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
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14
3.37k
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1
581
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1
433
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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
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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-02ee2261663048188cf6d85d2cc96e3f
ord-e04cbcb18b1d47e8b7a7115f33cccf17
Cc1ccsc1C(=O)O.O=C(Cl)C(=O)Cl>>Cc1ccsc1C(=O)Cl
CC1=C(SC=C1)C(=O)O.C(C(=O)Cl)(=O)Cl>>CC1=C(SC=C1)C(=O)Cl
O[C:7]([c:6]1[c:2]([CH3:1])[cH:3][cH:4][s:5]1)=[O:8].O=C(Cl)C(=O)[Cl:9]>>[CH3:1][c:2]1[cH:3][cH:4][s:5][c:6]1[C:7](=[O:8])[Cl:9]
Cc1ccsc1C(=O)O.O=C(Cl)C(=O)Cl
Cc1ccsc1C(=O)Cl
null
null
C1=CC=CC=C1
Functional Group Interconversion
Alcohol to chloride_Other
013cec2edeb273a7a148f349d36a52d99ff4e7bcf8eed78085df830088e387ac
aedb1f68dc5b7eb0583043e1125b741382b17974140a2f46554f0110e2ddc884
c1ccsc1
Cl-C(=O)-C(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[#16;a:6]:[c:7]>>[Cl;H0;D1;+0:1]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[#16;a:6]:[c:7]
100.3
[{"value": 100.3, "product": "CC1=C(SC=C1)C(=O)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In 100 ml of benzene was suspended 3.00 g (21.1 mmol) of 3-methyl-2-thiophenecarboxylic acid, oxalyl chloride [7.36 ml (84.4 mmol)] was added and the mixture was refluxed for 2 hours. After cooling, the solvent was distilled off to obtain 3.40 g of 3-methylthenoyl chloride (yield: quant.). To a solution of 1.50 g (6.23...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Acyl halide.Carboxylic acid
Acyl halide
null
null
c1ccsc1
HCl
C1=CC=CC=C1
null
null
Cc1ccsc1C(=O)O.O=C(Cl)C(=O)Cl>C1=CC=CC=C1>Cc1ccsc1C(=O)Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f56f6d364c6f42abae9c794c891f57f9
Cc1ccsc1C(=O)Cl.NCCCSc1ccncc1>>Cc1ccsc1C(=O)NCCCSc1ccncc1
Cl.Cl.NCCCSC1=CC=NC=C1.C(C)N(CC)CC.CC1=C(SC=C1)C(=O)Cl>>CC1=C(SC=C1)C(=O)NCCCSC1=CC=NC=C1
Cl[C:7]([c:6]1[c:2]([CH3:1])[cH:3][cH:4][s:5]1)=[O:8].[NH2:9][CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1>>[CH3:1][c:2]1[cH:3][cH:4][s:5][c:6]1[C:7](=[O:8])[NH:9][CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1
Cc1ccsc1C(=O)Cl.NCCCSc1ccncc1
Cc1ccsc1C(=O)NCCCSc1ccncc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCCCSc1ccncc1)c1cccs1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#16;a:5]:[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#16;a:5]:[c:6]
84.5
[{"value": 84.5, "product": "CC1=C(SC=C1)C(=O)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.5, "product": "CC1=C(SC=C1)C(=O)NCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
In 100 ml of benzene was suspended 3.00 g (21.1 mmol) of 3-methyl-2-thiophenecarboxylic acid, oxalyl chloride [7.36 ml (84.4 mmol)] was added and the mixture was refluxed for 2 hours. After cooling, the solvent was distilled off to obtain 3.40 g of 3-methylthenoyl chloride (yield: quant.). To a solution of 1.50 g (6.23...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccsc1.c1ccncc1
HCl
C(Cl)Cl
null
null
Cc1ccsc1C(=O)Cl.NCCCSc1ccncc1>C(Cl)Cl>Cc1ccsc1C(=O)NCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c3e25c8a85d44ea5a75bc8f82e1e111d
CCN(CC)CC.CN(C)C(=O)Sc1cccnc1.CO>>O=C1c2ccccc2C(=O)N1CSc1cccnc1
CN(C(=O)SC=1C=NC=CC1)C.[OH-].[Na+].CO.C(C)N(CC)CC>>C1(C=2C(C(N1CSC=1C=NC=CC1)=O)=CC=CC2)=O
C(N([CH2:4][CH3:3])[CH2:7][CH3:6])[CH3:5].[O:1]=[C:2]([N:11]([CH3:8])[CH3:12])[S:13][c:14]1[cH:15][cH:16][cH:17][n:18][cH:19]1.[CH3:9][OH:10]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][S:13][c:14]1[cH:15][cH:16][cH:17][n:18][cH:19]1
CCN(CC)CC.CN(C)C(=O)Sc1cccnc1.CO
O=C1c2ccccc2C(=O)N1CSc1cccnc1
null
null
C(C)O
Aromatic Heterocycle Formation
OtherReaction
f6e1d45e9221ee6e026b35747c95fb0c38d15ea43d755f8997202c8b68cc288f
0eafb27fde53390e73581c39f563745aa9ec1ae457b9845f07dfd55c08d54d24
O=C1c2ccccc2C(=O)N1CSc1cccnc1
[CH3;D1;+0:1]-[CH2;D2;+0:2]-N(-C-[CH3;D1;+0:3])-[CH2;D2;+0:4]-[CH3;D1;+0:5].[CH3;D1;+0:6]-[N;H0;D3;+0:7](-[CH3;D1;+0:8])-[C;H0;D3;+0:9](=[O;D1;H0:10])-[S;H0;D2;+0:11]-[c:12](:[c:13]):[c:14]:[#7;a:15]:[c:16].[CH3;D1;+0:17]-[OH;D1;+0:18]>>[O;D1;H0:10]=[C;H0;D3;+0:9]1-[N;H0;D3;+0:7](-[CH2;D2;+0:6]-[S;H0;D2;+0:11]-[c:12](:...
80.9
[{"value": 80.9, "product": "C1(C=2C(C(N1CSC=1C=NC=CC1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a solution of 1.00 g (5.49 mmol) of 3-(dimethylaminocarbonylthio)pyridine in 50 ml of methanol, 5.49 ml (5.49 mmol) of a 1N aqueous solution of sodium hydroxide was added. The mixture was heated at 60° C. for 1 hour with stirring. After cooling, the solvent was distilled off. The residue was dissolved in ethanol and...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amine.Monosulfide.Methanol
Substituted dicarboximide.Monosulfide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
Other
C(C)O
60
null
CCN(CC)CC.CN(C)C(=O)Sc1cccnc1.CO>C(C)O>O=C1c2ccccc2C(=O)N1CSc1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-dd7bd97cca9b4017bd4ae008bd7dac34
O=C1c2ccccc2C(=O)N1CCl.Oc1ccncc1>>O=C1c2ccccc2C(=O)N1COc1ccncc1
OC1=CC=NC=C1.ClCN1C(C=2C(C1=O)=CC=CC2)=O.C1CCC2=NCCCN2CC1>>C1(C=2C(C(N1COC1=CC=NC=C1)=O)=CC=CC2)=O
Cl[CH2:12][N:11]1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10].[OH:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][O:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1
O=C1c2ccccc2C(=O)N1CCl.Oc1ccncc1
O=C1c2ccccc2C(=O)N1COc1ccncc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
fdeaab08fdcfd316930ef1175816bd95f7da676fa892aa1cc7c464d4492570d3
fecbd7b649db84f1531203fbcee385caf3cdb6e47086797236a63b91a6e50ba8
O=C1c2ccccc2C(=O)N1COc1ccncc1
Cl-[CH2;D2;+0:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]-[C:7]-1=[O;D1;H0:8].[OH;D1;+0:9]-[c:10]1:[c:11]:[c:12]:[#7;a:13]:[c:14]:[c:15]:1>>[O;D1;H0:8]=[C:7]1-[c:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#7:2]-1-[CH2;D2;+0:1]-[O;H0;D2;+0:9]-[c:10]1:[c:11]:[c:12]:[#7;a:13]:[c:14]:[c:15]:1
21
[{"value": 21.0, "product": "C1(C=2C(C(N1COC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 21.0, "product": "C1(C=2C(C(N1COC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 4.76 g (50 mmol) of 4-hydroxypyridine and 10.76 g (55 mmol) of N-chloromethylphthalimide in 80 ml of DMF, 8.23 ml (55 mmol) of 1,8-diazabicyclo[5,4,0]-7-undecene was added. The mixture was stirred at room temperature for 2 hours. After the solvent was distilled off, the reaction mixture was poured into...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Substituted dicarboximide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
HCl
CN(C)C=O
null
2
O=C1c2ccccc2C(=O)N1CCl.Oc1ccncc1>CN(C)C=O>O=C1c2ccccc2C(=O)N1COc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-80d6d35a6b1b4822a93a6f325c74f83a
NCc1cccs1.OCCCSc1ccncc1>>c1csc(CNCCCSc2ccncc2)c1
OCCCSC1=CC=NC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl.S1C(=CC=C1)CN>>S1C(=CC=C1)CNCCCSC1=CC=NC=C1
[cH:1]1[cH:2][s:3][c:4]([CH2:5][NH2:6])[cH:17]1.O[CH2:7][CH2:8][CH2:9][S:10][c:11]1[cH:12][cH:13][n:14][cH:15][cH:16]1>>[cH:1]1[cH:2][s:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][CH2:9][S:10][c:11]2[cH:12][cH:13][n:14][cH:15][cH:16]2)[cH:17]1
NCc1cccs1.OCCCSc1ccncc1
c1csc(CNCCCSc2ccncc2)c1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1csc(CNCCCSc2ccncc2)c1
O-[CH2;D2;+0:1]-[C:2]-[C:3].[#16;a:4]:[c:5]-[C:6]-[NH2;D1;+0:7]>>[#16;a:4]:[c:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]
29.1
[{"value": 29.1, "product": "S1C(=CC=C1)CNCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 29.1, "product": "S1C(=CC=C1)CNCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
In 200 ml of methylene chloride were dissolved 10.34 g (61.1 mmol) of 4-(3-hydroxypropylthio)pyridine and 10.2 ml (73.3 mmol) of triethylamine, methanesulfonyl chloride [5.7 ml (73.3 mmol)] was added, and the mixture was stirred at room temperature for 30 minutes. The reaction mixture was washed with a saturated aqueou...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1ccsc1.c1ccncc1
HO-
C(Cl)Cl
null
0.5
NCc1cccs1.OCCCSc1ccncc1>C(Cl)Cl>c1csc(CNCCCSc2ccncc2)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6ab3399bbe384df4a016cb4e27a3ec16
Nc1ncccc1CCN1C(=O)c2ccccc2C1=O>>Nc1ncccc1CCN1C(=O)c2ccccc2C1=O
Cl.NC1=NC=CC=C1CCN1C(C=2C(C1=O)=CC=CC2)=O>>Cl.NC1=NC=CC=C1CCN1C(C=2C(C1=O)=CC=CC2)=O
[NH2:2][c:3]1[n:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][CH2:10][N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]>>[NH2:2][c:3]1[n:4][cH:5][cH:6][cH:7][c:8]1[CH2:9][CH2:10][N:11]1[C:12](=[O:13])[c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]2[C:20]1=[O:21]
Nc1ncccc1CCN1C(=O)c2ccccc2C1=O
Nc1ncccc1CCN1C(=O)c2ccccc2C1=O
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1c2ccccc2C(=O)N1CCc1cccnc1
null
79
[{"value": 79.0, "product": "Cl.NC1=NC=CC=C1CCN1C(C=2C(C1=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
In 5 ml of methanol was dissolved 237 mg (0.792 mmol) of 2-amino-3-[2-(phthalimido)ethyl]pyridine. The solution was treated with 5 ml (10 mmol) of a 2N solution of hydrogen chloride in methanol. The solvent was distilled off to obtain the desired powder. The powder thus obtained was washed with ether to obtain 233 mg o...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccncc1.c1ccc2c(c1)C[NH]C2
null
CO
null
null
Nc1ncccc1CCN1C(=O)c2ccccc2C1=O>CO>Nc1ncccc1CCN1C(=O)c2ccccc2C1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-78e604ab97a5457d90db9847ffc8eaa3
OCCCBr.Sc1ccncc1>>OCCCSc1ccncc1
SC1=CC=NC=C1.C(C)N(CC)CC.BrCCCO>>OCCCSC1=CC=NC=C1
Br[CH2:4][CH2:3][CH2:2][OH:1].[SH:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1>>[OH:1][CH2:2][CH2:3][CH2:4][S:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1
OCCCBr.Sc1ccncc1
OCCCSc1ccncc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
thioether_nucl_sub
26df88c6a3f5f203c89584658be4e126cb42994c98a2e16bc812e1036cdae857
8b2f52296c3a93039174c980b6042ba15754e04d6892a1284c3a32985220b214
c1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[SH;D1;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
62.9
[{"value": 62.9, "product": "OCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.9, "product": "OCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
In 250 ml of methylene chloride was dissolved 22.2 g (200 mmol) of 4-mercaptopyridine and 27.9 ml (200 mmol) of triethylamine. Thereto was added 18.1 g (200 mmol) of 3-bromo-1-propanol. The mixture was stirred at room temperature for 3 hours. The reaction mixture was washed with a 1N aqueous solution of sodium hydroxid...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic thiol
Monosulfide
null
null
c1ccncc1
HBr
C(Cl)Cl
null
3
OCCCBr.Sc1ccncc1>C(Cl)Cl>OCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cead92d510b44868b7a17bfdcce47e62
NCc1ccccc1.OCCCSc1ccncc1>>c1ccc(CNCCCSc2ccncc2)cc1
C(C1=CC=CC=C1)N.OCCCSC1=CC=NC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl>>C(C1=CC=CC=C1)NCCCSC1=CC=NC=C1
[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[cH:17][cH:18]1.O[CH2:7][CH2:8][CH2:9][S:10][c:11]1[cH:12][cH:13][n:14][cH:15][cH:16]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][CH2:9][S:10][c:11]2[cH:12][cH:13][n:14][cH:15][cH:16]2)[cH:17][cH:18]1
NCc1ccccc1.OCCCSc1ccncc1
c1ccc(CNCCCSc2ccncc2)cc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1ccc(CNCCCSc2ccncc2)cc1
O-[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]
16.1
[{"value": 16.1, "product": "C(C1=CC=CC=C1)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 16.1, "product": "C(C1=CC=CC=C1)NCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
In 150 ml of methylene chloride were dissolved 5.22 g (30.8 mmol) of 4-(3-hydroxypropylthio)pyridine and 5.16 ml (37.0 mmol) of triethylamine, methanesulfonyl chloride [2.86 ml (37.0 mmol)] was added, and the mixture was stirred at room temperature for 30 minutes. The reaction mixture was washed with a saturated aqueou...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccncc1
HO-
C(Cl)Cl
null
0.5
NCc1ccccc1.OCCCSc1ccncc1>C(Cl)Cl>c1ccc(CNCCCSc2ccncc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a2293b8478224028b214fce323cd3c06
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)cc1>>CC(=O)N(CCCSc1ccncc1)Cc1ccccc1
C(C1=CC=CC=C1)NCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C)(=O)Cl>>C(C1=CC=CC=C1)N(C(C)=O)CCCSC1=CC=NC=C1
Cl[C:2]([CH3:1])=[O:3].[NH:4]([CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][C:2](=[O:3])[N:4]([CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)cc1
CC(=O)N(CCCSc1ccncc1)Cc1ccccc1
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
c1ccc(CNCCCSc2ccncc2)cc1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[c:8]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[C:7]-[c:8])-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
84.3
[{"value": 84.2, "product": "C(C1=CC=CC=C1)N(C(C)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.3, "product": "C(C1=CC=CC=C1)N(C(C)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.0 g (3.87 mmol) of 4-[3-(N-benzylamino)propylthio)-pyridine and 0.65 ml (4.64 mmol) of triethylamine in 25 ml of methylene chloride, 0.49 ml (4.64 mmol) of acetyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The reaction mixture was w...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccncc1.c1ccccc1
HCl
C(Cl)Cl
null
null
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)cc1>C(Cl)Cl>CC(=O)N(CCCSc1ccncc1)Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0d1810d5f436433ea51dce05a3b95637
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)cc1>>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccc1
Cl.Cl.C(C1=CC=CC=C1)NCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C1=CC=CC=C1)(=O)Cl>>Cl.C(C1=CC=CC=C1)N(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1
Cl[C:3](=[O:2])[c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1.[NH:10]([CH2:11][CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1)[CH2:21][c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[O:2]=[C:3]([c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[N:10]([CH2:11][CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1)[CH...
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)cc1
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccc1
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[c:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[c:10])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
50.4
[{"value": 50.4, "product": "Cl.C(C1=CC=CC=C1)N(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 45.6, "product": "Cl.C(C1=CC=CC=C1)N(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 400 mg (1.21 mmol) of 4-[3-(N-benzylamino)propylthio] pyridine dihydrochloride and 0.55 ml (4.00 mmol) of triethylamine in 5 ml of methylene chloride, 0.17 ml (1.45 mmol) of benzoyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The react...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccncc1.c1ccccc1
HCl
C(Cl)Cl
null
null
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)cc1>C(Cl)Cl>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9a9a1fc08b224050b6bc9bda7fc64182
NCc1ccccn1.OCCCSc1ccncc1>>c1ccc(CNCCCSc2ccncc2)nc1
NCC1=NC=CC=C1.OCCCSC1=CC=NC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl>>N1=C(C=CC=C1)CNCCCSC1=CC=NC=C1
[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH2:6])[n:17][cH:18]1.O[CH2:7][CH2:8][CH2:9][S:10][c:11]1[cH:12][cH:13][n:14][cH:15][cH:16]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][CH2:9][S:10][c:11]2[cH:12][cH:13][n:14][cH:15][cH:16]2)[n:17][cH:18]1
NCc1ccccn1.OCCCSc1ccncc1
c1ccc(CNCCCSc2ccncc2)nc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1ccc(CNCCCSc2ccncc2)nc1
O-[CH2;D2;+0:1]-[C:2]-[C:3].[#7;a:4]:[c:5]-[C:6]-[NH2;D1;+0:7]>>[#7;a:4]:[c:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[C:2]-[C:3]
25.4
[{"value": 25.4, "product": "N1=C(C=CC=C1)CNCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 24.4, "product": "N1=C(C=CC=C1)CNCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
To a solution of 5.26 g (31.1 mmol) of 4-(3-hydroxypropylthio)pyridine and 5.20 ml (37.3 mmol) of triethylamine in 150 ml of methylene chloride, 2.90 ml (37.3 mmol) of methanesulfonyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The reaction mixture was...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1ccncc1.c1ccncc1
HO-
C(Cl)Cl
80
null
NCc1ccccn1.OCCCSc1ccncc1>C(Cl)Cl>c1ccc(CNCCCSc2ccncc2)nc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c1f38a3c62784772a0ad020614ddd68f
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)nc1>>CC(=O)N(CCCSc1ccncc1)Cc1ccccn1
N1=C(C=CC=C1)CNCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C)(=O)Cl>>N1=C(C=CC=C1)CN(C(C)=O)CCCSC1=CC=NC=C1
Cl[C:2]([CH3:1])=[O:3].[NH:4]([CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][n:21]1>>[CH3:1][C:2](=[O:3])[N:4]([CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][n:21]1
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)nc1
CC(=O)N(CCCSc1ccncc1)Cc1ccccn1
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
c1ccc(CNCCCSc2ccncc2)nc1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[#7;a:4]:[c:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[#7;a:4]:[c:5]-[C:6]-[N;H0;D3;+0:7](-[C:8]-[C:9])-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
85.6
[{"value": 85.6, "product": "N1=C(C=CC=C1)CN(C(C)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.6, "product": "N1=C(C=CC=C1)CN(C(C)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.62 g (6.24 mmol) of 4-[3-(N-2pyridylmethylamino)propylthio]pyridine and 1.10 ml (7.80 mmol) of triethylamine in 10 ml of methylene chloride, 0.51 ml (7.80 mmol) of acetyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The reaction mixtu...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccncc1.c1ccncc1
HCl
C(Cl)Cl
null
null
CC(=O)Cl.c1ccc(CNCCCSc2ccncc2)nc1>C(Cl)Cl>CC(=O)N(CCCSc1ccncc1)Cc1ccccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f6517c3bd51c417b92bd4b78dfc8e915
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)nc1>>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccn1
N1=C(C=CC=C1)CNCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C1=CC=CC=C1)(=O)Cl>>N1=C(C=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1
Cl[C:2](=[O:1])[c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1.[NH:9]([CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1)[CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][n:26]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]([CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1)[CH2:2...
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)nc1
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccn1
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccn1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#7;a:6]:[c:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]>>[#7;a:6]:[c:7]-[C:8]-[N;H0;D3;+0:9](-[C:10]-[C:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
58.9
[{"value": 58.9, "product": "N1=C(C=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.9, "product": "N1=C(C=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.60 g (6.17 mmol) of 4-[3-(N-2-pyridylmethylamino)propylthio)pyridine and 1.05 ml (7.40 mmol) of triethylamine in 10 ml of methylene chloride, 0.86 ml (7.40 mmol) of benzoyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The reaction mix...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccncc1.c1ccncc1
HCl
C(Cl)Cl
null
null
O=C(Cl)c1ccccc1.c1ccc(CNCCCSc2ccncc2)nc1>C(Cl)Cl>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1ccccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9416feec1e0e4637adb9bb2ca9dd4492
O=C1c2ccccc2C(=O)N1CCCBr.Oc1ccncc1>>O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
OC1=CC=NC=C1.BrCCCN1C(C=2C(C1=O)=CC=CC2)=O.C1CCC2=NCCCN2CC1>>C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O
Br[CH2:14][CH2:13][CH2:12][N:11]1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10].[OH:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1
O=C1c2ccccc2C(=O)N1CCCBr.Oc1ccncc1
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
16.4
[{"value": 16.4, "product": "C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 16.4, "product": "C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
6
HOUR
To a solution of 4.76 g (50 mmol) of 4-hydroxypyridine and 14.75 g (55 mmol) of N-(3-bromopropyl)phthalimide in 80 ml of DMF was added 8.23 ml (55 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene. The mixture was stirred at room temperature for 6 hours. After the solvent was distilled off, the mixture was poured into water ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
HBr
CN(C)C=O
null
6
O=C1c2ccccc2C(=O)N1CCCBr.Oc1ccncc1>CN(C)C=O>O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-8ddd5dd4e0684c5fbacd7457ef7264ca
O=C1c2ccccc2C(=O)N1CCCCBr.Oc1ccncc1>>O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
OC1=CC=NC=C1.BrCCCCN1C(C=2C(C1=O)=CC=CC2)=O.C1CCC2=NCCCN2CC1>>C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O
Br[CH2:15][CH2:14][CH2:13][CH2:12][N:11]1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10].[OH:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
O=C1c2ccccc2C(=O)N1CCCCBr.Oc1ccncc1
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
17.8
[{"value": 17.2, "product": "C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 17.8, "product": "C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
7
HOUR
To a solution of 4.76 g (50 mmol) of 4-hydroxypyridine and 15.52 g (55 mmol) of N-(4bromobutyl)phthalimide in 80 ml of DMF was added 8.23 ml (5 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene. The mixture was stirred at room temperature for 7 hours. After the solvent was distilled off, the mixture was poured into water and...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
HBr
CN(C)C=O
null
7
O=C1c2ccccc2C(=O)N1CCCCBr.Oc1ccncc1>CN(C)C=O>O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9078b706d8484760a405cf9de643eb4b
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>>NCCCOc1ccncc1
O.NN.C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O.C(C)(=O)OCC>>NCCCOC1=CC=NC=C1
O=C1c2ccccc2C(=O)[N:1]1[CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1>>[NH2:1][CH2:2][CH2:3][CH2:4][O:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
NCCCOc1ccncc1
null
null
C(C)O
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
c1ccncc1
O=C1-[N;H0;D3;+0:1](-[C:2]-[C:3])-C(=O)-c2:c:c:c:c:c:2-1>>[C:3]-[C:2]-[NH2;D1;+0:1]
99.5
[{"value": 99.5, "product": "NCCCOC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 0.1, "product": "NCCCOC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
Hydrazine monohydrate [2.99 ml (61.6 mmol)] was added to a suspension of 5.80 g (20.5 mol) of 4-(3-phthalimidopropyloxy)pyridine in 50 ml of ethanol, and the mixture was stirred at room temperature for 3 hours. 100 ml of ethyl acetate was added and insoluble materials were filtered off. The volatile component in the fi...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccncc1
HO-
C(C)O
null
3
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>C(C)O>NCCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cc46162356544f669d9d762c2d76ff4b
CC(C)(C)C(=O)Cl.NCCCOc1ccncc1>>CC(C)(C)C(=O)NCCCOc1ccncc1
NCCCOC1=CC=NC=C1.C(C)N(CC)CC.C(C(C)(C)C)(=O)Cl>>C(C(C)(C)C)(=O)NCCCOC1=CC=NC=C1
Cl[C:5]([C:2]([CH3:1])([CH3:3])[CH3:4])=[O:6].[NH2:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][n:15][cH:16][cH:17]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[C:5](=[O:6])[NH:7][CH2:8][CH2:9][CH2:10][O:11][c:12]1[cH:13][cH:14][n:15][cH:16][cH:17]1
CC(C)(C)C(=O)Cl.NCCCOc1ccncc1
CC(C)(C)C(=O)NCCCOc1ccncc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccncc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[C;D1;H3:6]
77.3
[{"value": 77.3, "product": "C(C(C)(C)C)(=O)NCCCOC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.3, "product": "C(C(C)(C)C)(=O)NCCCOC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 700 mg (4.60 mmol) of 4-(3-aminopropyloxy)pyridine and 0.77 ml (5.52 mmol) of triethylamine in 30 ml of methylene chloride, 0.57 ml (4.63 mmol) of pivaloyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 1.5 hours. The reaction mixture was washed succ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1
HCl
C(Cl)Cl
null
null
CC(C)(C)C(=O)Cl.NCCCOc1ccncc1>C(Cl)Cl>CC(C)(C)C(=O)NCCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-21c6230f734548bda488fe39bf56a85a
NCCCOc1ccncc1.O=C(Cl)c1cccnc1>>O=C(NCCCOc1ccncc1)c1cccnc1
NCCCOC1=CC=NC=C1.C(C)N(CC)CC.Cl.C(C1=CN=CC=C1)(=O)Cl>>C(C1=CN=CC=C1)(=O)NCCCOC1=CC=NC=C1
[NH2:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1.Cl[C:2](=[O:1])[c:14]1[cH:15][cH:16][cH:17][n:18][cH:19]1>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][n:18][cH:19]1
NCCCOc1ccncc1.O=C(Cl)c1cccnc1
O=C(NCCCOc1ccncc1)c1cccnc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCCCOc1ccncc1)c1cccnc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[#7;a:6]:[c:7]
88.7
[{"value": 85.8, "product": "C(C1=CN=CC=C1)(=O)NCCCOC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 88.7, "product": "C(C1=CN=CC=C1)(=O)NCCCOC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 700 mg (4.60 mmol) of 4-(3-aminopropyloxy)pyridine and 1.54 ml (11.0 mmol) of triethylamine in 30 ml of methylene chloride, 830 mg (4.66 mmol) of nicotinoyl chloride hydrochloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 1.5 hours. The reaction mixture ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccncc1
HCl
C(Cl)Cl
null
null
NCCCOc1ccncc1.O=C(Cl)c1cccnc1>C(Cl)Cl>O=C(NCCCOc1ccncc1)c1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-6aaafa271c764cd7bffa5143f19ab4b3
NCCCOc1ccncc1.O=C(Cl)c1cccs1>>O=C(NCCCOc1ccncc1)c1cccs1
NCCCOC1=CC=NC=C1.C(C)N(CC)CC.C1(=CC=CS1)C(=O)Cl>>C1(=CC=CS1)C(=O)NCCCOC1=CC=NC=C1
[NH2:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1.Cl[C:2](=[O:1])[c:14]1[cH:15][cH:16][cH:17][s:18]1>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][s:18]1
NCCCOc1ccncc1.O=C(Cl)c1cccs1
O=C(NCCCOc1ccncc1)c1cccs1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCCCOc1ccncc1)c1cccs1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#16;a:5]:[c:6].[C:7]-[C:8]-[NH2;D1;+0:9]>>[C:7]-[C:8]-[NH;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[#16;a:5]:[c:6]
70.4
[{"value": 70.0, "product": "C1(=CC=CS1)C(=O)NCCCOC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 70.4, "product": "C1(=CC=CS1)C(=O)NCCCOC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 700 mg (4.60 mmol) of 4-(3-aminopropyloxy)pyridine and 0.77 ml (5.52 mmol) of triethylamine in 30 ml of methylene chloride, 0.50 ml (4.68 mmol) of thenoyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 1.5 hours. The reaction mixture was washed succe...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccsc1
HCl
C(Cl)Cl
null
null
NCCCOc1ccncc1.O=C(Cl)c1cccs1>C(Cl)Cl>O=C(NCCCOc1ccncc1)c1cccs1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-531cdb8862114a2b971e4b24c41a9947
O=C(Cl)c1ccccc1.c1csc(CNCCCSc2ccncc2)c1>>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1cccs1
S1C(=CC=C1)CNCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C1=CC=CC=C1)(=O)Cl>>S1C(=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1
Cl[C:2](=[O:1])[c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1.[NH:9]([CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1)[CH2:20][c:21]1[cH:22][cH:23][cH:24][s:25]1>>[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][cH:8]1)[N:9]([CH2:10][CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1)[CH2:20][c:21...
O=C(Cl)c1ccccc1.c1csc(CNCCCSc2ccncc2)c1
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1cccs1
null
null
C(Cl)Cl
Acylation
N-alkylation of secondary amines with alkyl halides
b92e0bfd3d683c1f2a209adfe70a67ad7cb0d87749eb59e8fe0cf1689bc291e0
96cb0a2fed10552c5770a45a2d6523b47ac3e38928b4a9c698d8577451182dcd
O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1cccs1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[#16;a:6]:[c:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]>>[#16;a:6]:[c:7]-[C:8]-[N;H0;D3;+0:9](-[C:10]-[C:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
35.9
[{"value": 35.9, "product": "S1C(=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 35.9, "product": "S1C(=CC=C1)CN(C(C1=CC=CC=C1)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 2.5 g (9.45 mmol) of 4-[3-(N-(2-thienylmethyl)amino)propylthio]pyridine and 1.32 ml (9.45 mmol) of triethylamine in 50 ml of methylene chloride, 1.1 ml (9.45 mmol) of benzoyl chloride was added under ice-cooling with stirring. The mixture was stirred at room temperature for 30 minutes. The reaction mix...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Secondary amine
Tertiary amide
null
null
c1ccccc1.c1ccncc1.c1ccsc1
HCl
C(Cl)Cl
null
null
O=C(Cl)c1ccccc1.c1csc(CNCCCSc2ccncc2)c1>C(Cl)Cl>O=C(c1ccccc1)N(CCCSc1ccncc1)Cc1cccs1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e49129c86d4242ec88a7e0cdf427a563
CCCCCCCCCCCCN.OCCCSc1ccncc1>>CCCCCCCCCCCCNCCCSc1ccncc1
OCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(CCCCCCCCCCC)N.CS(=O)(=O)Cl>>C(CCCCCCCCCCC)NCCCSC1=CC=NC=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].O[CH2:14][CH2:15][CH2:16][S:17][c:18]1[cH:19][cH:20][n:21][cH:22][cH:23]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][S:17][c:18]1[cH:19][cH:20][n:2...
CCCCCCCCCCCCN.OCCCSc1ccncc1
CCCCCCCCCCCCNCCCSc1ccncc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1ccncc1
O-[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]
29.5
[{"value": 29.5, "product": "C(CCCCCCCCCCC)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 29.5, "product": "C(CCCCCCCCCCC)NCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
In 120 ml of methylene chloride was dissolved 5.60 g (33.1 mmol) of 4-(3-hydroxypropylthio)pyridine and 5.53 ml (39.7 mmol) of triethylamine. 3.07 ml (39.7 mmol) of methanesulfonyl chloride was added, and the mixture was stirred at room temperature for 30 minutes. The reaction mixture was washed with a saturated aqueou...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1ccncc1
HO-
C(Cl)Cl
null
0.5
CCCCCCCCCCCCN.OCCCSc1ccncc1>C(Cl)Cl>CCCCCCCCCCCCNCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c02e45927e744116961d5f80a7284f40
O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CCl.Sc1ccncc1>>O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CSc1ccncc1
ClCN1C(C=2C(C1=O)=CC(=CC2)[N+](=O)[O-])=O.SC1=CC=NC=C1.C(C)N(CC)CC>>[N+](=O)([O-])C=1C=C2C(C(=O)N(C2=O)CSC2=CC=NC=C2)=CC1
Cl[CH2:15][N:14]1[C:2](=[O:1])[c:3]2[cH:4][cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]2[C:12]1=[O:13].[SH:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][c:6]([N+:7](=[O:8])[O-:9])[cH:10][c:11]2[C:12](=[O:13])[N:14]1[CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CCl.Sc1ccncc1
O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CSc1ccncc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
thioether_nucl_sub
670a330769b87d9fd3df1128eae04bdefd1a0d70c3e632885aa0e6a5b15fccc1
fcd4bd1a4380f5eecf1a2477e13ea8343f264aec0388929401fe7448dc3025d8
O=C1c2ccccc2C(=O)N1CSc1ccncc1
Cl-[CH2;D2;+0:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]-[C:7]-1=[O;D1;H0:8].[SH;D1;+0:9]-[c:10]1:[c:11]:[c:12]:[#7;a:13]:[c:14]:[c:15]:1>>[O;D1;H0:4]=[C:3]1-[c:5]:[c:6]-[C:7](=[O;D1;H0:8])-[#7:2]-1-[CH2;D2;+0:1]-[S;H0;D2;+0:9]-[c:10]1:[c:11]:[c:12]:[#7;a:13]:[c:14]:[c:15]:1
63.1
[{"value": 63.1, "product": "[N+](=O)([O-])C=1C=C2C(C(=O)N(C2=O)CSC2=CC=NC=C2)=CC1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.1, "product": "[N+](=O)([O-])C=1C=C2C(C(=O)N(C2=O)CSC2=CC=NC=C2)=CC1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
N-Chloromethyl-4-nitrophthalimide [2.89 g (12 mmol)] was added under ice-cooling with stirring to a suspension of 1.11 g (10 mmol) of 4-mercaptopyridine and 1.4 ml (12 mmol) of triethylamine in 50 ml of ethanol. The mixture was stirred at room temperature for 16 hours. The solvent was distilled off and the residue was ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Substituted dicarboximide.Aromatic thiol
Substituted dicarboximide.Monosulfide
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
HCl
C(C)O
null
16
O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CCl.Sc1ccncc1>C(C)O>O=C1c2ccc([N+](=O)[O-])cc2C(=O)N1CSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d07aa11821184f368af462667f02ae8c
O=C1c2ccccc2C(=O)N1CSc1ccncc1>>O=C1c2ccccc2C(O)N1CSc1ccncc1
C1(C=2C(C(N1CSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+].C(C)(=O)O>>OC1N(C(C2=CC=CC=C12)=O)CSC1=CC=NC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1
O=C1c2ccccc2C(=O)N1CSc1ccncc1
O=C1c2ccccc2C(O)N1CSc1ccncc1
null
null
CO
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CSc1ccncc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
58.3
[{"value": 58.3, "product": "OC1N(C(C2=CC=CC=C12)=O)CSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.3, "product": "OC1N(C(C2=CC=CC=C12)=O)CSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a solution of 4.01 g (14.8 mmol) of 4-(phthalimidomethylthio)pyridine in 25 ml of methanol, a solution of 1.08 g (29.7 mmol) of sodium borohydride in 20 ml of methanol was added. The mixture was stirred at room temperature for 4 hours. Glacial acetic acid (0.5 ml) was added to quench the reaction, and then the solve...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
CO
null
4
O=C1c2ccccc2C(=O)N1CSc1ccncc1>CO>O=C1c2ccccc2C(O)N1CSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-73cf2bb5afde4483b79e29dae5dd822c
O=C1c2ccccc2C(=O)N1CCBr.Oc1ccncc1>>O=C1c2ccccc2C(=O)N1CCOc1ccncc1
OC1=CC=NC=C1.BrCCN1C(C=2C(C1=O)=CC=CC2)=O.C1CCC2=NCCCN2CC1>>C1(C=2C(C(N1CCOC1=CC=NC=C1)=O)=CC=CC2)=O
Br[CH2:13][CH2:12][N:11]1[C:2](=[O:1])[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9]1=[O:10].[OH:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][O:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1
O=C1c2ccccc2C(=O)N1CCBr.Oc1ccncc1
O=C1c2ccccc2C(=O)N1CCOc1ccncc1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C1c2ccccc2C(=O)N1CCOc1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[#7:3](-[C:4]=[O;D1;H0:5])-[C:6]=[O;D1;H0:7].[OH;D1;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1>>[O;D1;H0:7]=[C:6]-[#7:3](-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1)-[C:4]=[O;D1;H0:5]
3.1
[{"value": 3.1, "product": "C1(C=2C(C(N1CCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 3.1, "product": "C1(C=2C(C(N1CCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
32
HOUR
To a solution of 4.76 g (50 mmol) of 4-hydroxypyridine and 13.97 g (55 mmol) of N-(2-bromoethyl)phthalimide in 80 ml of DMF, 8.23 ml (55 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added. The mixture was stirred at room temperature for 32 hours. After the solvent was distilled off, the mixture was poured into water...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
HBr
CN(C)C=O
null
32
O=C1c2ccccc2C(=O)N1CCBr.Oc1ccncc1>CN(C)C=O>O=C1c2ccccc2C(=O)N1CCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-65c49a041cb1404cbaeaf61fdae85da3
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>>O=C1c2ccccc2C(O)N1CCCOc1ccncc1
[BH4-].[Na+].C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O>>OC1N(C(C2=CC=CC=C12)=O)CCCOC1=CC=NC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][CH2:13][CH2:14][O:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
O=C1c2ccccc2C(O)N1CCCOc1ccncc1
null
null
C(C)O
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CCCOc1ccncc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
54.2
[{"value": 54.2, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCOC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.2, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCOC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
Sodium borohydride [1.89 g (50 mmol)] was added to a solution of 2.82 g (10.0 mmol) of 4-(3-phthalimidopropyloxy)pyridine in 150 ml of ethanol. The mixture was stirred at room temperature for 15 minutes. After the solvent was distilled off, brine was added to the residue. The mixture was extracted with chloroform and d...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
C(C)O
null
0.25
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>C(C)O>O=C1c2ccccc2C(O)N1CCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4dbf302df4464d14a210fcb5a6554452
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>>O=C(NCCCOc1ccncc1)c1ccccc1CO
[BH4-].[Na+].C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O>>OCC1=C(C(=O)NCCCOC2=CC=NC=C2)C=CC=C1
[O:1]=[C:2]1[N:3]([CH2:4][CH2:5][CH2:6][O:7][c:8]2[cH:9][cH:10][n:11][cH:12][cH:13]2)[C:20](=[O:21])[c:19]2[c:14]1[cH:15][cH:16][cH:17][cH:18]2>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[CH2:20][OH:21]
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
O=C(NCCCOc1ccncc1)c1ccccc1CO
null
null
C(C)O
Reduction
OtherReaction
d08271d0eab427d20e9711b6b92c8b05348d13735b33b77d21de7bf6727ba260
a2b47173662031a6246dc71f980ac535bbdf2e2fb828bdc621ee9b3169b07859
O=C(NCCCOc1ccncc1)c1ccccc1
[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[CH2;D2;+0:9]-[OH;D1;+0:10]):[c:8]
52
[{"value": 52.0, "product": "OCC1=C(C(=O)NCCCOC2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 52.0, "product": "OCC1=C(C(=O)NCCCOC2=CC=NC=C2)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
Sodium borohydride [3.78 g (100 mmol)] was added to a solution of 2.82 g (10.0 mmol) of 4-(3-phthalimidopropyloxy)pyridine in 150 ml of ethanol. The mixture was stirred at room temperature for 3 hours. After the solvent was distiled off, brine was added to the residue. The mixture was extracted with chloroform and drie...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary amide.Primary alcohol
c1ccc2c(c1)C[NH]C2
null
c1ccncc1.c1ccccc1
null
C(C)O
null
3
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>C(C)O>O=C(NCCCOc1ccncc1)c1ccccc1CO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b2748f3faf0e4cadb94edae14f08f39f
O=C1c2ccccc2C(=O)N1CCSc1ccncc1>>O=C(NCCSc1ccncc1)c1ccccc1CO
C(C)O.C(C)(=O)OCC.C1(C=2C(C(N1CCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OCC1=C(C(=O)NCCSC2=CC=NC=C2)C=CC=C1
[O:1]=[C:2]1[N:3]([CH2:4][CH2:5][S:6][c:7]2[cH:8][cH:9][n:10][cH:11][cH:12]2)[C:19](=[O:20])[c:18]2[c:13]1[cH:14][cH:15][cH:16][cH:17]2>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][n:10][cH:11][cH:12]1)[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[CH2:19][OH:20]
O=C1c2ccccc2C(=O)N1CCSc1ccncc1
O=C(NCCSc1ccncc1)c1ccccc1CO
null
null
C(C)O
Reduction
OtherReaction
d08271d0eab427d20e9711b6b92c8b05348d13735b33b77d21de7bf6727ba260
a2b47173662031a6246dc71f980ac535bbdf2e2fb828bdc621ee9b3169b07859
O=C(NCCSc1ccncc1)c1ccccc1
[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[CH2;D2;+0:9]-[OH;D1;+0:10]):[c:8]
77.8
[{"value": 77.8, "product": "OCC1=C(C(=O)NCCSC2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 77.7, "product": "OCC1=C(C(=O)NCCSC2=CC=NC=C2)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 2.84 g (10.0 mmol) of 4-(2-phthalimidoethylthio)pyridine in 150 ml of ethanol, 3.78 g (100 mmol) of sodium borohydride was added, and the mixture was stirred at room temperature for 3 hours. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with chlo...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary amide.Primary alcohol
c1ccc2c(c1)C[NH]C2
null
c1ccncc1.c1ccccc1
null
C(C)O
null
3
O=C1c2ccccc2C(=O)N1CCSc1ccncc1>C(C)O>O=C(NCCSc1ccncc1)c1ccccc1CO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-971581ad4e8b4fdcb8263bf8c74245a7
O=C1c2ccccc2C(=O)N1CCSc1ccncc1>>O=C1c2ccccc2C(O)N1CCSc1ccncc1
C1(C=2C(C(N1CCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OC1N(C(C2=CC=CC=C12)=O)CCSC1=CC=NC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1
O=C1c2ccccc2C(=O)N1CCSc1ccncc1
O=C1c2ccccc2C(O)N1CCSc1ccncc1
null
null
C(C)O
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CCSc1ccncc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
63.4
[{"value": 63.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 63.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
To a solution of 5.69 g (20.0 mmol) of 4-(2-phthalimidoethylthio)pyridine in 150 ml of ethanol, 2.27 g (60 mmol) of sodium borohydride was added, and the mixture was stirred at room temperature for 15 minutes. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with ch...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
C(C)O
null
0.25
O=C1c2ccccc2C(=O)N1CCSc1ccncc1>C(C)O>O=C1c2ccccc2C(O)N1CCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a5cf6e169638414f92985c34a5a2a735
O=C(NCCSc1ccncc1)c1ccccc1CO>>O=C1c2ccccc2CN1CCSc1ccncc1
OCC1=C(C(=O)NCCSC2=CC=NC=C2)C=CC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl>>C1(N(CC2=CC=CC=C12)CCSC1=CC=NC=C1)=O
O[CH2:9][c:8]1[c:3]([C:2](=[O:1])[NH:10][CH2:11][CH2:12][S:13][c:14]2[cH:15][cH:16][n:17][cH:18][cH:19]2)[cH:4][cH:5][cH:6][cH:7]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][N:10]1[CH2:11][CH2:12][S:13][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1
O=C(NCCSc1ccncc1)c1ccccc1CO
O=C1c2ccccc2CN1CCSc1ccncc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
1b80d36cd86c1f0c2ab7ea6bfe3b27d1140e09d54a6c4337a116e3cf30d8d950
53e9ea6bdc0d22524e13e79960e55c0106a6cc8b9aed21c29c8c6a7e9792ce5b
O=C1c2ccccc2CN1CCSc1ccncc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:9]-[C:8]-[N;H0;D3;+0:7]1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5]-1=[O;D1;H0:6]
57.6
[{"value": 57.6, "product": "C1(N(CC2=CC=CC=C12)CCSC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 57.6, "product": "C1(N(CC2=CC=CC=C12)CCSC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.153 g (4.0 mmol) of 4-[2-(2-hydroxymethylbenzoyl)aminoethylthio]pyridine and 1.68 ml (12.1 mmol) of triethylamine in 50 ml of methylene chloride, 0.62 ml (8.0 mmol) of methanesulfonyl chloride was added with stirring at room temperature, and the mixture was stirred at room temperature for 30 minutes....
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary alcohol
Tertiary amide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
HO-
C(Cl)Cl
null
null
O=C(NCCSc1ccncc1)c1ccccc1CO>C(Cl)Cl>O=C1c2ccccc2CN1CCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b088d415086140f09c65a666de315251
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>>O=C(NCCCCSc1ccncc1)c1ccccc1CO
C1(C=2C(C(N1CCCCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OCC1=C(C(=O)NCCCCSC2=CC=NC=C2)C=CC=C1
[O:1]=[C:2]1[N:3]([CH2:4][CH2:5][CH2:6][CH2:7][S:8][c:9]2[cH:10][cH:11][n:12][cH:13][cH:14]2)[C:21](=[O:22])[c:20]2[c:15]1[cH:16][cH:17][cH:18][cH:19]2>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[c:15]1[cH:16][cH:17][cH:18][cH:19][c:20]1[CH2:21][OH:22]
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1
O=C(NCCCCSc1ccncc1)c1ccccc1CO
null
null
C(C)O
Reduction
OtherReaction
d08271d0eab427d20e9711b6b92c8b05348d13735b33b77d21de7bf6727ba260
a2b47173662031a6246dc71f980ac535bbdf2e2fb828bdc621ee9b3169b07859
O=C(NCCCCSc1ccncc1)c1ccccc1
[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[CH2;D2;+0:9]-[OH;D1;+0:10]):[c:8]
73.2
[{"value": 73.1, "product": "OCC1=C(C(=O)NCCCCSC2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.2, "product": "OCC1=C(C(=O)NCCCCSC2=CC=NC=C2)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
14
HOUR
To a solution of 6.25 g of (20.0 mmol) of 4-(4-phthalimidobutylthio)pyridine in 300 ml of ethanol, 7.57 g (200 mmol) of sodium borohydride was added, and the mixture was stirred at room temperature for 14 hours. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with ...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary amide.Primary alcohol
c1ccc2c(c1)C[NH]C2
null
c1ccncc1.c1ccccc1
null
C(C)O
null
14
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>C(C)O>O=C(NCCCCSc1ccncc1)c1ccccc1CO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-923c49f34b564c8dbe84a85dc91bb505
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>>O=C1c2ccccc2C(O)N1CCCCSc1ccncc1
C1(C=2C(C(N1CCCCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OC1N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1
O=C1c2ccccc2C(O)N1CCCCSc1ccncc1
null
null
C(C)O
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CCCCSc1ccncc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
27.5
[{"value": 27.5, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 0.0, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2.5
HOUR
To a solution of 6.25 g (20.0 mol) of 4-(4-phthalimidobutylthio)pyridine in 300 ml of ethanol, 1.51 g (40 mmol) of sodium borohydride was added, and the mixture was stirred at room temperature for 2.5 hours. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with chlo...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
C(C)O
null
2.5
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>C(C)O>O=C1c2ccccc2C(O)N1CCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f7c946d278a44fe28f799ef9783e5d4b
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1>>O=C(NCCCSc1ccncc1)c1ccccc1CO
C1(C=2C(C(N1CCCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OCC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1
[O:1]=[C:2]1[N:3]([CH2:4][CH2:5][CH2:6][S:7][c:8]2[cH:9][cH:10][n:11][cH:12][cH:13]2)[C:20](=[O:21])[c:19]2[c:14]1[cH:15][cH:16][cH:17][cH:18]2>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][cH:18][c:19]1[CH2:20][OH:21]
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1
O=C(NCCCSc1ccncc1)c1ccccc1CO
null
null
C(C)O
Reduction
OtherReaction
d08271d0eab427d20e9711b6b92c8b05348d13735b33b77d21de7bf6727ba260
a2b47173662031a6246dc71f980ac535bbdf2e2fb828bdc621ee9b3169b07859
O=C(NCCCSc1ccncc1)c1ccccc1
[C:1]-[C:2]-[N;H0;D3;+0:3]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;H0;D1;+0:10]>>[C:1]-[C:2]-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[CH2;D2;+0:9]-[OH;D1;+0:10]):[c:8]
78.2
[{"value": 78.2, "product": "OCC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.2, "product": "OCC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 5.97 g (20.0 mmol) of 4-(3-phthalimidopropylthio)pyridine in 300 ml of ethanol, 7.57 g (200 mmol) of sodium borohydride was added, and stirred at room temperature for 24 hours. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with chloroform and the...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary amide.Primary alcohol
c1ccc2c(c1)C[NH]C2
null
c1ccncc1.c1ccccc1
null
C(C)O
null
24
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1>C(C)O>O=C(NCCCSc1ccncc1)c1ccccc1CO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-84539951ddac46c78e3e61887eb06d08
O=C(NCCCCSc1ccncc1)c1ccccc1CO>>O=C1c2ccccc2CN1CCCCSc1ccncc1
OCC1=C(C(=O)NCCCCSC2=CC=NC=C2)C=CC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl>>C1(N(CC2=CC=CC=C12)CCCCSC1=CC=NC=C1)=O
O[CH2:9][c:8]1[c:3]([C:2](=[O:1])[NH:10][CH2:11][CH2:12][CH2:13][CH2:14][S:15][c:16]2[cH:17][cH:18][n:19][cH:20][cH:21]2)[cH:4][cH:5][cH:6][cH:7]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][N:10]1[CH2:11][CH2:12][CH2:13][CH2:14][S:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1
O=C(NCCCCSc1ccncc1)c1ccccc1CO
O=C1c2ccccc2CN1CCCCSc1ccncc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
1b80d36cd86c1f0c2ab7ea6bfe3b27d1140e09d54a6c4337a116e3cf30d8d950
53e9ea6bdc0d22524e13e79960e55c0106a6cc8b9aed21c29c8c6a7e9792ce5b
O=C1c2ccccc2CN1CCCCSc1ccncc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:9]-[C:8]-[N;H0;D3;+0:7]1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5]-1=[O;D1;H0:6]
72.1
[{"value": 72.1, "product": "C1(N(CC2=CC=CC=C12)CCCCSC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.1, "product": "C1(N(CC2=CC=CC=C12)CCCCSC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.58 g (5.0 mmol) of 4-[4-(2-hydroxymethylbenzoyl)aminobutylthio]pyridine and 2.09 ml (15.0 mmol) of triethylamine in 50 ml of methylene chloride, 0.77 ml (10.0 mmol) of methanesulfonyl chloride was added with stirring at room temperature, and the mixture was stirred at room temperature for 30 minutes....
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary alcohol
Tertiary amide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
HO-
C(Cl)Cl
null
null
O=C(NCCCCSc1ccncc1)c1ccccc1CO>C(Cl)Cl>O=C1c2ccccc2CN1CCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f61c39e9b64e46f3aa67a30fba7b886d
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1>>O=C1c2ccccc2C(O)N1CCCSc1ccncc1
C(C)O.C(C)(=O)OCC.C1(C=2C(C(N1CCCSC1=CC=NC=C1)=O)=CC=CC2)=O.[BH4-].[Na+]>>OC1N(C(C2=CC=CC=C12)=O)CCCSC1=CC=NC=C1
[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[C:9](=[O:10])[N:11]1[CH2:12][CH2:13][CH2:14][S:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH:9]([OH:10])[N:11]1[CH2:12][CH2:13][CH2:14][S:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1
O=C1c2ccccc2C(O)N1CCCSc1ccncc1
null
null
C(C)O
Reduction
OtherReaction
e8ffc87e9d14ec555652bcd3de186a7602297c1d65bf6096cdb1ce7e169ed644
6c2222fa5333790df8c936ae3761255cb080c6e237292637f62137781815b926
O=C1c2ccccc2CN1CCCSc1ccncc1
[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[C;H0;D3;+0:8]-1=[O;H0;D1;+0:9]>>[C:1]-[#7:2]1-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](:[c:7])-[CH;D3;+0:8]-1-[OH;D1;+0:9]
54.4
[{"value": 54.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.4, "product": "OC1N(C(C2=CC=CC=C12)=O)CCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a solution of 5.97 g (20.0 mmol) of 4-(3-phthalimidopropylthio)pyridine in 300 ml of ethanol, 1.51 g (40 mmol) of sodium borohydride was added, and the mixture was stirred at room temperature for 5 hours. The solvent was distilled off and saturated saline was added to the residue. The mixture was extracted with chlo...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Secondary alcohol
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
C(C)O
null
5
O=C1c2ccccc2C(=O)N1CCCSc1ccncc1>C(C)O>O=C1c2ccccc2C(O)N1CCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0be3a0bcf2234748992476eebd2f65be
O=C(NCCCSc1ccncc1)c1ccccc1CO>>O=C1c2ccccc2CN1CCCSc1ccncc1
OCC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1.C(C)N(CC)CC.CS(=O)(=O)Cl>>C1(N(CC2=CC=CC=C12)CCCSC1=CC=NC=C1)=O
O[CH2:9][c:8]1[c:3]([C:2](=[O:1])[NH:10][CH2:11][CH2:12][CH2:13][S:14][c:15]2[cH:16][cH:17][n:18][cH:19][cH:20]2)[cH:4][cH:5][cH:6][cH:7]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][N:10]1[CH2:11][CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1
O=C(NCCCSc1ccncc1)c1ccccc1CO
O=C1c2ccccc2CN1CCCSc1ccncc1
null
null
C(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
1b80d36cd86c1f0c2ab7ea6bfe3b27d1140e09d54a6c4337a116e3cf30d8d950
53e9ea6bdc0d22524e13e79960e55c0106a6cc8b9aed21c29c8c6a7e9792ce5b
O=C1c2ccccc2CN1CCCSc1ccncc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:9]-[C:8]-[N;H0;D3;+0:7]1-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5]-1=[O;D1;H0:6]
78.9
[{"value": 78.9, "product": "C1(N(CC2=CC=CC=C12)CCCSC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 78.8, "product": "C1(N(CC2=CC=CC=C12)CCCSC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.51 g (5.0 mmol) of 4-[3-(2-hydroxymethylbenzoyl)aminopropylthio]pyridine and 2.09 ml (15.0 mmol) of triethylamine in 50 ml of methylene chloride, 0.77 ml (10.0 mmol) of methanesulfonyl chloride was added with stirring at room temperature, and the mixture was stirred at room temperature for 30 minutes...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary alcohol
Tertiary amide
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
HO-
C(Cl)Cl
null
null
O=C(NCCCSc1ccncc1)c1ccccc1CO>C(Cl)Cl>O=C1c2ccccc2CN1CCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4a5162e35a304121b841b3e3f39d8e9f
CN.O=C1c2ccccc2C(=O)N1CSc1ccncc1>>CNC(=O)c1ccccc1C(=O)NCSc1ccncc1
CN.CO.C1(C=2C(C(N1CSC1=CC=NC=C1)=O)=CC=CC2)=O.CN.CO>>CNC(=O)C1=C(C(=O)NCSC2=CC=NC=C2)C=CC=C1
[CH3:1][NH2:2].[C:3]1(=[O:4])[c:5]2[cH:6][cH:7][cH:8][cH:9][c:10]2[C:11](=[O:12])[N:13]1[CH2:14][S:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1>>[CH3:1][NH:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[C:11](=[O:12])[NH:13][CH2:14][S:15][c:16]1[cH:17][cH:18][n:19][cH:20][cH:21]1
CN.O=C1c2ccccc2C(=O)N1CSc1ccncc1
CNC(=O)c1ccccc1C(=O)NCSc1ccncc1
null
null
C(Cl)(Cl)Cl
Acylation
OtherReaction
66718301acef3d8bc25ae8613c1648aa67ee84cf1a582b43da3ed3cccd3e499c
c5dbbff33268430c8bfa22331d710773ca50cd979a5fb6dcb4356e0495eb059b
O=C(NCSc1ccncc1)c1ccccc1
[#16:1]-[C:2]-[N;H0;D3;+0:3]1-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](:[c:8])-[C;H0;D3;+0:9]-1=[O;D1;H0:10].[C;D1;H3:11]-[NH2;D1;+0:12]>>[#16:1]-[C:2]-[NH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[c:6]:[c:7](-[C;H0;D3;+0:9](=[O;D1;H0:10])-[NH;D2;+0:12]-[C;D1;H3:11]):[c:8]
35.1
[{"value": 35.1, "product": "CNC(=O)C1=C(C(=O)NCSC2=CC=NC=C2)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
To a solution of 6.76 g (25.0 mmol) of 4-phthalimidomethylthiopyridine in 100 ml of chloroform, 5 ml of 40% methylamine-methanol solution was added, and the mixture was stirred at room temperature for 3 hours. Additional 5 ml of 40% methylamine-methanol solution was added, and the mixture was stirred at room temperatur...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide.Primary amine
Secondary amide.Secondary amide
c1ccc2c(c1)C[NH]C2
null
c1ccccc1.c1ccncc1
null
C(Cl)(Cl)Cl
null
3
CN.O=C1c2ccccc2C(=O)N1CSc1ccncc1>C(Cl)(Cl)Cl>CNC(=O)c1ccccc1C(=O)NCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c962e1c87c844b4594420eb59c04a717
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>>O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O.Cl.CO>>Cl.C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O
[O:2]=[C:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1>>[O:2]=[C:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][O:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
null
64.8
[{"value": 64.8, "product": "Cl.C1(C=2C(C(N1CCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.41 g (5.0 mmol) of 4-(3-phthalimidopropyloxy)pyridine in 20 ml of methanol, 10 ml of hydrogen chloride-methanol was added. The solvent was distilled off and acetone was added to the residue. The resulting crystals were collected by filtration and washed with acetone to give 1.03 g of the desired comp...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
CO
null
null
O=C1c2ccccc2C(=O)N1CCCOc1ccncc1>CO>O=C1c2ccccc2C(=O)N1CCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7872d2ae7d2e4c56a28ce90cf19a337d
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1>>O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O.Cl.CO>>Cl.C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O
[O:2]=[C:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][O:17][c:18]1[cH:19][cH:20][n:21][cH:22][cH:23]1>>[O:2]=[C:3]1[c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[C:10](=[O:11])[N:12]1[CH2:13][CH2:14][CH2:15][CH2:16][O:17][c:18]1[cH:19][cH:20][n:21][cH:22][cH:23]1
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
null
86.3
[{"value": 86.3, "product": "Cl.C1(C=2C(C(N1CCCCOC1=CC=NC=C1)=O)=CC=CC2)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a suspension of 1.48 g (5.0 mmol) of 4-(4-phthalimidobutyloxy)pyridine in 20 ml of methanol, 15 ml of hydrogen chloride-methanol was added and dissolve. The solvent was distilled off and the residue was crystallized from acetone-ether. The resulting crystals were collected by filtration and washed with ether to give...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccc2c(c1)C[NH]C2.c1ccncc1
null
CO
null
null
O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1>CO>O=C1c2ccccc2C(=O)N1CCCCOc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d55965f78437450f9aef72b94ae9f168
NCCCSc1ccncc1.O=C(O)c1cnccn1>>O=C(NCCCSc1ccncc1)c1cnccn1
Cl.Cl.NCCCSC1=CC=NC=C1.N1=C(C=NC=C1)C(=O)O.ON1C(CCC1=O)=O.Cl.C(C)N=C=NCCCN(C)C>>N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1
[NH2:3][CH2:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1.O[C:2](=[O:1])[c:14]1[cH:15][n:16][cH:17][cH:18][n:19]1>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][n:16][cH:17][cH:18][n:19]1
NCCCSc1ccncc1.O=C(O)c1cnccn1
O=C(NCCCSc1ccncc1)c1cnccn1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(NCCCSc1ccncc1)c1cnccn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:1.[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:1
34
[{"value": 34.0, "product": "N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 34.0, "product": "N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.00 g (8.06 mmol) of 2-pyrazinecarboxylic acid and 1.21 g (10.5 mmol) of N-hydroxysuccinimide in 70 ml of methylene-chloride, 1.85 g (9.67 mmol) of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (WSC) was added with stirring under ice-cooling, and the mixture was stirred at room temperatu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccncc1.c1cnccn1
HO-
C(Cl)Cl
null
null
NCCCSc1ccncc1.O=C(O)c1cnccn1>C(Cl)Cl>O=C(NCCCSc1ccncc1)c1cnccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-eada9dfe6c2247098ac3fc6740df3411
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>>NCCCCSc1ccncc1
C(C)(=O)OCC.C1(C=2C(C(N1CCCCSC1=CC=NC=C1)=O)=CC=CC2)=O.O.NN>>NCCCCSC1=CC=NC=C1
O=C1c2ccccc2C(=O)[N:1]1[CH2:2][CH2:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][n:10][cH:11][cH:12]1>>[NH2:1][CH2:2][CH2:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][n:10][cH:11][cH:12]1
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1
NCCCCSc1ccncc1
null
null
C(C)O
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
c1ccncc1
O=C1-[N;H0;D3;+0:1](-[C:2]-[C:3])-C(=O)-c2:c:c:c:c:c:2-1>>[C:3]-[C:2]-[NH2;D1;+0:1]
100.1
[{"value": 100.1, "product": "NCCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
4
HOUR
To a suspension of 12.50 g (40 mmol) of 4-(4-phthalimidobutylthio)pyridine in 200 ml of ethanol, 5.82 ml (120 mmol) of hydrazine monohydrate was added, and the mixture was stirred at room temperature for 4 hours. Then, 200 ml of ethyl acetate was-added, and the insoluble material was filtered off. The volatile componen...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccncc1
HO-
C(C)O
null
4
O=C1c2ccccc2C(=O)N1CCCCSc1ccncc1>C(C)O>NCCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b219b6ddb6814fc39f98caa37e23e5ac
NCCCCSc1ccncc1.O=C(Cl)c1ccccc1>>O=C(NCCCCSc1ccncc1)c1ccccc1
NCCCCSC1=CC=NC=C1.C(C)N(CC)CC.C(C1=CC=CC=C1)(=O)Cl>>C(C1=CC=CC=C1)(=O)NCCCCSC1=CC=NC=C1
[NH2:3][CH2:4][CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1.Cl[C:2](=[O:1])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][CH2:7][S:8][c:9]1[cH:10][cH:11][n:12][cH:13][cH:14]1)[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
NCCCCSc1ccncc1.O=C(Cl)c1ccccc1
O=C(NCCCCSc1ccncc1)c1ccccc1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCCCCSc1ccncc1)c1ccccc1
Cl-[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]
34.4
[{"value": 34.4, "product": "C(C1=CC=CC=C1)(=O)NCCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 34.3, "product": "C(C1=CC=CC=C1)(=O)NCCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 1.00 g (5.49 mmol) of 4-(4-aminobutylthio)pyridine and 0.92 ml (6.60 mmol) of triethylamine in 30 ml of methylene chloride, 0.67 ml (5.77 mmol) of benzoyl chloride was added with stirring under ice-cooling and the mixture was stirred at room temperature for 13 hours. The mixture was washed with saturat...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccccc1
HCl
C(Cl)Cl
null
null
NCCCCSc1ccncc1.O=C(Cl)c1ccccc1>C(Cl)Cl>O=C(NCCCCSc1ccncc1)c1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-eac925e9b2f940fdb1f04bc16132b520
O=C(NCO)c1cccnc1.Sc1ccncc1>>O=C(NCSc1ccncc1)c1cccnc1
SC1=CC=NC=C1.OCNC(C1=CN=CC=C1)=O>>N1=CC(=CC=C1)C(=O)NCSC1=CC=NC=C1
O[CH2:4][NH:3][C:2](=[O:1])[c:12]1[cH:13][cH:14][cH:15][n:16][cH:17]1.[SH:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1>>[O:1]=[C:2]([NH:3][CH2:4][S:5][c:6]1[cH:7][cH:8][n:9][cH:10][cH:11]1)[c:12]1[cH:13][cH:14][cH:15][n:16][cH:17]1
O=C(NCO)c1cccnc1.Sc1ccncc1
O=C(NCSc1ccncc1)c1cccnc1
null
null
FC(C(=O)O)(F)F
Heteroatom Alkylation and Arylation
OtherReaction
c119424abb7b621e5fb126e8156c5e4310815e8f2d609f48f2eb427b327d29ac
c1ccf05c97341d9cf75acae4c03f7d5a8212340a35905af6c8d60b4ccc775d1f
O=C(NCSc1ccncc1)c1cccnc1
O-[CH2;D2;+0:1]-[#7:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]:[#7;a:7].[SH;D1;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1>>[#7;a:7]:[c:6]:[c:5]-[C:3](=[O;D1;H0:4])-[#7:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1
15.9
[{"value": 15.9, "product": "N1=CC(=CC=C1)C(=O)NCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 15.9, "product": "N1=CC(=CC=C1)C(=O)NCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a mixture of 1.11 g (10 mmol) of 4-mercaptopyridine and 1.52 g (10 mmol) of N-(hydroxymethyl)nicotinamide, 30 ml of trifluoroacetic acid was added, and the mixture was stirred at room temperature for 1 hour. The solvent was distilled off and 30 ml of ethanol was added to the residue. The solvent was distilled off an...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Aromatic thiol
Monosulfide
null
null
c1ccncc1.c1ccncc1
HO-
FC(C(=O)O)(F)F
null
1
O=C(NCO)c1cccnc1.Sc1ccncc1>FC(C(=O)O)(F)F>O=C(NCSc1ccncc1)c1cccnc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-223b53ba401c4783b307cafc7579f4f4
CC1(C)NC(=O)NC1=O.ClCCCCSc1ccncc1>>CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O
C(C)(=O)OCC.CC1(C(NC(N1)=O)=O)C.ClCCCCSC1=CC=NC=C1.C1CCC2=NCCCN2CC1>>CC1(C(N(C(N1)=O)CCCCSC1=CC=NC=C1)=O)C
[CH3:1][C:2]1([CH3:3])[NH:4][C:5](=[O:6])[NH:7][C:19]1=[O:20].Cl[CH2:8][CH2:9][CH2:10][CH2:11][S:12][c:13]1[cH:14][cH:15][n:16][cH:17][cH:18]1>>[CH3:1][C:2]1([CH3:3])[NH:4][C:5](=[O:6])[N:7]([CH2:8][CH2:9][CH2:10][CH2:11][S:12][c:13]2[cH:14][cH:15][n:16][cH:17][cH:18]2)[C:19]1=[O:20]
CC1(C)NC(=O)NC1=O.ClCCCCSc1ccncc1
CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
4af6a84b2b0a49ef91adc20903acb4fb123b5aba0377309152c828b38a40c4ee
71185a09698a72d85470086badab5839fe3f255541f1fa400a1649b43c12f685
O=C1CNC(=O)N1CCCCSc1ccncc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[C:5]1-[C:6]-[#7:7]-[C:8](=[O;D1;H0:9])-[NH;D2;+0:10]-1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:10]1-[C:5](=[O;D1;H0:4])-[C:6]-[#7:7]-[C:8]-1=[O;D1;H0:9]
56.8
[{"value": 56.8, "product": "CC1(C(N(C(N1)=O)CCCCSC1=CC=NC=C1)=O)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.8, "product": "CC1(C(N(C(N1)=O)CCCCSC1=CC=NC=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
43
HOUR
To a solution of 2.56 g (20 mmol) of 5,5-dimethylhydantoin and 4.03 g (20 mmol) of 4-(4-chlorobutylthio)pyridine in 20 ml of N,N-dimethylformamide, 3.00 ml (20 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, and the mixture was stirred at room temperature for 43 hours, followed by further stirring at 70° C. for ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Urea
Urea.Substituted dicarboximide
C1CNCN1
C1C[NH]CN1
C1C[NH]CN1.c1ccncc1
HCl
CN(C=O)C
null
43
CC1(C)NC(=O)NC1=O.ClCCCCSc1ccncc1>CN(C=O)C>CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f99fd64ecadc4d6fbfc0db3ce5607ef8
O=C1CSC(=O)N1.O=Cc1ccccc1>>O=C1NC(=O)C(=Cc2ccccc2)S1
S1C(NC(C1)=O)=O.C(C1=CC=CC=C1)=O.N1CCCCC1>>C(C1=CC=CC=C1)=C1C(NC(S1)=O)=O
[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH2:6][S:14]1.O=[CH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[C:6](=[CH:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[S:14]1
O=C1CSC(=O)N1.O=Cc1ccccc1
O=C1NC(=O)C(=Cc2ccccc2)S1
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=O)C(=Cc2ccccc2)S1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#16:7]-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[#7:11]-1>>[O;D1;H0:5]=[C:6]1-[#16:7]-[C;H0;D3;+0:8](=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:9](=[O;D1;H0:10])-[#7:11]-1
90.4
[{"value": 90.4, "product": "C(C1=CC=CC=C1)=C1C(NC(S1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.2, "product": "C(C1=CC=CC=C1)=C1C(NC(S1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 20 g (171 mmol) of 2,4-thiazolidinedione and 17.4 ml (171 mmol) of benzaldehyde in 350 ml of ethanol, 1.68 ml (17.1 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cooled ethanol to give 31.67 g o...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
C1CSCN1.c1ccccc1
HO-
C(C)O
null
null
O=C1CSC(=O)N1.O=Cc1ccccc1>C(C)O>O=C1NC(=O)C(=Cc2ccccc2)S1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f955cb05073547f09e8e193f4ca25145
O=C1CSC(=O)N1.O=Cc1ccc(Cl)cc1>>O=C1NC(=O)C(=Cc2ccc(Cl)cc2)S1
S1C(NC(C1)=O)=O.ClC1=CC=C(C=O)C=C1.N1CCCCC1>>ClC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1
[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH2:6][S:15]1.O=[CH:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[C:6](=[CH:7][c:8]2[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]2)[S:15]1
O=C1CSC(=O)N1.O=Cc1ccc(Cl)cc1
O=C1NC(=O)C(=Cc2ccc(Cl)cc2)S1
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=O)C(=Cc2ccccc2)S1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#16:7]-[CH2;D2;+0:8]-[C:9](=[O;D1;H0:10])-[#7:11]-1>>[O;D1;H0:5]=[C:6]1-[#16:7]-[C;H0;D3;+0:8](=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4])-[C:9](=[O;D1;H0:10])-[#7:11]-1
43.4
[{"value": 43.4, "product": "ClC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 43.3, "product": "ClC1=CC=C(C=C2C(NC(S2)=O)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 20 g (171 mmol) of 2,4-thiazolidinedione and 17.4 ml (171 mmol) of 4-chlorobenzaldehyde in 350 ml of ethanol, 1.68 ml (17.1 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cooled ethanol to give 1...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
C1CSCN1.c1ccccc1
HO-
C(C)O
null
null
O=C1CSC(=O)N1.O=Cc1ccc(Cl)cc1>C(C)O>O=C1NC(=O)C(=Cc2ccc(Cl)cc2)S1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d824881d53434cb8beb91cc10043c497
O=C1CSC(=S)N1.O=Cc1ccccc1>>O=C1NC(=S)SC1=Cc1ccccc1
S1C(=S)NC(=O)C1.C(C1=CC=CC=C1)=O.N1CCCCC1>>C(C1=CC=CC=C1)=C1C(NC(S1)=S)=O
[O:1]=[C:2]1[NH:3][C:4](=[S:5])[S:6][CH2:7]1.O=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[O:1]=[C:2]1[NH:3][C:4](=[S:5])[S:6][C:7]1=[CH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
O=C1CSC(=S)N1.O=Cc1ccccc1
O=C1NC(=S)SC1=Cc1ccccc1
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=S)SC1=Cc1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#7:7]-[C:8](=[S;D1;H0:9])-[#16:10]-[CH2;D2;+0:11]-1>>[O;D1;H0:5]=[C:6]1-[#7:7]-[C:8](=[S;D1;H0:9])-[#16:10]-[C;H0;D3;+0:11]-1=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
66.6
[{"value": 66.6, "product": "C(C1=CC=CC=C1)=C1C(NC(S1)=S)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.6, "product": "C(C1=CC=CC=C1)=C1C(NC(S1)=S)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 10 g (75.1 mmol) of rhodanine and 7.63 ml (75.1 mmol) of benzaldehyde in 150 ml of ethanol, 0.74 ml (7.5 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cooled ethanol to give 11.07 g of the desir...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
C1CSCN1.c1ccccc1
HO-
C(C)O
null
null
O=C1CSC(=S)N1.O=Cc1ccccc1>C(C)O>O=C1NC(=S)SC1=Cc1ccccc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-fe71a2c02edc41da90a957171964ea9f
O=C1CSC(=O)N1.O=Cc1cccs1>>O=C1NC(=O)C(=Cc2cccs2)S1
S1C(NC(C1)=O)=O.S1C(=CC=C1)C=O.N1CCCCC1>>S1C(=CC=C1)C=C1C(NC(S1)=O)=O
[O:1]=[C:2]1[NH:3][C:4](=[O:5])[CH2:6][S:13]1.O=[CH:7][c:8]1[cH:9][cH:10][cH:11][s:12]1>>[O:1]=[C:2]1[NH:3][C:4](=[O:5])[C:6](=[CH:7][c:8]2[cH:9][cH:10][cH:11][s:12]2)[S:13]1
O=C1CSC(=O)N1.O=Cc1cccs1
O=C1NC(=O)C(=Cc2cccs2)S1
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=O)C(=Cc2cccs2)S1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[#16;a:4]:[c:5].[O;D1;H0:6]=[C:7]1-[#16:8]-[CH2;D2;+0:9]-[C:10](=[O;D1;H0:11])-[#7:12]-1>>[O;D1;H0:6]=[C:7]1-[#16:8]-[C;H0;D3;+0:9](=[CH;D2;+0:1]-[c:2](:[c:3]):[#16;a:4]:[c:5])-[C:10](=[O;D1;H0:11])-[#7:12]-1
66.6
[{"value": 66.6, "product": "S1C(=CC=C1)C=C1C(NC(S1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.5, "product": "S1C(=CC=C1)C=C1C(NC(S1)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 20 g (171 mmol) of 2,4-thiazolidinedione and 16.0 ml (171 mmol) of 2-thiophenecarboxaldehyde in 350 ml of ethanol, 1.68 ml (17.1 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cooled ethanol to g...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
C1CSCN1.c1ccsc1
HO-
C(C)O
null
null
O=C1CSC(=O)N1.O=Cc1cccs1>C(C)O>O=C1NC(=O)C(=Cc2cccs2)S1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e9a40193820a432da78afb9efd42f92a
ClCCCCBr.Sc1ccccn1>>ClCCCCSc1ccccn1
SC1=NC=CC=C1.C(C)N(CC)CC.BrCCCCCl>>ClCCCCSC1=NC=CC=C1
Br[CH2:5][CH2:4][CH2:3][CH2:2][Cl:1].[SH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][n:12]1>>[Cl:1][CH2:2][CH2:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][cH:10][cH:11][n:12]1
ClCCCCBr.Sc1ccccn1
ClCCCCSc1ccccn1
null
null
C(C)O
Heteroatom Alkylation and Arylation
thioether_nucl_sub
26df88c6a3f5f203c89584658be4e126cb42994c98a2e16bc812e1036cdae857
8b2f52296c3a93039174c980b6042ba15754e04d6892a1284c3a32985220b214
c1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[SH;D1;+0:4]-[c:5](:[c:6]):[#7;a:7]:[c:8]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[c:5](:[c:6]):[#7;a:7]:[c:8]
65.5
[{"value": 65.5, "product": "ClCCCCSC1=NC=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.5, "product": "ClCCCCSC1=NC=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 25.0 g (225 mmol) of 2-mercaptopyridine and 34.5 ml (247 mmol) of triethylamine in 300 ml of ethanol, 28.5 ml (247 mmol) of 1-bromo-4-chlorobutane was added with stirring under ice-cooling, and the mixture was stirred at room temperature for 16 hours. The solvent was distilled off and the residue was d...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic thiol
Monosulfide
null
null
c1ccncc1
HBr
C(C)O
null
null
ClCCCCBr.Sc1ccccn1>C(C)O>ClCCCCSc1ccccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d1d9d0850f644a438eba335e3ea1f8ab
NCCCSc1ccncc1.O=C(Cl)c1cnc2ccccc2n1>>O=C(NCCCSc1ccncc1)c1cnc2ccccc2n1
Cl.Cl.NCCCSC1=CC=NC=C1.C(C)N(CC)CC.N1=C(C=NC2=CC=CC=C12)C(=O)Cl>>N1=C(C=NC2=CC=CC=C12)C(=O)NCCCSC1=CC=NC=C1
[NH2:3][CH2:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1.Cl[C:2](=[O:1])[c:14]1[cH:15][n:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[n:23]1>>[O:1]=[C:2]([NH:3][CH2:4][CH2:5][CH2:6][S:7][c:8]1[cH:9][cH:10][n:11][cH:12][cH:13]1)[c:14]1[cH:15][n:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]2[n:23]1
NCCCSc1ccncc1.O=C(Cl)c1cnc2ccccc2n1
O=C(NCCCSc1ccncc1)c1cnc2ccccc2n1
null
null
C(Cl)Cl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
O=C(NCCCSc1ccncc1)c1cnc2ccccc2n1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:1.[C:9]-[C:10]-[NH2;D1;+0:11]>>[C:9]-[C:10]-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:[c:8]:1
48.9
[{"value": 48.9, "product": "N1=C(C=NC2=CC=CC=C12)C(=O)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.8, "product": "N1=C(C=NC2=CC=CC=C12)C(=O)NCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4.30 g (17.8 mmol) of 4-(3-aminopropylthio)pyridine dihydrochloride and 8.68 ml (62.3 mmol) of triethylamine in 200 ml of methylene chloride, 3.43 g (17.8 mmol) of 2-quinoxaloyl chloride was added with stirring under ice-cooling, and the mixture was stirred at room temperature for 4 hours. The reaction...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccncc1.c1ccc2nccnc2c1
HCl
C(Cl)Cl
null
null
NCCCSc1ccncc1.O=C(Cl)c1cnc2ccccc2n1>C(Cl)Cl>O=C(NCCCSc1ccncc1)c1cnc2ccccc2n1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-06a787a9c29b4bc098767573585c59cc
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=O)N1>>C=S1C(=O)NC(=O)C1c1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1
S1C(NC(C1)=O)=O.C(C)(C)(C)C=1C=C(C=O)C=C(C1O)C(C)(C)C.N1CCCCC1>>C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C1C(NC(S1=C)=O)=O
O=[CH:1][c:9]1[cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[c:16]([OH:17])[c:18]([C:19]([CH3:20])([CH3:21])[CH3:22])[cH:23]1.[S:2]1[C:3](=[O:4])[NH:5][C:6](=[O:7])[CH2:8]1>>[CH2:1]=[S:2]1[C:3](=[O:4])[NH:5][C:6](=[O:7])[CH:8]1[c:9]1[cH:10][c:11]([C:12]([CH3:13])([CH3:14])[CH3:15])[c:16]([OH:17])[c:18]([C:19]([CH3:2...
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=O)N1
C=S1C(=O)NC(=O)C1c1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
6e6467835f9a62a25304d3858bc1affbf4c7760e3ef4399f410153ebdcde4e82
d146119986570e7245608221d3867968dca480d3d9ca0151c47f335a9f4464ad
C=S1C(=O)NC(=O)C1c1ccccc1
O=[CH;D2;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[O;D1;H0:7]=[C:8]1-[#7:9]-[C:10](=[O;D1;H0:11])-[CH2;D2;+0:12]-[S;H0;D2;+0:13]-1>>[CH2;D1;+0:1]=[S;H0;D3;+0:13]1-[C:8](=[O;D1;H0:7])-[#7:9]-[C:10](=[O;D1;H0:11])-[CH;D3;+0:12]-1-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6]
424.3
[{"value": 42.8, "product": "C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C1C(NC(S1=C)=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 424.3, "product": "C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C1C(NC(S1=C)=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 12.5 g (107 mmol) of 2,4-thiazolidinedione and 25.0 g (107 mmol) of 3,5-di-tert-butyl-4-hydroxybenzaldehyde in 300 ml of ethanol, 1.05 ml (10.7 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cool...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
null
c1ccccc1.C1CSCN1
C1CSCN1.c1ccccc1
C1CSCN1.c1ccccc1
Other
C(C)O
null
null
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=O)N1>C(C)O>C=S1C(=O)NC(=O)C1c1cc(C(C)(C)C)c(O)c(C(C)(C)C)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1bac2bc6a24d41cca0817ee8dd549bfa
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=S)N1>>CC(C)(C)c1cc(C=C2SC(=S)NC2=O)cc(C(C)(C)C)c1O
S1C(=S)NC(=O)C1.C(C)(C)(C)C=1C=C(C=O)C=C(C1O)C(C)(C)C.N1CCCCC1>>C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C=C1C(NC(S1)=S)=O
O=[CH:8][c:7]1[cH:6][c:5]([C:2]([CH3:1])([CH3:3])[CH3:4])[c:22]([OH:23])[c:17]([C:18]([CH3:19])([CH3:20])[CH3:21])[cH:16]1.[CH2:9]1[S:10][C:11](=[S:12])[NH:13][C:14]1=[O:15]>>[CH3:1][C:2]([CH3:3])([CH3:4])[c:5]1[cH:6][c:7]([CH:8]=[C:9]2[S:10][C:11](=[S:12])[NH:13][C:14]2=[O:15])[cH:16][c:17]([C:18]([CH3:19])([CH3:20])[...
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=S)N1
CC(C)(C)c1cc(C=C2SC(=S)NC2=O)cc(C(C)(C)C)c1O
null
null
C(C)O
C-C Coupling
Aldol condensation
9a823fd9b4e4348a3556e295dbe35eee5775ba89af420a0e94956549a8f5e1f0
d1104e4dc387c28c5ac408eab23aa043e968d3cfd16e99022454bf87ce31f401
O=C1NC(=S)SC1=Cc1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[O;D1;H0:5]=[C:6]1-[#7:7]-[C:8](=[S;D1;H0:9])-[#16:10]-[CH2;D2;+0:11]-1>>[O;D1;H0:5]=[C:6]1-[#7:7]-[C:8](=[S;D1;H0:9])-[#16:10]-[C;H0;D3;+0:11]-1=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
69.7
[{"value": 69.7, "product": "C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C=C1C(NC(S1)=S)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.5, "product": "C(C)(C)(C)C=1C=C(C=C(C1O)C(C)(C)C)C=C1C(NC(S1)=S)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 14.6 g (110 mmol) of rhodanine and 25.7 g (110 mmol) of 3,5-di-tert-butyl-4-hydroxybenzaldehyde in 150 ml of ethanol, 1.08 ml (11.0 mmol) of piperidine was added, and the mixture was heated under reflux for 5 hours. After cooling, the precipitated crystals were filtered and washed with cooled ethanol t...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Monosulfide
Monosulfide
C1CSCN1
C1CSCN1
c1ccccc1.C1CSCN1
HO-
C(C)O
null
null
CC(C)(C)c1cc(C=O)cc(C(C)(C)C)c1O.O=C1CSC(=S)N1>C(C)O>CC(C)(C)c1cc(C=C2SC(=S)NC2=O)cc(C(C)(C)C)c1O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7c0a9d74a2794bf09aa140d9698f4f5f
O=C(NCCCSc1ccncc1)c1cnccn1>>Cl.O=C(NCCCSc1ccncc1)c1cnccn1
N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1.Cl.CO>>Cl.Cl.N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1
[O:3]=[C:4]([NH:5][CH2:6][CH2:7][CH2:8][S:9][c:10]1[cH:11][cH:12][n:13][cH:14][cH:15]1)[c:16]1[cH:17][n:18][cH:19][cH:20][n:21]1>>[ClH:2].[O:3]=[C:4]([NH:5][CH2:6][CH2:7][CH2:8][S:9][c:10]1[cH:11][cH:12][n:13][cH:14][cH:15]1)[c:16]1[cH:17][n:18][cH:19][cH:20][n:21]1
O=C(NCCCSc1ccncc1)c1cnccn1
Cl.O=C(NCCCSc1ccncc1)c1cnccn1
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C(NCCCSc1ccncc1)c1cnccn1
null
85.6
[{"value": 85.6, "product": "Cl.Cl.N1=C(C=NC=C1)C(=O)NCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 704.5 mg (2.57 mmol) of 4-[3-(2-pyrazinecarbonylamino)propylthio]pyridine in 30 ml of methanol, 70 ml of 10% hydrochloric acid-methanol was added, and the mixture was stirred at room temperature for 2 hours. The solvent was distilled off and the residue was purified by recrystallization (solvent: ethan...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccncc1.c1cnccn1
Other
CO
null
2
O=C(NCCCSc1ccncc1)c1cnccn1>CO>Cl.O=C(NCCCSc1ccncc1)c1cnccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bcf7a1386a3647debe56a5b796b263a1
O=C1c2ccccc2C(O)N1CSc1ccncc1>>O=C1c2ccccc2CN1CSc1ccncc1
O.N.OC1N(C(C2=CC=CC=C12)=O)CSC1=CC=NC=C1.[BH4-].[Na+]>>C1(N(CC2=CC=CC=C12)CSC1=CC=NC=C1)=O
O[CH:9]1[c:8]2[c:3]([cH:4][cH:5][cH:6][cH:7]2)[C:2](=[O:1])[N:10]1[CH2:11][S:12][c:13]1[cH:14][cH:15][n:16][cH:17][cH:18]1>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[CH2:9][N:10]1[CH2:11][S:12][c:13]1[cH:14][cH:15][n:16][cH:17][cH:18]1
O=C1c2ccccc2C(O)N1CSc1ccncc1
O=C1c2ccccc2CN1CSc1ccncc1
null
null
FC(C(=O)O)(F)F
Reduction
OtherReaction
6edf8215b233e57f6f4321f4b7bccecd4275fe90ce30e97960f31ca67074cfef
46f8a11b80b06e754a5a34198d843342612a5e7ede950bda52ce3a500cedba0b
O=C1c2ccccc2CN1CSc1ccncc1
O-[CH;D3;+0:1]1-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[c:6]:[c:7]-1:[c:8]>>[C:3]-[#7:2]1-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:6]-[C:4]-1=[O;D1;H0:5]
54.6
[{"value": 54.6, "product": "C1(N(CC2=CC=CC=C12)CSC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 54.6, "product": "C1(N(CC2=CC=CC=C12)CSC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
To a solution of 681 mg (2.5 mmol) of 4-[(3-hydroxyisoindolin-1-on-2-yl)methylthio]pyridine in 6 ml of trifluoroacetic acid, 0.30 g (7.93 mmol) of sodium borohydride was added in small portions, and the mixture was stirred for 15 minutes. The reaction mixture was poured into cold water and aqueous ammonia was added to ...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1ccncc1
Other
FC(C(=O)O)(F)F
null
0.25
O=C1c2ccccc2C(O)N1CSc1ccncc1>FC(C(=O)O)(F)F>O=C1c2ccccc2CN1CSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ec2bad3e6dba47c4a66e47e6b4dbd056
Nc1ccccc1C(=O)NCCCSc1ccncc1.O=C(n1ccnc1)n1ccnc1>>O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
NC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1.C(=O)(N1C=NC=C1)N1C=NC=C1>>N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O
[NH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[C:10](=[O:11])[NH:12][CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1.c1cn([C:2](n2ccnc2)=[O:1])cn1>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10](=[O:11])[n:12]1[CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
Nc1ccccc1C(=O)NCCCSc1ccncc1.O=C(n1ccnc1)n1ccnc1
O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
null
null
O1CCCC1
Miscellaneous
OtherReaction
3e8b3bc12468184c65ca5d4345dcd6a9a2bd9361910d94045ee52e07d8a4b796
fddc47fd7ce043f5eaeb1a75ba9d7112d180caa5d986cf9717333edef1364690
O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10].[O;D1;H0:11]=[C;H0;D3;+0:12](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[n;H0;D3;+0:3]1:[c;H0;D3;+0:4](=[O;D1;H0:5]):[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:12]:1=[O;D1;H0:11]
65.7
[{"value": 65.7, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 65.6, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Under nitrogen atmosphere, to a solution of 718 mg (2.5 mmol) of 4-[3-(2-aminobenzoylamino)propylthio]pyridine in 15 ml of tetrahydrofuran. 811 mg (5.0 mmol) of 1,1'carbonyldiimidazole was added, and the mixture was stirred at room temperature for 16 hours. The solvent was distilled off and the residue was dissolved in...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine
null
c1ccccc1.c1c[nH]cn1.c1c[nH]cn1
c1ncc2ccccc2n1
c1ncc2ccccc2n1.c1ccncc1
Other
O1CCCC1
null
16
Nc1ccccc1C(=O)NCCCSc1ccncc1.O=C(n1ccnc1)n1ccnc1>O1CCCC1>O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-60d992e5f70047c985ad708eb5f4a3b2
Nc1ccccc1C(=O)NCCCSc1ccncc1.S=C(n1ccnc1)n1ccnc1>>O=c1c2ccccc2[nH]c(=S)n1CCCSc1ccncc1
NC1=C(C(=O)NCCCSC2=CC=NC=C2)C=CC=C1.C(=S)(N1C=NC=C1)N1C=NC=C1>>N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=S
[O:1]=[C:2]([c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[NH2:9])[NH:12][CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1.c1cn([C:10](n2ccnc2)=[S:11])cn1>>[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[nH:9][c:10](=[S:11])[n:12]1[CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
Nc1ccccc1C(=O)NCCCSc1ccncc1.S=C(n1ccnc1)n1ccnc1
O=c1c2ccccc2[nH]c(=S)n1CCCSc1ccncc1
null
null
O1CCCC1
Miscellaneous
OtherReaction
2b1a5626aec4d5fa3a98e3e4c9eb7ca479c1fa140a59f5106857e53480b10644
ae2e858e699afe0a746047a0d81b45616cc8ac2e8f8c70be12af20e9ea591ceb
O=c1c2ccccc2[nH]c(=S)n1CCCSc1ccncc1
[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10].[S;D1;H0:11]=[C;H0;D3;+0:12](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[n;H0;D3;+0:3]1:[c;H0;D3;+0:12](=[S;D1;H0:11]):[nH;D2;+0:9]:[c:8](:[c:10]):[c:6](:[c:7]):[c;H0;D3;+0:4]:1=[O;D1;H0:5]
68.5
[{"value": 68.5, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=S", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.4, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
64
HOUR
Under nitrogen atmosphere, to a solution of 1.48 g (5.15 mmol) of 4-[3-(2-aminobenzoylamino)propylthio]pyridine in 30 ml of tetrahydrofuran, 1.84 g (10.3 mmol) of 1,1'-thiocarbonyldiimidazole was added, and the mixture was stirred at room temperature for 64 hours. The solvent was distilled off and the residue was washe...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine.Thiocarbonyl
Thiocarbonyl
c1ccccc1.c1c[nH]cn1.c1c[nH]cn1
c1ncc2ccccc2n1
c1ncc2ccccc2n1.c1ccncc1
Other
O1CCCC1
null
64
Nc1ccccc1C(=O)NCCCSc1ccncc1.S=C(n1ccnc1)n1ccnc1>O1CCCC1>O=c1c2ccccc2[nH]c(=S)n1CCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-32b0f994e35548499b85f980112ef12f
Nc1ccccc1C(=O)NCCCCSc1ccccn1.O=C(n1ccnc1)n1ccnc1>>O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccccn1
NC1=C(C(=O)NCCCCSC2=NC=CC=C2)C=CC=C1.C(=O)(N1C=NC=C1)N1C=NC=C1>>N1=C(C=CC=C1)SCCCCN1C(NC2=CC=CC=C2C1=O)=O
[NH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[C:10](=[O:11])[NH:12][CH2:13][CH2:14][CH2:15][CH2:16][S:17][c:18]1[cH:19][cH:20][cH:21][cH:22][n:23]1.c1cn([C:2](n2ccnc2)=[O:1])cn1>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10](=[O:11])[n:12]1[CH2:13][CH2:14][CH2:15][CH2:16][S:17][c:18]1[cH:19][cH:20][cH:21][...
Nc1ccccc1C(=O)NCCCCSc1ccccn1.O=C(n1ccnc1)n1ccnc1
O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccccn1
null
null
O1CCCC1
Miscellaneous
OtherReaction
3e8b3bc12468184c65ca5d4345dcd6a9a2bd9361910d94045ee52e07d8a4b796
fddc47fd7ce043f5eaeb1a75ba9d7112d180caa5d986cf9717333edef1364690
O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccccn1
[C:1]-[C:2]-[NH;D2;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6](:[c:7]):[c:8](-[NH2;D1;+0:9]):[c:10].[O;D1;H0:11]=[C;H0;D3;+0:12](-n1:c:c:n:c:1)-n1:c:c:n:c:1>>[C:1]-[C:2]-[n;H0;D3;+0:3]1:[c;H0;D3;+0:4](=[O;D1;H0:5]):[c:6](:[c:7]):[c:8](:[c:10]):[nH;D2;+0:9]:[c;H0;D3;+0:12]:1=[O;D1;H0:11]
68.8
[{"value": 68.8, "product": "N1=C(C=CC=C1)SCCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.6, "product": "N1=C(C=CC=C1)SCCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
Under nitrogen atmosphere, to a solution of 452 mg (1.5 mmol) of 2-[4-(2-aminobenzoylamino)butylthio]pyridine in 20 ml of tetrahydrofuran, 486 mg (3.0 mmol) of 1,1'-carbonyldiimidazole was added, and the mixture was stirred at room temperature for 16 hours. The solvent was distilled off and the residue was dissolved in...
10.6084/m9.figshare.5104873.v1
null
Secondary amide.Primary amine
null
c1ccccc1.c1c[nH]cn1.c1c[nH]cn1
c1ncc2ccccc2n1
c1ncc2ccccc2n1.c1ccncc1
Other
O1CCCC1
null
16
Nc1ccccc1C(=O)NCCCCSc1ccccn1.O=C(n1ccnc1)n1ccnc1>O1CCCC1>O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-1dd6d24ee72c4a7caa0ee1e9472a73e8
ClCCCSc1ccncc1.O=c1[nH]c(=O)c2ccccc2[nH]1>>O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
O.C1=CC=C2C(=C1)C(=O)NC(=O)N2.ClCCCSC1=CC=NC=C1.C1CCC2=NCCCN2CC1>>N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O
Cl[CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1.[O:1]=[c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10](=[O:11])[nH:12]1>>[O:1]=[c:2]1[nH:3][c:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[c:10](=[O:11])[n:12]1[CH2:13][CH2:14][CH2:15][S:16][c:17]1[cH:18][cH:19][n:20][cH:21][cH:22]1
ClCCCSc1ccncc1.O=c1[nH]c(=O)c2ccccc2[nH]1
O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
3708cb06644489eacd277cd5ae5b40bafb4efb35fe31ebfe1203528f95cc75ab
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[O;D1;H0:4]=[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9](=[O;D1;H0:10]):[nH;D2;+0:11]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:11]1:[c:5](=[O;D1;H0:4]):[c:6]:[c:7]:[#7;a:8]:[c:9]:1=[O;D1;H0:10]
31.1
[{"value": 31.1, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 31.0, "product": "N1=CC=C(C=C1)SCCCN1C(NC2=CC=CC=C2C1=O)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
16
HOUR
To a solution of 1.62 g (10 mmol) of benzoylene urea and 1.88 g (10 mmol) of 4-(3-chloropropylthio)pyridine in 50 ml of dimethylformamide, 1.65 ml (11 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, and the mixture was stirred at 80° C. for 16 hours. After cooling, water was added to the reaction mixture, and th...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2ccccc2n1
c1ncc2ccccc2n1
c1ncc2ccccc2n1.c1ccncc1
HCl
CN(C=O)C
80
16
ClCCCSc1ccncc1.O=c1[nH]c(=O)c2ccccc2[nH]1>CN(C=O)C>O=c1[nH]c2ccccc2c(=O)n1CCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-9bc7f16969ba4b2985a63d53dcd01956
C1CCC2=NCCCN2CC1.ClCCCCSc1ccccn1.O=c1[nH]c(=O)c2ccccc2[nH]1>>O=c1c2ccccc2n(CCCCSc2ccccn2)c(=O)n1CCCCSc1ccccn1
O.C1=CC=C2C(=C1)C(=O)NC(=O)N2.ClCCCCSC1=NC=CC=C1.C1CCC2=NCCCN2CC1>>N1=C(C=CC=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=NC=CC=C1)=O
N1=[C:27]2[CH2:31][CH2:30][CH2:29][CH2:32][CH2:33][N:34]2[CH2:24][CH2:25][CH2:26]1.Cl[CH2:10][CH2:11][CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][cH:18][cH:19][n:20]1.[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[nH:9][c:21](=[O:22])[nH:23]1>>[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[n:9]([CH2:10][CH2:11][CH2:...
C1CCC2=NCCCN2CC1.ClCCCCSc1ccccn1.O=c1[nH]c(=O)c2ccccc2[nH]1
O=c1c2ccccc2n(CCCCSc2ccccn2)c(=O)n1CCCCSc1ccccn1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
d8f534adcea29c7c6c43643fcd89ca9404f765d91ca336bdf1b590b13af086ba
f34bbe5984ba8bee4a20e6b052b51263121b2e0f3c1e349eaacd87d49f81c7ec
O=c1c2ccccc2n(CCCCSc2ccccn2)c(=O)n1CCCCSc1ccccn1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].N1=[C;H0;D3;+0:4]2-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[CH2;D2;+0:9]-[N;H0;D3;+0:10]-2-[CH2;D2;+0:11]-[C:12]-[CH2;D2;+0:13]-1.[O;D1;H0:14]=[c:15]1:[c:16]:[c:17](:[c:18]):[nH;D2;+0:19]:[c:20](=[O;D1;H0:21]):[nH;D2;+0:22]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:19]1:[c:20...
9
[{"value": 4.6, "product": "N1=C(C=CC=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=NC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 9.0, "product": "N1=C(C=CC=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=NC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
16
HOUR
To a solution of 1.62 g (10 mmol) of benzoylene urea and 2.02 g (10 mmol) of 2-(4-chlorobutylthio)pyridine in 50 ml of dimethylformamide, 1.65 ml (11 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, and the mixture was stirred at 80° C. for 16 hours. After cooling, water was added to the reaction mixture, and the...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary amine
Monosulfide
C1CCC2=NCCCN2CC1.c1ncc2ccccc2n1
c1ccc2ncncc2c1.c1ccncc1
c1ccc2ncncc2c1.c1ccncc1.c1ccncc1
HCl
CN(C=O)C
80
16
C1CCC2=NCCCN2CC1.ClCCCCSc1ccccn1.O=c1[nH]c(=O)c2ccccc2[nH]1>CN(C=O)C>O=c1c2ccccc2n(CCCCSc2ccccn2)c(=O)n1CCCCSc1ccccn1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-83a7c62c23a249aeb76e978fdd928305
ClCSc1ccncc1.O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccncc1>>O=c1c2ccccc2n(CSc2ccncc2)c(=O)n1CCCCSc1ccncc1
O.N1=CC=C(C=C1)SCCCCN1C(NC2=CC=CC=C2C1=O)=O.ClCSC1=CC=NC=C1.C1CCC2=NCCCN2CC1>>N1=CC=C(C=C1)SCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=O
Cl[CH2:10][S:11][c:12]1[cH:13][cH:14][n:15][cH:16][cH:17]1.[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[nH:9][c:18](=[O:19])[n:20]1[CH2:21][CH2:22][CH2:23][CH2:24][S:25][c:26]1[cH:27][cH:28][n:29][cH:30][cH:31]1>>[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[n:9]([CH2:10][S:11][c:12]2[cH:13][cH:14][n:15][cH:16][...
ClCSc1ccncc1.O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccncc1
O=c1c2ccccc2n(CSc2ccncc2)c(=O)n1CCCCSc1ccncc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
ed0ecfb808bbf35afb68da1838f95fdf0d1e93f83b5a2b57280fca17f7a0b388
1a7a00854822988bd22b9e70c1384da74bf98232059fa099ce8b594ffd264593
O=c1c2ccccc2n(CSc2ccncc2)c(=O)n1CCCCSc1ccncc1
Cl-[CH2;D2;+0:1]-[#16:2]-[c:3].[C:4]-[#7;a:5]1:[c:6]:[c:7]:[c:8](:[c:9]):[nH;D2;+0:10]:[c:11]:1=[O;D1;H0:12]>>[C:4]-[#7;a:5]1:[c:6]:[c:7]:[c:8](:[c:9]):[n;H0;D3;+0:10](-[CH2;D2;+0:1]-[#16:2]-[c:3]):[c:11]:1=[O;D1;H0:12]
46.7
[{"value": 46.7, "product": "N1=CC=C(C=C1)SCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 46.6, "product": "N1=CC=C(C=C1)SCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
16
HOUR
To a solution of 491 mg (1.5 mmol) of 3-[4-(4-pyridylthio)butyl]quinazoline-2,4(1H,3H)-dione and 287 mg (1.8 mmol) of 4-chloromethylthiopyridine in 15 ml of dimethylformamide, 0.27 ml (1.8 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, and the mixture was stirred at 80° C. for 16 hours. After cooling, water was...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Monosulfide
Monosulfide
c1ncc2ccccc2n1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.c1ccncc1.c1ccncc1
HCl
CN(C=O)C
80
16
ClCSc1ccncc1.O=c1[nH]c2ccccc2c(=O)n1CCCCSc1ccncc1>CN(C=O)C>O=c1c2ccccc2n(CSc2ccncc2)c(=O)n1CCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-190cc34a0d224df4a3612d1206af180e
ClCCCCSc1ccncc1.O=c1c2ccccc2[nH]c(=S)n1CCCCSc1ccncc1>>O=c1c2ccccc2n(CCCCSc2ccncc2)c(=S)n1CCCCSc1ccncc1
O.N1=CC=C(C=C1)SCCCCN1C(NC2=CC=CC=C2C1=O)=S.ClCCCCSC1=CC=NC=C1.C1CCC2=NCCCN2CC1>>N1=CC=C(C=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=S
Cl[CH2:10][CH2:11][CH2:12][CH2:13][S:14][c:15]1[cH:16][cH:17][n:18][cH:19][cH:20]1.[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[nH:9][c:21](=[S:22])[n:23]1[CH2:24][CH2:25][CH2:26][CH2:27][S:28][c:29]1[cH:30][cH:31][n:32][cH:33][cH:34]1>>[O:1]=[c:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[n:9]([CH2:10][CH2:11][CH2:12][...
ClCCCCSc1ccncc1.O=c1c2ccccc2[nH]c(=S)n1CCCCSc1ccncc1
O=c1c2ccccc2n(CCCCSc2ccncc2)c(=S)n1CCCCSc1ccncc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0024151b25c56ede0e7ce80f2021719ad30c68b18a1f302e7ad0ba2aa518bc5b
d72e642f974cd00fafea01e0aa99ac249acb85af83d41d15686326e5a60030bb
O=c1c2ccccc2n(CCCCSc2ccncc2)c(=S)n1CCCCSc1ccncc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[c:7]:[c:8](:[c:9]):[nH;D2;+0:10]:[c:11]:1=[S;D1;H0:12]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:10]1:[c:11](=[S;D1;H0:12]):[#7;a:5](-[C:4]):[c:6]:[c:7]:[c:8]:1:[c:9]
97.1
[{"value": 97.1, "product": "N1=CC=C(C=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=S", "details": "PERCENTYIELD", "is_desired": false}, {"value": 0.1, "product": "N1=CC=C(C=C1)SCCCCN1C(N(C(C2=CC=CC=C12)=O)CCCCSC1=CC=NC=C1)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
16
HOUR
To a solution of 515 mg (1.5 mmol) of 3-[4-(4-pyridylthio)butyl]quinazoline-2 (1H)-thion-4(3H)-one and 332 mg (1.65 mmol) of 4-(4-chlorobutylthio)pyridine in 15 ml of dimethylformamide, 0.25 ml (1.65 mmol) of 1,8-diazabicyclo[5.4.0]-7-undecene was added, and the mixture was stirred at 80° C. for 16 hours. After cooling...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Thiocarbonyl
Thiocarbonyl
c1ncc2ccccc2n1
c1ccc2ncncc2c1
c1ccc2ncncc2c1.c1ccncc1.c1ccncc1
HCl
CN(C=O)C
80
16
ClCCCCSc1ccncc1.O=c1c2ccccc2[nH]c(=S)n1CCCCSc1ccncc1>CN(C=O)C>O=c1c2ccccc2n(CCCCSc2ccncc2)c(=S)n1CCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a61d1f22e885485180fc72a79cdacf3e
CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O.ClCCCCSc1ccncc1>>CC1(C)C(=O)N(CCCCSc2ccncc2)C(=O)N1CCCCSc1ccncc1
O.ClCCCCSC1=CC=NC=C1.[H-].[Na+].N1=CC=C(C=C1)SCCCCN1C(NC(C1=O)(C)C)=O>>N1=CC=C(C=C1)SCCCCN1C(=O)N(C(=O)C1(C)C)CCCCSC1=CC=NC=C1
[CH3:1][C:2]1([CH3:3])[C:4](=[O:5])[N:6]([CH2:7][CH2:8][CH2:9][CH2:10][S:11][c:12]2[cH:13][cH:14][n:15][cH:16][cH:17]2)[C:18](=[O:19])[NH:20]1.Cl[CH2:21][CH2:22][CH2:23][CH2:24][S:25][c:26]1[cH:27][cH:28][n:29][cH:30][cH:31]1>>[CH3:1][C:2]1([CH3:3])[C:4](=[O:5])[N:6]([CH2:7][CH2:8][CH2:9][CH2:10][S:11][c:12]2[cH:13][cH...
CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O.ClCCCCSc1ccncc1
CC1(C)C(=O)N(CCCCSc2ccncc2)C(=O)N1CCCCSc1ccncc1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
1d1fbd8c788960a5b6c1c5f03d883d9998e8a29ba0dc902a98e33cdbd0c845a0
9068cdf0ef9ef7510e3ed725979384397a613e011a5abb0653feb8d5b2408c81
O=C1CN(CCCCSc2ccncc2)C(=O)N1CCCCSc1ccncc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7:5]1-[C:6](=[O;D1;H0:7])-[NH;D2;+0:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C:12]-1=[O;D1;H0:13]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:8]1-[C:6](=[O;D1;H0:7])-[#7:5](-[C:4])-[C:12](=[O;D1;H0:13])-[C:9]-1(-[C;D1;H3:10])-[C;D1;H3:11]
80.7
[{"value": 80.7, "product": "N1=CC=C(C=C1)SCCCCN1C(=O)N(C(=O)C1(C)C)CCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.7, "product": "N1=CC=C(C=C1)SCCCCN1C(=O)N(C(=O)C1(C)C)CCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
To a suspension of 96 mg (2.4 mmol) of 60% sodium hydride (oily) in 15 ml of dimethylformamide, 587 mg (2.0 mmol) of 3-[4-(4-pyridylthio)butyl]-5,5-dimethylhydantoin was added, and the mixture was stirred at room temperature for 10 minutes. To this reaction mixture, 807 mg (4.0 mmol) of 4-(4-chlorobutylthio)pyridine wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Urea
Urea
C1C[NH]CN1
C1C[NH]C[NH]1
C1C[NH]C[NH]1.c1ccncc1.c1ccncc1
HCl
CN(C=O)C
null
0.166667
CC1(C)NC(=O)N(CCCCSc2ccncc2)C1=O.ClCCCCSc1ccncc1>CN(C=O)C>CC1(C)C(=O)N(CCCCSc2ccncc2)C(=O)N1CCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-100d3d0cc94243f9be6bff4a345d975c
CCC(=O)Nc1ccccc1NC(=O)CC.ClCCCCBr>>CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC
C(CC)(=O)NC1=C(C=CC=C1)NC(CC)=O.BrCCCCCl>>ClCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCCl)C(CC)=O
[CH3:1][CH2:2][C:3](=[O:4])[NH:5][c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[NH:17][C:23](=[O:24])[CH2:25][CH3:26].Br[CH2:6][CH2:7][CH2:8][CH2:9][Cl:10]>>[CH3:1][CH2:2][C:3](=[O:4])[N:5]([CH2:6][CH2:7][CH2:8][CH2:9][Cl:10])[c:11]1[cH:12][cH:13][cH:14][cH:15][c:16]1[N:17]([CH2:18][CH2:19][CH2:20][CH2:21][Cl:22])[C:23](=[...
CCC(=O)Nc1ccccc1NC(=O)CC.ClCCCCBr
CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
[OH-].[Na+].C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
4558de55e09b8b817c30da9a143db92605f7343bd4b80f7284db3426de0bb3af
1b4d57d9adbf5ad6d8d51be36d67937944263d1424dbbd9216901e389aa3cf77
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5](=[O;D1;H0:6])-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10](-[NH;D2;+0:11]-[C:12](-[C:13])=[O;D1;H0:14]):[c:15]>>[C:16]-[C:17]-[N;H0;D3;+0:7](-[C:5](-[C:4])=[O;D1;H0:6])-[c:8](:[c:9]):[c:10](-[N;H0;D3;+0:11](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:12](-[C:13])=[O;D1;H0:14]):[c:15]
12.6
[{"value": 12.6, "product": "ClCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCCl)C(CC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 12.6, "product": "ClCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCCl)C(CC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
To a suspension of 3.27 g (15 mmol) of 1,2-di-propionylaminobenzene, 4.32 ml (37.5 mmol) of 4-bromo-1-chlorobutane, and 0.96 g (3.0 mmol) of tetrabutylammonium bromide in 25 ml of toluene, 5.6 ml of 50% aqueous sodium hydroxide was added at room temperature, and the mixture was stirred for 16 hours. The organic layer w...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amide.Secondary amide
Primary halide.Tertiary amide.Tertiary amide
null
null
c1ccccc1
Br-
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.[OH-].[Na+].C1(=CC=CC=C1)C
null
16
CCC(=O)Nc1ccccc1NC(=O)CC.ClCCCCBr>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.[OH-].[Na+].C1(=CC=CC=C1)C>CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-037000249bf248819c335444fe0d73ae
CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC.Sc1ccncc1>>CCC(=O)N(CCCCSc1ccncc1)c1ccccc1N(CCCCSc1ccncc1)C(=O)CC
O.SC1=CC=NC=C1.[OH-].[K+].ClCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCCl)C(CC)=O>>N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O
Cl[CH2:9][CH2:8][CH2:7][CH2:6][N:5]([C:3]([CH2:2][CH3:1])=[O:4])[c:17]1[cH:18][cH:19][cH:20][cH:21][c:22]1[N:23]([CH2:24][CH2:25][CH2:26][CH2:31]Cl)[C:35](=[O:36])[CH2:37][CH3:38].[SH:10][c:11]1[cH:12][cH:13][n:14][cH:15][cH:16]1>>[CH3:1][CH2:2][C:3](=[O:4])[N:5]([CH2:6][CH2:7][CH2:8][CH2:9][S:10][c:11]1[cH:12][cH:13][...
CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC.Sc1ccncc1
CCC(=O)N(CCCCSc1ccncc1)c1ccccc1N(CCCCSc1ccncc1)C(=O)CC
null
null
CS(=O)C
Aromatic Heterocycle Formation
OtherReaction
0a603e62127a82876015e05ff0fdd4be754b3daaa7727a875a252d121d24df21
48e4666c504a6dac125cad805af6583baf72152192dc93c9aef146ff85aee226
c1ccc(NCCCCSc2ccncc2)c(NCCCCSc2ccncc2)c1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[C:3]-[C:4].Cl-[CH2;D2;+0:5]-[C:6]-[C:7].[SH;D1;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1>>[C:4]-[C:3]-[CH2;D2;+0:2]-[C:15]-[#16:16]-[c:17]:[c:18]:[cH;D2;+0:1]:[#7;a:19]:[c:20].[C:7]-[C:6]-[CH2;D2;+0:5]-[S;H0;D2;+0:8]-[c:9]1:[c:10]:[c:11]:[#7;a:12]:[c:13]:[c:14]:1
81
[{"value": 81.0, "product": "N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 80.7, "product": "N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of 525 mg (4.7 mmol) of 4-mercaptopyridine and 265 mg (4.7 mmol) of potassium hydroxide in 20 ml of dimethyl sulfoxide, 760 mg (1.89 mmol) of 1,2-bis[N-(4-chlorobutyl)-N-propionylamino]benzene was added at room temperature, and the mixture was stirred for 2 hours. The reaction mixture was poured into wate...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aromatic thiol
Monosulfide.Monosulfide
null
c1ccncc1
c1ccncc1.c1ccccc1.c1ccncc1
null
CS(=O)C
null
2
CCC(=O)N(CCCCCl)c1ccccc1N(CCCCCl)C(=O)CC.Sc1ccncc1>CS(=O)C>CCC(=O)N(CCCCSc1ccncc1)c1ccccc1N(CCCCSc1ccncc1)C(=O)CC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-84de096b7dbe4838b438dd20613401fa
Cl>>Cl.Cl
N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O.Cl.CO>>Cl.Cl.N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O
[ClH:39]>>[ClH:39].[ClH:40]
Cl
Cl.Cl
null
null
CO
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
74.1
[{"value": 74.1, "product": "Cl.Cl.N1=CC=C(C=C1)SCCCCN(C(CC)=O)C1=C(C=CC=C1)N(CCCCSC1=CC=NC=C1)C(CC)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a solution of 840 mg (1.53 mmol) of 1,2-bis[N-[4-(4-pyridylthio)butyl]-N-propionylamino]benzene in 20 ml of methanol, 80 ml of 10% hydrochloric acid/methanol was added, and the mixture was stirred for 30 minutes. The solvent was distilled off and the residue was recrystallized from ethanol/ether to give 707 mg of th...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
CO
null
0.5
Cl>CO>Cl.Cl
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-15f297c6101148ec9fd927b43a15d2da
CC(C)(C)OC(=O)NCCCSc1ccncc1.O=C(OO)c1cccc(Cl)c1>>CC(C)(C)OC(=O)NCCCS(=O)c1ccncc1
C(C)(C)(C)OC(=O)NCCCSC1=CC=NC=C1.ClC1=CC(=CC=C1)C(=O)OO>>C(C)(C)(C)OC(=O)NCCCS(=O)C1=CC=NC=C1
[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH2:9][CH2:10][CH2:11][S:12][c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1.O=C(O[OH:13])c1cccc(Cl)c1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][CH2:9][CH2:10][CH2:11][S:12](=[O:13])[c:14]1[cH:15][cH:16][n:17][cH:18][cH:19]1
CC(C)(C)OC(=O)NCCCSc1ccncc1.O=C(OO)c1cccc(Cl)c1
CC(C)(C)OC(=O)NCCCS(=O)c1ccncc1
null
null
C(Cl)Cl
Oxidation
Sulfanyl to sulfinyl_peroxide
95b5106b07a173d8eafc1c9c8a6c938befe131c3d1caaf5886529b7aee55ea9d
7652b53bb02130dccfe4b1e8905d7f3db7f05ff3a95a0003c1bab09b1ad4083e
c1ccncc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C:2]-[C:3]-[S;H0;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1>>[C:2]-[C:3]-[S;H0;D3;+0:4](=[O;H0;D1;+0:1])-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
79
[{"value": 78.9, "product": "C(C)(C)(C)OC(=O)NCCCS(=O)C1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 79.0, "product": "C(C)(C)(C)OC(=O)NCCCS(=O)C1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 4.03 g (15.0 mmol) of 4-[3-(t-butoxycarbonylamino)propylthio]pyridine in 100 ml of methylene chloride, 3.05 g (15.0 mmol) of m-chloroperbenzoic acid was added with stirring under ice-cooling, and the mixture was stirred at the same temperature for 1 hour. The reaction mixture was washed two times with ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide.Monosulfide
Sulfoxide
c1ccccc1
null
c1ccncc1
HCl
C(Cl)Cl
null
null
CC(C)(C)OC(=O)NCCCSc1ccncc1.O=C(OO)c1cccc(Cl)c1>C(Cl)Cl>CC(C)(C)OC(=O)NCCCS(=O)c1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4aaaa3a6821445dabee298f6b50af2bd
ClCCCCBr.Sc1ccncc1>>ClCCCCSc1ccncc1
SC1=CC=NC=C1.BrCCCCCl.C(C)N(CC)CC>>ClCCCCSC1=CC=NC=C1
Br[CH2:5][CH2:4][CH2:3][CH2:2][Cl:1].[SH:6][c:7]1[cH:8][cH:9][n:10][cH:11][cH:12]1>>[Cl:1][CH2:2][CH2:3][CH2:4][CH2:5][S:6][c:7]1[cH:8][cH:9][n:10][cH:11][cH:12]1
ClCCCCBr.Sc1ccncc1
ClCCCCSc1ccncc1
null
null
C(C)O
Heteroatom Alkylation and Arylation
thioether_nucl_sub
26df88c6a3f5f203c89584658be4e126cb42994c98a2e16bc812e1036cdae857
8b2f52296c3a93039174c980b6042ba15754e04d6892a1284c3a32985220b214
c1ccncc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[SH;D1;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1>>[C:3]-[C:2]-[CH2;D2;+0:1]-[S;H0;D2;+0:4]-[c:5]1:[c:6]:[c:7]:[#7;a:8]:[c:9]:[c:10]:1
89.7
[{"value": 89.7, "product": "ClCCCCSC1=CC=NC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 89.7, "product": "ClCCCCSC1=CC=NC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
5
HOUR
To a suspension of 33.35 g (0.30 mol) of 4-mercaptopyridine and 51.44 g (0.30 mol) of 1-bromo-4-chlorobutane in 500 ml of ethanol, 41.9 ml (0.30 mol) of triethylamine was added, and the mixture was stirred at room temperature for 5 hours. The solvent was distilled off and chloroform was added to the residue. The mixtur...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic thiol
Monosulfide
null
null
c1ccncc1
HBr
C(C)O
null
5
ClCCCCBr.Sc1ccncc1>C(C)O>ClCCCCSc1ccncc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-0ab8bbc1253f48d2a40e581350c80b04
C=CC(=O)Cl.COC1(c2ccccc2)OCC(CO)O1>>C=CC(=O)OCC1COC(OC)(c2ccccc2)O1
OCC1OC(OC1)(C1=CC=CC=C1)OC.C(C)N(CC)CC.C(C=C)(=O)Cl>>C(C=C)(=O)OCC1OC(OC1)(C1=CC=CC=C1)OC
Cl[C:3]([CH:2]=[CH2:1])=[O:4].[OH:5][CH2:6][CH:7]1[CH2:8][O:9][C:10]([O:11][CH3:12])([c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[O:19]1>>[CH2:1]=[CH:2][C:3](=[O:4])[O:5][CH2:6][CH:7]1[CH2:8][O:9][C:10]([O:11][CH3:12])([c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[O:19]1
C=CC(=O)Cl.COC1(c2ccccc2)OCC(CO)O1
C=CC(=O)OCC1COC(OC)(c2ccccc2)O1
null
null
C(Cl)Cl
Acylation
Schotten-Baumann to ester
6cefe709828c5bd4655f254e75d5dff9e8876e192e7dd47256c1bc0067bc5291
d8a7643b81ed07a6f633aa99465180dfa0565e61ae25aef36338ebb9837c9cef
c1ccc(C2OCCO2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4].[#8:5]-[C:6]-[C:7]-[OH;D1;+0:8]>>[#8:5]-[C:6]-[C:7]-[O;H0;D2;+0:8]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]=[C;D1;H2:4]
null
[]
null
null
null
null
The procedure of Example A was repeated, employing 21 grams (100 mmol.) of 4-hydroxymethyl-2-methoxy-2-phenyl-1,3-dioxolane, 25.3 grams (250 mmol.) of triethylamine, 9.5 grams (105 mmol.) of acryloyl chloride and 150 ml. of methylene chloride. The crude product was purified by column chromatography over basic alumina, ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary alcohol
Ester
null
null
C1COCO1.c1ccccc1
HCl
C(Cl)Cl
null
null
C=CC(=O)Cl.COC1(c2ccccc2)OCC(CO)O1>C(Cl)Cl>C=CC(=O)OCC1COC(OC)(c2ccccc2)O1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-b17abff2b44840dd9b7ca02149e953e2
Nc1ccc(Nc2ccccc2)cc1.O=C(O)CCS>>O=C(CCS)Nc1ccc(Nc2ccccc2)cc1
C1(=CC=CC=C1)NC1=CC=C(C=C1)N.SCCC(=O)O.C=1(C(=CC=CC1)C)C>>N(C1=CC=CC=C1)C1=CC=C(C=C1)NC(CCS)=O
[NH2:6][c:7]1[cH:8][cH:9][c:10]([NH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1.O[C:2](=[O:1])[CH2:3][CH2:4][SH:5]>>[O:1]=[C:2]([CH2:3][CH2:4][SH:5])[NH:6][c:7]1[cH:8][cH:9][c:10]([NH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][cH:17]2)[cH:18][cH:19]1
Nc1ccc(Nc2ccccc2)cc1.O=C(O)CCS
O=C(CCS)Nc1ccc(Nc2ccccc2)cc1
null
null
CCCCCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccc(Nc2ccccc2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[NH2;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
140
CELSIUS
null
null
A mixture of 18.4 grams of N-phenyl-p-phenylene diamine, 10.6 grams of β-mercaptopropionic acid and 120 milliliters of xylene (technical grade) was heated to reflux (about 140° C.) under nitrogen atmosphere, with stirring. A 1.6 milliliter quantity of water (90% of theory) was removed from this mixture by azetropic dis...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CCCCCC
140
null
Nc1ccc(Nc2ccccc2)cc1.O=C(O)CCS>CCCCCC>O=C(CCS)Nc1ccc(Nc2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-2e9e9e922e064d3ba03f213d5729e9eb
N#Cc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2>>NCc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2
C1=CC2=C1C=CC(=C2)OC2=C(C#N)C(=CC=C2)OC2=CC1=C(C=C1)C=C2.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>C1=CC2=C1C=CC(=C2)OC2=C(CN)C(=CC=C2)OC2=CC1=C(C=C1)C=C2
[N:1]#[C:2][c:3]1[c:4]([O:5][c:6]2[cH:7][cH:8][c:9]3[c:10]([cH:11]2)[CH:12]=[CH:13]3)[cH:14][cH:15][cH:16][c:17]1[O:18][c:19]1[cH:20][cH:21][c:22]2[c:23]([cH:24]1)[CH:25]=[CH:26]2>>[NH2:1][CH2:2][c:3]1[c:4]([O:5][c:6]2[cH:7][cH:8][c:9]3[c:10]([cH:11]2)[CH:12]=[CH:13]3)[cH:14][cH:15][cH:16][c:17]1[O:18][c:19]1[cH:20][cH...
N#Cc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2
NCc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2
null
null
C(C)OCC
Reduction
Reduction of nitrile to amine
65bec2d9f430701d30dc9fcbe1c5418f3dfa174d67be035c50edfc71895dc9c7
e8d1bc928b94bd4f5bf4b23363ce8f88b1ce7d146ba93829e7b8ad8dbe0007a7
C1=Cc2cc(Oc3cccc(Oc4ccc5c(c4)C=C5)c3)ccc21
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[NH2;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
15
MINUTE
In a 500 ml, 4-necked round-bottomed flask equipped with an overhead mechanical stirrer, a thermometer/adaptor, a reflux condensor and a funnel was added 2,6-di-(4-benzocyclobutenoxy)benzonitrile followed by 260 ml of anhydrous diethyl ether. The resultant mixture was placed in an ice bath and stirred under anitrogen a...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amine
null
null
c1ccccc1.C1=Cc2ccccc21.C1=Cc2ccccc21
null
C(C)OCC
null
0.25
N#Cc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2>C(C)OCC>NCc1c(Oc2ccc3c(c2)C=C3)cccc1Oc1ccc2c(c1)C=C2
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-71e3ae6057b24905aebe514e2d6cc7ed
BrCCCCCCCCCCBr.CC(C)=O.COc1cc(C=O)ccc1O.O=C([O-])[O-]>>COc1cc(C=O)ccc1OCCCCCCCCCCOc1ccc(C=O)cc1OC
O=CC1=CC(OC)=C(O)C=C1.BrCCCCCCCCCCBr.C([O-])([O-])=O.[K+].[K+].CC(=O)C>>COC1=C(OCCCCCCCCCCOC2=C(C=C(C=C2)C=O)OC)C=CC(=C1)C=O
Br[CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][CH2:21]Br.O=[C:3]([CH3:1])[CH3:24].[c:5]1([CH:6]=[O:7])[cH:8][cH:9][c:23]([OH:22])[c:30]([O:31][CH3:32])[cH:29]1.[O-:2][C:27]([O-:11])=[O:28]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH:6]=[O:7])[cH:8][cH:9][c:10]1[O:11][CH2:12][CH2:13][CH2:14][CH2:15][C...
BrCCCCCCCCCCBr.CC(C)=O.COc1cc(C=O)ccc1O.O=C([O-])[O-]
COc1cc(C=O)ccc1OCCCCCCCCCCOc1ccc(C=O)cc1OC
null
null
O
Aromatic Heterocycle Formation
OtherReaction
d8b09204afcff0574fcc1e547d0c752ec6c19e94f0279576b6ad2c5cb824ae19
325f167d8f5f8c8d486fe211b7741ee3cecfa3178b343d3635d0779e7f4b61df
c1ccc(OCCCCCCCCCCOc2ccccc2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].Br-[CH2;D2;+0:4]-[C:5]-[C:6].O=[C;H0;D3;+0:7](-[CH3;D1;+0:8])-[CH3;D1;+0:9].[#8:10]-[c:11]1:[cH;D2;+0:12]:[c;H0;D3;+0:13](-[C:14]=[O;D1;H0:15]):[c:16]:[cH;D2;+0:17]:[c;H0;D3;+0:18]:1-[OH;D1;+0:19].[O-;H0;D1:20]-[C;H0;D3;+0:21](-[O-;H0;D1:22])=[O;D1;H0:23]>>[#8:10]-[c:11]1:[cH;D2;+0:12]:[c:2...
null
[]
5
CELSIUS
48
HOUR
A slurry of 13.42 g of vanillin, 11.99 g of 1,10-dibromodecane, 6.16 g of anhydrous potassium carbonate and 300 ml of acetone was refluxed with stirring for 48 h, cooled and diluted with 400 ml of water. After the salts had dissolved, the mixture was chilled overnight at 5° C. The solid product was filtered, washed twi...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Aldehyde.Ketone.Aromatic alcohol
Aldehyde.Aldehyde.Ether.Ether.Ether
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
Br-
O
5
48
BrCCCCCCCCCCBr.CC(C)=O.COc1cc(C=O)ccc1O.O=C([O-])[O-]>O>COc1cc(C=O)ccc1OCCCCCCCCCCOc1ccc(C=O)cc1OC
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-68af85f3122543a7bc6f77f268cb1285
CC(=O)c1ccc(F)cc1.Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1.Oc1cccc(-c2ccccc2O)c1>>CC(=O)c1ccc(Oc2ccc(C(c3ccccc3)(c3ccc(Oc4ccc(C(C)=O)cc4)cc3)C(F)(F)F)cc2)cc1
C([O-])([O-])=O.[K+].[K+].OC1=CC=C(C=C1)C(C(F)(F)F)(C1=CC=CC=C1)C1=CC=C(C=C1)O.C1=CC=C(C(=C1)C2=CC(=CC=C2)O)O.CC(=O)C1=CC=C(C=C1)F.C1=CC=C(C(=C1)C2=CC(=CC=C2)O)O>>C(C)(=O)C1=CC=C(OC2=CC=C(C=C2)C(C(F)(F)F)(C2=CC=CC=C2)C2=CC=C(C=C2)OC2=CC=C(C=C2)C(C)=O)C=C1
F[c:25]1[cH:26][cH:27][c:28]([C:29]([CH3:30])=[O:31])[cH:32][cH:33]1.[OH:8][c:9]1[cH:10][cH:11][c:12]([C:13]([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)([c:20]2[cH:21][cH:22][c:23]([OH:24])[cH:34][cH:35]2)[C:36]([F:37])([F:38])[F:39])[cH:40][cH:41]1.Oc1cc[cH:1]c(-[c:4]2[cH:5][cH:6][cH:7][cH:42][c:43]2O)c1>>[CH3:1][C:2...
CC(=O)c1ccc(F)cc1.Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1.Oc1cccc(-c2ccccc2O)c1
CC(=O)c1ccc(Oc2ccc(C(c3ccccc3)(c3ccc(Oc4ccc(C(C)=O)cc4)cc3)C(F)(F)F)cc2)cc1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
a384ee17c5b86ec6db3aa57afcafb5f4f8d0f89875ab9fb8f6d7035197efba77
64d1960390043da01c7e3d5fa149706f0e8b47a38c6e1cb9dc5f08e732a60424
c1ccc(Oc2ccc(C(c3ccccc3)c3ccc(Oc4ccccc4)cc3)cc2)cc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].O-[c;H0;D3;+0:6]1:[c:7]:[cH;D2;+0:8]:[c:9]:[c:10]:[c;H0;D3;+0:11]:1-c1:[cH;D2;+0:12]:c:c:c(-O):c:1.[OH;D1;+0:13]-[c:14](:[c:15]):[c:16].[OH;D1;+0:17]-[c:18](:[c:19]):[c:20]>>[CH3;D1;+0:12]-[C:21](=[O;D1;H0:22])-[c;H0;D3;+0:11]1:[c:10]:[c:9]:[c;H0;D3;+0:8](-[O;H0;D2;+0:17]-[c:1...
null
[]
null
null
null
null
A suspension of 15.2 grams (0.11 moles) anhydrous potassium carbonate in 370 milliliters of N2N'-dimethylacetamide is prepared in a 1 liter, 2-necked round bottom flask equipped with a reflux condensor and a nitrogen gas inlet. To the suspension is added 16.61 grams (0.05 moles) of 1,1-bis-(4-hydroxyphenyl)-1-phenyl-2,...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic alcohol.Aromatic alcohol.Aromatic alcohol.Aromatic alcohol
Ketone.Ether.Ether
c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
HF
null
null
null
CC(=O)c1ccc(F)cc1.Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1.Oc1cccc(-c2ccccc2O)c1>>CC(=O)c1ccc(Oc2ccc(C(c3ccccc3)(c3ccc(Oc4ccc(C(C)=O)cc4)cc3)C(F)(F)F)cc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7ba62443ec7649e18842d3f4e41dec27
COc1ccccc1.O=C(c1ccccc1)C(F)(F)F>>Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1
FC(C(=O)C1=CC=CC=C1)(F)F.FC(S(=O)(=O)O)(F)F.C1(=CC=CC=C1)OC.Br>>OC1=CC=C(C=C1)C(C(F)(F)F)(C1=CC=CC=C1)C1=CC=C(C=C1)O
[CH3:4][O:17][c:16]1[cH:15][cH:14][cH:13][cH:19][cH:18]1.[O:1]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:20]([F:21])([F:22])[F:23]>>[OH:1][c:2]1[cH:3][cH:4][c:5]([C:6]([c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)([c:13]2[cH:14][cH:15][c:16]([OH:17])[cH:18][cH:19]2)[C:20]([F:21])([F:22])[F:23])[cH:24][cH:25]1
COc1ccccc1.O=C(c1ccccc1)C(F)(F)F
Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1
null
null
C(C)(=O)O
Aromatic Heterocycle Formation
OtherReaction
a72ec60e45c36f8c7f1bc4c1f3a2bfbd3a7fbd4644c34189c3a0c1d7665ae4d4
604a51ed69f11cbca51f2d4914d9db2bcecd47e66534bb9a0d52940ec959a73c
c1ccc(C(c2ccccc2)c2ccccc2)cc1
[CH3;D1;+0:1]-[O;H0;D2;+0:2]-[c:3]1:[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]:1.[F;D1;H0:9]-[C:10](-[F;D1;H0:11])(-[F;D1;H0:12])-[C;H0;D3;+0:13](=[O;H0;D1;+0:14])-[c:15](:[c:16]):[c:17]>>[F;D1;H0:9]-[C:10](-[F;D1;H0:11])(-[F;D1;H0:12])-[C;H0;D4;+0:13](-[c:18]1:[c:19]:[c:20]:[c:21](-[OH;D1;+0:14]):[c:22]:[cH;D2;+0:1]:1)(-[c:...
null
[]
null
null
24
HOUR
A mixture of 100 grams (0.57 mol) of trifluoroacetophenone, 100 grams (0.7 mol) trifluoromethane sulfonic acid, and 100 grams (10.9 mol) anisole is stirred at room temperature for 24 hours. The mixture is then transferred to a separatory funnel and the organic material is washed with water (3×11), saturated bicarbonate...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ether
Aromatic alcohol.Aromatic alcohol
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1
Other
C(C)(=O)O
null
24
COc1ccccc1.O=C(c1ccccc1)C(F)(F)F>C(C)(=O)O>Oc1ccc(C(c2ccccc2)(c2ccc(O)cc2)C(F)(F)F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5e96e77a6ea242f0b4bfc5496ffdd983
CCNCCO.O=Cc1ccc(F)cc1>>CCN(CCO)c1ccc(C=O)cc1
FC1=CC=C(C=O)C=C1.C(C)NCCO.C([O-])([O-])=O.[K+].[K+]>>OCCN(CC)C1=CC=C(C=O)C=C1
[CH3:1][CH2:2][NH:3][CH2:4][CH2:5][OH:6].F[c:7]1[cH:8][cH:9][c:10]([CH:11]=[O:12])[cH:13][cH:14]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][OH:6])[c:7]1[cH:8][cH:9][c:10]([CH:11]=[O:12])[cH:13][cH:14]1
CCNCCO.O=Cc1ccc(F)cc1
CCN(CCO)c1ccc(C=O)cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation secondary amine
705933786518ece8447c3a260ed1708cc50b5b37b829540bc5bba9d6bb1dde91
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C;D1;H3:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C;D1;H3:10])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
95
CELSIUS
null
null
To a three neck flask fitted with a mechanical stirrer, a thermometer, and a condenser, is added 124 g (1 mole) of 4-fluorobenzaldehyde, 89.1 g (1 mole) of 2-(N-ethylamino)ethanol, 138.2 g (1 mole) of anhydrous potassium carbonate, and dimethylsulfoxide. The mixture is heated at 95° C. for 3 hours. After cooling to roo...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
CS(=O)C
95
null
CCNCCO.O=Cc1ccc(F)cc1>CS(=O)C>CCN(CCO)c1ccc(C=O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-e8332f792cb943259f780b7e96c92708
CCN(CCOC(C)=O)c1ccc(C=O)cc1>>CCN(CCO)c1ccc(C=CC=O)cc1
[Cl-].[Na+].C(C)(=O)OCCN(CC)C1=CC=C(C=O)C=C1.[Br-].O1C(OCC1)C[P+](CCCC)(CCCC)CCCC.CC(C)([O-])C.[K+]>>OCCN(CC)C1=CC=C(C=CC=O)C=C1
O=[CH:11][c:10]1[cH:9][cH:8][c:7]([N:3]([CH2:2][CH3:1])[CH2:4][CH2:5][O:6][C:13]([CH3:12])=[O:14])[cH:16][cH:15]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][OH:6])[c:7]1[cH:8][cH:9][c:10]([CH:11]=[CH:12][CH:13]=[O:14])[cH:15][cH:16]1
CCN(CCOC(C)=O)c1ccc(C=O)cc1
CCN(CCO)c1ccc(C=CC=O)cc1
null
null
CN(C=O)C.Cl.O
Miscellaneous
OtherReaction
716d431b21b76dc7be86288acf6b079ba424a010e3c36e2883035373997c7f75
8312bfe1cc7896204f42ca6a876ec15c050ef293944cf9da7ac1091018dad53e
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:8](-[CH3;D1;+0:9])=[O;D1;H0:10]>>[C:5]-[C:6]-[OH;D1;+0:7].[O;D1;H0:10]=[CH;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
90
CELSIUS
16
HOUR
To a solution of 235.3 g (1 mole) of 4-(N-2-acetoxyethyl-N-ethylamino)benzaldehyde in dimethylformamide is added 738.7 g (2.0 moles) of 1,3-dioxolan-2-ylmethyltributylphosphonium bromide in dimethylformamide, and the mixture is heated at 90° C. Potassium t-butoxide (224.4 g, 2.0 moles) is added, and heating is continue...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Aldehyde.Primary alcohol
null
null
c1ccccc1
Other
CN(C=O)C.Cl.O
90
16
CCN(CCOC(C)=O)c1ccc(C=O)cc1>CN(C=O)C.Cl.O>CCN(CCO)c1ccc(C=CC=O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a7fdbb7f8cd94053be30d2daa540915e
CCN(CCO)c1ccc(C=CC=O)cc1.Nc1ccccc1.O=C(O)Cc1ccc([N+](=O)[O-])cc1>>CCN(CCO)C(=CC=Cc1ccccc1)c1ccc([N+](=O)[O-])cc1
OCCN(CC)C1=CC=C(C=CC=O)C=C1.NC1=CC=CC=C1.C=1(C(=CC=CC1)S(=O)(=O)O)C.C(C(=C)C)(=O)O.[N+](=O)([O-])C1=CC=C(C=C1)CC(=O)O>>OCCN(CC)C(=CC=CC1=CC=CC=C1)C1=CC=C(C=C1)[N+](=O)[O-]
O=C[CH:9]=[CH:10][c:11]1ccc([N:3]([CH2:2][CH3:1])[CH2:4][CH2:5][OH:6])c[cH:16]1.Nc1c[cH:15][cH:14][cH:13][cH:12]1.O=[C:8](O)[CH2:7][c:17]1[cH:18][cH:19][c:20]([N+:21](=[O:22])[O-:23])[cH:24][cH:25]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH2:5][OH:6])[C:7](=[CH:8][CH:9]=[CH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[c:17]1[...
CCN(CCO)c1ccc(C=CC=O)cc1.Nc1ccccc1.O=C(O)Cc1ccc([N+](=O)[O-])cc1
CCN(CCO)C(=CC=Cc1ccccc1)c1ccc([N+](=O)[O-])cc1
null
null
C1(=CC=CC=C1)C.O
Heteroatom Alkylation and Arylation
OtherReaction
9e2980e417c83e0bf41fd27676942bc4bd19d262e4edb49eda3aeea031ce50ea
1a583843e9b96e1db3bc4296c45825b4414c285767a137bcc7a95757ef2442ec
C(C=Cc1ccccc1)=Cc1ccccc1
N-c1:[cH;D2;+0:1]:[c:2]:[c:3]:[cH;D2;+0:4]:c:1.O-[C;H0;D3;+0:5](=O)-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9].O=C-[CH;D2;+0:10]=[C:11]-[c;H0;D3;+0:12]1:[cH;D2;+0:13]:c:c(-[N;H0;D3;+0:14](-[C:15]-[C;D1;H3:16])-[C:17]-[C:18]):c:c:1>>[C:18]-[C:17]-[N;H0;D3;+0:14](-[C:15]-[C;D1;H3:16])-[C;H0;D3;+0:6](=[CH;D2;+0:5]-[CH;D2;+0:10]=[C...
null
[]
null
null
3
HOUR
A solution of 21.9 g (0.1 mole) of 4-(N-2-hydroxyethyl-N-ethylamino)cinnamaldehyde, 9.3 g (1 mole) of aniline, and 0.19 g (1 mole %) of toluenesulfonic acid in toluene is heated at reflux for 17 hours with azeotropic removal of water. After the mixture is cooled to room temperature, 17.2 g (0.2 mole) of methacrylic aci...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid.Primary amine.Tertiary amine
Enamine.Conjugated diene
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
C1(=CC=CC=C1)C.O
null
3
CCN(CCO)c1ccc(C=CC=O)cc1.Nc1ccccc1.O=C(O)Cc1ccc([N+](=O)[O-])cc1>C1(=CC=CC=C1)C.O>CCN(CCO)C(=CC=Cc1ccccc1)c1ccc([N+](=O)[O-])cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-4683026ba7114d0ab4a570be14f1d8a7
CCCCNCCCCO.O=Cc1ccc(F)cc1>>CCCCN(CCCCO)c1ccc(C=O)cc1
FC1=CC=C(C=O)C=C1.C(CCC)NCCCCO.C([O-])([O-])=O.[K+].[K+]>>OCCCCN(CCCC)C1=CC=C(C=O)C=C1
[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH2:8][CH2:9][OH:10].F[c:11]1[cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17][cH:18]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[c:11]1[cH:12][cH:13][c:14]([CH:15]=[O:16])[cH:17][cH:18]1
CCCCNCCCCO.O=Cc1ccc(F)cc1
CCCCN(CCCCO)c1ccc(C=O)cc1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
Buchwald-Hartwig/Ullmann-Goldberg/N-arylation secondary amine
705933786518ece8447c3a260ed1708cc50b5b37b829540bc5bba9d6bb1dde91
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccccc1
F-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[C:9]-[C:10])-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5]
null
[]
95
CELSIUS
null
null
To a three neck flask fitted with a mechanical stirrer, a thermometer, and a condenser, is added 124 g (1 mole) of 4-fluorobenzaldehyde, 145.3 g (1 mole) of N-butyl-N-4-hydroxybutylamine, 138.2 g (1 mole) of anhydrous potassium carbonate, and dimethylsulfoxide. The mixture is then heated at 95° C. until the reaction is...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1
c1ccccc1
c1ccccc1
HF
CS(=O)C
95
null
CCCCNCCCCO.O=Cc1ccc(F)cc1>CS(=O)C>CCCCN(CCCCO)c1ccc(C=O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-3b600f4c7ca4476a9e47d62d4b288b7e
CC(=O)OC(C)=O.CCCCN(CCCCO)c1ccc(C=O)cc1>>CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1
OCCCCN(CCCC)C1=CC=C(C=O)C=C1.C(C)(=O)OC(C)=O.C(C)N(CC)CC>>C(C)(=O)OCCCCN(CCCC)C1=CC=C(C=O)C=C1
CC(=O)O[C:11]([CH3:12])=[O:13].[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[c:14]1[cH:15][cH:16][c:17]([CH:18]=[O:19])[cH:20][cH:21]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH2:9][O:10][C:11]([CH3:12])=[O:13])[c:14]1[cH:15][cH:16][c:17]([CH:18]=[O:19])[cH:20][cH:21]1
CC(=O)OC(C)=O.CCCCN(CCCCO)c1ccc(C=O)cc1
CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1
null
null
ClCCl
Acylation
Transesterification
f81e513b7b512b10157c16426844efd8d88e34c97987c1347c6ba8a688351205
fc27d67c790d5fb520ba5d49de1490661fa5b822b714863734ce7e3029dfa84f
c1ccccc1
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[OH;D1;+0:6]>>[C:4]-[C:5]-[O;H0;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
16
HOUR
To a stirred solution of 249.4 g (1 mole) of 4-(N-4-hydroxybutyl-N-butylamino)benzaldehyde in dichloromethane are added 153.1 g (1.5 moles) of acetic anhydride, 151.8 g (1.5 moles) of triethylamine, and 8.5 g (7 mole %) of 4-N,N-dimethylaminopyridine. The reaction mixture is stirred at room temperature for 16 hours. Th...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary alcohol
Ester
null
null
c1ccccc1
HO-
ClCCl
null
16
CC(=O)OC(C)=O.CCCCN(CCCCO)c1ccc(C=O)cc1>ClCCl>CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a8052ae73acf41bcbeb0aa54d437ed4a
CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1>>CCCCN(CCCCO)c1ccc(C=CC=O)cc1
[Cl-].[Na+].C(C)(=O)OCCCCN(CCCC)C1=CC=C(C=O)C=C1.[Br-].O1C(OCC1)C[P+](CCCC)(CCCC)CCCC.CC(C)([O-])C.[K+]>>OCCCCN(CCCC)C1=CC=C(C=CC=O)C=C1
O=[CH:15][c:14]1[cH:13][cH:12][c:11]([N:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][CH2:8][CH2:9][O:10][C:17]([CH3:16])=[O:18])[cH:20][cH:19]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH2:9][OH:10])[c:11]1[cH:12][cH:13][c:14]([CH:15]=[CH:16][CH:17]=[O:18])[cH:19][cH:20]1
CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1
CCCCN(CCCCO)c1ccc(C=CC=O)cc1
null
null
CN(C=O)C.Cl.O
Miscellaneous
OtherReaction
716d431b21b76dc7be86288acf6b079ba424a010e3c36e2883035373997c7f75
8312bfe1cc7896204f42ca6a876ec15c050ef293944cf9da7ac1091018dad53e
c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:8](-[CH3;D1;+0:9])=[O;D1;H0:10]>>[C:5]-[C:6]-[OH;D1;+0:7].[O;D1;H0:10]=[CH;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
90
CELSIUS
16
HOUR
To a solution of 29.1 g (0.1 mole) of 4-(N-4-acetoxybutyl-N-butylamino)benzaldehyde in dimethylformamide is added 73.9 g (0.2 mole) of 1,3-dioxolan-2-ylmethyltributylphosphonium bromide in dimethylformamide, and the mixture is heated at 90° C. Potassium t-butoxide (22.4 g, 0.2 mole) is added, and heating is continued a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Aldehyde.Primary alcohol
null
null
c1ccccc1
Other
CN(C=O)C.Cl.O
90
16
CCCCN(CCCCOC(C)=O)c1ccc(C=O)cc1>CN(C=O)C.Cl.O>CCCCN(CCCCO)c1ccc(C=CC=O)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7218c825a19c4b7087dc142778ad78c1
Cc1ccc(S(=O)(=O)C(F)(F)F)cc1.O=C1CCC(=O)N1Br>>O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F
S(=O)(=O)(C(F)(F)F)C1=CC=C(C=C1)C.BrN1C(CCC1=O)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O>>S(=O)(=O)(C(F)(F)F)C1=CC=C(C=C1)CBr
[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][c:7]([CH3:8])[cH:10][cH:11]1)[C:12]([F:13])([F:14])[F:15].O=C1CCC(=O)N1[Br:9]>>[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][c:7]([CH2:8][Br:9])[cH:10][cH:11]1)[C:12]([F:13])([F:14])[F:15]
Cc1ccc(S(=O)(=O)C(F)(F)F)cc1.O=C1CCC(=O)N1Br
O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
4366c8ed5252d87d3b8aede79b191acca5264a1f31dcbbbe406186fea61ecf72
0e509ce434521037e1886dc905c022287322e8fdd0d4706b9bfbbfdc0a5969b8
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A stirred solution of 22.4 g (0.1 mole) of 4-triflyltoluene, 178 g (0.1 mole) of N-bromosuccinimide, and 0.48 g (0.2 mole %) of benzoyl peroxide in carbon tetrachloride is heated at reflux for 20 hours. After cooling to room temperature, the reaction is diluted by the addition of carbon tetrachloride, and the solid byp...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(Cl)(Cl)(Cl)Cl
null
null
Cc1ccc(S(=O)(=O)C(F)(F)F)cc1.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c752070c8b524cd1886a9e0e3e0ee605
O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F.c1ccc(P(c2ccccc2)c2ccccc2)cc1>>O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F.[Br-]
S(=O)(=O)(C(F)(F)F)C1=CC=C(C=C1)CBr.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>[Br-].S(=O)(=O)(C(F)(F)F)C1=CC=C(C[P+](C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)C=C1
[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][c:7]([CH2:8][Br:34])[cH:28][cH:29]1)[C:30]([F:31])([F:32])[F:33].[P:9]([c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)([c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1>>[O:1]=[S:2](=[O:3])([c:4]1[cH:5][cH:6][c:7]([CH2:8][P+:9]([c:10]2[cH:11][cH:...
O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F.c1ccc(P(c2ccccc2)c2ccccc2)cc1
O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F.[Br-]
null
null
C=1(C(=CC=CC1)C)C
Functional Group Interconversion
OtherReaction
72a5231b07f184f0ef4a0648badd4176f521b95f1ba3340a0f90d8894af47260
47a659f5704a5b7ca1b92ff731f18f109c6bde1d45152a3a393eefbd10265508
c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1
[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5].[c:6]:[c:7](-[P;H0;D3;+0:8](-[c:9](:[c:10]):[c:11])-[c:12](:[c:13]):[c:14]):[c:15]>>[Br-;H0;D0:1].[c:6]:[c:7](-[P+;H0;D4:8](-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5])(-[c:9](:[c:10]):[c:11])-[c:12](:[c:13]):[c:14]):[c:15]
null
[]
null
null
null
null
A solution of 30.3 g (0.1 mole) of 4-triflyl-alpha-bromotoluene and 28.8 g (0.1 mole) of triphenylphosphine in xylene is heated at reflux for 19 hours. 4-Triflylbenzyltriphenylphosphonium bromide is then isolated by filtration, washed with additional portions of xylene, and dried. Conditions: See reaction.notes.procedu...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
null
null
O=S(=O)(c1ccc(CBr)cc1)C(F)(F)F.c1ccc(P(c2ccccc2)c2ccccc2)cc1>C=1(C(=CC=CC1)C)C>O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F.[Br-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-d48d928ccbcc4d238b26df05d712c5e6
CCCCN(CCCCO)c1ccc(C=CC=O)cc1.O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F>>CCCCN(CCCCO)C(=CC=Cc1ccccc1)c1ccc(S(=O)(=O)C(F)(F)F)cc1
O.OCCCCN(CCCC)C1=CC=C(C=CC=O)C=C1.[Br-].S(=O)(=O)(C(F)(F)F)C1=CC=C(C[P+](C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)C=C1.[Li]CCCC>>OCCCCN(CCCC)C(=CC=CC1=CC=CC=C1)C1=CC=C(C=C1)S(=O)(=O)C(F)(F)F
O=[CH:12][CH:13]=[CH:14][c:15]1ccc([N:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][CH2:8][CH2:9][OH:10])c[cH:20]1.c1ccc([P+](c2ccccc2)(c2c[cH:19][cH:18][cH:17][cH:16]2)[CH2:11][c:21]2[cH:22][cH:23][c:24]([S:25](=[O:26])(=[O:27])[C:28]([F:29])([F:30])[F:31])[cH:32][cH:33]2)cc1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6...
CCCCN(CCCCO)c1ccc(C=CC=O)cc1.O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F
CCCCN(CCCCO)C(=CC=Cc1ccccc1)c1ccc(S(=O)(=O)C(F)(F)F)cc1
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
ccfa34830e99154215dc9efa804c077a8eae3d186500f5a39b4a3d89c379fb59
486671fa43642ccee0acbfcc882f81c1972f06f8ac2d1775b3a21b51993e48a6
C(C=Cc1ccccc1)=Cc1ccccc1
O=[CH;D2;+0:1]-[C:2]=[C:3]-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:c:c(-[N;H0;D3;+0:6](-[C:7]-[C:8])-[C:9]-[C:10]):c:c:1.[c:11]:[c:12](-[CH2;D2;+0:13]-[P+](-c1:[cH;D2;+0:14]:[c:15]:[c:16]:[cH;D2;+0:17]:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[c:18]>>[C:8]-[C:7]-[N;H0;D3;+0:6](-[C:9]-[C:10])-[C;H0;D3;+0:13](=[CH;D2;+0:1]-[C:2]=[C:3]...
null
[]
null
null
18
HOUR
To a stirred solution of 110 g (0.2 mole) of 4-triflylbenzyltriphenylphosphonium bromide in toluene is added dropwise 0.2 moles of n-BuLi at room temperature. After 2 hours a solution of 27.5 g (0.1 mole) of 4[N-4-hydroxybutyl-N-butylamino]cinnamaldehyde in toluene is added dropwise to the mixture, and the reaction is ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Tertiary amine
Enamine.Conjugated diene
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
HO-
C1(=CC=CC=C1)C
null
18
CCCCN(CCCCO)c1ccc(C=CC=O)cc1.O=S(=O)(c1ccc(C[P+](c2ccccc2)(c2ccccc2)c2ccccc2)cc1)C(F)(F)F>C1(=CC=CC=C1)C>CCCCN(CCCCO)C(=CC=Cc1ccccc1)c1ccc(S(=O)(=O)C(F)(F)F)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-002d9f5f7d094a87a267a18d90638473
OCCCCCCBr.c1ccc2c(c1)CCCN2>>OCCCCCCN1CCCc2ccccc21
N1CCCC2=CC=CC=C12.BrCCCCCCO.C([O-])([O-])=O.[K+].[K+]>>OCCCCCCN1CCCC2=CC=CC=C12
Br[CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][OH:1].[NH:8]1[CH2:9][CH2:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]21>>[OH:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][N:8]1[CH2:9][CH2:10][CH2:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]21
OCCCCCCBr.c1ccc2c(c1)CCCN2
OCCCCCCN1CCCc2ccccc21
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
219d202b93cb5a235df7e6646f3b9409e60d3c325f1ec37d9b75eb0c3554d20f
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
c1ccc2c(c1)CCCN2
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C:3])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
A stirred solution of 133.2 g (1 mole) of 1,2,3,4-tetrahydroquinoline, 181.1 g (1 mole) of 6-bromohexanol, and 138.2 g (1 mole) of potassium carbonate in toluene is heated at 80° C. for 3 hours. The solution is cooled to room temperature, and the solids are removed by filtration. The solvent is removed in vacuo, and th...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
c1ccc2c(c1)CCCN2
c1ccc2c(c1)CCC[NH]2
c1ccc2c(c1)CCC[NH]2
HBr
C1(=CC=CC=C1)C
null
null
OCCCCCCBr.c1ccc2c(c1)CCCN2>C1(=CC=CC=C1)C>OCCCCCCN1CCCc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-bf199b56f7eb4319ac3c695eb26223f8
CC(=O)OC(C)=O.OCCCCCCN1CCCC2CC=CC=C21>>CC(=O)OCCCCCCN1CCCc2ccccc21
OCCCCCCN1CCCC2CC=CC=C12.C(C)(=O)OC(C)=O.C(C)N(CC)CC>>C(C)(=O)OCCCCCCN1CCCC2=CC=CC=C12
CC(=O)O[C:2]([CH3:1])=[O:3].[OH:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][N:11]1[CH2:12][CH2:13][CH2:14][CH:15]2[CH2:16][CH:17]=[CH:18][CH:19]=[C:20]12>>[CH3:1][C:2](=[O:3])[O:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][N:11]1[CH2:12][CH2:13][CH2:14][c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]21
CC(=O)OC(C)=O.OCCCCCCN1CCCC2CC=CC=C21
CC(=O)OCCCCCCN1CCCc2ccccc21
null
null
ClCCl
Aromatic Heterocycle Formation
OtherReaction
71a761ab5a61f07a9fddedefd628ef697febf2d90d3066ee73430c34a3b09da3
222fe5df041850e8bab46bf3676deadbb615af526f2aae9d8f614b82fc5895d7
c1ccc2c(c1)CCCN2
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[#7:5]1-[C:6]-[C:7]-[C:8]-[CH;D3;+0:9]2-[CH2;D2;+0:10]-[CH;D2;+0:11]=[CH;D2;+0:12]-[CH;D2;+0:13]=[C;H0;D3;+0:14]-1-2.[C:15]-[C:16]-[OH;D1;+0:17]>>[C:4]-[#7:5]1-[C:6]-[C:7]-[C:8]-[c;H0;D3;+0:9]2:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[c;H0;D3;+0:1...
null
[]
null
null
3
HOUR
To a stirred solution of 233.4 g (1 mole) of N-hydroxyhexyltetrahydroquinoline and 153.1 g (1.5 moles) of acetic anhydride in dichloromethane are added 151.8 g (1.5 moles) of triethylamine and 8.5 g (1 mole %) of 4-N,N-dimethylaminopyridine, and the reaction is stirred at room temperature for 3 hours. The product solut...
10.6084/m9.figshare.5104873.v1
null
Enamine.Anhydride.Primary alcohol.Conjugated diene
Ester
C1=CCC2CCC[NH]C2=C1
c1ccc2c(c1)CCC[NH]2
c1ccc2c(c1)CCC[NH]2
HO-
ClCCl
null
3
CC(=O)OC(C)=O.OCCCCCCN1CCCC2CC=CC=C21>ClCCl>CC(=O)OCCCCCCN1CCCc2ccccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f11fb9357654407f897a52ae5b73be5e
CC(=O)OCCCCCCN1CCCc2cc(C=O)ccc21>>O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO
[Cl-].[Na+].C(C)(=O)OCCCCCCN1CCCC2=CC(=CC=C12)C=O.[Br-].O1C(OCC1)C[P+](CCCC)(CCCC)CCCC.CC(C)([O-])C.[K+]>>OCCCCCCN1CCCC2=CC(=CC=C12)C=CC=O
O=[CH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH2:12][CH2:13][N:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][O:21][C:2](=[O:1])[CH3:3]>>[O:1]=[CH:2][CH:3]=[CH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]([cH:10]1)[CH2:11][CH2:12][CH2:13][N:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19][CH2:20][OH:21]
CC(=O)OCCCCCCN1CCCc2cc(C=O)ccc21
O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO
null
null
CN(C=O)C.Cl.O
Miscellaneous
OtherReaction
716d431b21b76dc7be86288acf6b079ba424a010e3c36e2883035373997c7f75
8312bfe1cc7896204f42ca6a876ec15c050ef293944cf9da7ac1091018dad53e
c1ccc2c(c1)CCCN2
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6]-[O;H0;D2;+0:7]-[C;H0;D3;+0:8](-[CH3;D1;+0:9])=[O;D1;H0:10]>>[C:5]-[C:6]-[OH;D1;+0:7].[O;D1;H0:10]=[CH;D2;+0:8]-[CH;D2;+0:9]=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
90
CELSIUS
16
HOUR
To a solution 30.3 g (0.1 mole) of N-acetoxyhexyl-1,2,3,4-tetrahydroquinoline-6-carboxaldehyde in dimethylformamide is added 7.4 g (0.2 mole) of 1,3-dioxolan-2-ylmethyltributylphosphonium bromide in dimethylformamide with magnetic stirring, and the mixture is heated at 90° C. Potassium t-butoxide (22.4 g, 0.2 mole) is ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ester
Aldehyde.Primary alcohol
null
null
c1ccc2c(c1)CCC[NH]2
Other
CN(C=O)C.Cl.O
90
16
CC(=O)OCCCCCCN1CCCc2cc(C=O)ccc21>CN(C=O)C.Cl.O>O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-a8c9dc88ef314c6e9a5ee94f173add5d
Cc1ccc(C=O)cc1.Nc1ccccc1O>>Cc1ccc(-c2nc3ccccc3o2)cc1
C(C)(=O)[O-].C(C)(=O)[O-].C(C)(=O)[O-].C(C)(=O)[O-].[Pb+4].C1(=CC=C(C=C1)C=O)C.NC1=C(C=CC=C1)O.O>>CC1=CC=C(C=C1)C=1OC2=C(N1)C=CC=C2
O=[CH:6][c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:16][cH:15]1.[NH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][c:13]1[OH:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[o:14]2)[cH:15][cH:16]1
Cc1ccc(C=O)cc1.Nc1ccccc1O
Cc1ccc(-c2nc3ccccc3o2)cc1
null
null
C1(=CC=CC=C1)C
Aromatic Heterocycle Formation
Benzoxazole formation from aldehyde
3007b82893b25bcfc73c3208dc34ba7e37187776b8cbc5d23974d3df8a2d6e45
3b6ccbcd4ed8797e873d439bcb50326831cedfa183da57a93f69bf0c36077684
c1ccc(-c2nc3ccccc3o2)cc1
O=[CH;D2;+0:1]-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6].[NH2;D1;+0:7]-[c:8](:[c:9]):[c:10](-[OH;D1;+0:11]):[c:12]>>[c:12]:[c:10]1:[o;H0;D2;+0:11]:[c;H0;D3;+0:1](-[c;H0;D3;+0:2](:[c:3]:[c:4]):[c:5]:[c:6]):[n;H0;D2;+0:7]:[c:8]:1:[c:9]
null
[]
null
null
8
HOUR
A solution of 12 g (0.1 mole) of 4-tolualdehyde and 10.9 g (0.1 mole) of 2-aminophenol in toluene is heated at reflux with azeotropic removal of water. After 20 hours at reflux, the reaction is cooled to room temperature, 44.3 g (0.1 mole) of lead tetraacetate is added, and the mixture is stirred at room temperature ov...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Aromatic alcohol.Primary amine
null
c1ccccc1
c1ccc2ocnc2c1
c1ccccc1.c1ccc2ocnc2c1
HO-
C1(=CC=CC=C1)C
null
8
Cc1ccc(C=O)cc1.Nc1ccccc1O>C1(=CC=CC=C1)C>Cc1ccc(-c2nc3ccccc3o2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5c4084f677714fefb5da04262b23b483
Cc1ccc(-c2nc3ccccc3o2)cc1.O=C1CCC(=O)N1Br>>BrCc1ccc(-c2nc3ccccc3o2)cc1
CC1=CC=C(C=C1)C=1OC2=C(N1)C=CC=C2.BrN1C(CCC1=O)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O>>BrCC1=CC=C(C=C1)C=1OC2=C(N1)C=CC=C2
[CH3:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[n:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[o:15]2)[cH:16][cH:17]1.O=C1CCC(=O)N1[Br:1]>>[Br:1][CH2:2][c:3]1[cH:4][cH:5][c:6](-[c:7]2[n:8][c:9]3[cH:10][cH:11][cH:12][cH:13][c:14]3[o:15]2)[cH:16][cH:17]1
Cc1ccc(-c2nc3ccccc3o2)cc1.O=C1CCC(=O)N1Br
BrCc1ccc(-c2nc3ccccc3o2)cc1
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccc(-c2nc3ccccc3o2)cc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
A stirred solution of 20.9 g (0.1 mole) of 2-(4-methylphenyl)benzoxazole, 17.8 g (0.1 mole) of N-bromosuccinimide, and 0.4 g (0.2 mole %) of benzoyl peroxide in carbon tetrachloride is heated at reflux for 20 hours. After cooling to room temperature, the reaction is diluted by the addition of carbon tetrachloride, and ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1.c1ccc2ocnc2c1
HO-
C(Cl)(Cl)(Cl)Cl
null
null
Cc1ccc(-c2nc3ccccc3o2)cc1.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>BrCc1ccc(-c2nc3ccccc3o2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-c3e99be3835445b2abbdee8d3ce15e26
BrCc1ccc(-c2nc3ccccc3o2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1>>Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.[Br-]
BrCC1=CC=C(C=C1)C=1OC2=C(N1)C=CC=C2.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>[Br-].O1C(=NC2=C1C=CC=C2)C2=CC(=C(C=C2)C)[P+](C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2
[CH2:1]([c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][c:8]3[cH:9][cH:10][cH:11][cH:12][c:13]3[o:14]2)[cH:15][cH:16]1)[Br:36].[P:17]([c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)([c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1)[c:30]1[cH:31][cH:32][cH:33][cH:34][cH:35]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[n:7][c:8]3[cH:9][cH:10][...
BrCc1ccc(-c2nc3ccccc3o2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1
Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.[Br-]
null
null
C=1(C(=CC=CC1)C)C
Miscellaneous
OtherReaction
580dbda2d71c1ade592946b82319659b10473e14402a8d60005effee81e40ce7
60e0209a3e01281b77ea7e07e181a846736713b5a4a90ae8d47a0480f9ce79e5
c1ccc([P+](c2ccccc2)(c2ccccc2)c2cccc(-c3nc4ccccc4o3)c2)cc1
[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[c:3](:[c:4]):[cH;D2;+0:5]:[c:6]:[c:7].[c:8]:[c:9](-[P;H0;D3;+0:10](-[c:11](:[c:12]):[c:13])-[c:14](:[c:15]):[c:16]):[c:17]>>[Br-;H0;D0:1].[CH3;D1;+0:2]-[c:3](:[c:4]):[c;H0;D3;+0:5](-[P+;H0;D4:10](-[c:9](:[c:8]):[c:17])(-[c:11](:[c:12]):[c:13])-[c:14](:[c:15]):[c:16]):[c:6]:[c:7]
null
[]
null
null
null
null
A stirred solution of 28.8 g (0.1 mole) of 2-(4-bromomethylphenyl)benzoxazole and 28.8 g (0.1 mole) of triphenylphosphine in xylene is heated at reflux for 19 hours. The product is then isolated by filtration, washed with additional portions of xylene, and dried. Conditions: See reaction.notes.procedure_details. Workup...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2ocnc2c1.c1ccccc1.c1ccccc1.c1ccccc1
null
C=1(C(=CC=CC1)C)C
null
null
BrCc1ccc(-c2nc3ccccc3o2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1>C=1(C(=CC=CC1)C)C>Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.[Br-]
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-56e0c8bc731e4aa9a568d920148f452a
Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO>>OCCCCCCN1CCCc2cc(C=CC=Cc3ccc(-c4nc5ccccc5o4)cc3)ccc21
O.[Li]CCCC.[Br-].O1C(=NC2=C1C=CC=C2)C2=CC(=C(C=C2)C)[P+](C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2.OCCCCCCN1CCCC2=CC(=CC=C12)C=CC=O>>OCCCCCCN1CCCC2=CC(=CC=C12)C=CC=CC1=CC=C(C=C1)C=1OC2=C(N1)C=CC=C2
c1ccc([P+](c2ccccc2)(c2ccccc2)[c:33]2[c:19]([CH3:18])[cH:20][cH:21][c:22](-[c:23]3[n:24][c:25]4[cH:26][cH:27][cH:28][cH:29][c:30]4[o:31]3)[cH:32]2)cc1.O=[CH:17][CH:16]=[CH:15][c:14]1[cH:13][c:12]2[c:36]([cH:35][cH:34]1)[N:8]([CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][OH:1])[CH2:9][CH2:10][CH2:11]2>>[OH:1][CH2:2][CH2:3]...
Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO
OCCCCCCN1CCCc2cc(C=CC=Cc3ccc(-c4nc5ccccc5o4)cc3)ccc21
null
null
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
543566f4a6674a0bb62a9939a29cc850ad54f05e50d928975c9c5f4e9fb14baf
d70fa5718646c1ca7d5c68acab5b524370b238501cb432d711539d0f01ee6d2b
C(C=Cc1ccc2c(c1)CCCN2)=Cc1ccc(-c2nc3ccccc3o2)cc1
O=[CH;D2;+0:1]-[C:2]=[C:3]-[c:4].[CH3;D1;+0:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[P+](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[c:9]:[c:10]>>[c:4]-[C:3]=[C:2]-[CH;D2;+0:1]=[CH;D2;+0:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]
null
[]
null
null
18
HOUR
To a stirred mixture of 110 g (0.2 mole) of 4-(benzoxazol-2-yl)tolyltriphenylphosphonium bromide in toluene is added dropwise 0.2 mole of n-BuLi at room temperature. After 2 hours a solution of 28.7 g (0.1 mole) of 3-(N-hydroxyhexyl-1,2,3,4-tetrahydroquinolin-6-yl)acrolein in toluene is added dropwise to the mixture, a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Conjugated diene
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1
c1ccc2c(c1)CCC[NH]2.c1ccccc1.c1ccc2ocnc2c1
HO-
C1(=CC=CC=C1)C
null
18
Cc1ccc(-c2nc3ccccc3o2)cc1[P+](c1ccccc1)(c1ccccc1)c1ccccc1.O=CC=Cc1ccc2c(c1)CCCN2CCCCCCO>C1(=CC=CC=C1)C>OCCCCCCN1CCCc2cc(C=CC=Cc3ccc(-c4nc5ccccc5o4)cc3)ccc21
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ed7c34e35eb445bc9fee78139710e092
CC(C)(C)OC(=O)NC1C=NC=CS1.Nc1cccnc1>>Nc1cnccc1S
NC=1C=NC=CC1.[Cl-].[NH4+].C(C)(C)(C)OC(=O)NC1C=NC=CS1.Cl.NC=1C=NC=CC1.[S].C(C)(C)(C)OC(=O)OC(=O)OC(C)(C)C.C(CCC)[Li].NC1=NC=CC=C1>>Cl.NC=1C=NC=CC1S
CC(C)(C)OC(=O)N[CH:8]1[CH:7]=NC=C[S:9]1.c1c[cH:6][n:5][cH:4][c:3]1[NH2:2]>>[NH2:2][c:3]1[cH:4][n:5][cH:6][cH:7][c:8]1[SH:9]
CC(C)(C)OC(=O)NC1C=NC=CS1.Nc1cccnc1
Nc1cnccc1S
null
null
C(C)(=O)O.O1CCCC1
Miscellaneous
OtherReaction
4e53348320e93bccd881d297828ae2b10fd6c1a6b366daeec84e9b9206498efd
bd2e00fab2599223209d95fda741085272d9281a066aab16d41f2878f6c425f2
c1ccncc1
C-C(-C)(-C)-O-C(=O)-N-[CH;D3;+0:1]1-[CH;D2;+0:2]=N-C=C-[S;H0;D2;+0:3]-1.[N;D1;H2:4]-[c;H0;D3;+0:5]1:[c:6]:[#7;a:7]:[cH;D2;+0:8]:c:c:1>>[N;D1;H2:4]-[c;H0;D3;+0:5]1:[c:6]:[#7;a:7]:[cH;D2;+0:8]:[cH;D2;+0:2]:[c;H0;D3;+0:1]:1-[SH;D1;+0:3]
null
[]
null
null
null
null
In Scheme (3), 3-aminopyridine is acylated with di-t-butyldicarbonate to introduce the t-butoxycarbonyl (t-BOC) protecting group. (It will be appreciated that two other pyridinothiazolothio mercaptans may be prepared by known methodology using other amino pyridine isomers.) The t-BOC protected 3-aminopyridine is then t...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Substituted imine.Monosulfide.Boc
Aromatic thiol
C1=CSCC=N1.c1ccncc1
c1ccncc1
c1ccncc1
HO-
C(C)(=O)O.O1CCCC1
null
null
CC(C)(C)OC(=O)NC1C=NC=CS1.Nc1cccnc1>C(C)(=O)O.O1CCCC1>Nc1cnccc1S
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-cc2ccc9b22a849008c758e58842ddd19
CC(C)(C)OC(=O)Nc1cnccc1S>>Nc1cnccc1S
C(C)(C)(C)OC(=O)NC=1C=NC=CC1S.Cl>>Cl.NC=1C=NC=CC1S
CC(C)(C)OC(=O)[NH:2][c:3]1[cH:4][n:5][cH:6][cH:7][c:8]1[SH:9]>>[NH2:2][c:3]1[cH:4][n:5][cH:6][cH:7][c:8]1[SH:9]
CC(C)(C)OC(=O)Nc1cnccc1S
Nc1cnccc1S
null
null
C(C)(=O)O
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1ccncc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]:[#7;a:5]:[c:6]
100
[{"value": 100.0, "product": "Cl.NC=1C=NC=CC1S", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A 13.78 g (0.06 mol) sample of 3-(t-butyloxycarbonyl)amino-4-mercapto pyridine was dissolved with acetic acid (250 mL) and added to an ice cold solution of ~3N HCl in acetic acid which had been made by bubbling HCl(g) through glacial acetic acid (100 mL). After about four hours the resulting solid was filtered, washed ...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccncc1
HO-
C(C)(=O)O
null
null
CC(C)(C)OC(=O)Nc1cnccc1S>C(C)(=O)O>Nc1cnccc1S
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-f8af3a28440c4b40b27400296150885d
O=[N+]([O-])c1cccnc1Cl.[N-]=C=S>>O=[N+]([O-])c1cccnc1N=C=S
ClC1=NC=CC=C1[N+](=O)[O-].[N-]=C=S.[K+]>>N(=C=S)C1=NC=CC=C1[N+](=O)[O-]
Cl[c:9]1[c:4]([N+:2](=[O:1])[O-:3])[cH:5][cH:6][cH:7][n:8]1.[N-:10]=[C:11]=[S:12]>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][n:8][c:9]1[N:10]=[C:11]=[S:12]
O=[N+]([O-])c1cccnc1Cl.[N-]=C=S
O=[N+]([O-])c1cccnc1N=C=S
null
null
C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
27647861574f183f1d13ed634cc9d1fa17a57d6f7f63bbfc9e771872c68742a9
be6b4969b868b064acf38b0c49ccd15931f1d8d0783e14c59d28ff8ffeddba70
c1ccncc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].[N-;H0;D1:7]=[C:8]=[S;D1;H0:9]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[N;H0;D2;+0:7]=[C:8]=[S;D1;H0:9]):[#7;a:2]:[c:3]
null
[]
null
null
null
null
A 10 g sample of 2-chloro-3-nitropyridine, an 8 g sample of potassium isothiocyanate, and 75 ml of acetic acid were combined and refluxed for 2 h. The reaction mixture was then cooled and poured into 400 ml of ice/H2O. The resulting solid was washed with water, redissolved in ethyl acetate and washed (4×) with water. T...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
Isothiocyanate
c1ccncc1
c1ccncc1
c1ccncc1
Other
C(C)(=O)O
null
null
O=[N+]([O-])c1cccnc1Cl.[N-]=C=S>C(C)(=O)O>O=[N+]([O-])c1cccnc1N=C=S
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-79ee1b74b31a41bdac5b200a71352fcd
ClCCOCCOCCCl.NCc1ccccc1>>c1ccc(CNCCOCCOCCNCc2ccccc2)cc1
C(C1=CC=CC=C1)N.ClCCOCCOCCCl>>C(C1=CC=CC=C1)NCCOCCOCCNCC1=CC=CC=C1
Cl[CH2:1][CH2:2][O:12][CH2:11][CH2:3][O:9][CH2:8][CH2:7]Cl.[c:4]1([CH2:5][NH2:6])[cH:18][cH:19][cH:20][cH:21][cH:22]1>>[cH:1]1[cH:2][cH:3][c:4]([CH2:5][NH:6][CH2:7][CH2:8][O:9][CH2:10][CH2:11][O:12][CH2:13][CH2:14][NH:15][CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[cH:23][cH:24]1
ClCCOCCOCCCl.NCc1ccccc1
c1ccc(CNCCOCCOCCNCc2ccccc2)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
b3892053c1eafd59ea3e581bb7123385d14c234c00bae7d2bac72faed5d9fb7e
9ca3e54d8c2d9428f8929837b66b2f22c82679eae81ee5f0378e863125572ea4
c1ccc(CNCCOCCOCCNCc2ccccc2)cc1
Cl-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[O;H0;D2;+0:3]-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[O;H0;D2;+0:6]-[C:7]-[CH2;D2;+0:8]-Cl.[NH2;D1;+0:9]-[C:10]-[c;H0;D3;+0:11]1:[cH;D2;+0:12]:[c:13]:[c:14]:[c:15]:[cH;D2;+0:16]:1>>[C:17]-[C:18]-[O;H0;D2;+0:3]-[CH2;D2;+0:4]-[C:19]-[O;H0;D2;+0:6]-[C:7]-[CH2;D2;+0:8]-[NH;D2;+0:9]-[C:10]-[c;H0;D3;+0:1...
null
[]
null
null
null
null
J. Gatto, et al. in "4,13-Diaza-18-Crown-6 (1,4,10,13-Tetraoxa-7,16-diazacyclooctadecane)," Organic Synthesis, Vol. 68, 1989, pp. 227-233, teach the preparation of the title compound by a three-step procedure that might be considered the standard preparation for these materials. First, benzylamine is reacted with 1,2-b...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ether.Ether.Primary amine
Ether.Ether.Secondary amine.Secondary amine
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
null
null
null
null
ClCCOCCOCCCl.NCc1ccccc1>>c1ccc(CNCCOCCOCCNCc2ccccc2)cc1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5d6c2380db7048b1ba438d1bba8589f6
BrC1CC1.CN1Cc2c(C=O)ncn2-c2ccncc2C1=O>>OC(C1=CNc2ccncc2C=N1)C1CC1
O1CCCC1.C1(CC1)[Mg]Br.[Mg].C1(CC1)Br.O1CCCC1.O1CCCC1.CN1CC=2N(C3=C(C1=O)C=NC=C3)C=NC2C=O>>N1C=C(N=CC2=C1C=CN=C2)C(O)C2CC2
Br[CH:14]1[CH2:15][CH2:16]1.C[N:13]1Cc2[c:3]([CH:2]=[O:1])n[cH:4][n:5]2-[c:6]2[cH:7][cH:8][n:9][cH:10][c:11]2[C:12]1=O>>[OH:1][CH:2]([C:3]1=[CH:4][NH:5][c:6]2[cH:7][cH:8][n:9][cH:10][c:11]2[CH:12]=[N:13]1)[CH:14]1[CH2:15][CH2:16]1
BrC1CC1.CN1Cc2c(C=O)ncn2-c2ccncc2C1=O
OC(C1=CNc2ccncc2C=N1)C1CC1
null
null
CN(P(=O)(N(C)C)N(C)C)C
Heteroatom Alkylation and Arylation
OtherReaction
195c597aab917323d56570a8e26a88ebc9fc82bd44b596ae21b64111ec4616b8
36df40030e480a3681c84c70c6280636c63a4235eafcc1fa595964e12f7e847a
C1=NC(CC2CC2)=CNc2ccncc21
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-1.C-[N;H0;D3;+0:4]1-C-c2:[c;H0;D3;+0:5](-[CH;D2;+0:6]=[O;H0;D1;+0:7]):n:[cH;D2;+0:8]:[n;H0;D3;+0:9]:2-[c;H0;D3;+0:10]2:[c:11]:[c:12]:[#7;a:13]:[c:14]:[c:15]:2-[C;H0;D3;+0:16]-1=O>>[OH;D1;+0:7]-[CH;D3;+0:6](-[C;H0;D3;+0:5]1=[CH;D2;+0:8]-[NH;D2;+0:9]-[c;H0;D3;+0:10]2:[c:11]:[c:12]:[#7;a:13]:[...
5
[{"value": 5.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of cyclopropyl magnesium bromide in dry tetrahydrofuran (prepared from 72 mg (3 mmole)) of magnesium and 362 mg (3 mmole) of cyclopropyl bromide in 4 ml of tetrahydrofuran was added at room temperature in one portion a suspension of 240 mg (1 mmole)of 5,6-dihydro-5-methyl-6-oxo-4H-imidazo [1,5-a]-pyrido [...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aldehyde.Tertiary amide
Enamine.Substituted imine.Secondary alcohol
C1CC1.c1cc2c(cn1)C[NH]Cc1cncn12
C1=CNc2ccncc2C=N1.C1CC1
C1=CNc2ccncc2C=N1.C1CC1
HBr
CN(P(=O)(N(C)C)N(C)C)C
null
1
BrC1CC1.CN1Cc2c(C=O)ncn2-c2ccncc2C1=O>CN(P(=O)(N(C)C)N(C)C)C>OC(C1=CNc2ccncc2C=N1)C1CC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-5669067be2dd44efab57c051c34b17f5
NC(=O)c1cnn2c1NCC=C2c1cccc(C(F)(F)F)c1.S=C=S>>CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
FC(C=1C=C(C=CC1)C1=CCNC=2N1N=CC2C(=O)N)(F)F.CC(C)([O-])C.[K+].C(=S)=S>>CSC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O
[NH2:4][C:5](=[O:6])[c:7]1[cH:8][n:9][n:10]2[c:11]1[NH:12][CH2:13][CH:14]=[C:15]2[c:16]1[cH:17][cH:18][cH:19][c:20]([C:21]([F:22])([F:23])[F:24])[cH:25]1.S=[C:3]=[S:2]>>[CH3:1][S:2][c:3]1[n:4][c:5](=[O:6])[c:7]2[cH:8][n:9][n:10]3[c:11]2[n:12]1[CH2:13][CH:14]=[C:15]3[c:16]1[cH:17][cH:18][cH:19][c:20]([C:21]([F:22])([F:2...
NC(=O)c1cnn2c1NCC=C2c1cccc(C(F)(F)F)c1.S=C=S
CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
null
null
O1CCCC1
Aromatic Heterocycle Formation
OtherReaction
159a87f29c09ab117d87c33456fa0aa717d0c1b5ab1dc6117e9039650144895f
52ca609e0ddb9fbbdbd11d400361a38aa8d2c2913a103a89bb982ae5f37d98a5
O=c1ncn2c3c1cnn3C(c1ccccc1)=CC2
S=[C;H0;D2;+0:1]=[S;H0;D1;+0:2].[NH2;D1;+0:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[c:6]1:[c:7]:[#7;a:8]:[#7;a:9]2:[c:10]:1-[NH;D2;+0:11]-[C:12]-[C:13]=[C:14]-2-[c:15]>>[C;D1;H3:16]-[S;H0;D2;+0:2]-[c;H0;D3;+0:1]1:[n;H0;D2;+0:3]:[c;H0;D3;+0:4](=[O;D1;H0:5]):[c:6]2:[c:7]:[#7;a:8]:[#7;a:9]3:[c:10]:2:[n;H0;D3;+0:11]:1-[C:12]-[C:13...
90.5
[{"value": 90.0, "product": "CSC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.5, "product": "CSC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-6.2
CELSIUS
45
MINUTE
A solution of 3.18 kg of 4,5-dihydro-7-[3-(trifluoromethyl)-phenyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide in 30 L of tetrahydrofuran is cooled to 2.8° C. under nitrogen and stirred while 1370 g of potassium tert-butoxide is added portionwise over 25 minutes while maintaining a temperature less than 4° C. The reaction ...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Secondary amine
Monosulfide
C1=Cn2nccc2NC1
C1=CCn2cncc3cnn1c32
C1=CCn2cncc3cnn1c32.c1ccccc1
null
O1CCCC1
-6.2
0.75
NC(=O)c1cnn2c1NCC=C2c1cccc(C(F)(F)F)c1.S=C=S>O1CCCC1>CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-eadcefa2a05d42d58610fc3268716e7a
CC(C)N.CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1>>CC(C)Nc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
CSC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O.C(C)(C)N.C(C)O.C(C)O>>CC(C)NC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O
[CH3:1][CH:2]([CH3:3])[NH2:4].CS[c:5]1[n:6][c:7](=[O:8])[c:9]2[cH:10][n:11][n:12]3[c:13]2[n:14]1[CH2:15][CH:16]=[C:17]3[c:18]1[cH:19][cH:20][cH:21][c:22]([C:23]([F:24])([F:25])[F:26])[cH:27]1>>[CH3:1][CH:2]([CH3:3])[NH:4][c:5]1[n:6][c:7](=[O:8])[c:9]2[cH:10][n:11][n:12]3[c:13]2[n:14]1[CH2:15][CH:16]=[C:17]3[c:18]1[cH:1...
CC(C)N.CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
CC(C)Nc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
null
null
C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
ba5bcb07336db7f2300c2868569a4481815a759d4c806fe39f12f9bc7feed0b0
88e0224d19b2dce8f9987d52554afb32090d36ff7ee19e89dc5bf66d30974ec4
O=c1ncn2c3c1cnn3C(c1ccccc1)=CC2
C-S-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]2:[c:5]:[#7;a:6]:[#7;a:7]3:[c:8]:2:[#7;a:9]:1-[C:10]-[C:11]=[C:12]-3.[C;D1;H3:13]-[C:14](-[C;D1;H3:15])-[NH2;D1;+0:16]>>[C;D1;H3:13]-[C:14](-[C;D1;H3:15])-[NH;D2;+0:16]-[c;H0;D3;+0:1]1:[#7;a:2]:[c:3]:[c:4]2:[c:5]:[#7;a:6]:[#7;a:7]3:[c:8]:2:[#7;a:9]:1-[C:10]-[C:11]=[C:12]-3
62.3
[{"value": 62.3, "product": "CC(C)NC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 62.1, "product": "CC(C)NC1=NC(C=2C=NN3C(=CCN1C32)C3=CC(=CC=C3)C(F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
To a suspension of 5.0 g of 5-(methylthio)-8-[3-(trifluoromethyl)phenyl]-3H,6H-1,4,5a,8a-tetraazaacenaphthylen-3-one in 35 ml of acetic acid is added 2.64 g of isopropylamine. The reaction mixture is heated on a steambath for 18 hours. The resulting solution is cooled to room temperature and 17 ml of ethanol added. The...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Monosulfide
Secondary amine
C1=CCn2cncc3cnn1c32
C1=CCn2cncc3cnn1c32
C1=CCn2cncc3cnn1c32.c1ccccc1
Other
C(C)(=O)O
null
0.5
CC(C)N.CSc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1>C(C)(=O)O>CC(C)Nc1nc(=O)c2cnn3c2n1CC=C3c1cccc(C(F)(F)F)c1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-695590d38ba04361a966067c6963981f
N#Cc1ccccc1N.O=C1CCCC(=O)C1>>N#Cc1ccccc1NC1=CC(=O)CCC1
NC1=C(C#N)C=CC=C1.C1(CC(CCC1)=O)=O>>O=C1C=C(CCC1)NC1=C(C#N)C=CC=C1
[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[NH2:9].O=[C:10]1[CH2:11][C:12](=[O:13])[CH2:14][CH2:15][CH2:16]1>>[N:1]#[C:2][c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[NH:9][C:10]1=[CH:11][C:12](=[O:13])[CH2:14][CH2:15][CH2:16]1
N#Cc1ccccc1N.O=C1CCCC(=O)C1
N#Cc1ccccc1NC1=CC(=O)CCC1
null
O.CC1=CC=C(C=C1)S(=O)(=O)O
O
Heteroatom Alkylation and Arylation
OtherReaction
b5fad61eda15276f50ae7bc35245e587435b6eeee71b12fe6b584707eb92cb10
9b8ae7e5b30e191314c6441607ab55dc332b8bb8a66eba32f5a7b73c6f6f2034
O=C1C=C(Nc2ccccc2)CCC1
O=[C;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5](=[O;D1;H0:6])-[CH2;D2;+0:7]-1.[NH2;D1;+0:8]-[c:9](:[c:10]):[c:11]>>[O;D1;H0:6]=[C:5]1-[C:4]-[C:3]-[C:2]-[C;H0;D3;+0:1](-[NH;D2;+0:8]-[c:9](:[c:10]):[c:11])=[CH;D2;+0:7]-1
93
[{"value": 93.0, "product": "O=C1C=C(CCC1)NC1=C(C#N)C=CC=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.8, "product": "O=C1C=C(CCC1)NC1=C(C#N)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-aminobenzonitrile (120 g) and 1,3-cyclohexandione (120 g) in water (400 ml) was heated to 40° and 4-methylbenzenesulfonic acid monohydrate (6.2 g) was added, with stirring. The mixture was stirred at 40° for 1 hr. The mixture was filtered, and the filter cake was washed with water to provide 200 g (93%) ...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Primary amine
Enamine
C1CCCCC1
C1=CCCCC1
c1ccccc1.C1=CCCCC1
HO-
O.CC1=CC=C(C=C1)S(=O)(=O)O.O
null
null
N#Cc1ccccc1N.O=C1CCCC(=O)C1>O.CC1=CC=C(C=C1)S(=O)(=O)O.O>N#Cc1ccccc1NC1=CC(=O)CCC1
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-ef26d013c4cc405e8068592ad63dfa26
N#Cc1ccccc1N.O=C1CCCCC1>>Nc1c2c(nc3ccccc13)CCCC2.O
Cl.NC1=C(C#N)C=CC=C1.C1(CCCCC1)=O.Cl>>O.NC=1C2=CC=CC=C2N=C2CCCCC12
[N:1]#[C:2][c:11]1[c:6]([NH2:5])[cH:7][cH:8][cH:9][cH:10]1.[C:3]1(=[O:16])[CH2:4][CH2:12][CH2:13][CH2:14][CH2:15]1>>[NH2:1][c:2]1[c:3]2[c:4]([n:5][c:6]3[cH:7][cH:8][cH:9][cH:10][c:11]13)[CH2:12][CH2:13][CH2:14][CH2:15]2.[OH2:16]
N#Cc1ccccc1N.O=C1CCCCC1
Nc1c2c(nc3ccccc13)CCCC2.O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
2dd1f9e0e8eafd34226d7996df8c63bc3e7f04d2db44935e4c1d66db8009fc46
cba055f16bb6d8902fe3b7ee13bd8e7822896a26eeb51828f22dbf1978e995c7
c1ccc2nc3c(cc2c1)CCCC3
[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5](-[NH2;D1;+0:6]):[c:7].[O;H0;D1;+0:8]=[C;H0;D3;+0:9]1-[C:10]-[C:11]-[C:12]-[C:13]-[CH2;D2;+0:14]-1>>[NH2;D1;+0:1]-[c;H0;D3;+0:2]1:[c:3](:[c:4]):[c:5](:[c:7]):[n;H0;D2;+0:6]:[c;H0;D3;+0:14]2:[c;H0;D3;+0:9]:1-[C:10]-[C:11]-[C:12]-[C:13]-2.[OH2;D0;+0:8]
67
[{"value": 67.0, "product": "O.NC=1C2=CC=CC=C2N=C2CCCCC12", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-aminobenzonitrile (120 g), cyclohexanone (115.8 ml), conc hydrochloric acid (9.2 ml), and cuprous chloride (1.21 g) was heated under reflux for 3 days, with stirring. At the end of each 24 hr period, additional cuprous chloride (1.21 g) was added. At the end of the 3rd day, additional conc hydrochloric a...
10.6084/m9.figshare.5104873.v1
null
Ketone.Nitrile.Primary amine
Primary amine
c1ccccc1.C1CCCCC1
c1ccc2nc3c(cc2c1)CCCC3
c1ccc2nc3c(cc2c1)CCCC3
null
null
null
null
N#Cc1ccccc1N.O=C1CCCCC1>>Nc1c2c(nc3ccccc13)CCCC2.O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-63b9b2d355cb436f8db69da91037fe95
CN(C)C=O.COc1cccc(Cl)n1>>COc1nc(Cl)ccc1C=O
C(C)(=O)O.CN(C=O)C.C(C)(C)(C)[Li].ClC1=CC=CC(=N1)OC>>ClC1=CC=C(C(=N1)OC)C=O
CN(C)[CH:10]=[O:11].[CH3:1][O:2][c:3]1[n:4][c:5]([Cl:6])[cH:7][cH:8][cH:9]1>>[CH3:1][O:2][c:3]1[n:4][c:5]([Cl:6])[cH:7][cH:8][c:9]1[CH:10]=[O:11]
CN(C)C=O.COc1cccc(Cl)n1
COc1nc(Cl)ccc1C=O
null
null
CCOCC.C1CCOC1
C-C Coupling
OtherReaction
fdadf445bc7330d90b7bd9b20fa76e9137f072d7efd4f8187f2f956f7d29eb78
f0bd75a0630092c31f21f61f4a015c77ae0dff14a0b742b4370d7a38fda490f7
c1ccncc1
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].[#8:3]-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[cH;D2;+0:9]:1>>[#8:3]-[c:4]1:[#7;a:5]:[c:6]:[c:7]:[c:8]:[c;H0;D3;+0:9]:1-[CH;D2;+0:1]=[O;D1;H0:2]
75
[{"value": 75.0, "product": "ClC1=CC=C(C(=N1)OC)C=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 74.6, "product": "ClC1=CC=C(C(=N1)OC)C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
1
HOUR
To a solution of tert-butyllithium (1.7 M in pentane, 48.5 mL, 83.0 mmol) in 150 mL of THF at -78° C. was added 6-chloro-2-methoxypyridine (8.94 mL, 75.0 mmol) over 5 min. The reaction mixture was stirred at -78° C. for 1 h, then dimethylformamide (7.55 mL, 97 mmol) was added and the mixture was stirred at this tempera...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Aldehyde
c1ccncc1
c1ccncc1
c1ccncc1
Other
CCOCC.C1CCOC1
-78
1
CN(C)C=O.COc1cccc(Cl)n1>CCOCC.C1CCOC1>COc1nc(Cl)ccc1C=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-7c63c4175fe54b74b2ffdf5c102f7d48
COc1nc(Cl)ccc1C=O.II>>COc1nc(Cl)cc(I)c1C=O
II.ClC1=CC=C(C(=N1)OC)C=O.[Li]CCCC.CN(CCNC)C.[Li]CCCC>>ClC1=CC(=C(C(=N1)OC)C=O)I
[CH3:1][O:2][c:3]1[n:4][c:5]([Cl:6])[cH:7][cH:8][c:10]1[CH:11]=[O:12].I[I:9]>>[CH3:1][O:2][c:3]1[n:4][c:5]([Cl:6])[cH:7][c:8]([I:9])[c:10]1[CH:11]=[O:12]
COc1nc(Cl)ccc1C=O.II
COc1nc(Cl)cc(I)c1C=O
null
null
COCCOC
Functional Group Interconversion
OtherReaction
66a492ff31bfcbb52d9a760416ba269a4cf5a439a6c2ca9c2c3a3ed0a750b974
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccncc1
I-[I;H0;D1;+0:1].[#8:2]-[c:3]1:[#7;a:4]:[c:5](-[Cl;D1;H0:6]):[c:7]:[cH;D2;+0:8]:[c:9]:1-[C:10]=[O;D1;H0:11]>>[#8:2]-[c:3]1:[#7;a:4]:[c:5](-[Cl;D1;H0:6]):[c:7]:[c;H0;D3;+0:8](-[I;H0;D1;+0:1]):[c:9]:1-[C:10]=[O;D1;H0:11]
51.3
[{"value": 51.3, "product": "ClC1=CC(=C(C(=N1)OC)C=O)I", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-23
CELSIUS
20
MINUTE
To a solution of N,N,N'-trimethylethylenediamine (2.46 mL, 19.23 mmol) in 15 mL of 1,2-dimethoxyethane at -23° C. was added n-BuLi (9.22 mL, 19.23 mmol), and the solution was stirred at -23° C. for 20 min. The mixture was transferred using a double-tipped needle to a solution of 6-chloro-2-methoxy-3-pyridinecarboxaldeh...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncc1
c1ccncc1
c1ccncc1
HI
COCCOC
-23
0.333333
COc1nc(Cl)ccc1C=O.II>COCCOC>COc1nc(Cl)cc(I)c1C=O
ord_dataset-02ee2261663048188cf6d85d2cc96e3f
ord-36aa6e8ebe7944bf8139e096653ebd8c
CO.COc1nc(Cl)cc(I)c1C=O>>COCc1c(I)cc(Cl)nc1OC
FC(C(=O)O)(F)F.ClC1=CC(=C(C(=N1)OC)C=O)I.C(C)[SiH](CC)CC.CO.C(=O)(O)[O-].[Na+]>>ClC1=NC(=C(C(=C1)I)COC)OC
O[CH3:1].[O:2]=[CH:3][c:4]1[c:5]([I:6])[cH:7][c:8]([Cl:9])[n:10][c:11]1[O:12][CH3:13]>>[CH3:1][O:2][CH2:3][c:4]1[c:5]([I:6])[cH:7][c:8]([Cl:9])[n:10][c:11]1[O:12][CH3:13]
CO.COc1nc(Cl)cc(I)c1C=O
COCc1c(I)cc(Cl)nc1OC
null
null
CCOCC
Heteroatom Alkylation and Arylation
OtherReaction
1d76918cc19966c7516bfe9a97a96abd1d20ff1b6b551b7a2a7721be5b12e885
a9e58bdb270b8602210135fa12a97050bf42474a87c9f2c3a2f396b5330373a5
c1ccncc1
O-[CH3;D1;+0:1].[#8:2]-[c:3](:[#7;a:4]:[c:5]):[c:6](-[CH;D2;+0:7]=[O;H0;D1;+0:8]):[c:9]>>[#8:2]-[c:3](:[#7;a:4]:[c:5]):[c:6](-[CH2;D2;+0:7]-[O;H0;D2;+0:8]-[CH3;D1;+0:1]):[c:9]
93
[{"value": 93.0, "product": "ClC1=NC(=C(C(=C1)I)COC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.0, "product": "ClC1=NC(=C(C(=C1)I)COC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
25
CELSIUS
14
HOUR
To a mixture of 6-chloro-4-iodo-2-methoxy-3-pyridinecarboxaldehyde (1.07 g, 3.60 mmol), triethylsilane (0.86 mL, 5.40 mmol) and methanol (0.43 mL, 10.6 mmol) at 0° C. was added trifluoroacetic acid (2.2 mL, 28.6 mmol), and the resulting solution was stirred at 25° C. for 14 h. After dilution with ether (30 mL), saturat...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Methanol
Ether
null
null
c1ccncc1
Other
CCOCC
25
14
CO.COc1nc(Cl)cc(I)c1C=O>CCOCC>COCc1c(I)cc(Cl)nc1OC