCCC1
null
1
COC(=O)C#N.O=C1CCSc2ccccc21>O1CCCC1>COC(=O)C1CSc2ccccc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3c02072ef1c74c44a9c0d13dfd9d66f4
O=C(O)c1ccc(N2N=C3c4ccccc4SCC3C2=O)cc1>>O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
O.O=C1C2C(=NN1C1=CC=C(C(=O)O)C=C1)C=1C=CC=CC1SC2.C1(=C(C(=O)C(=O)C(=C1Cl)Cl)Cl)Cl>>O=C1C=2C(=NN1C1=CC=C(C(=O)O)C=C1)C=1C=CC=CC1SC2
[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([N:8]2[N:9]=[C:10]3[c:11]4[cH:12][cH:13][cH:14][cH:15][c:16]4[S:17][CH2:18][CH:19]3[C:20]2=[O:21])[cH:22][cH:23]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7](-[n:8]2[n:9][c:10]3[c:11]4[cH:12][cH:13][cH:14][cH:15][c:16]4[s:17][cH:18][c:19]-3[c:20]2=[O:21])[cH:22][cH:23]1
O=C(O)c1ccc(N2N=C3c4ccccc4SCC3C2=O)cc1
O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
null
null
CS(=O)C
Miscellaneous
OtherReaction
b54080b6cee2de4ba45f1f1c5e85b56fa423cf6d6c29328f1c24155da83e50e1
54f05125c5e4f16b58b7c0463d2268ccbc57ca95bcd8d4cbe5653d15b69e77ad
O=c1c2csc3ccccc3c-2nn1-c1ccccc1
[O;D1;H0:1]=[C;H0;D3;+0:2]1-[CH;D3;+0:3]2-[CH2;D2;+0:4]-[S;H0;D2;+0:5]-[c:6](:[c:7]):[c:8](:[c:9])-[C;H0;D3;+0:10]-2=[N;H0;D2;+0:11]-[N;H0;D3;+0:12]-1-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:16]:[c:17]>>[O;D1;H0:1]=[c;H0;D3;+0:2]1:[c;H0;D3;+0:3]2:[cH;D2;+0:4]:[s;H0;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:9]):[c;H0;D3;+0:10]-2:[n;H...
92.2
[{"value": 92.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.2, "product": null, "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
Crude 4-(3-Oxo-3a,4-dihydro-3H-thiochromeno[4,3-c]pyrazol-2-yl)-benzoic acid (250 mg, 0.77 mmol) was dissolved in dimethyl sulphoxide (6 ml). O-Chloranil (189 mg, 0.77 mmol) was added and the mixture was stirred at room temperature overnight. Water (20 ml) was added and the solids were collected by filtration and washe...
10.6084/m9.figshare.5104873.v1
null
Hydrazone amide.Monosulfide
null
c1ccc2c(c1)SCC1C[NH]N=C21
c1ccc2c(c1)scc1cnnc12
c1ccccc1.c1ccc2c(c1)scc1cnnc12
null
CS(=O)C
null
8
O=C(O)c1ccc(N2N=C3c4ccccc4SCC3C2=O)cc1>CS(=O)C>O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4bc137e7d1804b629cef2ec91fc0bb15
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1>>CN(C)CCCNC(=O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)OC(N(C)C)=[N+](C)C.O=C1C=2C(=NN1C1=CC=C(C(=O)O)C=C1)C=1C=CC=CC1SC2.C(C)(C)N(CC)C(C)C.CN(CCCN)C>>CN(CCCNC(C1=CC=C(C=C1)N1N=C2C(C1=O)=CSC=1C=CC=CC12)=O)C
[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH2:7].O[C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13](-[n:14]2[n:15][c:16]3[c:17]4[cH:18][cH:19][cH:20][cH:21][c:22]4[s:23][cH:24][c:25]-3[c:26]2=[O:27])[cH:28][cH:29]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13](-[n:14]2[n:15][c:16]3[c...
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
CN(C)CCCNC(=O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
null
null
CC(=O)N(C)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=c1c2csc3ccccc3c-2nn1-c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[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](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
4
HOUR
4-(3-oxothiochromeno[4,3-c]pyrazol-2(3H)-yl)benzoic acid (55 mg, 0.17 mmol) was suspended in anhydrous dimethyl acetamide (1 ml). Diisopropyl-ethyl amine (46.5 mg, 0.36 mmol, 62μl) was added followed by 3-dimethylaminopropylamine (17.5 mg, 0.17 mmol) and [(benzotriazol-1-yloxy)-dimethylamino-methylene]-dimethyl-ammoniu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2c(c1)scc1cnnc12
HO-
CC(=O)N(C)C
null
4
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1>CC(=O)N(C)C>CN(C)CCCNC(=O)c1ccc(-n2nc3c4ccccc4scc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7cd3c411adac4a7fa21536a15e530d0e
C=CC(=O)O.Fc1ccccc1S>>O=C(O)CCSc1ccccc1F
Cl.C(C=C)(=O)O.FC1=C(C=CC=C1)S.C(C)N(CC)CC>>FC1=C(C=CC=C1)SCCC(=O)O
[O:1]=[C:2]([OH:3])[CH:4]=[CH2:5].[SH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[F:13]>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[F:13]
C=CC(=O)O.Fc1ccccc1S
O=C(O)CCSc1ccccc1F
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
thia-Michael addition
9c1714ade80d0bfd6c4747e19bbd5e181aebdd6e70fcf1c4b03944a726aeaf5d
ff275b76dc1ff1d0f3afaf057f654852a0a807709b71c50992bfc9df07afc001
c1ccccc1
[CH2;D1;+0:1]=[CH;D2;+0:2]-[C:3](=[O;D1;H0:4])-[O;D1;H1:5].[SH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:4]=[C:3](-[O;D1;H1:5])-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
54
[{"value": 54.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}, {"value": 53.6, "product": null, "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
2-Fluorothiophenol (5.0 g, 39 mmol) was dissolved in tetrahydrofuran (50 ml) under a nitrogen atmosphere. Triethylamine (3.94 g, 5.33 ml, 85.8 mmol) was added. Acrylic acid (2.81 g, 2.67 ml, 39 mmol) was dissolved in tetrahydrofuran and added dropwise to the reaction solution over 2 h at room temperature. The mixture w...
10.6084/m9.figshare.5104873.v1
null
Aromatic thiol.Vinyl
Monosulfide
null
null
c1ccccc1
null
O1CCCC1
null
8
C=CC(=O)O.Fc1ccccc1S>O1CCCC1>O=C(O)CCSc1ccccc1F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a0ed496bc0d24e5ea9c582b5cb459602
O=C(O)CCSc1ccccc1F>>O=C1CCSc2c(F)cccc21
FC1=C(C=CC=C1)SCCC(=O)O>>FC=1C=CC=C2C(CCSC12)=O
O[C:2](=[O:1])[CH2:3][CH2:4][S:5][c:6]1[c:7]([F:8])[cH:9][cH:10][cH:11][cH:12]1>>[O:1]=[C:2]1[CH2:3][CH2:4][S:5][c:6]2[c:7]([F:8])[cH:9][cH:10][cH:11][c:12]21
O=C(O)CCSc1ccccc1F
O=C1CCSc2c(F)cccc21
null
null
S(O)(O)(=O)=O
Functional Group Interconversion
OtherReaction
2b3e47a7492da189595533ae2c2253a30a5eb1f4c16186cb22b5c4ebaba9bbba
6a71bb5a71b59feeb4f6a39b1b66fa450a058b64b0a3909e1a51c22473a141c5
O=C1CCSc2ccccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]-[#16:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1]1-[C:3]-[C:4]-[#16:5]-[c:6](:[c:7]):[c;H0;D3;+0:8]-1:[c:9]:[c:10]
58
[{"value": 58.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.5, "product": null, "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
2.5
CELSIUS
3
HOUR
3-[(2-Fluorophenyl)sulfanyl]propanoic acid (4.0 g, 20 mmol) was mixed with concentrated sulphuric acid (20 ml) at 0–5° C. The reaction solution was stirred at 0 to 5° C. for 3 h then allowed to warm up to room temperature overnight. The mixture was quenched dropwise into ice to give a white suspension. The aqueous phas...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ketone
c1ccccc1
c1ccc2c(c1)CCCS2
c1ccc2c(c1)CCCS2
HO-
S(O)(O)(=O)=O
2.5
3
O=C(O)CCSc1ccccc1F>S(O)(O)(=O)=O>O=C1CCSc2c(F)cccc21
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-849badeab25e42c8b3d493e2813469e2
COC(=O)C#N.O=C1CCSc2c(F)cccc21>>COC(=O)C1CSc2c(F)cccc2C1=O
[Cl-].[NH4+].C[Si]([N-][Si](C)(C)C)(C)C.[Li+].C(#N)C(=O)OC.FC=1C=CC=C2C(CCSC12)=O>>FC=1C=CC=C2C(C(CSC12)C(=O)OC)=O
N#C[C:3]([O:2][CH3:1])=[O:4].[CH2:5]1[CH2:6][S:7][c:8]2[c:9]([F:10])[cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16]>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][S:7][c:8]2[c:9]([F:10])[cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16]
COC(=O)C#N.O=C1CCSc2c(F)cccc21
COC(=O)C1CSc2c(F)cccc2C1=O
null
null
O1CCCC1.O.CCCCCC
C-C Coupling
OtherReaction
3f5e1dab2b9ef219d58e7426e20576645bbd1219860adff413bd963c90326325
ea62efa90ef3cfb13125a23e62e9e1787aa2a0b0ee48c8a61b3326a3bda24134
O=C1CCSc2ccccc21
N#C-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C;D1;H3:4].[O;D1;H0:5]=[C:6]1-[CH2;D2;+0:7]-[C:8]-[#16:9]-[c:10]:[c:11]-1>>[C;D1;H3:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:7]1-[C:8]-[#16:9]-[c:10]:[c:11]-[C:6]-1=[O;D1;H0:5]
45
[{"value": 45.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}, {"value": 45.0, "product": null, "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
2
HOUR
1M Lithium hexamethyldisilazide solution in hexane (13.2 ml) was dissolved in anhydrous tetrahydrofuran (20 ml) under nitrogen atmosphere. The solution was cooled to −78° C. 8-Fluoro-2,3-dihydro-4H-thiochromen-4-one (2.00 g, 11 mmol) was dissolved in tetrahydrofuran (40 ml), the solution was transferred to the dropping...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester.Nitrile
Ketone.Ester
c1ccc2c(c1)CCCS2
c1ccc2c(c1)CCCS2
c1ccc2c(c1)CCCS2
Other
O1CCCC1.O.CCCCCC
-78
2
COC(=O)C#N.O=C1CCSc2c(F)cccc21>O1CCCC1.O.CCCCCC>COC(=O)C1CSc2c(F)cccc2C1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-849c69306ec241d49b259195912ecea5
COC(=O)C1CSc2c(F)cccc2C1=O.NNc1ccc(C(=O)O)cc1>>O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
FC=1C=CC=C2C(C(CSC12)C(=O)OC)=O.N(N)C1=CC=C(C(=O)O)C=C1.C(C)(=O)O>>FC1=CC=CC2=C1SC=C1C2=NN(C1=O)C1=CC=C(C(=O)O)C=C1
CO[C:21]([CH:20]1[C:10](=O)[c:11]2[cH:12][cH:13][cH:14][c:15]([F:16])[c:17]2[S:18][CH2:19]1)=[O:22].[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7]([NH:8][NH2:9])[cH:23][cH:24]1>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][c:7](-[n:8]2[n:9][c:10]3[c:11]4[cH:12][cH:13][cH:14][c:15]([F:16])[c:17]4[s:18][cH:19][c:20]-3[c:21]2=[O:22]...
COC(=O)C1CSc2c(F)cccc2C1=O.NNc1ccc(C(=O)O)cc1
O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
null
null
C(C)(=O)OCC
Aromatic Heterocycle Formation
OtherReaction
0a103335ebcf29bf85a9dd659e53557f54e3dfd714c998dc25bfbdea06ab977b
b73272fe514a017930912c98f85fb1ccc55aa3f60622ec45b0daa39338a9b767
O=c1c2csc3ccccc3c-2nn1-c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D3;+0:3]1-[CH2;D2;+0:4]-[S;H0;D2;+0:5]-[c:6](:[c:7]):[c:8](:[c:9])-[C;H0;D3;+0:10]-1=O.[NH2;D1;+0:11]-[NH;D2;+0:12]-[c;H0;D3;+0:13](:[c:14]:[c:15]):[c:16]:[c:17]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[c;H0;D3;+0:3]2:[cH;D2;+0:4]:[s;H0;D2;+0:5]:[c:6](:[c:7]):[c:8](:[c:9]):[c;H0;D3;+0:10]-2:[n...
10.3
[{"value": 10.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}, {"value": 10.3, "product": null, "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Methyl 8-fluoro-4-oxothiochromane-3-carboxylate (1.19 g, 4.95 mmol) and 4-hydrazinobenzoic acid (755 mg, 4.95 mmol) were mixed with glacial acetic acid (10 ml). The mixture was heated to reflux for 4 h. Excess acetic acid was removed under vacuum to give an orange oil. Ethyl acetate (10 ml) was added and the mixture so...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone.Ester.Monosulfide
null
c1ccc2c(c1)CCCS2
c1ccc2c(c1)scc1cnnc12
c1ccccc1.c1ccc2c(c1)scc1cnnc12
HO-
C(C)(=O)OCC
null
null
COC(=O)C1CSc2c(F)cccc2C1=O.NNc1ccc(C(=O)O)cc1>C(C)(=O)OCC>O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-7211bc94ac1349c49ceee66c042b8421
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1>>CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
CN(CCCN)C.C(C)(C)N(CC)C(C)C.FC1=CC=CC2=C1SC=C1C2=NN(C1=O)C1=CC=C(C(=O)O)C=C1.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)OC(N(C)C)=[N+](C)C>>CN(CCCNC(C1=CC=C(C=C1)N1N=C2C(C1=O)=CSC=1C(=CC=CC12)F)=O)C
[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH2:7].O[C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13](-[n:14]2[n:15][c:16]3[c:17]4[cH:18][cH:19][cH:20][c:21]([F:22])[c:23]4[s:24][cH:25][c:26]-3[c:27]2=[O:28])[cH:29][cH:30]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH2:5][CH2:6][NH:7][C:8](=[O:9])[c:10]1[cH:11][cH:12][c:13](-[n:14]2[n:15][c...
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
null
null
CC(=O)N(C)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=c1c2csc3ccccc3c-2nn1-c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[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](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
8
HOUR
4-(6-Fluoro-3-oxothiochromeno[4,3-c]pyrazol-2(3H)-yl)benzoic acid (41 mg, 0.12 mmol) was dissolved in anhydrous dimethyl-acetamide(1 ml). Diisopropyl-ethyl amine (46 mg, 0.36 mmol, 62 μl) was added followed by [(benzotriazol-1-yloxy)-dimethylamino-methylene]-dimethyl-ammonium hexafluoro phosphate (65 mg, 0.17 mmol) and...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccc2c(c1)scc1cnnc12
HO-
CC(=O)N(C)C
null
8
CN(C)CCCN.O=C(O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1>CC(=O)N(C)C>CN(C)CCCNC(=O)c1ccc(-n2nc3c4cccc(F)c4scc-3c2=O)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-5a30e635efc747dabd7838cc8a808026
COc1cc(N)c(C(=O)O)cc1OC.NC=O>>COc1cc2nc[nH]c(=O)c2cc1OC
COC=1C=C(C(C(=O)O)=CC1OC)N.C(=O)N>>COC=1C=C2C(NC=NC2=CC1OC)=O
O[C:9](=[O:10])[c:11]1[c:5]([NH2:6])[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH3:15])[cH:12]1.O=[CH:7][NH2:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][nH:8][c:9](=[O:10])[c:11]2[cH:12][c:13]1[O:14][CH3:15]
COc1cc(N)c(C(=O)O)cc1OC.NC=O
COc1cc2nc[nH]c(=O)c2cc1OC
null
null
O
Aromatic Heterocycle Formation
OtherReaction
5215b2aebdf37498a4d4a87048f2b5a68a2aa2731f8695ccc5897fee02296c51
42d7d0d29a255bcbf4fdad9c0b39487d2cf609ac6796e99c9c033d59efbdbdc9
O=c1[nH]cnc2ccccc12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].O=[CH;D2;+0:8]-[NH2;D1;+0:9]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[cH;D2;+0:8]:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3]:1:[c:4]
18
[{"value": 18.0, "product": "COC=1C=C2C(NC=NC2=CC1OC)=O", "details": "PERCENTYIELD", "is_desired": false}]
190
CELSIUS
3
HOUR
A mixture of 4,5-dimethoxyanthranilic acid (19.7 g, 100 mmol) and formamide (10 ml) was heated at 190° C. for 5 hours. The mixture was allowed to cool to approximately 80° C. and water (50 ml) was added. The mixture was then allowed to stand at ambient temperature for 3 hours. Collection of the solid by suction filtrat...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amide.Primary amine
null
c1ccccc1
c1ccc2ncncc2c1
c1ccc2ncncc2c1
HO-
O
190
3
COc1cc(N)c(C(=O)O)cc1OC.NC=O>O>COc1cc2nc[nH]c(=O)c2cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-52fa94082cc6450aa658d5bcc31e2e0f
COc1cc2nc[nH]c(=O)c2cc1OC.O=S(Cl)Cl>>COc1cc2ncnc(Cl)c2cc1OC
CN(C=O)C.COC=1C=C2C(NC=NC2=CC1OC)=O.S(=O)(Cl)Cl>>ClC1=NC=NC2=CC(=C(C=C12)OC)OC
O=[c:9]1[nH:8][cH:7][n:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH3:15])[cH:12][c:11]21.O=S(Cl)[Cl:10]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][n:8][c:9]([Cl:10])[c:11]2[cH:12][c:13]1[O:14][CH3:15]
COc1cc2nc[nH]c(=O)c2cc1OC.O=S(Cl)Cl
COc1cc2ncnc(Cl)c2cc1OC
null
null
null
Functional Group Interconversion
OtherReaction
3788560e87eee8765e749543914a91a512631307b97fad163ebef894d2a0ea68
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2ncncc2c1
Cl-S(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
98
[{"value": 98.0, "product": "ClC1=NC=NC2=CC(=C(C=C12)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dimethylformamide (0.2 ml) was added dropwise to a solution of 6,7-dimethoxy-3,4-dihydro-quinazolin-4-one (10.0 g, 48.5 mmol) in thionyl chloride (200 ml) and the reaction was heated at reflux for 6 hours. The reaction was cooled, excess thionyl chloride was removed in vacuo and the residue was azeotroped with toluene ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1
HCl
null
null
null
COc1cc2nc[nH]c(=O)c2cc1OC.O=S(Cl)Cl>>COc1cc2ncnc(Cl)c2cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-843c3ac7f2d94cf9be1593fb8f68f4b4
COc1cc(C(N)=O)c(N)cc1OCc1ccccc1>>COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1
NC1=C(C(=O)N)C=C(C(=C1)OCC1=CC=CC=C1)OC.CN(C)C=NC=[N+](C)C.[Cl-].C(C)(=O)[O-].[Na+].C(C)(=O)O>>C(C1=CC=CC=C1)OC1=C(C=C2C(NC=NC2=C1)=O)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6](=[O:7])[NH2:8])[c:11]([NH2:10])[cH:12][c:13]1[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6](=[O:7])[nH:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
COc1cc(C(N)=O)c(N)cc1OCc1ccccc1
COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1
null
null
O1CCOCC1
Aromatic Heterocycle Formation
OtherReaction
0798449d56bc7e7756a703d33bd60780d26c4986e39e1809e15228456c95135b
3074b6c74bc99545969aa05d42dae7b149d9d6bb1b36a52cec3a362e1e7f7ca0
O=c1[nH]cnc2cc(OCc3ccccc3)ccc12
[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4](-[C;H0;D3;+0:5](-[NH2;D1;+0:6])=[O;D1;H0:7]):[c:8]>>[O;D1;H0:7]=[c;H0;D3;+0:5]1:[nH;D2;+0:6]:[c:9]:[n;H0;D2;+0:1]:[c:2](:[c:3]):[c:4]:1:[c:8]
84
[{"value": 84.0, "product": "C(C1=CC=CC=C1)OC1=C(C=C2C(NC=NC2=C1)=O)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.0, "product": "C(C1=CC=CC=C1)OC1=C(C=C2C(NC=NC2=C1)=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-amino-4-benzyloxy-5-methoxybenzamide (10 g, 0.04 mol), (prepared according to J Med. Chem. 1977, 20, 146–149), and Gold's reagent (7.4 g, 0.05 mol) in dioxane (100 ml) was stirred and heated at reflux for 24 hours. Sodium acetate (3.02 g, 0.037 mol) and acetic acid (1.65 ml, 0.029 mol) were added to the ...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Primary amine
null
c1ccccc1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.c1ccccc1
Other
O1CCOCC1
null
null
COc1cc(C(N)=O)c(N)cc1OCc1ccccc1>O1CCOCC1>COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2180fb6bfb1f4374a267f228137b431d
COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCc1ccccc1
CN(C=O)C.COC=1C=C2C(NC=NC2=CC1OCC1=CC=CC=C1)=O.S(=O)(Cl)Cl>>ClC1=NC=NC2=CC(=C(C=C12)OC)OCC1=CC=CC=C1
O=[c:6]1[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH2:15][c:16]3[cH:17][cH:18][cH:19][cH:20][cH:21]3)[cH:12][c:11]2[n:10][cH:9][nH:8]1.O=S(Cl)[Cl:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([Cl:7])[n:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1.O=S(Cl)Cl
COc1cc2c(Cl)ncnc2cc1OCc1ccccc1
null
null
null
Functional Group Interconversion
OtherReaction
3788560e87eee8765e749543914a91a512631307b97fad163ebef894d2a0ea68
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc(COc2ccc3cncnc3c2)cc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
90
[{"value": 90.0, "product": "ClC1=NC=NC2=CC(=C(C=C12)OC)OCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-amino-4-benzyloxy-5-methoxybenzamide (10 g, 0.04 mol), (prepared according to J Med. Chem. 1977, 20, 146–149), and Gold's reagent (7.4 g, 0.05 mol) in dioxane (100 ml) was stirred and heated at reflux for 24 hours. Sodium acetate (3.02 g, 0.037 mol) and acetic acid (1.65 ml, 0.029 mol) were added to the ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.c1ccccc1
HCl
null
null
null
COc1cc2c(=O)[nH]cnc2cc1OCc1ccccc1.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-40883f32ac2e49d894bc6c508a078743
CC(C)(C)OC(=O)Nc1ccc(N)cc1.COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1>>COc1cc2c(Nc3ccc(NC(=O)OC(C)(C)C)cc3)ncnc2cc1OCCCN1CCOCC1.Cl.Cl
C(C)(C)(C)OC(=O)NC1=CC=C(C=C1)N.ClC1=NC=NC2=CC(=C(C=C12)OC)OCCCN1CCOCC1>>Cl.Cl.C(=O)(OC(C)(C)C)NC1=CC=C(NC2=NC=NC3=CC(=C(C=C23)OC)OCCCN2CCOCC2)C=C1
[NH2:7][c:8]1[cH:9][cH:10][c:11]([NH:12][C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19])[cH:20][cH:21]1.[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([Cl:38])[n:22][cH:23][n:24][c:25]2[cH:26][c:27]1[O:28][CH2:29][CH2:30][CH2:31][N:32]1[CH2:33][CH2:34][O:35][CH2:36][CH2:37]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([NH:7][c:8...
CC(C)(C)OC(=O)Nc1ccc(N)cc1.COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1
COc1cc2c(Nc3ccc(NC(=O)OC(C)(C)C)cc3)ncnc2cc1OCCCN1CCOCC1.Cl.Cl
null
null
C(C)(C)O
Functional Group Addition
Goldberg coupling aryl amine-aryl chloride
c6cd75578a0e012699a72b942ff8ae972025db694d8529f29ae62196b2270816
6f78585f8136bfeb64030c4a3c4021c4cf8a554288637e24070b99b83b5f9b48
c1ccc(Nc2ncnc3cc(OCCCN4CCOCC4)ccc23)cc1
[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9].[NH2;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[ClH;D0;+0:1].[c:12]:[c:11](-[NH;D2;+0:10]-[c;H0;D3;+0:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]):[c:13]
189.4
[{"value": 95.0, "product": "Cl.Cl.C(=O)(OC(C)(C)C)NC1=CC=C(NC2=NC=NC3=CC(=C(C=C23)OC)OCCCN2CCOCC2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 189.4, "product": "Cl.Cl.C(=O)(OC(C)(C)C)NC1=CC=C(NC2=NC=NC3=CC(=C(C=C23)OC)OCCCN2CCOCC2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of N-(t-butoxycarbonyl) 4-aminoaniline (5.73 g, 27.5 mmol), and 4-chloro-6-methoxy-7-(3-morpholinopropoxy)quinazoline (8.44 g, 25.0 mmol), in isopropanol (100 ml) was heated at reflux for 3.5 hours before the reaction was allowed to cool to ambient temperature. The solid which had precipitated was collected ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccccc1.c1ccc2ncncc2c1.C1COCC[NH]1
Other
C(C)(C)O
null
null
CC(C)(C)OC(=O)Nc1ccc(N)cc1.COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1>C(C)(C)O>COc1cc2c(Nc3ccc(NC(=O)OC(C)(C)C)cc3)ncnc2cc1OCCCN1CCOCC1.Cl.Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9315e24e2cc145ea9b69ce2304646676
COc1cc2ncnc(Cl)c2cc1OC.Cc1cc(N)ccc1O>>COc1cc2ncnc(Nc3ccc(O)c(C)c3)c2cc1OC
NC1=CC(=C(C=C1)O)C.Cl.ClC1=NC=NC2=CC(=C(C=C12)OC)OC>>OC1=C(C=C(NC2=NC=NC3=CC(=C(C=C23)OC)OC)C=C1)C
Cl[c:9]1[n:8][cH:7][n:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:21]([O:22][CH3:23])[cH:20][c:19]21.[NH2:10][c:11]1[cH:12][cH:13][c:14]([OH:15])[c:16]([CH3:17])[cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][n:8][c:9]([NH:10][c:11]3[cH:12][cH:13][c:14]([OH:15])[c:16]([CH3:17])[cH:18]3)[c:19]2[cH:20][c:21]1[O:22][CH3:23]
COc1cc2ncnc(Cl)c2cc1OC.Cc1cc(N)ccc1O
COc1cc2ncnc(Nc3ccc(O)c(C)c3)c2cc1OC
null
null
null
Heteroatom Alkylation and Arylation
Goldberg coupling aryl amine-aryl chloride
94bd1d6b149f0eabeae34be7987089f25636bc079a6d701a568fe61e8bfdb7f3
71a04ae650defc5edd86a92f43c304e981a05f07ff76248da8d4155f3905a29d
c1ccc(Nc2ncnc3ccccc23)cc1
Cl-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8].[NH2;D1;+0:9]-[c:10](:[c:11]):[c:12]>>[c:11]:[c:10](-[NH;D2;+0:9]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[#7;a:4]:[c:5](:[c:6]):[c:7]:1:[c:8]):[c:12]
100.4
[{"value": 90.0, "product": "OC1=C(C=C(NC2=NC=NC3=CC(=C(C=C23)OC)OC)C=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.4, "product": "OC1=C(C=C(NC2=NC=NC3=CC(=C(C=C23)OC)OC)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
An analogous reaction to that described in example 17, but starting with 4-amino-2-methylphenol (6.98 g, 56.7 mmol) and 4-chloro-6,7-dimethoxyquinazoline hydrochloride (14.79 g, 56.7 mmol), yielded 4-(4-hydroxy-3-methylanilino)-6,7-dimethoxyquinazoline (17.72 g, 90% yield) as a white solid: Conditions: See reaction.not...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary amine
Secondary amine
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.c1ccccc1
HCl
null
null
null
COc1cc2ncnc(Cl)c2cc1OC.Cc1cc(N)ccc1O>>COc1cc2ncnc(Nc3ccc(O)c(C)c3)c2cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3d0f46ed66344ababd2968acf69646d1
Cc1ccnc(C)c1>>Cc1ccnc(CO)c1
C(CCC)[Li].N1=C(C=C(C=C1)C)C.O1CCCC1>>OCC1=NC=CC(=C1)C
[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH3:7])[cH:9]1>>[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH2:7][OH:8])[cH:9]1
Cc1ccnc(C)c1
Cc1ccnc(CO)c1
null
null
null
Oxidation
OtherReaction
36edec4b18ce2c3a7fbeb76481511ea71ce3ba4a327f9e1abe4335c19ec851f6
3084524a2724b3ba38ce3a72d459533eef64cd59178be6bea9c6cc1599f7369b
c1ccncc1
[CH3;D1;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]>>[O;D1;H1:6]-[CH2;D2;+0:1]-[c:2](:[c:3]):[#7;a:4]:[c:5]
14
[{"value": 14.0, "product": "OCC1=NC=CC(=C1)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
n-Butyllithium (24 ml of a 1.6 N solution in hexanes, 38.4 mmol) was added to a stirred solution of 2,4-lutidine (4.28 g, 40 mmol) in tetrahydrofuran (70 ml) at −70° C. under an inert atmosphere. After 1 hour, air was bubbled through (for 1 hour), methanol (50 ml) was added and the reaction allowed to warm to ambient t...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol
null
null
c1ccncc1
Other
null
null
1
Cc1ccnc(C)c1>>Cc1ccnc(CO)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-10cc6fb9e6c1443a9c00431dcefdc644
Cc1cc([N+](=O)[O-])ccc1F.Cc1ccnc(CO)c1>>Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1
O.[H-].[Na+].OCC1=NC=CC(=C1)C.FC1=C(C=C(C=C1)[N+](=O)[O-])C>>CC1=CC(=NC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])C
F[c:9]1[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]1[CH3:18].[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH2:7][OH:8])[cH:19]1>>[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([N+:13](=[O:14])[O-:15])[cH:16][c:17]2[CH3:18])[cH:19]1
Cc1cc([N+](=O)[O-])ccc1F.Cc1ccnc(CO)c1
Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1
null
null
CN1CCCC1
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(OCc2ccccn2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;D1;H3:5]):[c:6].[#7;a:7]:[c:8]-[C:9]-[OH;D1;+0:10]>>[#7;a:7]:[c:8]-[C:9]-[O;H0;D2;+0:10]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C;D1;H3:5]):[c:6]
70
[{"value": 70.0, "product": "CC1=CC(=NC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.7, "product": "CC1=CC(=NC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
n-Butyllithium (24 ml of a 1.6 N solution in hexanes, 38.4 mmol) was added to a stirred solution of 2,4-lutidine (4.28 g, 40 mmol) in tetrahydrofuran (70 ml) at −70° C. under an inert atmosphere. After 1 hour, air was bubbled through (for 1 hour), methanol (50 ml) was added and the reaction allowed to warm to ambient t...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccncc1.c1ccccc1
HF
CN1CCCC1
null
18
Cc1cc([N+](=O)[O-])ccc1F.Cc1ccnc(CO)c1>CN1CCCC1>Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-11cd4acbba344daca3f83b1f8d725a79
Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1>>Cc1ccnc(COc2ccc(N)cc2C)c1
CC1=CC(=NC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])C>>CC=1C=C(N)C=CC1OCC1=NC=CC(=C1)C
O=[N+:13]([O-])[c:12]1[cH:11][cH:10][c:9]([O:8][CH2:7][c:6]2[n:5][cH:4][cH:3][c:2]([CH3:1])[cH:17]2)[c:15]([CH3:16])[cH:14]1>>[CH3:1][c:2]1[cH:3][cH:4][n:5][c:6]([CH2:7][O:8][c:9]2[cH:10][cH:11][c:12]([NH2:13])[cH:14][c:15]2[CH3:16])[cH:17]1
Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1
Cc1ccnc(COc2ccc(N)cc2C)c1
null
[Pt]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc(OCc2ccccn2)cc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
63.2
[{"value": 63.0, "product": "CC=1C=C(N)C=CC1OCC1=NC=CC(=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.2, "product": "CC=1C=C(N)C=CC1OCC1=NC=CC(=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
n-Butyllithium (24 ml of a 1.6 N solution in hexanes, 38.4 mmol) was added to a stirred solution of 2,4-lutidine (4.28 g, 40 mmol) in tetrahydrofuran (70 ml) at −70° C. under an inert atmosphere. After 1 hour, air was bubbled through (for 1 hour), methanol (50 ml) was added and the reaction allowed to warm to ambient t...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccncc1.c1ccccc1
Other
[Pt].C(C)O
null
2
Cc1ccnc(COc2ccc([N+](=O)[O-])cc2C)c1>[Pt].C(C)O>Cc1ccnc(COc2ccc(N)cc2C)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3139add950a241538b1fdd06676b0e95
COC(=O)C1(C)C=C(OC)C=CN1>>COc1ccnc(CO)c1
[C@@H]([C@H](C(=O)[O-])O)(C(=O)[O-])O.[Na+].[K+].[H-].[Al+3].[Li+].[H-].[H-].[H-].COC1=CC(NC=C1)(C)C(=O)OC>>OCC1=NC=CC(=C1)OC
CO[C:8]([C:7]1(C)[NH:6][CH:5]=[CH:4][C:3]([O:2][CH3:1])=[CH:10]1)=[O:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH2:8][OH:9])[cH:10]1
COC(=O)C1(C)C=C(OC)C=CN1
COc1ccnc(CO)c1
null
null
C(C)OCC
Aromatic Heterocycle Formation
OtherReaction
e214d0dac7edc86590150c7ec7e9615b1f4d1464d7c6672345c4d03da25bfbce
31939348e3671c2efe091cd0d39835c9d512402ac09689f0d7586bbfec0be7a5
c1ccncc1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C;H0;D4;+0:3]1(-C)-[CH;D2;+0:4]=[C;H0;D3;+0:5](-[#8:6]-[C;D1;H3:7])-[CH;D2;+0:8]=[CH;D2;+0:9]-[NH;D2;+0:10]-1>>[C;D1;H3:7]-[#8:6]-[c;H0;D3;+0:5]1:[cH;D2;+0:4]:[c;H0;D3;+0:3](-[CH2;D2;+0:1]-[OH;D1;+0:2]):[n;H0;D2;+0:10]:[cH;D2;+0:9]:[cH;D2;+0:8]:1
36
[{"value": 36.0, "product": "OCC1=NC=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.9, "product": "OCC1=NC=CC(=C1)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
A solution of 2-picolinic acid (10.7 g, 87 mmol) in thionyl chloride (50 ml) was heated at reflux for 18 hours before being cooled and evaporated in vacuo. The residue was treated with methanol (25 ml) and then added to a solution of sodium methoxide prepared from sodium (1.0 g, 43 mmol) and methanol (100 ml). The reac...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ester.Ether
Ether.Primary alcohol
C1=CCNC=C1
c1ccncc1
c1ccncc1
HO-
C(C)OCC
null
1
COC(=O)C1(C)C=C(OC)C=CN1>C(C)OCC>COc1ccnc(CO)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a267dfe4796e473a80c2c1022be2cf59
CCOC(=O)c1ccc(O)c(OC)c1.CS(=O)(=O)OCC(F)(F)F>>CCOC(=O)c1ccc(OCC(F)(F)F)c(OC)c1
C(C)OCC.C([O-])([O-])=O.[K+].[K+].C(C1=CC(OC)=C(O)C=C1)(=O)OCC.CS(=O)(=O)OCC(F)(F)F>>FC(COC1=C(C=C(C(=O)OCC)C=C1)OC)(F)F
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([OH:10])[c:16]([O:17][CH3:18])[cH:19]1.CS(=O)(=O)O[CH2:11][C:12]([F:13])([F:14])[F:15]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([O:10][CH2:11][C:12]([F:13])([F:14])[F:15])[c:16]([O:17][CH3:18])[cH:19]1
CCOC(=O)c1ccc(O)c(OC)c1.CS(=O)(=O)OCC(F)(F)F
CCOC(=O)c1ccc(OCC(F)(F)F)c(OC)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
57201f1afbda3b7775282ca8e3c59a4fb8e542f888bbdbfa994f08238598f88e
b300ae9ac00448343b04f8595ac10c40ddc175401f75ad1a9cb423839305bb59
c1ccccc1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2](-[F;D1;H0:3])(-[F;D1;H0:4])-[F;D1;H0:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[F;D1;H0:3]-[C:2](-[F;D1;H0:4])(-[F;D1;H0:5])-[CH2;D2;+0:1]-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
52
[{"value": 52.0, "product": "FC(COC1=C(C=C(C(=O)OCC)C=C1)OC)(F)F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 51.5, "product": "FC(COC1=C(C=C(C(=O)OCC)C=C1)OC)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
120
CELSIUS
null
null
Potassium carbonate (62.2 g, 450 mmol) was added to a solution of ethyl vanillate (58.9 g, 300 mmol) in dimethylformamide (400 ml) and the reaction heated to 120° C. 2,2,2-Trifluoroethyl methanesulphonate (63.4 g, 360 mmol) was added over 15 minutes and the reaction heated at 120° C. for 15 hours. The reaction was cool...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Aromatic alcohol
Ether
null
null
c1ccccc1
MsOH.HO-
CN(C=O)C
120
null
CCOC(=O)c1ccc(O)c(OC)c1.CS(=O)(=O)OCC(F)(F)F>CN(C=O)C>CCOC(=O)c1ccc(OCC(F)(F)F)c(OC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-eb55cb51d0694342836c240203e8b7f3
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1[N+](=O)[O-]>>CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N
COC=1C=C(C(=O)OCC)C(=CC1OCC(F)(F)F)[N+](=O)[O-]>>COC=1C=C(C(=O)OCC)C(=CC1OCC(F)(F)F)N
O=[N+:20]([O-])[c:19]1[c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][C:14]([F:15])([F:16])[F:17])[cH:18]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][C:14]([F:15])([F:16])[F:17])[cH:18][c:19]1[NH2:20]
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1[N+](=O)[O-]
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N
null
[Pd]
C(C)(=O)OCC.C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
93
[{"value": 93.0, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCC(F)(F)F)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.7, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCC(F)(F)F)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A suspension of ethyl 3-methoxy-4-(2,2,2-trifluoroethoxy)-6-nitrobenzoate (24.0 g, 74.3 mmol) and 10% palladium on carbon (3.0 g) in a mixture of ethanol (100 ml) and ethyl acetate (750 ml) was stirred under an atmosphere of hydrogen for 18 hours. Removal of the catalyst by filtration, followed by solvent evaporation i...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[Pd].C(C)(=O)OCC.C(C)O
null
18
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1[N+](=O)[O-]>[Pd].C(C)(=O)OCC.C(C)O>CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d5317865b9a9429683071815e99f9e03
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N.NC=O>>COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F
NC1=C(C(=O)OCC)C=C(C(=C1)OCC(F)(F)F)OC.C(=O)N>>COC=1C=C2C(NC=NC2=CC1OCC(F)(F)F)=O
CCO[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH2:15][C:16]([F:17])([F:18])[F:19])[cH:12][c:11]1[NH2:10])=[O:7].O=[CH:9][NH2:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6](=[O:7])[nH:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][C:16]([F:17])([F:18])[F:19]
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N.NC=O
COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
558d5445f0c25c1dc397039ffc1d62ab1323fa9420a98d9844188fc8b8f58e63
d6f61cafbdd5f7299eb67523ae66e4a00c7f515735b0b03d65ed431c679d1e30
O=c1[nH]cnc2ccccc12
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].O=[CH;D2;+0:8]-[NH2;D1;+0:9]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[cH;D2;+0:8]:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3]:1:[c:4]
84
[{"value": 84.0, "product": "COC=1C=C2C(NC=NC2=CC1OCC(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}]
175
CELSIUS
18
HOUR
A mixture of ethyl 2-amino-4-(2,2,2-trifluoroethoxy)-5-methoxybenzoate (20.2 g, 69.1 mmol) and formamide (50 ml) was heated at 175° C. for 6 hours. The mixture was allowed to cool to ambient temperature, ethanol (150 ml) was added and the reaction allowed to stand for 18 hours. Collection of the solid which had precipi...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amide.Primary amine
null
c1ccccc1
c1ccc2ncncc2c1
c1ccc2ncncc2c1
HO-
C(C)O
175
18
CCOC(=O)c1cc(OC)c(OCC(F)(F)F)cc1N.NC=O>C(C)O>COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a78ce87a98a84bd4bb83cc911f6b6dde
COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCC(F)(F)F
CN(C=O)C.COC=1C=C2C(NC=NC2=CC1OCC(F)(F)F)=O.S(=O)(Cl)Cl>>ClC1=NC=NC2=CC(=C(C=C12)OC)OCC(F)(F)F
O=[c:6]1[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH2:15][C:16]([F:17])([F:18])[F:19])[cH:12][c:11]2[n:10][cH:9][nH:8]1.O=S(Cl)[Cl:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([Cl:7])[n:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][C:16]([F:17])([F:18])[F:19]
COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F.O=S(Cl)Cl
COc1cc2c(Cl)ncnc2cc1OCC(F)(F)F
null
null
null
Functional Group Interconversion
OtherReaction
3788560e87eee8765e749543914a91a512631307b97fad163ebef894d2a0ea68
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2ncncc2c1
Cl-S(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
97
[{"value": 97.0, "product": "ClC1=NC=NC2=CC(=C(C=C12)OC)OCC(F)(F)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dimethylformamide (0.1 ml) was added dropwise to a solution of 6-methoxy-7-(2,2,2-trifluoroethoxy)-3,4-dihydroquinazolin-4-one (15.8 g, 57.7 mmol) in thionyl chloride (200 ml) and the reaction was heated at reflux for 6 hours. The reaction was cooled, excess thionyl chloride was removed in vacuo and the residue was aze...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1
HCl
null
null
null
COc1cc2c(=O)[nH]cnc2cc1OCC(F)(F)F.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCC(F)(F)F
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-435ac2340289451286b26b02ee408ad2
C1COCCN1.ClCCCBr>>ClCCCN1CCOCC1
N1CCOCC1.BrCCCCl.BrCCCCl>>ClCCCN1CCOCC1
[NH:5]1[CH2:6][CH2:7][O:8][CH2:9][CH2:10]1.Br[CH2:4][CH2:3][CH2:2][Cl:1]>>[Cl:1][CH2:2][CH2:3][CH2:4][N:5]1[CH2:6][CH2:7][O:8][CH2:9][CH2:10]1
C1COCCN1.ClCCCBr
ClCCCN1CCOCC1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2bad30dcdb0a20edb8ce877f072b133eedfd870621da393ec393128bfee00977
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
C1COCCN1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[#8:4]1-[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[#8:4]-[C:5]-[C:6]-1
49
[{"value": 49.0, "product": "ClCCCN1CCOCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.6, "product": "ClCCCN1CCOCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A mixture of morpholine (261 ml, 3.00 mol) and 1-bromo-3-chloropropane (148 ml, 1.50 mol) in toluene (900 ml) was stirred for 18 hours at ambient temperature. Additional 1-bromo-3-chloropropane (25 ml, 0.25 mol) was added, the reaction was stirred for a further 1 hour and then filtered to remove the precipitated solid ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1COCCN1
C1COCC[NH]1
C1COCC[NH]1
HBr
C1(=CC=CC=C1)C
null
18
C1COCCN1.ClCCCBr>C1(=CC=CC=C1)C>ClCCCN1CCOCC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8be430819dbb4a75bfe5bbc25789aab5
CCOC(=O)c1ccc(O)c(OC)c1.ClCCCN1CCOCC1>>CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1
ClCCCN1CCOCC1.C(C1=CC(OC)=C(O)C=C1)(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>COC=1C=C(C(=O)OCC)C=CC1OCCCN1CCOCC1
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([OH:10])[c:20]([O:21][CH3:22])[cH:23]1.Cl[CH2:11][CH2:12][CH2:13][N:14]1[CH2:15][CH2:16][O:17][CH2:18][CH2:19]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][cH:8][c:9]([O:10][CH2:11][CH2:12][CH2:13][N:14]2[CH2:15][CH2:16][O:17][CH2:18][CH2:19]2)[c:20]([O:21][CH3:...
CCOC(=O)c1ccc(O)c(OC)c1.ClCCCN1CCOCC1
CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc(OCCCN2CCOCC2)cc1
Cl-[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]
100
[{"value": 100.0, "product": "COC=1C=C(C(=O)OCC)C=CC1OCCCN1CCOCC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.9, "product": "COC=1C=C(C(=O)OCC)C=CC1OCCCN1CCOCC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
N-(3-Chloropropyl)morpholine (90 g, 0.55 mol) was added dropwise, over 30 minutes, to a solution of ethyl vanillate (98 g, 0.50 mol) and powdered potassium carbonate (104 g, 0.75 mol) in dimethylformamide (300 ml) at 80° C. The reaction was heated at 80° C. for 90 minutes, cooled to ambient temperature, filtered and th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.C1COCC[NH]1
HCl
CN(C=O)C
80
null
CCOC(=O)c1ccc(O)c(OC)c1.ClCCCN1CCOCC1>CN(C=O)C>CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-2add9ebfbf024e819ea7f340e75950e4
CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1.O=[N+]([O-])O>>CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]
COC=1C=C(C(=O)OCC)C=CC1OCCCN1CCOCC1.S(O)(O)(=O)=O.[N+](=O)(O)[O-]>>COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)[N+](=O)[O-]
[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][CH2:14][CH2:15][N:16]2[CH2:17][CH2:18][O:19][CH2:20][CH2:21]2)[cH:22][cH:23]1.O[N+:24](=[O:25])[O-:26]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][CH2:14][CH2:15][N:16]2[CH2:17][CH2:18][O:19]...
CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1.O=[N+]([O-])O
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]
null
null
ClCCl.O.C(C)(=O)O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccc(OCCCN2CCOCC2)cc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[c:8](:[c:9]):[cH;D2;+0:10]:[c:11]:[c:12]>>[C:4]-[#8:5]-[C:6](=[O;D1;H0:7])-[c:8](:[c:9]):[c;H0;D3;+0:10](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:11]:[c:12]
161.8
[{"value": 86.0, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 161.8, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Concentrated sulphuric acid (110 ml) and concentrated nitric acid (19.0 ml, 0.289 mol) were added cautiously, over a 50 minute period, to a two-phase system containing a stirred solution of ethyl 3-methoxy-4-(3-morpholinopropoxy)benzoate (76.5 g, 0.237 mol) in dichloromethane (600 ml), acetic acid (300 ml) and water (7...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1.C1COCC[NH]1
HO-
ClCCl.O.C(C)(=O)O
null
null
CCOC(=O)c1ccc(OCCCN2CCOCC2)c(OC)c1.O=[N+]([O-])O>ClCCl.O.C(C)(=O)O>CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3e775ad05f214a308776e9dbbbd2beae
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]>>CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N
COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)[N+](=O)[O-]>>COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)N
O=[N+:24]([O-])[c:23]1[c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][CH2:14][CH2:15][N:16]2[CH2:17][CH2:18][O:19][CH2:20][CH2:21]2)[cH:22]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[cH:7][c:8]([O:9][CH3:10])[c:11]([O:12][CH2:13][CH2:14][CH2:15][N:16]2[CH2:17][CH2:18][O:19][CH2:20][...
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N
null
[Pd]
C(C)(=O)OCC.C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccc(OCCCN2CCOCC2)cc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[NH2;D1;+0:1]):[c:3]
100.4
[{"value": 100.0, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 100.4, "product": "COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
A suspension of ethyl 3-methoxy-4-(3-morpholinopropoxy)-6-nitrobenzoate (132.2 g, 359 mmol) and 10% palladium on carbon (3.0 g) in a mixture of ethanol (200 ml) and ethyl acetate (2000 ml) was stirred under an atmosphere of hydrogen for 18 hours. Removal of the catalyst by filtration, followed by solvent evaporation in...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.C1COCC[NH]1
Other
[Pd].C(C)(=O)OCC.C(C)O
null
18
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1[N+](=O)[O-]>[Pd].C(C)(=O)OCC.C(C)O>CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-df02568b306e4b00b5f95b85ecf630db
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N.NC=O>>COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1
COC=1C=C(C(=O)OCC)C(=CC1OCCCN1CCOCC1)N.C(=O)N>>COC=1C=C2C(NC=NC2=CC1OCCCN1CCOCC1)=O
CCO[C:6]([c:5]1[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH2:15][CH2:16][CH2:17][N:18]2[CH2:19][CH2:20][O:21][CH2:22][CH2:23]2)[cH:12][c:11]1[NH2:10])=[O:7].O=[CH:9][NH2:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6](=[O:7])[nH:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][O:21][CH2:22]...
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N.NC=O
COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
558d5445f0c25c1dc397039ffc1d62ab1323fa9420a98d9844188fc8b8f58e63
d6f61cafbdd5f7299eb67523ae66e4a00c7f515735b0b03d65ed431c679d1e30
O=c1[nH]cnc2cc(OCCCN3CCOCC3)ccc12
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].O=[CH;D2;+0:8]-[NH2;D1;+0:9]>>[O;D1;H0:2]=[c;H0;D3;+0:1]1:[nH;D2;+0:9]:[cH;D2;+0:8]:[n;H0;D2;+0:6]:[c:5](:[c:7]):[c:3]:1:[c:4]
68
[{"value": 68.0, "product": "COC=1C=C2C(NC=NC2=CC1OCCCN1CCOCC1)=O", "details": "PERCENTYIELD", "is_desired": false}]
125
CELSIUS
null
null
A solution of ethyl 3-methoxy-4-(3-morpholinopropoxy)-6-aminobenzoate (130 g, 384 mmol) in formamide (280 ml) was heated at 180° C. for 3 hours, during which time a small amount (25 ml) of liquid distilled out of the reaction. The reaction was cooled to 125° C. and the excess formamide was evaporated in vacuo. Triturat...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amide.Primary amine
null
c1ccccc1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.C1COCC[NH]1
HO-
null
125
null
CCOC(=O)c1cc(OC)c(OCCCN2CCOCC2)cc1N.NC=O>>COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-531b0617f1c04b48bde5a40121a490f9
COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1
CN(C=O)C.COC=1C=C2C(NC=NC2=CC1OCCCN1CCOCC1)=O.S(=O)(Cl)Cl>>ClC1=NC=NC2=CC(=C(C=C12)OC)OCCCN1CCOCC1
O=[c:6]1[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH2:15][CH2:16][CH2:17][N:18]3[CH2:19][CH2:20][O:21][CH2:22][CH2:23]3)[cH:12][c:11]2[n:10][cH:9][nH:8]1.O=S(Cl)[Cl:7]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[c:6]([Cl:7])[n:8][cH:9][n:10][c:11]2[cH:12][c:13]1[O:14][CH2:15][CH2:16][CH2:17][N:18]1[CH2:19][CH2:20][O:21][CH2:22]...
COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1.O=S(Cl)Cl
COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1
null
null
null
Functional Group Interconversion
OtherReaction
3788560e87eee8765e749543914a91a512631307b97fad163ebef894d2a0ea68
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ncc2ccc(OCCCN3CCOCC3)cc2n1
Cl-S(=O)-[Cl;H0;D1;+0:1].O=[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2]1:[n;H0;D2;+0:3]:[c:4]:[#7;a:5]:[c:6](:[c:7]):[c:8]:1:[c:9]
60
[{"value": 60.0, "product": "ClC1=NC=NC2=CC(=C(C=C12)OC)OCCCN1CCOCC1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dimethylformamide (2.0 ml) was added dropwise to a solution of 6-methoxy-7-(3-morpholinopropoxy)-3,4-dihydro-quinazolin-4-one (83.0 g, 261 mmol) in thionyl chloride (700 ml) and the reaction was heated at reflux for 3.5 hours. The reaction was cooled, excess thionyl chloride was removed in vacuo, the residue was taken ...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.C1COCC[NH]1
HCl
null
null
null
COc1cc2c(=O)[nH]cnc2cc1OCCCN1CCOCC1.O=S(Cl)Cl>>COc1cc2c(Cl)ncnc2cc1OCCCN1CCOCC1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-317c8be1d0594abeac97a3292b5127f9
COc1cc2nc[nH]c(=O)c2cc1OC.CSCC[C@H](N)C(=O)O>>COc1cc2nc[nH]c(=O)c2cc1OC(C)=O
[OH-].[Na+].COC=1C=C2C(NC=NC2=CC1OC)=O.N[C@@H](CCSC)C(=O)O.O>>C(C)(=O)OC=1C=C2C(NC=NC2=CC1OC)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][nH:8][c:9](=[O:10])[c:11]2[cH:12][c:13]1[O:14][CH3:15].N[C@@H](CCS[CH3:16])C(O)=[O:17]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][nH:8][c:9](=[O:10])[c:11]2[cH:12][c:13]1[O:14][C:15]([CH3:16])=[O:17]
COc1cc2nc[nH]c(=O)c2cc1OC.CSCC[C@H](N)C(=O)O
COc1cc2nc[nH]c(=O)c2cc1OC(C)=O
null
null
CS(=O)(=O)O
C-C Coupling
OtherReaction
3b06da3fae32f95a45189e2935fa8587553b2c5cd1a498dbf590b1ce528f905c
9cb00d8d3217954441d0b4f8c6749015a87dd991589f75a5f47658f24fe005c6
O=c1[nH]cnc2ccccc12
N-[C@@H](-C-C-S-[CH3;D1;+0:1])-C(-O)=[O;H0;D1;+0:2].[CH3;D1;+0:3]-[#8:4]-[c:5]>>[CH3;D1;+0:1]-[C;H0;D3;+0:3](=[O;H0;D1;+0:2])-[#8:4]-[c:5]
57
[{"value": 57.0, "product": "C(C)(=O)OC=1C=C2C(NC=NC2=CC1OC)=O", "details": "PERCENTYIELD", "is_desired": false}]
100
CELSIUS
null
null
A mixture of 6,7-dimethoxy-3,4-dihydroquinazolin-4-one (20.0 g, 97 mmol) and racemic methionine (21.7 g, 146 mmol) in methanesulphonic acid (150 ml) were heated at 100° C. for 5.5 hours and then allowed to cool to ambient temperature over 18 hours. The reaction was poured into cold water (750 ml), the pH of the aqueous...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Primary amine.Monosulfide
Ester
null
null
c1ccc2ncncc2c1
Other
CS(=O)(=O)O
100
null
COc1cc2nc[nH]c(=O)c2cc1OC.CSCC[C@H](N)C(=O)O>CS(=O)(=O)O>COc1cc2nc[nH]c(=O)c2cc1OC(C)=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1471d90fa01040128232ed4bb91f676d
COc1cc2nc[nH]c(=O)c2cc1OC(C)=O.O=S(Cl)Cl>>COc1cc2ncnc(Cl)c2cc1OC(C)=O.Cl
CN(C=O)C.C(C)(=O)OC=1C=C2C(NC=NC2=CC1OC)=O.S(=O)(Cl)Cl>>Cl.ClC1=NC=NC2=CC(=C(C=C12)OC(C)=O)OC
O=[c:9]1[nH:8][cH:7][n:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][C:15]([CH3:16])=[O:17])[cH:12][c:11]21.O=S([Cl:10])[Cl:18]>>[CH3:1][O:2][c:3]1[cH:4][c:5]2[n:6][cH:7][n:8][c:9]([Cl:10])[c:11]2[cH:12][c:13]1[O:14][C:15]([CH3:16])=[O:17].[ClH:18]
COc1cc2nc[nH]c(=O)c2cc1OC(C)=O.O=S(Cl)Cl
COc1cc2ncnc(Cl)c2cc1OC(C)=O.Cl
null
null
null
Functional Group Interconversion
OtherReaction
3788560e87eee8765e749543914a91a512631307b97fad163ebef894d2a0ea68
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccc2ncncc2c1
O=S(-[Cl;H0;D1;+0:1])-[Cl;H0;D1;+0:2].O=[c;H0;D3;+0:3]1:[nH;D2;+0:4]:[c:5]:[#7;a:6]:[c:7](:[c:8]):[c:9]:1:[c:10]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:3]1:[n;H0;D2;+0:4]:[c:5]:[#7;a:6]:[c:7](:[c:8]):[c:9]:1:[c:10].[ClH;D0;+0:2]
87
[{"value": 87.0, "product": "Cl.ClC1=NC=NC2=CC(=C(C=C12)OC(C)=O)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Dimethylformamide (0.25 ml) was added dropwise to a solution of 6-acetoxy-7-methoxy-3,4-dihydro-quinazolin-4-one (13.8 g, 59.0 mmol) in thionyl chloride (150 ml) and the reaction was heated at reflux for 1.5 hours. The reaction was cooled, excess thionyl chloride was removed in vacuo and the residue was azeotroped with...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccc2ncncc2c1
c1ccc2ncncc2c1
c1ccc2ncncc2c1
Other
null
null
null
COc1cc2nc[nH]c(=O)c2cc1OC(C)=O.O=S(Cl)Cl>>COc1cc2ncnc(Cl)c2cc1OC(C)=O.Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-10b4a1e360fd44fd8067583fd1414ad1
O=[N+]([O-])c1ccc(F)c(F)c1.OCc1ccccn1>>O=[N+]([O-])c1ccc(OCc2ccccn2)c(F)c1
OCC1=NC=CC=C1.FC=1C=C(C=CC1F)[N+](=O)[O-]>>N1=C(C=CC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])F
F[c:7]1[cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[cH:18][c:16]1[F:17].[OH:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][n:15]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][c:10]2[cH:11][cH:12][cH:13][cH:14][n:15]2)[c:16]([F:17])[cH:18]1
O=[N+]([O-])c1ccc(F)c(F)c1.OCc1ccccn1
O=[N+]([O-])c1ccc(OCc2ccccn2)c(F)c1
null
null
null
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
4821d6d7238522ee9ef4538c00647e855becf4de3d9c939c0cec2b01c1e5e915
a4cafa7bcd156e21cca6eaac1b32e28ec8540642a31181122e6957f3d7559631
c1ccc(OCc2ccccn2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[F;D1;H0:5]):[c:6].[#7;a:7]:[c:8]-[C:9]-[OH;D1;+0:10]>>[#7;a:7]:[c:8]-[C:9]-[O;H0;D2;+0:10]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[F;D1;H0:5]):[c:6]
58
[{"value": 58.0, "product": "N1=C(C=CC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])F", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.7, "product": "N1=C(C=CC=C1)COC1=C(C=C(C=C1)[N+](=O)[O-])F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
An analogous reaction to that described in example 42b, but starting with 2-(hydroxymethyl)pyridine (3.50 g, 36 mmol) and 3,4-difluoronitrobenzene (5.00 g, 31.4 mmol), yielded 2-((2-pyridyl)methoxy)-5-nitrofluorobenzene (4.50 g, 58% yield) as a yellow solid. d) An analogous reaction to that described in example 42c, bu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Primary alcohol
Ether
c1ccccc1
c1ccccc1
c1ccccc1.c1ccncc1
HF
null
null
null
O=[N+]([O-])c1ccc(F)c(F)c1.OCc1ccccn1>>O=[N+]([O-])c1ccc(OCc2ccccn2)c(F)c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-70296c78e31344738708a81a3be49637
NN.O=C1NC(=O)c2ccccc21>>NCCc1ccc[nH]c1=O
C1(C=2C(C(N1)=O)=CC=CC2)=O.O.NN>>NCCC=1C(NC=CC1)=O
N[NH2:1].O=[C:2]1[NH:8][C:3](=[O:10])[c:4]2[cH:5][cH:6][cH:7]c[c:9]21>>[NH2:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][cH:7][nH:8][c:9]1=[O:10]
NN.O=C1NC(=O)c2ccccc21
NCCc1ccc[nH]c1=O
null
null
ClCCl.CO
C-C Coupling
OtherReaction
03662bd10049b4ab9b31ad02144021924fa52ff65543d64aab667e5e90135d81
308f75b738848e24fb4e299b1496b46700df7b98fa2f71103674d0faeb151880
O=c1cccc[nH]1
N-[NH2;D1;+0:1].O=[C;H0;D3;+0:2]1-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[c:6]2:[c:7]:[c:8]:[cH;D2;+0:9]:c:[c;H0;D3;+0:10]:2-1>>[NH2;D1;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:4]-[c:6]1:[c:7]:[c:8]:[cH;D2;+0:9]:[nH;D2;+0:3]:[c;H0;D3;+0:10]:1=[O;H0;D1;+0:5]
55
[{"value": 55.0, "product": "NCCC=1C(NC=CC1)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To a suspension of 1.2 g (2.5 mmol) of phthalimide 4 in 100 ml of methanol was added 6 ml of hydrazine monohydrate. This was stirred at room temperature overnight upon which the suspension turned into a clear yellow solution. The mixture was concentrated and residue was diluted with water and extracted with chloroform....
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Unsubstituted dicarboximide
Primary amine
c1ccc2c(c1)CNC2
c1cnccc1
c1cnccc1
Other
ClCCl.CO
null
8
NN.O=C1NC(=O)c2ccccc21>ClCCl.CO>NCCc1ccc[nH]c1=O
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c30303655a2b4a24becb86513c91bcf9
CCN(CC)CC.NC1CCN(Cc2ccccc2)CC1.O=C(Cl)OCc1ccccc1>>CCCCCCCCCCCCN
NC1CCN(CC1)CC1=CC=CC=C1.C(C)N(CC)CC.ClC(=O)OCC1=CC=CC=C1>>CCCCCCCCCCCCN
CCN(CC)C[CH3:1].C1C[CH:12]([NH2:13])[CH2:11][CH2:10]N1C[c:7]1[cH:2][cH:3][cH:4][cH:5][cH:6]1.O=C(Cl)OCc1ccc[cH:8][cH:9]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH2:13]
CCN(CC)CC.NC1CCN(Cc2ccccc2)CC1.O=C(Cl)OCc1ccccc1
CCCCCCCCCCCCN
null
null
O1CCCC1
C-C Coupling
OtherReaction
21e9f45c202f89b4c7f3ea9e8916a0233c0d2b6c43e742b89236499ec5df4cfa
b4ef3b86ebd0fc68614170fa576ee7f8bd9b131a1ad54d9d4947eab135b76a2e
null
C-C-N(-C-C)-C-[CH3;D1;+0:1].Cl-C(=O)-O-C-c1:[cH;D2;+0:2]:[cH;D2;+0:3]:c:c:c:1.[N;D1;H2:4]-[CH;D3;+0:5]1-C-C-N(-C-[c;H0;D3;+0:6]2:[cH;D2;+0:7]:[cH;D2;+0:8]:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:2)-[CH2;D2;+0:12]-[C:13]-1>>[CH3;D1;+0:1]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[CH2;D2;+0:10]-[CH2;D2;+0:11]-[CH2;D2;+0...
69.3
[{"value": 69.3, "product": "CCCCCCCCCCCCN", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
12
HOUR
To a 0° C. solution of 4-amino-1-benzylpiperidine 11 (41.2 g, 216.5 mmol) and triethylamine (51.3 mL, 369 mmol) in 600 mL of tetrahydrofuran was added benzyl chloroformate (31 mL, 217 mmol) dropwise over a period of 30 to 45 min. at such a rate that the reaction temperature was kept between 5° C. and 10° C. After the a...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Tertiary amine.Tertiary amine
null
C1CCNCC1.c1ccccc1.c1ccccc1
null
null
HCl
O1CCCC1
null
12
CCN(CC)CC.NC1CCN(Cc2ccccc2)CC1.O=C(Cl)OCc1ccccc1>O1CCCC1>CCCCCCCCCCCCN
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8959c8c81cd14d269a4648ed8f87ce0e
COc1ccc(C=O)cc1OC.COc1nc(N2CCNCC2)ccc1Br>>COc1ccc(CN2CCN(c3ccc(Br)c(OC)n3)CC2)cc1OC
BrC=1C=CC(=NC1OC)N1CCNCC1.COC=1C=C(C=O)C=CC1OC.[BH-](OC(=O)C)(OC(=O)C)OC(=O)C.[Na+]>>BrC=1C=CC(=NC1OC)N1CCN(CC1)CC1=CC(=C(C=C1)OC)OC
O=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:24]([O:25][CH3:26])[cH:23]1.[NH:8]1[CH2:9][CH2:10][N:11]([c:12]2[cH:13][cH:14][c:15]([Br:16])[c:17]([O:18][CH3:19])[n:20]2)[CH2:21][CH2:22]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][N:8]2[CH2:9][CH2:10][N:11]([c:12]3[cH:13][cH:14][c:15]([Br:16])[c:17]([O:18][CH3:19])[...
COc1ccc(C=O)cc1OC.COc1nc(N2CCNCC2)ccc1Br
COc1ccc(CN2CCN(c3ccc(Br)c(OC)n3)CC2)cc1OC
null
C(C)(=O)O
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
reductive amination
7a1842565a3c73c1d6bba5dccafef60d48e9eaf6e4a0871f60e828bcbdf26fb1
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(CN2CCN(c3ccccn3)CC2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:9]-[C:10]-[#7:5]-[C:6]-[C:7]-1):[c:4]
null
[]
null
null
null
null
A quantity of 0.1 g (0.4 mmole, 1 eq) of 1-(5-Bromo-6-methoxy-pyridin-2-yl)-piperazine and 0.061 g (0.4 mmole, 1 eq) of 3,4-dimethoxybenzaldehyde is dissolved in 5 mL of anhydrous toluene, and 3 drops of glacial acetic acid is added. An excess of NaBH(OAc)3 is added to the solution and stirred at room temperature under...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccncc1
Other
C(C)(=O)O.C1(=CC=CC=C1)C
null
null
COc1ccc(C=O)cc1OC.COc1nc(N2CCNCC2)ccc1Br>C(C)(=O)O.C1(=CC=CC=C1)C>COc1ccc(CN2CCN(c3ccc(Br)c(OC)n3)CC2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c0a1f86b44244d6ba10f1cf103692e8a
COc1ccc(C(C)=O)cc1OC.FC(F)(F)c1cc(N2CCNCC2)ccc1Cl>>COc1ccc(C(C)N2CCN(c3ccc(Cl)c(C(F)(F)F)c3)CC2)cc1OC
ClC1=C(C=C(C=C1)N1CCNCC1)C(F)(F)F.CC(=O)C1=CC(=C(C=C1)OC)OC.[BH4-].[Na+]>>ClC1=C(C=C(C=C1)N1CCN(CC1)C(C)C1=CC(=C(C=C1)OC)OC)C(F)(F)F
O=[C:7]([c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:27]([O:28][CH3:29])[cH:26]1)[CH3:8].[NH:9]1[CH2:10][CH2:11][N:12]([c:13]2[cH:14][cH:15][c:16]([Cl:17])[c:18]([C:19]([F:20])([F:21])[F:22])[cH:23]2)[CH2:24][CH2:25]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([CH3:8])[N:9]2[CH2:10][CH2:11][N:12]([c:13]3[cH:14][cH:15][c:16...
COc1ccc(C(C)=O)cc1OC.FC(F)(F)c1cc(N2CCNCC2)ccc1Cl
COc1ccc(C(C)N2CCN(c3ccc(Cl)c(C(F)(F)F)c3)CC2)cc1OC
null
CC(C)O[Ti](OC(C)C)(OC(C)C)OC(C)C
CO
Heteroatom Alkylation and Arylation
reductive amination
d4cc9a2a46f538d7a2ff577eac4d4531ea828578c3aec2ccd0e8c1d501914fc6
99acf13bfcfe579f51ccb82c65e4ca039ee7ca9b6fcd2747a3d9a292a88e564e
c1ccc(CN2CCN(c3ccccc3)CC2)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[c:5].[#7:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[C;D1;H3:2]-[CH;D3;+0:1](-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#7:6]-[C:11]-[C:10]-1)-[c:3](:[c:4]):[c:5]
null
[]
null
null
2
HOUR
A quantity of 0.17 g (0.6 mmole, 1 eq) of 1-(4-chloro-3-trifluoromethyl-phenyl)-piperazine and 0.1 g (0.6 mmole, 1 eq) of 3,4-dimethoxyacetophenone and 2 mL of Ti(OiPr)4 are warmed to 70° C. for 2 hours. The reaction solution is cooled to room temperature and 20 mL of anhydrous methanol is added followed by 1.0 g of Na...
10.6084/m9.figshare.5104873.v1
null
Ketone.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
Other
CC(C)O[Ti](OC(C)C)(OC(C)C)OC(C)C.CO
null
2
COc1ccc(C(C)=O)cc1OC.FC(F)(F)c1cc(N2CCNCC2)ccc1Cl>CC(C)O[Ti](OC(C)C)(OC(C)C)OC(C)C.CO>COc1ccc(C(C)N2CCN(c3ccc(Cl)c(C(F)(F)F)c3)CC2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1bb7eedc81724abd9e07461551a2da24
COc1cc(N2CCNCC2)ccc1Br.O=Cc1cnc2ccccc2c1>>COc1cc(N2CCN(C(C)c3cnc4ccccc4c3)CC2)ccc1Br
N1=CC(=CC2=CC=CC=C12)C=O.N1N=NC2=C1C=CC=C2.BrC1=C(C=C(C=C1)N1CCNCC1)OC.C[Mg]Br.C(C)OCC>>BrC1=C(C=C(C=C1)N1CCN(CC1)C(C)C=1C=NC2=CC=CC=C2C1)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][NH:9][CH2:22][CH2:23]2)[cH:24][cH:25][c:26]1[Br:27].O=[CH:10][c:12]1[cH:13][n:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][N:9]([CH:10]([CH3:11])[c:12]3[cH:13][n:14][c:15]4[cH:16][cH:17][cH:18][cH:19][c:20]4[...
COc1cc(N2CCNCC2)ccc1Br.O=Cc1cnc2ccccc2c1
COc1cc(N2CCN(C(C)c3cnc4ccccc4c3)CC2)ccc1Br
null
null
C1(=CC=CC=C1)C.C(C)(=O)OCC.C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
66e6667395903ee1c54d8aecc784ece1bccbdcbc9661ebcae0e6a980f9380640
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(N2CCN(Cc3cnc4ccccc4c3)CC2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6].[#7:7]1-[C:8]-[C:9]-[NH;D2;+0:10]-[C:11]-[C:12]-1>>[C;D1;H3:13]-[CH;D3;+0:1](-[N;H0;D3;+0:10]1-[C:9]-[C:8]-[#7:7]-[C:12]-[C:11]-1)-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]
null
[]
60
CELSIUS
18
HOUR
A solution containing 3-quinolinecarboxaldehyde (25 mg, 0.16 mmol, 1.0 equivalents), benzotriazole (19 mg, 0.16 mmol, 1.0 equivalents) and 1-(4-bromo-3-methoxy-phenyl)-piperazine (39 mg, 0.17 mmol, 1.1 equivalents) in ethanol (1 ml) and toluene (2 ml) was heated 20 minutes at 60° C. Solution was concentrated. Residue w...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
C1C[NH]CCN1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccc2ncccc2c1
null
C1(=CC=CC=C1)C.C(C)(=O)OCC.C(C)O
60
18
COc1cc(N2CCNCC2)ccc1Br.O=Cc1cnc2ccccc2c1>C1(=CC=CC=C1)C.C(C)(=O)OCC.C(C)O>COc1cc(N2CCN(C(C)c3cnc4ccccc4c3)CC2)ccc1Br
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e708439672104902ad9652f8c150d57e
COc1cc(Br)ccc1Cl.COc1ccc([C@@H](C)N2CCNCC2)cc1OC>>COc1cc(N2CCN([C@H](C)c3ccc(OC)c(OC)c3)CC2)ccc1Cl
CC(C)([O-])C.[K+].COC=1C=C(C=CC1OC)[C@@H](C)N1CCNCC1.BrC=1C=CC(=C(C1)OC)Cl.Cl>>ClC1=C(C=C(C=C1)N1CCN(CC1)[C@H](C)C1=CC(=C(C=C1)OC)OC)OC
Br[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:26]([Cl:27])[cH:25][cH:24]1.[NH:6]1[CH2:7][CH2:8][N:9]([C@H:10]([CH3:11])[c:12]2[cH:13][cH:14][c:15]([O:16][CH3:17])[c:18]([O:19][CH3:20])[cH:21]2)[CH2:22][CH2:23]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][N:9]([C@H:10]([CH3:11])[c:12]3[cH:13][cH:14][c:15]([O:16][CH3:17])[...
COc1cc(Br)ccc1Cl.COc1ccc([C@@H](C)N2CCNCC2)cc1OC
COc1cc(N2CCN([C@H](C)c3ccc(OC)c(OC)c3)CC2)ccc1Cl
null
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd]
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
75de53007ec0cb91435746fdefbf3b121f745fc71ddebd19c6e45a5212b3f56a
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(CN2CCN(c3ccccc3)CC2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[#7:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#7:6]-[C:11]-[C:10]-1):[c:4]:[c:5]
61.7
[{"value": 53.0, "product": "ClC1=C(C=C(C=C1)N1CCN(CC1)[C@H](C)C1=CC(=C(C=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 61.7, "product": "ClC1=C(C=C(C=C1)N1CCN(CC1)[C@H](C)C1=CC(=C(C=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A quantity of 4.2 g (17 mmoles, 1 eq) of (R)-1-[1-(3,4-dimethoxy-phenyl)-ethyl]-piperazine and 4.4 g (20 mmoles, 1.2 eq) of 5-Bromo-2-chloro-anisole was dissolved in 110 mL of anhydrous toluene, and the solution is purged with N2 for 20 minutes. To the solution was added 0.33 g (0.5 mmoles, 0.03 eq) of rac-2, 2′-Bis(di...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1.C1CNCC[NH]1
c1ccccc1.C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1.c1ccccc1
HBr
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C
80
null
COc1cc(Br)ccc1Cl.COc1ccc([C@@H](C)N2CCNCC2)cc1OC>C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C>COc1cc(N2CCN([C@H](C)c3ccc(OC)c(OC)c3)CC2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8ba6604103bb4174bb8504f5dd723b6b
COC(=O)C(CSCC(=O)c1ccc(OC)c(OC)c1)NC(=O)OC(C)(C)C>>COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1
COC(C(CSCC(=O)C1=CC(=C(C=C1)OC)OC)NC(=O)OC(C)(C)C)=O.FC(C(=O)O)(F)F.C([O-])(O)=O.[Na+].C(C)(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+]>>COC(=O)C1NC(CSC1)C1=CC(=C(C=C1)OC)OC
CC(C)(C)OC(=O)[NH:20][CH:5]([C:3]([O:2][CH3:1])=[O:4])[CH2:6][S:7][CH2:8][C:9](=O)[c:10]1[cH:11][cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[cH:19]1>>[CH3:1][O:2][C:3](=[O:4])[CH:5]1[CH2:6][S:7][CH2:8][CH:9]([c:10]2[cH:11][cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[cH:19]2)[NH:20]1
COC(=O)C(CSCC(=O)c1ccc(OC)c(OC)c1)NC(=O)OC(C)(C)C
COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1
null
null
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
8fb261716131fb768ea924fd38d1e19554b4bbefd281d07fe864aedc9d8e88cb
1c4cec4730086d81e4d619e804478e6e78c92525d3d5a05dc2fde7b44b847d30
c1ccc(C2CSCCN2)cc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3]-[#16:4]-[C:5]-[C;H0;D3;+0:6](=O)-[c:7](:[c:8]):[c:9])-[C:10](=[O;D1;H0:11])-[#8:12]-[C;D1;H3:13]>>[C;D1;H3:13]-[#8:12]-[C:10](=[O;D1;H0:11])-[C:2]1-[C:3]-[#16:4]-[C:5]-[CH;D3;+0:6](-[c:7](:[c:8]):[c:9])-[NH;D2;+0:1]-1
59
[{"value": 59.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To an ice chilled solution of 2-tert-butoxycarbonylamino-3-[2-(3,4-dimethoxy-phenyl)-2-oxo-ethylsulfanyl]-propionic acid methyl ester (2.00 g, 9.34 mmol, 1.0 equivalents) in dichloromethane (9 ml) was added trifluoroacetic acid (9 ml). The reaction solution was stirred on ice for 4 hours. The solution was concentrated,...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ketone.Ether.Boc
Secondary amine
null
C1CSCCN1
C1CSCCN1.c1ccccc1
HO-
ClCCl
null
4
COC(=O)C(CSCC(=O)c1ccc(OC)c(OC)c1)NC(=O)OC(C)(C)C>ClCCl>COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-98b259cb2faf4ca8837e87a42fc7b395
COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1.COc1cc(N)ccc1Cl>>COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
C[Al](C)C.COC(=O)C1NC(CSC1)C1=CC(=C(C=C1)OC)OC.ClC1=C(C=C(N)C=C1)OC>>ClC1=C(C=C(C=C1)NC(=O)C1NC(CSC1)C1=CC(=C(C=C1)OC)OC)OC
CO[C:7](=[O:8])[CH:9]1[CH2:10][S:11][CH2:12][CH:13]([c:14]2[cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]([O:21][CH3:22])[cH:23]2)[NH:24]1.[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[cH:25][cH:26][c:27]1[Cl:28]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][C:7](=[O:8])[CH:9]2[CH2:10][S:11][CH2:12][CH:13]([c:14]3[cH:15][cH:16][c:17]([O:...
COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1.COc1cc(N)ccc1Cl
COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
null
null
null
Acylation
Aminolysis of esters
04c54ce22aa9bc0cea0de3d900446bcab51cf02bebeb606fa788a47dcd0e37ff
4335147c9ad02004b7c12428d7eac0b2e7e0e2017adc471d01c387239de8017d
O=C(Nc1ccccc1)C1CSCC(c2ccccc2)N1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[#7:4]-[C:5])-[C:6]-[#16:7].[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[#16:7]-[C:6]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])-[#7:4]-[C:5]
76
[{"value": 76.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
18
HOUR
A 2.0M solution of trimethylaluminum (0.39 ml, 0.78 mmol, 3.5 equivalents) was added to a solution of 5-(3,4-dimethoxy-phenyl)-thiomorpholine-3-carboxylic acid methyl ester (67 mg, 0.22 mmol, 1.0 equivalents) and 4-chloro-3-methoxyaniline (106 mg, 0.68 mmol, 3.0 equivalents). The solution was stirred at 50° C. for 18 h...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Secondary amide
null
null
c1ccccc1.C1CSCCN1.c1ccccc1
HO-
null
50
18
COC(=O)C1CSCC(c2ccc(OC)c(OC)c2)N1.COc1cc(N)ccc1Cl>>COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0e5cc19961ba4827bae115bd31489e70
COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl>>COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
ClC1=C(C=C(C=C1)NC(=O)C1NC(CSC1)C1=CC(=C(C=C1)OC)OC)OC>>ClC1=C(C=C(C=C1)NCC1NC(CSC1)C1=CC(=C(C=C1)OC)OC)OC
O=[C:7]([NH:6][c:5]1[cH:4][c:3]([O:2][CH3:1])[c:26]([Cl:27])[cH:25][cH:24]1)[CH:8]1[CH2:9][S:10][CH2:11][CH:12]([c:13]2[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([O:20][CH3:21])[cH:22]2)[NH:23]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][CH2:7][CH:8]2[CH2:9][S:10][CH2:11][CH:12]([c:13]3[cH:14][cH:15][c:16]([O:17][CH3:18])[c...
COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
null
null
C1(=CC=CC=C1)C
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(NCC2CSCC(c3ccccc3)N2)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[c:3])-[C:4](-[#7:5]-[C:6])-[C:7]-[#16:8]>>[#16:8]-[C:7]-[C:4](-[CH2;D2;+0:1]-[#7:2]-[c:3])-[#7:5]-[C:6]
95
[{"value": 95.0, "product": "ClC1=C(C=C(C=C1)NCC1NC(CSC1)C1=CC(=C(C=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To an ice chilled suspension containing 5-(3,4-dimethoxy-phenyl)-thiomorpholine-3-carboxylic acid (4-chloro-3-methoxy-phenyl)-amide n(71 mg, 0.17 mmol, 1.0 equivalents) in toluene (1.5 ml) was added a 0.5M solution of alane (1.6 ml, 0.8 mmol, 4.8 equivalents). The reaction was stirred at room temperature for 2 hours. T...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.C1CSCCN1.c1ccccc1
Other
C1(=CC=CC=C1)C
null
2
COc1cc(NC(=O)C2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl>C1(=CC=CC=C1)C>COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e46feeb8a4a04376ae885d905c5c4b2a
CC(Br)Br.COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl>>COc1cc(N2CCN3C(CSCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
BrC(C)Br.C(C)N(CC)CC.BrC(C)Br.C(C)N(CC)CC.ClC1=C(C=C(C=C1)NCC1NC(CSC1)C1=CC(=C(C=C1)OC)OC)OC.BrC(C)Br.C(C)N(CC)CC>>ClC1=C(C=C(C=C1)N1CC2CSCC(N2CC1)C1=CC(=C(C=C1)OC)OC)OC
Br[CH:8](Br)[CH3:7].[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][CH2:25][CH:10]2[NH:9][CH:14]([c:15]3[cH:16][cH:17][c:18]([O:19][CH3:20])[c:21]([O:22][CH3:23])[cH:24]3)[CH2:13][S:12][CH2:11]2)[cH:26][cH:27][c:28]1[Cl:29]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][N:9]3[CH:10]([CH2:11][S:12][CH2:13][CH:14]3[c:15]3[cH:1...
CC(Br)Br.COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl
COc1cc(N2CCN3C(CSCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
null
null
CC(=O)N(C)C
Heteroatom Alkylation and Arylation
OtherReaction
c17a52e5d43aa1d9cd5a1f06f97c42e464d08975157fe0a3f55e314e9bfaf306
a4f9aac18aa96dbf899d70608583d8fd7f3c4f3b117366bea2604d063aa01548
c1ccc(C2CSCC3CN(c4ccccc4)CCN32)cc1
Br-[CH;D3;+0:1](-Br)-[CH3;D1;+0:2].[c:3]-[C:4]1-[C:5]-[#16:6]-[C:7]-[C:8](-[C:9]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[NH;D2;+0:14]-1>>[c:3]-[C:4]1-[C:5]-[#16:6]-[C:7]-[C:8]2-[C:9]-[N;H0;D3;+0:10](-[c:11](:[c:12]):[c:13])-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:14]-2-1
31.9
[{"value": 31.9, "product": "ClC1=C(C=C(C=C1)N1CC2CSCC(N2CC1)C1=CC(=C(C=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
90
CELSIUS
4
HOUR
A solution of (4-chloro-3-methoxy-phenyl)-[5-(3,4-dimethoxy-phenyl)-thiomorpholin-3-ylmethyl]-amine (100 mg, 0.245 mmol, 1.0 equivalents), dibromoethane (0.31 ml, 3.55 mmol, 14.5 equivalents) and triethylamine (0.15 ml, 1.09 mmol, 4.5 equivalents) in dimethylacetamide (2 ml) was heated at 90° C. for 4 hours. Additional...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Secondary amine.Secondary amine
Tertiary amine.Tertiary amine
C1CSCCN1
C1CN2CCSCC2C[NH]1
c1ccccc1.C1CN2CCSCC2C[NH]1.c1ccccc1
HBr
CC(=O)N(C)C
90
4
CC(Br)Br.COc1cc(NCC2CSCC(c3ccc(OC)c(OC)c3)N2)ccc1Cl>CC(=O)N(C)C>COc1cc(N2CCN3C(CSCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ccf46ede910d40369dee25ac8de4f6cf
COc1ccc(B(O)O)cc1OC.O=C(NCCO)c1cccc(Br)n1>>COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC
OCCNC(=O)C1=NC(=CC=C1)Br.COC=1C=C(C=CC1OC)B(O)O.C(C)O.C(=O)([O-])[O-].[Na+].[Na+]>>OCCNC(=O)C1=NC(=CC=C1)C1=CC(=C(C=C1)OC)OC
OB(O)[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:20]([O:21][CH3:22])[cH:19]1.Br[c:7]1[cH:8][cH:9][cH:10][c:11]([C:12](=[O:13])[NH:14][CH2:15][CH2:16][OH:17])[n:18]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][c:11]([C:12](=[O:13])[NH:14][CH2:15][CH2:16][OH:17])[n:18]2)[cH:19][c:20]1[O:21][CH3:22]
COc1ccc(B(O)O)cc1OC.O=C(NCCO)c1cccc(Br)n1
COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC
null
[Pd].[Pd].C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1
COCCOC
C-C Coupling
Suzuki coupling with boronic acids
07e9b6e71d806aa92d4573f3838e77c7c8344de3e5d5735ebdb5fc6862ebf27d
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccccn2)cc1
Br-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]-[C:4](-[#7:5])=[O;D1;H0:6]):[c:7]:[c:8].O-B(-O)-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]>>[#7:5]-[C:4](=[O;D1;H0:6])-[c:3]:[#7;a:2]:[c;H0;D3;+0:1](-[c;H0;D3;+0:9](:[c:10]:[c:11]):[c:12]:[c:13]):[c:7]:[c:8]
69.5
[{"value": 69.0, "product": "OCCNC(=O)C1=NC(=CC=C1)C1=CC(=C(C=C1)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.5, "product": "OCCNC(=O)C1=NC(=CC=C1)C1=CC(=C(C=C1)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A quantity of 0.25 g (1.0 mmoles, 1 eq) of 6-bromo-pyridine-2-carboxylic acid (2-hydroxy-ethyl)-amide and 0.28 g (1.5 mmoles, 1.5 eq) of 3,4-dimethoxyphenyl boronic acid are added in 20 mL of ethylene glycol dimethyl ether with 2 ml of ethanol and 2 ml of 2 M Na2CO3. The mixture is purged with N2 for 20 minutes, and th...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccncc1
c1ccccc1.c1ccncc1
c1ccccc1.c1ccncc1
HBr.B
[Pd].[Pd].C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.COCCOC
80
null
COc1ccc(B(O)O)cc1OC.O=C(NCCO)c1cccc(Br)n1>[Pd].[Pd].C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.C(C1=CC=CC=C1)=CC(=O)C=CC1=CC=CC=C1.COCCOC>COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c0754a353ee9414ead2818ed353c537a
COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC>>COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC
OCCNC(=O)C1=NC(=CC=C1)C1=CC(=C(C=C1)OC)OC.Cl>>OCCNC(=O)C1NC(CCC1)C1=CC(=C(C=C1)OC)OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[cH:8][cH:9][cH:10][c:11]([C:12](=[O:13])[NH:14][CH2:15][CH2:16][OH:17])[n:18]2)[cH:19][c:20]1[O:21][CH3:22]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9][CH2:10][CH:11]([C:12](=[O:13])[NH:14][CH2:15][CH2:16][OH:17])[NH:18]2)[cH:19][c:20]1[O:21][CH3:22]
COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC
COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC
null
[Pt](=O)=O
C(C)O
Reduction
OtherReaction
8a6c78a63989dd47e282eb33ae5ce6bfcead5defaa210963e9125c31297ee886
2b7f370a519e29b4dede190aa36b37f30822496e32f2c8bfa9736e631bde52e2
c1ccc(C2CCCCN2)cc1
[C:1]-[#7:2]-[C:3](=[O;D1;H0:4])-[c;H0;D3;+0:5]1:[cH;D2;+0:6]:[cH;D2;+0:7]:[cH;D2;+0:8]:[c;H0;D3;+0:9](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14]):[n;H0;D2;+0:15]:1>>[C:1]-[#7:2]-[C:3](=[O;D1;H0:4])-[CH;D3;+0:5]1-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH;D3;+0:9](-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14])-...
null
[]
null
null
8
HOUR
A quantity of 3.0 g (10 mmoles, 1 eq) of 6-(3,4-dimethoxy-phenyl)-pyridine-2-carboxylic acid (2-hydroxy-ethyl)-amide and 0.23 g (1.0 mmoles, 0.1 eq) of platinum dioxide are added into 35 mL of ethanol and 2.0 ml concentrated HCl. The suspension is hydrogenated under 50 psi of H2 at room temperature overnight. After TLC...
10.6084/m9.figshare.5104873.v1
null
null
Secondary amine
c1ccncc1
C1CCNCC1
c1ccccc1.C1CCNCC1
null
[Pt](=O)=O.C(C)O
null
8
COc1ccc(-c2cccc(C(=O)NCCO)n2)cc1OC>[Pt](=O)=O.C(C)O>COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ba9af9d5a2b5441a870843b3f061c6cf
COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC>>COc1ccc(C2CCCC(CNCCO)N2)cc1OC
[O-]S(=O)(=O)[O-].[Mg+2].OCCNC(=O)C1NC(CCC1)C1=CC(=C(C=C1)OC)OC.[H-].[H-].[H-].[H-].[Li+].[Al+3].[OH-].[Na+]>>COC=1C=C(C=CC1OC)C1CCCC(N1)CNCCO
O=[C:12]([CH:11]1[CH2:10][CH2:9][CH2:8][CH:7]([c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:19]([O:20][CH3:21])[cH:18]2)[NH:17]1)[NH:13][CH2:14][CH2:15][OH:16]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9][CH2:10][CH:11]([CH2:12][NH:13][CH2:14][CH2:15][OH:16])[NH:17]2)[cH:18][c:19]1[O:20][CH3:21]
COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC
COc1ccc(C2CCCC(CNCCO)N2)cc1OC
null
null
O.C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccc(C2CCCCN2)cc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[C:4](-[C:5])-[#7:6]-[C:7]>>[C:5]-[C:4](-[CH2;D2;+0:1]-[#7:2]-[C:3])-[#7:6]-[C:7]
101.9
[{"value": 68.0, "product": "COC=1C=C(C=CC1OC)C1CCCC(N1)CNCCO", "details": "PERCENTYIELD", "is_desired": false}, {"value": 101.9, "product": "COC=1C=C(C=CC1OC)C1CCCC(N1)CNCCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
A solution of 1.5 g (5.0 mmoles, 1 eq) of 6-(3,4-Dimethoxy-phenyl)-piperidine-2-carboxylic acid (2-hydroxy-ethyl)-amide in 18 mL of THF is added slowly into 15 mL of 1 M LiAlH4 solution in THF. The reaction is heated at 60° C. under N2 for 6 hours. At that time there is no starting material shown on TLC. Cooled in ice ...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1.C1CCNCC1
Other
O.C1CCOC1
60
null
COc1ccc(C2CCCC(C(=O)NCCO)N2)cc1OC>O.C1CCOC1>COc1ccc(C2CCCC(CNCCO)N2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-854a1310fbdb40e5bb98d77d007479bf
CCOC(=O)N=NC(=O)OCC.COc1ccc(C2CCCC(CNCCO)N2)cc1OC>>COc1ccc(C2CCCC3CNCCN32)cc1OC.[NH4+].[OH-]
COC=1C=C(C=CC1OC)C1CCCC(N1)CNCCO.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.N(=NC(=O)OCC)C(=O)OCC>>[NH4+].[OH-].COC=1C=C(C=CC1OC)C1CCCC2N1CCNC2
CCOC(=O)[N:21]=NC(=O)[O:22]CC.O[CH2:15][CH2:14][NH:13][CH2:12][CH:11]1[CH2:10][CH2:9][CH2:8][CH:7]([c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:18]([O:19][CH3:20])[cH:17]2)[NH:16]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]2[CH2:8][CH2:9][CH2:10][CH:11]3[CH2:12][NH:13][CH2:14][CH2:15][N:16]23)[cH:17][c:18]1[O:19][CH3:20].[...
CCOC(=O)N=NC(=O)OCC.COc1ccc(C2CCCC(CNCCO)N2)cc1OC
COc1ccc(C2CCCC3CNCCN32)cc1OC.[NH4+].[OH-]
null
null
C1CCOC1
Heteroatom Alkylation and Arylation
OtherReaction
4cc975100256eeb284c00324f9d9c3705e02c5f7ff6f803641e3b753ac272f90
8613fd4fe042f0ebb8c19cdf4435b54eded2fa5b8cc5e22bd29bc67fc0f8b53e
c1ccc(C2CCCC3CNCCN32)cc1
C-C-O-C(=O)-[N;H0;D2;+0:1]=N-C(=O)-[O;H0;D2;+0:2]-C-C.O-[CH2;D2;+0:3]-[C:4]-[#7:5]-[C:6]-[C:7](-[C:8])-[NH;D2;+0:9]-[C:10](-[c:11])-[C:12]>>[C:8]-[C:7]1-[C:6]-[#7:5]-[C:4]-[CH2;D2;+0:3]-[N;H0;D3;+0:9]-1-[C:10](-[c:11])-[C:12].[NH4+;D0:1].[OH-;D0:2]
27
[{"value": 27.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
To the solution of 3.4 g (11.6 mmoles, 1 eq) of 2-{[6-(3,4-dimethoxy-phenyl)-piperidin-2-ylmethyl]-amino}-ethanol and 0.20 g (17.5 mmoles, 1.5 eq) of triphenyl phosphine in 120 mL of THF, is added 1.9 mL (12.7 mmoles, 1.1 eq) of diethyl azodicarboxylate, and the reaction is stirred at room temperature overnight. At tha...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Diazene.Primary alcohol.Secondary amine
Tertiary amine
C1CCNCC1
C1CCN2CCNCC2C1
c1ccccc1.C1CCN2CCNCC2C1
HO-
C1CCOC1
null
8
CCOC(=O)N=NC(=O)OCC.COc1ccc(C2CCCC(CNCCO)N2)cc1OC>C1CCOC1>COc1ccc(C2CCCC3CNCCN32)cc1OC.[NH4+].[OH-]
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-913878cf886e4fed88af97f8d493ec75
COc1cc(Br)ccc1Cl.COc1ccc(C2CCCC3CNCCN32)cc1OC>>COc1cc(N2CCN3C(CCCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
COC=1C=C(C=CC1OC)C1CCCC2N1CCNC2.BrC=1C=CC(=C(C1)OC)Cl.CC(C)([O-])C.[K+]>>ClC1=C(C=C(C=C1)N1CC2N(CC1)C(CCC2)C2=CC(=C(C=C2)OC)OC)OC
Br[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:28]([Cl:29])[cH:27][cH:26]1.[NH:6]1[CH2:7][CH2:8][N:9]2[CH:10]([CH2:11][CH2:12][CH2:13][CH:14]2[c:15]2[cH:16][cH:17][c:18]([O:19][CH3:20])[c:21]([O:22][CH3:23])[cH:24]2)[CH2:25]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][N:9]3[CH:10]([CH2:11][CH2:12][CH2:13][CH:14]3[c:15]3[...
COc1cc(Br)ccc1Cl.COc1ccc(C2CCCC3CNCCN32)cc1OC
COc1cc(N2CCN3C(CCCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
null
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd]
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
42bc18fc6e327c51abf0c17c233ad0e8e8c69664054ccc1eec7570fa43a2138e
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(C2CCCC3CN(c4ccccc4)CCN32)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[#7:6]1-[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[#7:6]-[C:11]-[C:10]-1):[c:4]:[c:5]
68
[{"value": 68.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A quantity of 0.85 g (3.0 mmoles, 1 eq) of 6-(3,4-dimethoxy-phenyl)-octahydropyrido[1,2-a]pyrazine and 0.76 g (3.4 mmoles, 1.1 eq) of 5-bromo-2-chloro-anisole is dissolved in 25 mL of anhydrous toluene, and the solution is purged with N2 for 20 min. To the solution is added 0.18 g (0.30 mmoles, 0.10 eq) of rac-2, 2′-Bi...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1.C1CCN2CCNCC2C1
c1ccccc1.C1CCN2CC[NH]CC2C1
c1ccccc1.C1CCN2CC[NH]CC2C1.c1ccccc1
HBr
C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C
80
null
COc1cc(Br)ccc1Cl.COc1ccc(C2CCCC3CNCCN32)cc1OC>C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.C=1C=CC(=CC1)/C=C/C(=O)/C=C/C2=CC=CC=C2.[Pd].[Pd].C1(=CC=CC=C1)C>COc1cc(N2CCN3C(CCCC3c3ccc(OC)c(OC)c3)C2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-302383b5d1ae466490342ab67ce79b14
BrCc1ccccc1.CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)O>>CC(C)(C)OC(=O)N1C(=O)CCC1C(=O)OCc1ccccc1
C(C)(C)(C)OC(=O)N1[C@@H](CCC1=O)C(=O)O.C(C1=CC=CC=C1)Br.C([O-])([O-])=O.[K+].[K+]>>C(C)(C)(C)OC(=O)N1C(CCC1=O)C(=O)OCC1=CC=CC=C1
Br[CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1.[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[C:9](=[O:10])[CH2:11][CH2:12][C@H:13]1[C:14](=[O:15])[OH:16]>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[N:8]1[C:9](=[O:10])[CH2:11][CH2:12][CH:13]1[C:14](=[O:15])[O:16][CH2:17][c:18]1[cH:19][cH:20][cH:21]...
BrCc1ccccc1.CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)O
CC(C)(C)OC(=O)N1C(=O)CCC1C(=O)OCc1ccccc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
O=C1CCC(C(=O)OCc2ccccc2)N1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]-[C:6]-[C:7](=[O;D1;H0:8])-[OH;D1;+0:9]>>[#7:5]-[C:6]-[C:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
59.1
[{"value": 59.0, "product": "C(C)(C)(C)OC(=O)N1C(CCC1=O)C(=O)OCC1=CC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 59.1, "product": "C(C)(C)(C)OC(=O)N1C(CCC1=O)C(=O)OCC1=CC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
65
CELSIUS
8
HOUR
A suspension containing (2S)5-oxo-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (10.00 g, 0.044 mol, 1.0 equivalent), benzyl bromide (7.88 g, 0.046 mol, 1.05 equivalents), and potassium carbonate (15.20 g, 0.11 mol, 2.5 equivalents) in DMF (200 ml) was allowed to stir at 65° C. overnight. The reaction was allowe...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
C1CC[NH]C1.c1ccccc1
HBr
CN(C)C=O
65
8
BrCc1ccccc1.CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)O>CN(C)C=O>CC(C)(C)OC(=O)N1C(=O)CCC1C(=O)OCc1ccccc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-89129204560a4d65af30a3ddcfdac19d
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)OCc1ccccc1.COc1cc[c]([Mg][Br])cc1OC>>COc1ccc(C(=O)CCC(NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC
COC=1C=C(C=CC1OC)[Mg]Br.C(C)(C)(C)OC(=O)N1[C@@H](CCC1=O)C(=O)OCC1=CC=CC=C1>>C(C1=CC=CC=C1)OC(C(CCC(=O)C1=CC(=C(C=C1)OC)OC)NC(=O)OC(C)(C)C)=O
[C:7]1(=[O:8])[CH2:9][CH2:10][C@@H:11]([C:20](=[O:21])[O:22][CH2:23][c:24]2[cH:25][cH:26][cH:27][cH:28][cH:29]2)[N:12]1[C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19].[Br][Mg][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:31]([O:32][CH3:33])[cH:30]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][CH:...
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)OCc1ccccc1.COc1cc[c]([Mg][Br])cc1OC
COc1ccc(C(=O)CCC(NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC
null
null
C1CCOC1
C-C Coupling
OtherReaction
080c2b43d0a0b8f931d6213b8b72dc78f67fa8812b391d600ecdd636d8f3d301
9f2c6224204fc882d6f480ccf7ad879a9274e7067e43b7e1ce90a3411c5ff012
O=C(CCCC(=O)c1ccccc1)OCc1ccccc1
[Br]-[Mg]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[C@@H;D3;+0:10]1-[C:11]-[C:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[N;H0;D3;+0:15]-1-[C:16](=[O;D1;H0:17])-[#8:18]-[C:19](-[C;D1;H3:20])(-[C;D1;H3:21])-[C;D1;H3:22]>>[C:6]-[#8:7]-[C:8](=[O;D1;H0:9])-[CH;D3;+0:10](-[C:11]-[C:12]-[C;H0;D3;+0:1...
88
[{"value": 88.0, "product": "C(C1=CC=CC=C1)OC(C(CCC(=O)C1=CC(=C(C=C1)OC)OC)NC(=O)OC(C)(C)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
A solution of (2S)5-oxo-pyrrolidine-1,2-dicarboxylic acid 2-benzyl ester 1-tert-butyl ester (8.20 g, 0.026 mol, 1.0 equivalent) in anhydrous THF was cooled to 0° C. in an ice bath under N2. A chilled 0.5M solution of 3,4-dimethoxyphenylmagnesium bromide in THF (52.1 mL, 0.026 mol, 1.0 equivalent) was slowly added. The ...
10.6084/m9.figshare.5104873.v1
null
Magnesium halide.Carbamic ester.Substituted dicarboximide
Carbamic ester.Ketone
C1CC[NH]C1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
Br-.Mg
C1CCOC1
null
2
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1C(=O)OCc1ccccc1.COc1cc[c]([Mg][Br])cc1OC>C1CCOC1>COc1ccc(C(=O)CCC(NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-88e5f4886b544106b08fb0d1153cf862
COc1ccc(C(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC>>COc1ccc(C2=N[C@H](C(=O)OCc3ccccc3)CC2)cc1OC
C(C1=CC=CC=C1)OC([C@H](CCC(=O)C1=CC(=C(C=C1)OC)OC)NC(=O)OC(C)(C)C)=O.C(=O)(C(F)(F)F)O>>OC(=O)C(F)(F)F.C(C1=CC=CC=C1)OC(=O)[C@H]1N=C(CC1)C1=CC(=C(C=C1)OC)OC
CC(C)(C)OC(=O)[NH:8][C@H:9]([C:10](=[O:11])[O:12][CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[CH2:20][CH2:21][C:7](=O)[c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:23]([O:24][CH3:25])[cH:22]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([C:7]2=[N:8][C@H:9]([C:10](=[O:11])[O:12][CH2:13][c:14]3[cH:15][cH:16][cH:17][cH:18][cH:1...
COc1ccc(C(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC
COc1ccc(C2=N[C@H](C(=O)OCc3ccccc3)CC2)cc1OC
null
null
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
bf06db3989591852ea9db145104dbc3920fa3e3bda459d735b6db3b71960304d
e05aa79ef606717adc4e7888ef27556c844e93bba271333333a92976508744aa
O=C(OCc1ccccc1)[C@@H]1CCC(c2ccccc2)=N1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3]-[C:4]-[C;H0;D3;+0:5](=O)-[c:6](:[c:7]):[c:8])-[C:9](=[O;D1;H0:10])-[#8:11]-[C:12]>>[C:12]-[#8:11]-[C:9](=[O;D1;H0:10])-[C:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](-[c:6](:[c:7]):[c:8])=[N;H0;D2;+0:1]-1
91
[{"value": 91.0, "product": "OC(=O)C(F)(F)F.C(C1=CC=CC=C1)OC(=O)[C@H]1N=C(CC1)C1=CC(=C(C=C1)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of (2S)2-tert-butoxycarbonylamino-5-(3,4-dimethoxy-phenyl)-5-oxo-pentanoic acid benzyl ester (10.46 g, 0.023 mol) in dichloromethane (150 ml) was cooled to 0° C. in an ice bath. TFA (40 ml) was slowly added to the stirring mixture and the reaction was allowed to warm to room temperature over two hours. The r...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ketone.Ether.Boc
Substituted imine
null
C1=NCCC1
c1ccccc1.C1=NCCC1.c1ccccc1
HO-
ClCCl
null
null
COc1ccc(C(=O)CC[C@H](NC(=O)OC(C)(C)C)C(=O)OCc2ccccc2)cc1OC>ClCCl>COc1ccc(C2=N[C@H](C(=O)OCc3ccccc3)CC2)cc1OC
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-82d2100e72634c39bb308f04cdedd33c
COc1cc(N)ccc1Cl.COc1ccc([C@H]2CC[C@@H](C(=O)O)N2C(=O)OC(C)(C)C)cc1OC>>COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2C(=O)OC(C)(C)C)ccc1Cl
C(C)(C)(C)OC(=O)N1[C@@H](CC[C@@H]1C1=CC(=C(C=C1)OC)OC)C(=O)O.ClC1=C(C=C(N)C=C1)OC.CCN(C(C)C)C(C)C.C1CCN(C1)[P+](N2CCCC2)(N3CCCC3)Br.F[P-](F)(F)(F)(F)F>>C(C)(C)(C)OC(=O)N1[C@@H](CC[C@@H]1C1=CC(=C(C=C1)OC)OC)C(NC1=CC(=C(C=C1)Cl)OC)=O
[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[cH:31][cH:32][c:33]1[Cl:34].O[C:7](=[O:8])[C@@H:9]1[CH2:10][CH2:11][C@H:12]([c:13]2[cH:14][cH:15][c:16]([O:17][CH3:18])[c:19]([O:20][CH3:21])[cH:22]2)[N:23]1[C:24](=[O:25])[O:26][C:27]([CH3:28])([CH3:29])[CH3:30]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][C:7](=[O:8])[C@@H:9]2[CH2:10][...
COc1cc(N)ccc1Cl.COc1ccc([C@H]2CC[C@@H](C(=O)O)N2C(=O)OC(C)(C)C)cc1OC
COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2C(=O)OC(C)(C)C)ccc1Cl
null
null
ClCCl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1ccccc1)[C@@H]1CC[C@H](c2ccccc2)N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:13].[NH2;D1;+0:14]-[c:15](:[c:16]):[c:17]>>[C:4]-[C:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:14]-[c:15](:[c:16]):[c:17])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H...
100
[{"value": 100.0, "product": "C(C)(C)(C)OC(=O)N1[C@@H](CC[C@@H]1C1=CC(=C(C=C1)OC)OC)C(NC1=CC(=C(C=C1)Cl)OC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.7, "product": "C(C)(C)(C)OC(=O)N1[C@@H](CC[C@@H]1C1=CC(=C(C=C1)OC)OC)C(NC1=CC(=C(C=C1)Cl)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired"...
null
null
8
HOUR
A solution of (2S,5R)5-(3,4-dimethoxy-phenyl)-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (2.50 g, 7.11 mmol, 1.0 equivalent), 4-chloro-3-methoxyaniline (1.12 g, 7.11 mmol, 1.0 equivalent), PyBrop coupling reagent (3.98 g, 8.54 mmol, 1.2 equivalents), and DIEA (1.86 ml, 10.7 mmol, 1.5 equivalents) in dichlorom...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.C1CC[NH]C1.c1ccccc1
HO-
ClCCl
null
8
COc1cc(N)ccc1Cl.COc1ccc([C@H]2CC[C@@H](C(=O)O)N2C(=O)OC(C)(C)C)cc1OC>ClCCl>COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2C(=O)OC(C)(C)C)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-be5af26909e14ae8ae732c45c2af424c
COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2)ccc1Cl>>COc1cc(NC[C@@H]2CC[C@H](C3=CC=CC(OC)(OC)C3)N2)ccc1Cl
ClC1=C(C=C(C=C1)NC(=O)[C@H]1N[C@H](CC1)C1=CC(=C(C=C1)OC)OC)OC.C1CCOC1.C1(=CC=CC=C1)C>>ClC1=C(C=C(C=C1)NC[C@H]1N[C@H](CC1)C=1CC(C=CC1)(OC)OC)OC
O=[C:7]([NH:6][c:5]1[cH:4][c:3]([O:2][CH3:1])[c:25]([Cl:26])[cH:24][cH:23]1)[C@@H:8]1[CH2:9][CH2:10][C@H:11]([c:12]2[cH:13][cH:14][c:15]([O:17][CH3:18])[c:16]([O:19][CH3:20])[cH:21]2)[NH:22]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH:6][CH2:7][C@@H:8]2[CH2:9][CH2:10][C@H:11]([C:12]3=[CH:13][CH:14]=[CH:15][C:16]([O:17][CH3:18]...
COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2)ccc1Cl
COc1cc(NC[C@@H]2CC[C@H](C3=CC=CC(OC)(OC)C3)N2)ccc1Cl
null
null
null
Reduction
OtherReaction
42907729ce9539517327a3317ef865152d70eb13b6298dab79a9f19adb21a369
6113d4b86087fc72521fab67142160242079f55ebd915b93533d21ea0c3fe1be
C1=CCCC([C@H]2CC[C@@H](CNc3ccccc3)N2)=C1
O=[C;H0;D3;+0:1](-[#7:2]-[c:3])-[C:4]1-[#7:5]-[C:6](-[c;H0;D3;+0:7]2:[cH;D2;+0:8]:[cH;D2;+0:9]:[c;H0;D3;+0:10](-[O;H0;D2;+0:11]-[C;D1;H3:12]):[c;H0;D3;+0:13](-[#8:14]-[C;D1;H3:15]):[cH;D2;+0:16]:2)-[C:17]-[C:18]-1>>[C;D1;H3:12]-[O;H0;D2;+0:11]-[C;H0;D4;+0:13]1(-[#8:14]-[C;D1;H3:15])-[CH2;D2;+0:16]-[C;H0;D3;+0:7](-[C:6]...
67
[{"value": 67.0, "product": "ClC1=C(C=C(C=C1)NC[C@H]1N[C@H](CC1)C=1CC(C=CC1)(OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
(2S,5R)5-(3,4-Dimethoxy-phenyl)-pyrrolidine-2-carboxylic acid (4-chloro-3-methoxy-phenyl)-amide was dissolved in anhydrous THF and cooled to 0° C. in an ice bath. A 0.5M solution of alane complex in toluene (42.6 ml, 21.3 mmol, 3.0 equivalents) was added slowly and the reaction was allowed to stir and warm to room temp...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Secondary amide
Ether.Ether.Conjugated diene
c1ccccc1
C1=CCCC=C1
c1ccccc1.C1CCNC1.C1=CCCC=C1
Other
null
0
null
COc1cc(NC(=O)[C@@H]2CC[C@H](c3ccc(OC)c(OC)c3)N2)ccc1Cl>>COc1cc(NC[C@@H]2CC[C@H](C3=CC=CC(OC)(OC)C3)N2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-52a4e43096c64d72824bb0f4146df619
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(C=O)c(C)c1C>>COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C
CC1=C(C=O)C=CC(=C1C)OC.C(C)(C)(C)OC(=O)N1CCNCC1.N1N=NC2=C1C=CC=C2.C[Mg]Br>>C(C)(C)(C)OC(=O)N1CCN(CC1)C(C)C1=C(C(=C(C=C1)OC)C)C
[NH:9]1[CH2:10][CH2:11][N:12]([C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19])[CH2:20][CH2:21]1.O=[CH:7][c:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:24]([CH3:25])[c:22]1[CH3:23]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([CH3:8])[N:9]2[CH2:10][CH2:11][N:12]([C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19])[C...
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(C=O)c(C)c1C
COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
7a1842565a3c73c1d6bba5dccafef60d48e9eaf6e4a0871f60e828bcbdf26fb1
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc(CN2CCNCC2)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[#7:5]1-[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]-1>>[C;D1;H3:11]-[CH;D3;+0:1](-[N;H0;D3;+0:8]1-[C:7]-[C:6]-[#7:5]-[C:10]-[C:9]-1)-[c:2](:[c:3]):[c:4]
56
[{"value": 56.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
A mixture of 2,3-dimethyl 4-methoxy benzaldehyde (1 g, 3.05 mmol), 1 equivalent of piperazine-1-carboxylic acid tert-butyl ester (0.57 g, 3.05 mmol), 1 equivalent of benzotriazole in ethanol was stirred at room temperature for 30 minutes. The solvent was removed and the reaction was dried under vacuum. The reaction mix...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
C1CNCC[NH]1
C1C[NH]CC[NH]1
c1ccccc1.C1C[NH]CC[NH]1
null
C(C)O
null
0.5
CC(C)(C)OC(=O)N1CCNCC1.COc1ccc(C=O)c(C)c1C>C(C)O>COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fee3f409c19c4c92bf946efbde3c383f
COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C>>COc1ccc(C(C)N2CCNCC2)c(C)c1C
C(C)(C)(C)OC(=O)N1CCN(CC1)C(C)C1=C(C(=C(C=C1)OC)C)C.FC(C(=O)O)(F)F>>COC1=C(C(=C(C=C1)C(C)N1CCNCC1)C)C
CC(C)(C)OC(=O)[N:12]1[CH2:11][CH2:10][N:9]([CH:7]([c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[c:17]([CH3:18])[c:15]2[CH3:16])[CH3:8])[CH2:14][CH2:13]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH:7]([CH3:8])[N:9]2[CH2:10][CH2:11][NH:12][CH2:13][CH2:14]2)[c:15]([CH3:16])[c:17]1[CH3:18]
COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C
COc1ccc(C(C)N2CCNCC2)c(C)c1C
null
null
ClCCl
Reduction
Boc amine deprotection
2c25e19aee181a3c5131cfdfda27035fd54d4379a11d745dfb75d386bacfd500
a94b29c7264c852156fc1cdd4a0951a4fc26c06d0edc9e50c743825dbf79e3fd
c1ccc(CN2CCNCC2)cc1
C-C(-C)(-C)-O-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-[C:6]-1>>[#7:4]1-[C:3]-[C:2]-[NH;D2;+0:1]-[C:6]-[C:5]-1
null
[]
null
null
2
HOUR
To an ice chilled solution containing 4-[1-(4-methoxy-2,3-dimethyl-phenyl)-ethyl]-piperazine-1-carboxylic acid tert-butyl ester (0.4 g 1.38 mmol) and 10 ml dichloromethane, was added trifluoroacetic acid (2 ml) dropwise. The reaction was stirred at room temperature for 2 hours. The reaction was concentrated. The residu...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Secondary amine
C1C[NH]CC[NH]1
C1C[NH]CCN1
c1ccccc1.C1C[NH]CCN1
HO-
ClCCl
null
2
COc1ccc(C(C)N2CCN(C(=O)OC(C)(C)C)CC2)c(C)c1C>ClCCl>COc1ccc(C(C)N2CCNCC2)c(C)c1C
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-24de49017a5a42adad724ff1a71c63b1
COc1cc(N2C[C@@H]3CC[C@@H](c4ccc(OC)c(OC)c4)N3C(=O)C2=O)ccc1Cl>>COc1cc(N2CCN3[C@H](CC[C@H]3c3ccc(OC)c(OC)c3)C2)ccc1Cl
ClC1=C(C=C(C=C1)N1C[C@H]2N(C(C1=O)=O)[C@@H](CC2)C2=CC(=C(C=C2)OC)OC)OC.B.C1CCOC1.CO>>ClC1=C(C=C(C=C1)N1C[C@@H]2N(CC1)[C@@H](CC2)C2=CC(=C(C=C2)OC)OC)OC
O=[C:7]1[N:6]([c:5]2[cH:4][c:3]([O:2][CH3:1])[c:27]([Cl:28])[cH:26][cH:25]2)[CH2:24][C@H:10]2[N:9]([C:8]1=O)[C@H:13]([c:14]1[cH:15][cH:16][c:17]([O:18][CH3:19])[c:20]([O:21][CH3:22])[cH:23]1)[CH2:12][CH2:11]2>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N:6]2[CH2:7][CH2:8][N:9]3[C@H:10]([CH2:11][CH2:12][C@H:13]3[c:14]3[cH:15][cH:16...
COc1cc(N2C[C@@H]3CC[C@@H](c4ccc(OC)c(OC)c4)N3C(=O)C2=O)ccc1Cl
COc1cc(N2CCN3[C@H](CC[C@H]3c3ccc(OC)c(OC)c3)C2)ccc1Cl
null
null
C1CCOC1
Reduction
OtherReaction
c92b2334b2d0c93d61ecf7829bb0b5a5e6074a5d300a1b627ba002642a5dcc3f
872327d0f5317db5811f770a2ef4e16f48610c72bf7cae5526f2a2a33aa26523
c1ccc([C@@H]2CC[C@@H]3CN(c4ccccc4)CCN32)cc1
O=[C;H0;D3;+0:1]1-[#7:2](-[c:3])-[C:4]-[C:5]-[#7:6](-[C:7])-[C;H0;D3;+0:8]-1=O>>[C:7]-[#7:6]1-[C:5]-[C:4]-[#7:2](-[c:3])-[CH2;D2;+0:1]-[CH2;D2;+0:8]-1
30.9
[{"value": 30.9, "product": "ClC1=C(C=C(C=C1)N1C[C@@H]2N(CC1)[C@@H](CC2)C2=CC(=C(C=C2)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.9, "product": "ClC1=C(C=C(C=C1)N1C[C@@H]2N(CC1)[C@@H](CC2)C2=CC(=C(C=C2)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
(±)-cis-2-(4-Chloro-3-methoxy-phenyl)-6-(3,4-dimethoxy-phenyl)-hexahydro-pyrrolo[1,2-a]pyrazine-3,4-dione (49.7 mg, 0.115 mmol) was dissolved in dry THF (10 mL) and BH3.THF (1 mL, 1 mmol) was added dropwise to the mixture, which was then heated at reflux overnight. The solution was cooled to 0° C. and MeOH (2 mL) was a...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
null
C1C[C@H]2C[NH]CCN2C1
C1C[C@@H]2C[NH]CCN2C1
c1ccccc1.C1C[C@@H]2C[NH]CCN2C1.c1ccccc1
Other
C1CCOC1
0
null
COc1cc(N2C[C@@H]3CC[C@@H](c4ccc(OC)c(OC)c4)N3C(=O)C2=O)ccc1Cl>C1CCOC1>COc1cc(N2CCN3[C@H](CC[C@H]3c3ccc(OC)c(OC)c3)C2)ccc1Cl
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8deb4794e9dc40f1ab3e81c5e63b38a3
Nc1cc2cn[nH]c2cc1Cl.O=C(O)c1ccccc1NCc1ccncc1>>O=C(Nc1cc2cn[nH]c2cc1Cl)c1ccccc1NCc1ccncc1
CN1CCOCC1.F[P-](F)(F)(F)(F)F.N1(N=NC2=C1N=CC=C2)OC(=[N+](C)C)N(C)C.N1=CC=C(C=C1)CNC1=C(C(=O)O)C=CC=C1.NC=1C=C2C=NNC2=CC1Cl>>ClC1=C(C=C2C=NNC2=C1)NC(C1=C(C=CC=C1)NCC1=CC=NC=C1)=O
[NH2:3][c:4]1[cH:5][c:6]2[cH:7][n:8][nH:9][c:10]2[cH:11][c:12]1[Cl:13].O[C:2](=[O:1])[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[NH:20][CH2:21][c:22]1[cH:23][cH:24][n:25][cH:26][cH:27]1>>[O:1]=[C:2]([NH:3][c:4]1[cH:5][c:6]2[cH:7][n:8][nH:9][c:10]2[cH:11][c:12]1[Cl:13])[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[NH:20][CH...
Nc1cc2cn[nH]c2cc1Cl.O=C(O)c1ccccc1NCc1ccncc1
O=C(Nc1cc2cn[nH]c2cc1Cl)c1ccccc1NCc1ccncc1
null
null
O.CN(C=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(Nc1ccc2[nH]ncc2c1)c1ccccc1NCc1ccncc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH2;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[c:3](:[c:4]):[c:5]
30.2
[{"value": 30.2, "product": "ClC1=C(C=C2C=NNC2=C1)NC(C1=C(C=CC=C1)NCC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 30.2, "product": "ClC1=C(C=C2C=NNC2=C1)NC(C1=C(C=CC=C1)NCC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
194 mg (0.85 mmol) of 2-(4-pyridylmethyl)aminobenzoic acid is mixed in 8 ml of dimethylformamide with 283 mg (1.69 mmol) of 5-amino-6-chloroindazole. Under argon and in a moisture-free environment, 215 mg (2.13 mmol) of N-methylmorpholine and 386 mg (1.02 mmol) of O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium h...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2n[nH]cc2c1.c1ccccc1.c1ccncc1
HO-
O.CN(C=O)C
null
4
Nc1cc2cn[nH]c2cc1Cl.O=C(O)c1ccccc1NCc1ccncc1>O.CN(C=O)C>O=C(Nc1cc2cn[nH]c2cc1Cl)c1ccccc1NCc1ccncc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-872a222fc12d4d10aafedfb92c226363
ClCCBr.Oc1ccc2ccccc2c1>>ClCCOc1ccc2ccccc2c1
C1=C(C=CC2=CC=CC=C12)O.C(=O)([O-])[O-].[K+].[K+].BrCCCl>>C1=C(C=CC2=CC=CC=C12)OCCCl
Br[CH2:3][CH2:2][Cl:1].[OH:4][c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[cH:14]1>>[Cl:1][CH2:2][CH2:3][O:4][c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c:13]2[cH:14]1
ClCCBr.Oc1ccc2ccccc2c1
ClCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2ccccc2c1
Br-[CH2;D2;+0:1]-[C:2]-[Cl;D1;H0:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[Cl;D1;H0:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A mixture of β-naphthol (1 gm, 0.006 mole), anhydrous K2CO3 (10 gm, in excess) and 1-bromo-2-chloroethane (0.6 ml, 0.006 mole) was refluxed in dry acetone (50 ml) for 6 hours. Reaction mixture was filtered and filtrate was concentrated to get oily compound, which was crystallized with benzene-hexane to give the colorle...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2ccccc2c1
HBr
CC(=O)C
null
null
ClCCBr.Oc1ccc2ccccc2c1>CC(=O)C>ClCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-334d3d2c74964efbacc5b02732ba8a8a
ClCCCBr.Oc1ccc2ccccc2c1>>ClCCCOc1ccc2ccccc2c1
C1=C(C=CC2=CC=CC=C12)O.C(=O)([O-])[O-].[K+].[K+].BrCCCCl>>C1=C(C=CC2=CC=CC=C12)OCCCCl
Br[CH2:4][CH2:3][CH2:2][Cl:1].[OH:5][c:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1>>[Cl:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1
ClCCCBr.Oc1ccc2ccccc2c1
ClCCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2ccccc2c1
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]
null
[]
null
null
null
null
A mixture of β-naphthol (1 gm, 0.006 mole), anhydrous K2CO3 (10 gm, in excess) and 1-bromo-3-chloropropane (0.7 ml, 0.006 mole) was refluxed in dry acetone (50 ml) for 6 hours. Reaction mixture was filtered and filtrate was concentrated to get oily compound which was crystallized with benzene-hexane to give the colorle...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2ccccc2c1
HBr
CC(=O)C
null
null
ClCCCBr.Oc1ccc2ccccc2c1>CC(=O)C>ClCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-75b4cf608c3c4ee085a72555b323ce4b
ClCCCCBr.Oc1ccc2ccccc2c1>>ClCCCCOc1ccc2ccccc2c1
C1=C(C=CC2=CC=CC=C12)O.C(=O)([O-])[O-].[K+].[K+].BrCCCCCl>>C1=C(C=CC2=CC=CC=C12)OCCCCCl
Br[CH2:5][CH2:4][CH2:3][CH2:2][Cl:1].[OH:6][c:7]1[cH:8][cH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[cH:16]1>>[Cl:1][CH2:2][CH2:3][CH2:4][CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[cH:16]1
ClCCCCBr.Oc1ccc2ccccc2c1
ClCCCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccc2ccccc2c1
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]
null
[]
null
null
null
null
A mixture of β-naphthol (1gm, 0.006 mole), anhydrous K2CO3 (10 gm, in excess) and 1-bromo 4-chlorobutane (0.8 ml, 0.006 mole) was refluxed in dry acetone (50 ml) for 6 hours. Reaction mixture was filtered and filtrate was concentrated to get oily compound, which was crystallized with benzene-hexane to give the colorles...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2ccccc2c1
HBr
CC(=O)C
null
null
ClCCCCBr.Oc1ccc2ccccc2c1>CC(=O)C>ClCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c27f54bad9cb44dea52e951ac239cabf
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].COC1=CC=C(C=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:22][cH:23]1.Cl[CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][cH:23]1
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and p-anisidine (0.42 gm, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0c6366e473ff4c269f7ad5920603d475
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].COC1=CC=C(C=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:22][cH:23]1.Cl[CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][cH:23]1
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
null
null
O.CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and p-anisidine (0.42 gm, 0.003 mole) was taken in dry DMF (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mixt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CN(C)C=O
140
null
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>O.CN(C)C=O>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8297a3a940124a04810cb043346523bc
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>NCCCOc1ccc2ccccc2c1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.C(CC)Br>>C1=C(C=CC2=CC=CC=C12)OCCCN
COc1ccc([NH:1][CH2:2][CH2:3][CH2:4][O:5][c:6]2[cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[cH:15]2)cc1>>[NH2:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
NCCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Reduction
OtherReaction
bd6cc2ddd30b209c36eb43f9e2d163a4da40f8a48bda8b578aa13caf5d4fe5dd
79272555d5bd71219cf9e8b42c4ac12a30bbf383c58cfbccf49a5a990e3653c1
c1ccc2ccccc2c1
C-O-c1:c:c:c(-[NH;D2;+0:1]-[C:2]-[C:3]):c:c:1>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A mixture of N-(4-methoxyphenyl)-[3-(naphthalen-2-yloxy)propyl]amine (0.5 gm, 0.002 mole) and propyl bromide (0.54ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 12 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get oily compound...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Primary amine
c1ccccc1
null
c1ccc2ccccc2c1
HO-
CC(=O)C
null
null
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>NCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6aa15b9e0d5e4d5689c8e3e7869b00d6
ClCCOc1ccc2ccccc2c1.NCc1ccccc1>>c1ccc(CNCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>C(C1=CC=CC=C1)NCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[cH:20][cH:21]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][O:9][c:10]2[cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[cH:19]2)[cH:20][cH:21]1
ClCCOc1ccc2ccccc2c1.NCc1ccccc1
c1ccc(CNCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CNCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[NH2;D1;+0:4]-[C:5]-[c:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[C:5]-[c:6]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and benzyl amine (0.38 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
ClCCOc1ccc2ccccc2c1.NCc1ccccc1>O.CS(=O)C>c1ccc(CNCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-fc70e18baee047c6b3a9f591ed865c1a
COc1ccc(N)cc1.ClCCOc1ccc2ccccc2c1>>COc1ccc(NCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].COC1=CC=C(C=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>COC1=CC=C(C=C1)NCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:21][cH:22]1.Cl[CH2:8][CH2:9][O:10][c:11]1[cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[cH:20]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[cH:20]2)[cH:21][cH:22]1
COc1ccc(N)cc1.ClCCOc1ccc2ccccc2c1
COc1ccc(NCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
145
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and p-anisidine (0.45 gm, 0.003 mole) was taken in dry dimethylsulphoxide (DMSO, 40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 145° C. for 7 hrs. The reaction was completed as checked by T...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
145
null
COc1ccc(N)cc1.ClCCOc1ccc2ccccc2c1>O.CS(=O)C>COc1ccc(NCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-a0ba771660de423884499ae8eb049417
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].COC1=CC=C(C=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:22][cH:23]1.Cl[CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][cH:23]1
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
135
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and p-anisidine (0.42 gm, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 135° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
135
null
COc1ccc(N)cc1.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c1e4717643944f04b05d68febe48cea9
COc1ccc(N)cc1.ClCCCCOc1ccc2ccccc2c1>>COc1ccc(NCCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].COC1=CC=C(C=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>COC1=CC=C(C=C1)NCCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH2:7])[cH:23][cH:24]1.Cl[CH2:8][CH2:9][CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[cH:22]2...
COc1ccc(N)cc1.ClCCCCOc1ccc2ccccc2c1
COc1ccc(NCCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(NCCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
null
[]
130
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and p-anisidine (0.4 gm, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 130° C. for 7 hrs. and the reaction was completed as checked by TLC. Reaction mixt...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
130
null
COc1ccc(N)cc1.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>COc1ccc(NCCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-3b5dae56ffa342f4b1bec6b0e9c69b52
ClCCOc1ccc2ccccc2c1.NCc1ccccc1>>c1ccc(CNCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>C(C1=CC=CC=C1)NCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[cH:20][cH:21]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][O:9][c:10]2[cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]3[cH:19]2)[cH:20][cH:21]1
ClCCOc1ccc2ccccc2c1.NCc1ccccc1
c1ccc(CNCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CNCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[NH2;D1;+0:4]-[C:5]-[c:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[C:5]-[c:6]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and benzyl amine (0.38 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
ClCCOc1ccc2ccccc2c1.NCc1ccccc1>O.CS(=O)C>c1ccc(CNCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6ad4f3d5f1eb4c0894cae60ad0a95936
ClCCCOc1ccc2ccccc2c1.NCc1ccccc1>>c1ccc(CNCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(C1=CC=CC=C1)NCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:7][CH2:8][CH2:9][O:10][c:11]1[cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[cH:20]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[cH:21][cH:22]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][CH2:9][O:10][c:11]2[cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]3[cH:20]2)[cH:21][cH:22]1
ClCCCOc1ccc2ccccc2c1.NCc1ccccc1
c1ccc(CNCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CNCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[C:5]-[c:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[C:5]-[c:6]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and benzyl amine (0.36 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 6 hrs. and the reaction was completed as checked by TLC. Reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
ClCCCOc1ccc2ccccc2c1.NCc1ccccc1>O.CS(=O)C>c1ccc(CNCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ede520b1da234a4faea4ad902d89bfcb
ClCCCCOc1ccc2ccccc2c1.NCc1ccccc1>>c1ccc(CNCCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(C1=CC=CC=C1)NCCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[cH:22][cH:23]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][c...
ClCCCCOc1ccc2ccccc2c1.NCc1ccccc1
c1ccc(CNCCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CNCCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[NH2;D1;+0:4]-[C:5]-[c:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:4]-[C:5]-[c:6]
null
[]
150
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and benzylamine (0.34 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 150° C. for 5 hrs. and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
150
null
ClCCCCOc1ccc2ccccc2c1.NCc1ccccc1>O.CS(=O)C>c1ccc(CNCCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-1a88f068295e44a0826659c21b8f3605
ClCCOc1ccc2ccccc2c1.NC1CCCCC1>>c1ccc2cc(OCCNC3CCCCC3)ccc2c1
C([O-])([O-])=O.[K+].[K+].C1(CCCCC1)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>C1(CCCCC1)NCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:9][CH2:8][O:7][c:6]1[cH:5][c:4]2[cH:3][cH:2][cH:1][cH:20][c:19]2[cH:18][cH:17]1.[NH2:10][CH:11]1[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]1>>[cH:1]1[cH:2][cH:3][c:4]2[cH:5][c:6]([O:7][CH2:8][CH2:9][NH:10][CH:11]3[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16]3)[cH:17][cH:18][c:19]2[cH:20]1
ClCCOc1ccc2ccccc2c1.NC1CCCCC1
c1ccc2cc(OCCNC3CCCCC3)ccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2cc(OCCNC3CCCCC3)ccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5](-[NH2;D1;+0:6])-[C:7]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5](-[C:4])-[C:7]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and cyclohexylamine (0.32 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloro ethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1.C1CCCCC1
HCl
O.CS(=O)C
140
null
ClCCOc1ccc2ccccc2c1.NC1CCCCC1>O.CS(=O)C>c1ccc2cc(OCCNC3CCCCC3)ccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ebfa2a55d911477f9e169e9be028ddb7
ClCCCOc1ccc2ccccc2c1.NC1CCCCC1>>c1ccc2cc(OCCCNC3CCCCC3)ccc2c1
C([O-])([O-])=O.[K+].[K+].C1(CCCCC1)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C1(CCCCC1)NCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:10][CH2:9][CH2:8][O:7][c:6]1[cH:5][c:4]2[cH:3][cH:2][cH:1][cH:21][c:20]2[cH:19][cH:18]1.[NH2:11][CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]1>>[cH:1]1[cH:2][cH:3][c:4]2[cH:5][c:6]([O:7][CH2:8][CH2:9][CH2:10][NH:11][CH:12]3[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17]3)[cH:18][cH:19][c:20]2[cH:21]1
ClCCCOc1ccc2ccccc2c1.NC1CCCCC1
c1ccc2cc(OCCCNC3CCCCC3)ccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2cc(OCCCNC3CCCCC3)ccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5](-[NH2;D1;+0:6])-[C:7]>>[C:4]-[C:5](-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:7]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and cyclohexylamine (0.29 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1.C1CCCCC1
HCl
O.CS(=O)C
140
null
ClCCCOc1ccc2ccccc2c1.NC1CCCCC1>O.CS(=O)C>c1ccc2cc(OCCCNC3CCCCC3)ccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0d26b68af0fc4534abf38b5d89464753
ClCCCCOc1ccc2ccccc2c1.NC1CCCCC1>>CC(CCNC1CCCCC1)Oc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C1(CCCCC1)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C1(CCCCC1)NCCC(C)OC1=CC2=CC=CC=C2C=C1
Cl[CH2:1][CH2:4][CH2:3][CH2:2][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1.[NH2:5][CH:6]1[CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]1>>[CH3:1][CH:2]([CH2:3][CH2:4][NH:5][CH:6]1[CH2:7][CH2:8][CH2:9][CH2:10][CH2:11]1)[O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1
ClCCCCOc1ccc2ccccc2c1.NC1CCCCC1
CC(CCNC1CCCCC1)Oc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
b600a81df87bea1685df54aaf8b30bd23674e9b7dd2a3cc8662e71bd3684ebef
d995b0d46e4aacf6b403d700b3e57edde7ae1aa34d450d1418ad3604b33a8a71
c1ccc2cc(OCCCNC3CCCCC3)ccc2c1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]-[CH2;D2;+0:4]-[#8:5]-[c:6].[C:7]-[C:8](-[NH2;D1;+0:9])-[C:10]>>[C:7]-[C:8](-[NH;D2;+0:9]-[CH2;D2;+0:2]-[C:3]-[CH;D3;+0:4](-[CH3;D1;+0:1])-[#8:5]-[c:6])-[C:10]
null
[]
150
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and cyclohexylamine (0.28 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 150° C. for 5 hrs and the reaction was completed as checked by TLC. Reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine
Ether.Secondary amine
null
null
C1CCCCC1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
150
null
ClCCCCOc1ccc2ccccc2c1.NC1CCCCC1>O.CS(=O)C>CC(CCNC1CCCCC1)Oc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-50a3b7481f7245e08b80179a6c14c38b
CCCCC(CC)CN.ClCCOc1ccc2ccccc2c1>>CCCCC(CC)CNCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(C)C(CN)CCCC.C1=C(C=CC2=CC=CC=C12)OCCCl>>C(C)C(CNCCOC1=CC2=CC=CC=C2C=C1)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH2:9].Cl[CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH:9][CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1
CCCCC(CC)CN.ClCCOc1ccc2ccccc2c1
CCCCC(CC)CNCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 2-ethyl n-hexylamine (0.37 ml, 0.003 mole) was taken in dry DMSO(40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. React...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCC(CC)CN.ClCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCC(CC)CNCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8791a47137a4489b86340d1a667d0da7
CCCCC(CC)CN.ClCCCOc1ccc2ccccc2c1>>CCCCC(CC)CNCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(C)C(CN)CCCC.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(C)C(CNCCCOC1=CC2=CC=CC=C2C=C1)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH2:9].Cl[CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[cH:23]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][...
CCCCC(CC)CN.ClCCCOc1ccc2ccccc2c1
CCCCC(CC)CNCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 2-ethyl-n-hexylamine (0.35 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Rea...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCC(CC)CN.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCC(CC)CNCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-0e82c47d51844dcf87ffb1f9d87321d5
CCCCC(CC)CN.ClCCCCOc1ccc2ccccc2c1>>CCCCC(CC)CNCCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(C)C(CN)CCCC.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(C)C(CNCCCCOC1=CC2=CC=CC=C2C=C1)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH2:9].Cl[CH2:10][CH2:11][CH2:12][CH2:13][O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[cH:24]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH:5]([CH2:6][CH3:7])[CH2:8][NH:9][CH2:10][CH2:11][CH2:12][CH2:13][O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20...
CCCCC(CC)CN.ClCCCCOc1ccc2ccccc2c1
CCCCC(CC)CNCCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 2-ethyl-n-hexylamine (0.33 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reac...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCC(CC)CN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCC(CC)CNCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-75300d78ff744fbdbf03028d1cea250e
CCCCCCCCCCCCN.ClCCCOc1ccc2ccccc2c1>>CCCCCCCCCCCCNCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCCCCCCCCCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(CCCCCCCCCCC)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH2:13].Cl[CH2:14][CH2:15][CH2:16][O:17][c:18]1[cH:19][cH:20][c:21]2[cH:22][cH:23][cH:24][cH:25][c:26]2[cH:27]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH:13][CH2:14][CH2:15][CH2:16][...
CCCCCCCCCCCCN.ClCCCOc1ccc2ccccc2c1
CCCCCCCCCCCCNCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-dodecylamine (0.51 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCCCCCCCCCN.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCCCCCCCCCNCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-6d91696f5b474ac78bdd9d7fc336a7a0
CCCCCCCCCCCCN.ClCCCCOc1ccc2ccccc2c1>>CCCCCCCCCCCCNCCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCCCCCCCCCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(CCCCCCCCCCC)NCCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH2:13].Cl[CH2:14][CH2:15][CH2:16][CH2:17][O:18][c:19]1[cH:20][cH:21][c:22]2[cH:23][cH:24][cH:25][cH:26][c:27]2[cH:28]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][NH:13][CH2:14][CH2:15][...
CCCCCCCCCCCCN.ClCCCCOc1ccc2ccccc2c1
CCCCCCCCCCCCNCCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
150
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-dodecylamine (0.48 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 150° C. for 8 hrs and the reaction was completed as checked by TLC. Reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
150
null
CCCCCCCCCCCCN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCCCCCCCCCNCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c862ba0c653749aab182a8023ae75593
CC(C)CCN.ClCCOc1ccc2ccccc2c1>>CC(C)CCNCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CC(C)C)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>C(CC(C)C)NCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][NH2:6].Cl[CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][NH:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1
CC(C)CCN.ClCCOc1ccc2ccccc2c1
CC(C)CCNCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and isoamylamine (0.24 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 6 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CC(C)CCN.ClCCOc1ccc2ccccc2c1>O.CS(=O)C>CC(C)CCNCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d1a55cd73fce4f19a47d33a5d5d31392
CC(C)CCN.ClCCCCOc1ccc2ccccc2c1>>CC(C)CCNCCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CC(C)C)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(CC(C)C)NCCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][NH2:6].Cl[CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1>>[CH3:1][CH:2]([CH3:3])[CH2:4][CH2:5][NH:6][CH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1
CC(C)CCN.ClCCCCOc1ccc2ccccc2c1
CC(C)CCNCCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and isoamylamine (0.21 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CC(C)CCN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CC(C)CCNCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-41c68876c5e943088c6dc928e9621008
ClCCOc1ccc2ccccc2c1.NCCCc1ccccc1>>c1ccc(CCCNCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCCN.C1=C(C=CC2=CC=CC=C12)OCCCl>>C1(=CC=CC=C1)CCCNCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH2:8])[cH:22][cH:23]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][c...
ClCCOc1ccc2ccccc2c1.NCCCc1ccccc1
c1ccc(CCCNCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CCCNCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
150
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 3-phenylpropylamine (0.47 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 150° C. for 6 hrs and the reaction was completed as checked by TLC. React...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
150
null
ClCCOc1ccc2ccccc2c1.NCCCc1ccccc1>O.CS(=O)C>c1ccc(CCCNCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-f08dd98c57df4068864f8171af8f0cf3
ClCCCOc1ccc2ccccc2c1.NCCCc1ccccc1>>c1ccc(CCCNCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCCN.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C1(=CC=CC=C1)CCCNCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:9][CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH2:8])[cH:23][cH:24]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH:8][CH2:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[c...
ClCCCOc1ccc2ccccc2c1.NCCCc1ccccc1
c1ccc(CCCNCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CCCNCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
150
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 3-phenylpropylamine (0.44 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 150° C. for 7 hrs and the reaction was completed as checked by TLC. Reac...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
150
null
ClCCCOc1ccc2ccccc2c1.NCCCc1ccccc1>O.CS(=O)C>c1ccc(CCCNCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-4732845dcb994dd2967780f7cdb7a7c9
ClCCCCOc1ccc2ccccc2c1.NCCCc1ccccc1>>c1ccc(CCCNCCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCCN.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C1(=CC=CC=C1)CCCNCCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[cH:23]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH2:8])[cH:24][cH:25]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][CH2:7][NH:8][CH2:9][CH2:10][CH2:11][CH2:12][O:13][c:14]2[cH:15][cH:16][c:17]3[cH:18][cH:19][cH:20]...
ClCCCCOc1ccc2ccccc2c1.NCCCc1ccccc1
c1ccc(CCCNCCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CCCNCCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
145
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 3-phenylpropylamine (0.42 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 145° C. for 7 hrs and the reaction was completed as checked by TLC. React...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
145
null
ClCCCCOc1ccc2ccccc2c1.NCCCc1ccccc1>O.CS(=O)C>c1ccc(CCCNCCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-666043bb3b4c49b583eaa97ec264d731
CCCCCCCCN.ClCCOc1ccc2ccccc2c1>>CCCCCCCCNCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCCCCCC)N.C1=C(C=CC2=CC=CC=C12)OCCCl>>C(CCCCCCC)NCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH2:9].Cl[CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH2:11][O:12][c:13]1[cH:14][cH:15][c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[cH:22]1
CCCCCCCCN.ClCCOc1ccc2ccccc2c1
CCCCCCCCNCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[#8:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[#8:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-octylamine (0.37 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 2-(2-naphthyloxy)-1-chloroethane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCCCCCN.ClCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCCCCCNCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-e1bf0c8ca6614d2d9469a700579bf704
CCCCCCCCN.ClCCCOc1ccc2ccccc2c1>>CCCCCCCCNCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCCCCCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(CCCCCCC)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH2:9].Cl[CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[cH:23]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:15][cH:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:...
CCCCCCCCN.ClCCCOc1ccc2ccccc2c1
CCCCCCCCNCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-octylamine (0.35 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 6 hrs and the reaction was completed as checked by TLC. Reaction mi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCCCCCN.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCCCCCNCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9bff22f4c0924063a2d2a6d97eb21165
CCCCCCCCN.ClCCCCOc1ccc2ccccc2c1>>CCCCCCCCNCCC(C)Oc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCCCCCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(CCCCCCC)NCCC(C)OC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH2:9].Cl[CH2:10][CH2:11][CH2:13][CH2:12][O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[cH:24]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][NH:9][CH2:10][CH2:11][CH:12]([CH3:13])[O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20]...
CCCCCCCCN.ClCCCCOc1ccc2ccccc2c1
CCCCCCCCNCCC(C)Oc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
b600a81df87bea1685df54aaf8b30bd23674e9b7dd2a3cc8662e71bd3684ebef
d995b0d46e4aacf6b403d700b3e57edde7ae1aa34d450d1418ad3604b33a8a71
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:4]-[#8:5]-[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH;D3;+0:4](-[CH3;D1;+0:3])-[#8:5]-[c:6]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-octylamine (0.33 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine
Ether.Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCCCCCN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCCCCCNCCC(C)Oc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-534a0f1c23614f0d8bd825d6f36911c4
CCCCN.ClCCCCOc1ccc2ccccc2c1>>CCCCNCCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(CCC)NCCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][NH2:5].Cl[CH2:6][CH2:7][CH2:8][CH2:9][O:10][c:11]1[cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[cH:20]1>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH2:8][CH2:9][O:10][c:11]1[cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[cH:20]1
CCCCN.ClCCCCOc1ccc2ccccc2c1
CCCCNCCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-butylamine (0.32 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 8 hrs and the reaction was completed as checked by TLC. Reaction mix...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCCN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCNCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-ecd6745b85834cb7aedc1c85943beb78
CCCN.ClCCCCOc1ccc2ccccc2c1>>CCCNCCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CC)N.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C(CC)NCCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][NH2:4].Cl[CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1>>[CH3:1][CH2:2][CH2:3][NH:4][CH2:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1
CCCN.ClCCCCOc1ccc2ccccc2c1
CCCNCCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-propyl amine (0.26 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
CCCN.ClCCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCNCCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-d1a84167fdfa4a05958f2dc9d7eb359b
ClCCCCOc1ccc2ccccc2c1.NCCc1ccccc1>>CCC(CNCCc1ccccc1)Oc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCN.C1=C(C=CC2=CC=CC=C12)OCCCCCl>>C1(=CC=CC=C1)CCNCC(CC)OC1=CC2=CC=CC=C2C=C1
Cl[CH2:4][CH2:1][CH2:2][CH2:3][O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]2[cH:24]1.[NH2:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][CH2:2][CH:3]([CH2:4][NH:5][CH2:6][CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[O:14][c:15]1[cH:16][cH:17][c:18]2[cH:19][cH:20][cH:21][cH...
ClCCCCOc1ccc2ccccc2c1.NCCc1ccccc1
CCC(CNCCc1ccccc1)Oc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
b600a81df87bea1685df54aaf8b30bd23674e9b7dd2a3cc8662e71bd3684ebef
d995b0d46e4aacf6b403d700b3e57edde7ae1aa34d450d1418ad3604b33a8a71
c1ccc(CCNCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]-[CH2;D2;+0:4]-[#8:5]-[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[CH2;D2;+0:1]-[CH;D3;+0:4](-[#8:5]-[c:6])-[C:3]-[CH3;D1;+0:2]
null
[]
140
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and phenylethylamine (0.4 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 4-(2-naphthyloxy)-1-chlorobutane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 140° C. for 8 hrs and the reaction was completed as checked by TLC. Reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether.Primary amine
Ether.Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
140
null
ClCCCCOc1ccc2ccccc2c1.NCCc1ccccc1>O.CS(=O)C>CCC(CNCCc1ccccc1)Oc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-11b1fe37bbbc49e2a48c308a8d40ee1c
CCCCN.ClCCCOc1ccc2ccccc2c1>>CCCCNCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CCC)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(CCC)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][NH2:5].Cl[CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1
CCCCN.ClCCCOc1ccc2ccccc2c1
CCCCNCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
135
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-butylamine (0.34 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 135° C. for 7 hrs and the reaction was completed as checked by TLC. Reaction mi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
135
null
CCCCN.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCCNCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b3102b1a1d544a3ebb6092b02e0c3ca2
CCCN.ClCCCOc1ccc2ccccc2c1>>CCCNCCCOc1ccc2ccccc2c1
C([O-])([O-])=O.[K+].[K+].C(CC)N.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C(CC)NCCCOC1=CC2=CC=CC=C2C=C1
[CH3:1][CH2:2][CH2:3][NH2:4].Cl[CH2:5][CH2:6][CH2:7][O:8][c:9]1[cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[cH:18]1>>[CH3:1][CH2:2][CH2:3][NH:4][CH2:5][CH2:6][CH2:7][O:8][c:9]1[cH:10][cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[cH:18]1
CCCN.ClCCCOc1ccc2ccccc2c1
CCCNCCCOc1ccc2ccccc2c1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc2ccccc2c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[CH2;D2;+0:1]-[C:2]-[C:3]
null
[]
145
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and n-propylamine (0.28 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 145° C. for 8 hrs and the reaction was completed as checked by TLC. Reaction m...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccc2ccccc2c1
HCl
O.CS(=O)C
145
null
CCCN.ClCCCOc1ccc2ccccc2c1>O.CS(=O)C>CCCNCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-971ce324064948c4830c7e2b7b24e9f7
ClCCCOc1ccc2ccccc2c1.NCCc1ccccc1>>c1ccc(CCNCCCOc2ccc3ccccc3c2)cc1
C([O-])([O-])=O.[K+].[K+].C1(=CC=CC=C1)CCN.C1=C(C=CC2=CC=CC=C12)OCCCCl>>C1(=CC=CC=C1)CCNCCCOC1=CC2=CC=CC=C2C=C1
Cl[CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1.[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][NH2:7])[cH:22][cH:23]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][CH2:6][NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][cH:18][cH:19][c:20]3[cH:21]2)[cH:22][c...
ClCCCOc1ccc2ccccc2c1.NCCc1ccccc1
c1ccc(CCNCCCOc2ccc3ccccc3c2)cc1
null
null
O.CS(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of primary amines with alkyl halides
fc19a1445ff204e66e51735d0191465bda3c6691fd233624a54742c9d4828411
0b1d32f56ad00f1e5bdae9390f9227bbea012fa2f8203aac34726b8a6761cc7c
c1ccc(CCNCCCOc2ccc3ccccc3c2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[NH;D2;+0:6]-[C:5]-[C:4]
null
[]
145
CELSIUS
null
null
A mixture of anhydrous potassium carbonate (10 gm, in excess) and 2-phenylethylamine (0.51 ml, 0.003 mole) was taken in dry DMSO (40 ml). Now 3-(2-naphthyloxy)-1-chloropropane (0.5 gm, 0.002 mole) was added in it. Reaction mixture was refluxed at 145° C. for 7 hrs and the reaction was completed as checked by TLC. React...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HCl
O.CS(=O)C
145
null
ClCCCOc1ccc2ccccc2c1.NCCc1ccccc1>O.CS(=O)C>c1ccc(CCNCCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-b5c41d7fab414a0c80ca766a87813d22
CI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>COc1ccc(N(C)CCCOc2ccc3ccccc3c2)cc1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.CI>>COC1=CC=C(C=C1)N(C)CCCOC1=CC2=CC=CC=C2C=C1
I[CH3:8].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[cH:22]2)[cH:23][cH:24]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([N:7]([CH3:8])[CH2:9][CH2:10][CH2:11][O:12][c:13]2[cH:14][cH:15][c:16]3[cH:17][cH:18][cH:19][cH:20][c:21]3[cH:22]2)...
CI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
COc1ccc(N(C)CCCOc2ccc3ccccc3c2)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
e1587a52a1bca6a80c6048d43276d8bccf8d3e94e692e6b210e5fd3b22494187
7cc25fba33369069673bac5bd8fc404dc064da8d6c8cf4a77f21f4df0a617fe3
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
I-[CH3;D1;+0:1].[C:2]-[C:3]-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]>>[C:2]-[C:3]-[N;H0;D3;+0:4](-[CH3;D1;+0:1])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
A mixture of (4-methoxyphenyl)-[3-(naphthalen-2-yloxy)propyl]amine (0.5 gm, 0.002 mole) and methyl iodide (0.49 ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 12 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get oily compound w...
10.6084/m9.figshare.5104873.v1
null
Secondary amine
Tertiary amine
null
null
c1ccccc1.c1ccc2ccccc2c1
HI
CC(=O)C
null
null
CI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>COc1ccc(N(C)CCCOc2ccc3ccccc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-c7a8b54195494acfa10a4169a5ff2089
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>NCCCOc1ccc2ccccc2c1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.C(C)Br>>C1=C(C=CC2=CC=CC=C12)OCCCN
COc1ccc([NH:1][CH2:2][CH2:3][CH2:4][O:5][c:6]2[cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[cH:15]2)cc1>>[NH2:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
NCCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Reduction
OtherReaction
bd6cc2ddd30b209c36eb43f9e2d163a4da40f8a48bda8b578aa13caf5d4fe5dd
79272555d5bd71219cf9e8b42c4ac12a30bbf383c58cfbccf49a5a990e3653c1
c1ccc2ccccc2c1
C-O-c1:c:c:c(-[NH;D2;+0:1]-[C:2]-[C:3]):c:c:1>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A mixture of N-(4-methoxyphenyl)-[3-(naphthalen-2-yloxy)propyl]amine (0.5 gm, 0.002 mole) and ethyl bromide(0.52 ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 12 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get oily compound ...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Primary amine
c1ccccc1
null
c1ccc2ccccc2c1
HO-
CC(=O)C
null
null
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>NCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9831cd3ecab94533a34687b31311ae20
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>NCCCOc1ccc2ccccc2c1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.C(CC)Br>>C1=C(C=CC2=CC=CC=C12)OCCCN
COc1ccc([NH:1][CH2:2][CH2:3][CH2:4][O:5][c:6]2[cH:7][cH:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[cH:15]2)cc1>>[NH2:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[cH:15]1
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
NCCCOc1ccc2ccccc2c1
null
null
CC(=O)C
Reduction
OtherReaction
bd6cc2ddd30b209c36eb43f9e2d163a4da40f8a48bda8b578aa13caf5d4fe5dd
79272555d5bd71219cf9e8b42c4ac12a30bbf383c58cfbccf49a5a990e3653c1
c1ccc2ccccc2c1
C-O-c1:c:c:c(-[NH;D2;+0:1]-[C:2]-[C:3]):c:c:1>>[C:3]-[C:2]-[NH2;D1;+0:1]
null
[]
null
null
null
null
A mixture of N-(4-methoxyphenyl)-[3-(naphthalen-2-yloxy)propyl]amine (0.5 gm, 0.002 mole) and propyl bromide (0.54 ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 12 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get oily compoun...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Primary amine
c1ccccc1
null
c1ccc2ccccc2c1
HO-
CC(=O)C
null
null
COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>NCCCOc1ccc2ccccc2c1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-9aff86da42f3474f91f2aca17137269e
CCCCI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>CCCCN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.C(CCC)I>>COC1=CC=C(C=C1)N(CCCC)CCCOC1=CC2=CC=CC=C2C=C1
I[CH2:4][CH2:3][CH2:2][CH3:1].[NH:5]([CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[cH:19]1)[c:20]1[cH:21][cH:22][c:23]([O:24][CH3:25])[cH:26][cH:27]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][O:9][c:10]1[cH:11][cH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]2[c...
CCCCI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
CCCCN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
6d58cac08ccced0a33ed16fbca180bc12aa011288d6476106d98a7b2cbc3d709
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
I-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:6](-[C:5]-[C:4])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
A mixture of N-(4-methoxyphenyl)-(3-(naphthalen-2-yloxy)propyl)amine (0.5 gm, 0.002 mole) and butyl iodide(1 ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 12 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get oily compound whic...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
null
null
c1ccc2ccccc2c1.c1ccccc1
HI
CC(=O)C
null
null
CCCCI.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>CCCCN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-de5caab12b234d198645976888681713
CCOC(=O)CBr.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>>CCOC(=O)CN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
COC1=CC=C(C=C1)NCCCOC1=CC2=CC=CC=C2C=C1.BrCC(=O)OCC>>C(C)OC(CN(C1=CC=C(C=C1)OC)CCCOC1=CC2=CC=CC=C2C=C1)=O
Br[CH2:6][C:4]([O:3][CH2:2][CH3:1])=[O:5].[NH:7]([CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[cH:21]1)[c:22]1[cH:23][cH:24][c:25]([O:26][CH3:27])[cH:28][cH:29]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][N:7]([CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][c:15]2[cH:16][cH...
CCOC(=O)CBr.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1
CCOC(=O)CN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0aa79e0969c91fcc78d2e2c57a034d94cf8ba395b1aac7787417752a9d5314e2
e09591825c4808efe257024fb4bbe3690a7cda9ee664fef9727988761bae5b4a
c1ccc(NCCCOc2ccc3ccccc3c2)cc1
Br-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#8:4]-[C:5].[C:6]-[C:7]-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11]>>[C:5]-[#8:4]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:1]-[N;H0;D3;+0:8](-[C:7]-[C:6])-[c:9](:[c:10]):[c:11]
96
[{"value": 96.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of (4-methoxyphenyl)-(3-(naphthalen-2-yloxy)propyl)amine (0.5 gm, 0.002 mole) and ethyl bromoacetate (0.62 ml, 0.003 mole) was taken in dry acetone (40 ml). It was refluxed for 10 hrs and the progress of reaction checked by TLC. Reaction mixture was filtered and the filtrate was concentrated to get the oily c...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Secondary amine
Ester.Tertiary amine
null
null
c1ccc2ccccc2c1.c1ccccc1
HBr
CC(=O)C
null
null
CCOC(=O)CBr.COc1ccc(NCCCOc2ccc3ccccc3c2)cc1>CC(=O)C>CCOC(=O)CN(CCCOc1ccc2ccccc2c1)c1ccc(OC)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-20916a283f7b4e35ae8b97c1acc5e84b
COc1ccc(N)cc1.ClCCCOc1ccc2ccc(OCCCCl)cc2c1>>COc1ccc(NCCCOc2ccc3ccc(OCCCNc4ccc(OC)cc4)cc3c2)cc1
ClCCCOC1=CC2=CC(=CC=C2C=C1)OCCCCl.COC1=CC=C(C=C1)N>>COC1=CC=C(C=C1)NCCCOC1=CC2=CC(=CC=C2C=C1)OCCCNC1=CC=C(C=C1)OC
[cH:4]1[cH:5][c:6]([NH2:7])[cH:35][cH:30][c:27]1[O:28][CH3:29].Cl[CH2:3][CH2:21][CH2:10][O:11][c:12]1[cH:26][cH:14][c:15]2[cH:16][cH:17][c:18]([O:2][CH2:1][CH2:9][CH2:8]Cl)[cH:32][c:33]2[cH:34]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][cH:17][c:18]([O:19...
COc1ccc(N)cc1.ClCCCOc1ccc2ccc(OCCCCl)cc2c1
COc1ccc(NCCCOc2ccc3ccc(OCCCNc4ccc(OC)cc4)cc3c2)cc1
null
null
CS(=O)C
Aromatic Heterocycle Formation
OtherReaction
c5a6acf2a9d145fae494c59c817cbad6ce41356c70dafa4e9410e44578c4a1ba
e0bd9dacf65ab682499fd530e948686e7eb66ed45de4d8b873b0b4f10b43569a
c1ccc(NCCCOc2ccc3ccc(OCCCNc4ccccc4)cc3c2)cc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[#8:4]-[c;H0;D3;+0:5]1:[c:6]:[c:7]2:[c:8]:[c;H0;D3;+0:9](-[O;H0;D2;+0:10]-[CH2;D2;+0:11]-[CH2;D2;+0:12]-[CH2;D2;+0:13]-Cl):[c:14]:[c:15]:[c:16]:2:[cH;D2;+0:17]:[cH;D2;+0:18]:1.[C;D1;H3:19]-[#8:20]-[c;H0;D3;+0:21]1:[cH;D2;+0:22]:[cH;D2;+0:23]:[c:24](-[NH2;D1;+0:25]):[c:26]:[c...
null
[]
140
CELSIUS
null
null
A mixture of 2,7-bis(3-chloropropyloxy)naphthalene (1 gm, 0.003 mole) and p-anisidine (1.17 gm, 0.005 mole) were taken in 60 ml dry DMSO. It was refluxed at 140° C. for 12 hrs the completion of the reaction was checked by TLC. The reaction mixture was poured into distilled water (80 ml) and extracted with ethyl acetate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ether.Ether.Ether.Primary amine
Ether.Ether.Ether.Ether.Secondary amine.Secondary amine
c1ccccc1.c1ccc2ccccc2c1
c1ccccc1.c1ccc2ccccc2c1.c1ccccc1
c1ccccc1.c1ccc2ccccc2c1.c1ccccc1
null
CS(=O)C
140
null
COc1ccc(N)cc1.ClCCCOc1ccc2ccc(OCCCCl)cc2c1>CS(=O)C>COc1ccc(NCCCOc2ccc3ccc(OCCCNc4ccc(OC)cc4)cc3c2)cc1
ord_dataset-c3a75813d0b24864aa4f7cd526efd6aa
ord-8602afcfcfc34702adeae4b8cb6b6cad
COc1ccc(N)cc1.ClCCCOc1ccc2cc(OCCCCl)ccc2c1>>COc1ccc(NCCCOc2ccc3cc(OCCCNc4ccc(OC)cc4)ccc3c2)cc1
ClCCCOC1=CC2=CC=C(C=C2C=C1)OCCCCl.COC1=CC=C(C=C1)N>>COC1=CC=C(C=C1)NCCCOC1=CC2=CC=C(C=C2C=C1)OCCCNC1=CC=C(C=C1)OC
[cH:4]1[cH:5][c:6]([NH2:7])[cH:35][cH:29][c:26]1[O:27][CH3:28].Cl[CH2:8][CH2:1][CH2:3][O:2][c:17]1[cH:16][c:15]2[cH:14][cH:13][c:12]([O:11][CH2:10][CH2:30][CH2:23]Cl)[cH:34][c:33]2[cH:32][cH:31]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]2[cH:13][cH:14][c:15]3[cH:16][c:17]([O:18][CH2:...
COc1ccc(N)cc1.ClCCCOc1ccc2cc(OCCCCl)ccc2c1
COc1ccc(NCCCOc2ccc3cc(OCCCNc4ccc(OC)cc4)ccc3c2)cc1
null
null
CS(=O)C
Aromatic Heterocycle Formation
OtherReaction
c5a6acf2a9d145fae494c59c817cbad6ce41356c70dafa4e9410e44578c4a1ba
e0bd9dacf65ab682499fd530e948686e7eb66ed45de4d8b873b0b4f10b43569a
c1ccc(NCCCOc2ccc3cc(OCCCNc4ccccc4)ccc3c2)cc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[#8:4]-[c:5].Cl-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-[c;H0;D3;+0:10](:[c:11]:[c:12]):[c:13]:[c:14].[C;D1;H3:15]-[#8:16]-[c;H0;D3;+0:17]1:[cH;D2;+0:18]:[cH;D2;+0:19]:[c:20](-[NH2;D1;+0:21]):[c:22]:[cH;D2;+0:23]:1>>[CH3;D1;+0:7]-[O;H0;D2;+0:9]-[c;H0;D3;+0:8...
null
[]
140
CELSIUS
null
null
A mixture of 2,6-bis(3-chloropropyloxy)naphthalene(1 gm, 0.003 mole) and p-anisidine(1.17 gm, 0.005 mole) was taken in 60 ml dry DMSO. It was refluxed at 140° C. for 12 hrs. The completion of the reaction was checked by TLC. The reaction mixture was poured into distilled water (80 ml) and extracted with ethyl acetate t...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ether.Ether.Ether.Primary amine
Ether.Ether.Ether.Ether.Secondary amine.Secondary amine
c1ccccc1.c1ccc2ccccc2c1
c1ccccc1.c1ccc2ccccc2c1.c1ccccc1
c1ccccc1.c1ccc2ccccc2c1.c1ccccc1
null
CS(=O)C
140
null
COc1ccc(N)cc1.ClCCCOc1ccc2cc(OCCCCl)ccc2c1>CS(=O)C>COc1ccc(NCCCOc2ccc3cc(OCCCNc4ccc(OC)cc4)ccc3c2)cc1