dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
time_units
large_stringclasses
4 values
procedure_details
large_stringlengths
1
23.6k
reference
large_stringclasses
96 values
doi
large_stringclasses
19 values
functional_groups_reactants
large_stringlengths
3
716
functional_groups_products
large_stringlengths
3
539
participating_rings_reactants
large_stringlengths
5
293
participating_rings_products
large_stringlengths
5
271
all_rings_products
large_stringlengths
5
271
byproduct_smiles
large_stringclasses
176 values
agent_smiles
large_stringlengths
1
712
temperature_c
float64
-230
30.1k
reaction_time_hours
float64
0
2.16k
reaction_smiles_with_agents
large_stringlengths
4
882
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d5d90023934e416fa9241ef7aa4c808a
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
Cl.CN(CCCN=C=NCC)C.C(C1=CC=CC=C1)OC([C@H](N)CC1=CNC2=CC=CC=C12)=O.O.ON1N=NC2=C1C=CC=C2.C(C)(C)(C)OC(=O)NC(C)(C(=O)O)C>>C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)OCC1=CC=CC=C1)CC1=CNC2=CC=CC=C12)(C)C
O[C:12]([C:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])([CH3:10])[CH3:11])=[O:13].[NH2:14][C@H:15]([CH2:16][c:17]1[cH:18][nH:19][c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]12)[C:26](=[O:27])[O:28][CH2:29][c:30]1[cH:31][cH:32][cH:33][cH:34][cH:35]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C:9](...
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
null
null
C(Cl)(Cl)Cl.O
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCc1c[nH]c2ccccc12)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[C;D1;H3:13].[C:14]-[C:15](-[NH2;D1;+0:16])-[C:17](=[O;D1;H0:18])-[#8:19]-[C:20]>>[C:14]-[C:15](-[NH;D2;+0:16]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:...
null
[]
null
null
4
HOUR
Crude D-tryptophan benzyl ester (1.0 g, 3.40 mmol), 1-hydroxybenztriazole hydrate (0.63 g, 4.1 mmol) and t-butoxycarbonyl-α-methylalanine (0.84 g, 4.11 mmol) were stirred together at room temperature in chloroform (20 mL). 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (980 mg, 5.11 mmol) was added to this...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
C(Cl)(Cl)Cl.O
null
4
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>C(Cl)(Cl)Cl.O>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-80904ffecdf74601af3321b00e801887
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O
C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)OCC1=CC=CC=C1)CC1=CNC2=CC=CC=C12)(C)C>>C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)O)CC1=CNC2=CC=CC=C12)(C)C
c1ccc(C[O:28][C:26]([C@H:15]([NH:14][C:12]([C:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])([CH3:10])[CH3:11])=[O:13])[CH2:16][c:17]2[cH:18][nH:19][c:20]3[cH:21][cH:22][cH:23][cH:24][c:25]23)=[O:27])cc1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C:9]([CH3:10])([CH3:11])[C:12](=[O:13])[NH:14][C...
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O
null
[Pd]
C(C)(=O)OCC
Deprotection
Ester saponification (alkyl deprotection)
86a971d3e4f88009ab4c98512e9f1deb51b2f0ce5cbd068cc61ae878c1e58e2a
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccc2[nH]ccc2c1
[C:1]-[C:2](=[O;D1;H0:3])-[O;H0;D2;+0:4]-C-c1:c:c:c:c:c:1>>[C:1]-[C:2](=[O;D1;H0:3])-[OH;D1;+0:4]
102.1
[{"value": 102.0, "product": "C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)O)CC1=CNC2=CC=CC=C12)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 102.1, "product": "C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)O)CC1=CNC2=CC=CC=C12)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
The benzyl ester (0.82 g, 1.71 mmol) obtained in Step C and 10% palladium on carbon (150 mg) were stirred together in ethyl acetate (5 mL). The solution was degassed and a hydrogen atmosphere introduced over the reactants using a balloon for 32 hours. The reaction products were isolated by filtering the reaction mixtur...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
c1ccccc1
null
c1ccc2[nH]ccc2c1
Other
[Pd].C(C)(=O)OCC
null
null
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>[Pd].C(C)(=O)OCC>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eb2559d3fc404f17a5ecee988d37d685
Cc1ccc(B(O)O)cc1.O=[N+]([O-])c1ccccc1Br>>Cc1ccc(-c2ccccc2[N+](=O)[O-])cc1
O.CC(C)O.C1(=CC=C(C=C1)B(O)O)C.BrC1=C(C=CC=C1)[N+](=O)[O-]>>CC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-]
OB(O)[c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:16][cH:15]1.Br[c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[N+:12](=[O:13])[O-:14]>>[CH3:1][c:2]1[cH:3][cH:4][c:5](-[c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[N+:12](=[O:13])[O-:14])[cH:15][cH:16]1
Cc1ccc(B(O)O)cc1.O=[N+]([O-])c1ccccc1Br
Cc1ccc(-c2ccccc2[N+](=O)[O-])cc1
null
null
[OH-].[Na+].C1=CC=CC=C1
C-C Coupling
Suzuki coupling with boronic acids
d79a78c79f0c392f0911481acf5c300cc98205269acdb93c24fb610a61c4c868
08d2969413ef1a2cd5b43667268ba178160c7b55545bf48018e31f2b019632ec
c1ccc(-c2ccccc2)cc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#7;+:5]):[c:6].O-B(-O)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[#7;+:5]-[c:4](:[c:6]):[c;H0;D3;+0:1](-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]):[c:2]:[c:3]
77.4
[{"value": 77.4, "product": "CC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A vigorously stirred mixture of 34 g (0.25 mol) of 4-tolylboronic acid and 34 g (0.17 mol) of 2-bromo-1-nitrobenzene in a mixture of 170 mL of 5N sodium hydroxide, 57 mL of water, 215 mL of 2-propanol and 1080 mL of benzene was treated with 11.9 g of (tetrakis)triphenylphosphine palladium(0). The two-phase mixture was ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Boronic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
HBr.B
[OH-].[Na+].C1=CC=CC=C1
null
null
Cc1ccc(B(O)O)cc1.O=[N+]([O-])c1ccccc1Br>[OH-].[Na+].C1=CC=CC=C1>Cc1ccc(-c2ccccc2[N+](=O)[O-])cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-27a0a2a0c29c44ca8129b0684f542de9
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O.NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1>>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1
C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)O)CC1=CNC2=CC=CC=C12)(C)C.NCC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-].C(C)N(CC)CC>>C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)NCC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-])CC1=CNC2=CC=CC=C12)(C)C
O[C:26]([C@H:15]([NH:14][C:12]([C:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])([CH3:10])[CH3:11])=[O:13])[CH2:16][c:17]1[cH:18][nH:19][c:20]2[cH:21][cH:22][cH:23][cH:24][c:25]12)=[O:27].[NH2:28][CH2:29][c:30]1[cH:31][cH:32][c:33](-[c:34]2[cH:35][cH:36][cH:37][cH:38][c:39]2[N+:40](=[O:41])[O-:42])[cH:43][c...
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O.NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCc1c[nH]c2ccccc12)NCc1ccc(-c2ccccc2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6]=[O;D1;H0:7].[NH2;D1;+0:8]-[C:9]-[c:10]>>[C:4]-[C:3](-[#7:5]-[C:6]=[O;D1;H0:7])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:8]-[C:9]-[c:10]
56.9
[{"value": 50.0, "product": "C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)NCC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-])CC1=CNC2=CC=CC=C12)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 56.9, "product": "C(C)(C)(C)OC(=O)NC(C(=O)N[C@@H](C(=O)NCC1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-])CC1=CNC2=CC=CC=C12)(C)C", "detai...
null
null
null
null
The acid (338 mg, 0.87 mmol) from Step D and 4-aminomethyl-2'-nitro-1,1'-biphenyl (200 mg, 0.87 mmol) and triethylamine (0.245 mL, 1.76 mmol) were dissolved in methylene chloride (8 mL) and stirred at room temperature. Benzotriazolyl-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (388 mg, 0.87 mmol) was adde...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
null
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O.NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1>C(Cl)Cl>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)NCc1ccc(-c2ccccc2[N+](=O)[O-])cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-30601e26cfe949648c03f18ace9a74dc
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1>>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C1=CC=CC=C1)OC([C@H](N)CCC1=CC=CC=C1)=O.C(C)N(CC)CC.C(C)(C)(C)OC(=O)NC(C)(C(=O)O)C>>C(C1=CC=CC=C1)OC([C@@H](CCC1=CC=CC=C1)NC(C(C)(C)NC(=O)OC(C)(C)C)=O)=O
O[C:12]([C:9]([NH:8][C:6]([O:5][C:2]([CH3:1])([CH3:3])[CH3:4])=[O:7])([CH3:10])[CH3:11])=[O:13].[NH2:14][C@H:15]([CH2:16][CH2:17][c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1)[C:24](=[O:25])[O:26][CH2:27][c:28]1[cH:29][cH:30][cH:31][cH:32][cH:33]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[O:5][C:6](=[O:7])[NH:8][C:9]([CH3:10])([CH...
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1
CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCCc1ccccc1)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7](=[O;D1;H0:8])-[#8:9]-[C:10](-[C;D1;H3:11])(-[C;D1;H3:12])-[C;D1;H3:13].[C:14]-[C:15](-[NH2;D1;+0:16])-[C:17](=[O;D1;H0:18])-[#8:19]-[C:20]>>[C:14]-[C:15](-[NH;D2;+0:16]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:...
null
[]
null
null
10
MINUTE
D-Homophenylalanine benzyl ester (0.87 g; 3.23 mmol), triethylamine (900 ml) and N-(t-butoxycarbonyl)-α-methylalanine (656 mg; 3.23 mmol) were dissolved in dry methylene chloride (6.5 ml) and benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP-reagent) (1.43 g; 3.23 mmol) was added with stirring...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
0.166667
CC(C)(C)OC(=O)NC(C)(C)C(=O)O.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1>C(Cl)Cl>CC(C)(C)OC(=O)NC(C)(C)C(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a50f7cac2645481a8747ad859fb15edc
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1>>CC(C)(CC(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C1=CC=CC=C1)OC([C@H](N)CCC1=CC=CC=C1)=O.C(C)N(CC)CC.C(C)(C)(C)OC(=O)NC(CC(=O)O)(C)C>>C(C1=CC=CC=C1)OC([C@@H](CCC1=CC=CC=C1)NC(CC(C)(C)NC(=O)OC(C)(C)C)=O)=O
O[C:5]([CH2:4][C:2]([CH3:1])([CH3:3])[NH:27][C:28](=[O:29])[O:30][C:31]([CH3:32])([CH3:33])[CH3:34])=[O:6].[NH2:7][C@H:8]([CH2:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[C:17](=[O:18])[O:19][CH2:20][c:21]1[cH:22][cH:23][cH:24][cH:25][cH:26]1>>[CH3:1][C:2]([CH3:3])([CH2:4][C:5](=[O:6])[NH:7][C@H:8]([CH2:9][C...
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1
CC(C)(CC(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCCc1ccccc1)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9](-[C:10])-[NH2;D1;+0:11]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9](-[C:10])-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
D-Homophenylalanine benzyl ester (725 mg; 3.23 mmol) whose preparation was described in Example 7 Step B, triethylamine (750 ml; 5,38 mmol) and 3-t-butoxycarbonylamino-3-methylbutanoic acid (585 mg; 2.69 mmol) were dissolved in dry methylene chloride (10 ml) and BOP (1.19 g, 2.69 mmol) was added with stirring in small ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
null
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1>C(Cl)Cl>CC(C)(CC(=O)N[C@H](CCc1ccccc1)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dbb9dc3e9fc84d65b7962d36a9ed7bea
C=CCO.CC(C)(C)OC(=O)N[C@H](CCc1ccccc1)C(=O)O>>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C
C(C)(C)(C)OC(=O)N[C@H](CCC1=CC=CC=C1)C(=O)O.C(C=C)O.C(CCl)Cl>>C(C=C)OC([C@H](NC(=O)OC(C)(C)C)CCC1=CC=CC=C1)=O
[CH2:1]=[CH:2][CH2:3][OH:4].O[C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[NH:16][C:17](=[O:18])[O:19][C:20]([CH3:21])([CH3:22])[CH3:23]>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[NH:16][C:17](=[O:18])[O:19][C:20]([CH3:2...
C=CCO.CC(C)(C)OC(=O)N[C@H](CCc1ccccc1)C(=O)O
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C
null
CN(C1=CC=NC=C1)C
C(Cl)Cl
Protection
Esterification of Carboxylic Acids
070670f68a20c1021da94fabee54def4688122fb721af5f52cd5a03630845d0e
0d8a72b7375d91aa7263e766e03a3cb7c4fa91e27abcd590409ff03b98eed690
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12].[C;D1;H2:13]=[C:14]-[C:15]-[OH;D1;+0:16]>>[C:4]-[C:3](-[#7:5]-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:16]-[C:15]-[...
null
[]
null
null
null
null
N-(t-Butoxycarbonyl)-D-homophenylalanine (2.0 g; 7.16 mmol), allyl alcohol (500 ml; 7.35 mmol) and 4-dimethylaminopyridine (88 mg; 0.72 mmol) were dissolved in dry methylene chloride and stirred at room temperature. EDC (1.4 g; 7.30 mmol) was added to the solution in small batches over 15 minutes and the reaction mixtu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccccc1
HO-
CN(C1=CC=NC=C1)C.C(Cl)Cl
null
null
C=CCO.CC(C)(C)OC(=O)N[C@H](CCc1ccccc1)C(=O)O>CN(C1=CC=NC=C1)C.C(Cl)Cl>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-65e718a8f3934e1487660a0d4b652d2f
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C>>C=CCOC(=O)[C@H](N)CCc1ccccc1
C(C=C)OC([C@H](NC(=O)OC(C)(C)C)CCC1=CC=CC=C1)=O.C([O-])(O)=O.[Na+].C1(=CC=CC=C1)OC.FC(C(=O)O)(F)F>>C(C=C)OC([C@H](N)CCC1=CC=CC=C1)=O
CC(C)(C)OC(=O)[NH:8][C@@H:7]([C:5]([O:4][CH2:3][CH:2]=[CH2:1])=[O:6])[CH2:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@H:7]([NH2:8])[CH2:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C
C=CCOC(=O)[C@H](N)CCc1ccccc1
null
null
C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
c1ccccc1
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7]-[C:8]=[C;D1;H2:9]>>[C:3]-[C:2](-[NH2;D1;+0:1])-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7]-[C:8]=[C;D1;H2:9]
null
[]
null
null
null
null
The allyl ester from Step A of this Example (1.96 g; 6.136 mmol) was dissolved in dry methylene chloride (10 ml) and anisole (5 ml) was added. The mixture was stirred at room temperature and trifluoroacetic acid was added drop by drop to the ester over 5 minutes. The reaction mixture was stirred at room temperature for...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
c1ccccc1
HO-
C(Cl)Cl
null
null
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)OC(C)(C)C>C(Cl)Cl>C=CCOC(=O)[C@H](N)CCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2788899244b0487da69285b0cbf52602
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(NC(=O)OCc1ccccc1)C(=O)O>>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C=C)OC([C@H](N)CCC1=CC=CC=C1)=O.C(C)N(CC)CC.C(=O)(OCC1=CC=CC=C1)NC(C)(C(=O)O)C>>C(C=C)OC([C@@H](CCC1=CC=CC=C1)NC(C(C)(C)NC(=O)OCC1=CC=CC=C1)=O)=O
[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[NH2:16].O[C:17](=[O:18])[C:19]([CH3:20])([CH3:21])[NH:22][C:23](=[O:24])[O:25][CH2:26][c:27]1[cH:28][cH:29][cH:30][cH:31][cH:32]1>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:11][cH:12...
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(NC(=O)OCc1ccccc1)C(=O)O
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CNC(=O)OCc1ccccc1)NCCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10](-[NH2;D1;+0:11])-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15]-[C:16]=[C;D1;H2:17]>>[C:9]-[C:10](-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8])-[C:12](=[O;D1;H0:13])-[#8...
69.7
[{"value": 69.7, "product": "C(C=C)OC([C@@H](CCC1=CC=CC=C1)NC(C(C)(C)NC(=O)OCC1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
The amine obtained in Step B of this Example (300 mg; 1.37 mmol) triethylamine (380 ml; 2.73 mmol) and N-carbobenzyloxy-2-methylalanine (278 mg; 1.37 mmol) were dissolved in dry methylene chloride (3 ml) and BOP (605 mg; 1.37 mmol) was added. The reaction mixture was stirred at room temperature for 2 h and the resultan...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
2
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(NC(=O)OCc1ccccc1)C(=O)O>C(Cl)Cl>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f14a773ff3c34c0780dd20f31d997bc1
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.CCN(CC)CC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CC(C)(C)NC(=O)OCc1ccccc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C=C)OC([C@H](N)CCC1=CC=CC=C1)=O.C(C)N(CC)CC.C(C)(C)(C)OC(=O)NC(CC(=O)O)(C)C>>C(C=C)OC([C@@H](CCC1=CC=CC=C1)NC(CC(C)(C)NC(=O)OCC1=CC=CC=C1)=O)=O
[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:15][cH:14][cH:13][cH:12][cH:29]1)[NH2:16].C[C:27]([CH3:11])([O:26][C:24]([NH:23][C:20]([CH2:19][C:17](O)=[O:18])([CH3:21])[CH3:22])=[O:25])[CH3:28].CCN(CC)[CH2:33][CH3:32].CN(C)[P+](On1nnc2ccc[cH:30][c:31]21)(N(C)C)N(C)C>>[CH2:1]=[CH:2][CH2:3][O:4...
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.CCN(CC)CC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CC(C)(C)NC(=O)OCc1ccccc1
null
null
C(Cl)Cl.C(C)(=O)OCC
Acylation
OtherReaction
e4ae9f4bd64d994c4bf6cf3491c65a63d610338daa37edabdc3519564d0e669e
7e47d41c0b43d83b0d84b675f0592f9db7d4836f9998b833a5561e73434c6363
O=C(CCNC(=O)OCc1ccccc1)NCCCc1ccccc1
C-C-N(-C-C)-[CH2;D2;+0:1]-[CH3;D1;+0:2].C-N(-C)-[P+](-O-n1:n:n:c2:c:c:c:[cH;D2;+0:3]:[c;H0;D3;+0:4]:2:1)(-N(-C)-C)-N(-C)-C.C-[C;H0;D4;+0:5](-[CH3;D1;+0:6])(-[CH3;D1;+0:7])-[#8:8]-[C:9](=[O;D1;H0:10])-[#7:11]-[C:12]-[C:13]-[C;H0;D3;+0:14](-O)=[O;D1;H0:15].[C;D1;H2:16]=[C:17]-[C:18]-[#8:19]-[C:20](=[O;D1;H0:21])-[C:22](-...
59.7
[{"value": 59.7, "product": "C(C=C)OC([C@@H](CCC1=CC=CC=C1)NC(CC(C)(C)NC(=O)OCC1=CC=CC=C1)=O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
D-Homophenylalanine allyl ester (350 mg; 1.60 mmol), triethylamine (445 μl; 3.19 mmol) and 3-t-butoxycarbonylamino-3-methylbutanoic acid (412.8 mg; 1.64 mmol) were dissolved in dry methylene chloride (3 ml) and stirred at room temperature to give a homogeneous solution. BOP was added to the solution over 5 minutes and ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Ether.Primary amine.Tertiary amine.Tertiary amine.Tertiary amine.Tertiary amine.Boc
Ether.Secondary amide
c1ccccc1.c1ccc2[nH]nnc2c1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl.C(C)(=O)OCC
null
null
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.CCN(CC)CC.CN(C)[P+](On1nnc2ccccc21)(N(C)C)N(C)C>C(Cl)Cl.C(C)(=O)OCC>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CC(C)(C)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-82c7b29aec314de1861faac34ed15227
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CCC(=O)O)NC(=O)OCc1ccccc1>>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CCC(C)(C)NC(=O)OCc1ccccc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C=C)OC([C@H](N)CCC1=CC=CC=C1)=O.C(C)N(CC)CC.C(C1=CC=CC=C1)OC(=O)NC(CCC(=O)O)(C)C>>C(C=C)OC([C@@H](CCC1=CC=CC=C1)NC(CCC(C)(C)NC(=O)OCC1=CC=CC=C1)=O)=O
[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:10]1[cH:11][cH:12][cH:13][cH:14][cH:15]1)[NH2:16].O[C:17](=[O:18])[CH2:19][CH2:20][C:21]([CH3:22])([CH3:23])[NH:24][C:25](=[O:26])[O:27][CH2:28][c:29]1[cH:30][cH:31][cH:32][cH:33][cH:34]1>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][CH2:9][c:1...
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CCC(=O)O)NC(=O)OCc1ccccc1
C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CCC(C)(C)NC(=O)OCc1ccccc1
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCCNC(=O)OCc1ccccc1)NCCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[C:6](-[NH2;D1;+0:7])-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]-[C:12]=[C;D1;H2:13]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:6](-[C:5])-[C:8](=[O;D1;H0:9])-[#8:10]-[C:11]-[C:12]=[C;D1;H2:13]
null
[]
null
null
null
null
D-Homophenylalanine allyl ester (175 mg; 0.80 mmol) (see Example 9, Step B), triethylamine (222 μl; 1.59 mmol) were dissolved in dry methylene chloride (2 ml) and 4-(benzyloxycarbonylamino)-4-methyl-pentanoic acid (211 mg; 0.80 mmol) added. The solution was stirred at room temperature and BOP (353 mg; 0.80 mmol) was ad...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
null
C=CCOC(=O)[C@H](N)CCc1ccccc1.CC(C)(CCC(=O)O)NC(=O)OCc1ccccc1>C(Cl)Cl>C=CCOC(=O)[C@@H](CCc1ccccc1)NC(=O)CCC(C)(C)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-76eb407e00c64615a297c82a5b981a5c
C=CCBr.CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O>>C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C
C(C)(C)(C)OC(=O)N[C@H](CC1=CNC2=CC=CC=C12)C(=O)O.C([O-])([O-])=O.[K+].[K+].C(C=C)Br>>C(C=C)OC([C@H](NC(=O)OC(C)(C)C)CC1=CNC2=CC=CC=C12)=O
Br[CH2:3][CH:2]=[CH2:1].[OH:4][C:5](=[O:6])[C@@H:7]([CH2:8][c:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12)[NH:18][C:19](=[O:20])[O:21][C:22]([CH3:23])([CH3:24])[CH3:25]>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][c:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12)[NH:18][C:19](...
C=CCBr.CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O
C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
06c4f868ad4646eea8208ecb83f54ca035dd62d04f0d8101641a4f487f2c695c
8446834f0edd1e71a2dcaffc09b80c7367abf3407263a8998354a2d20c1766bb
c1ccc2[nH]ccc2c1
Br-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]>>[C:4]-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3]
56
[{"value": 56.0, "product": "C(C=C)OC([C@H](NC(=O)OC(C)(C)C)CC1=CNC2=CC=CC=C12)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
N-(t-Butoxycarbonyl)-D-tryptophan (3 g; 9.868 mmol) was dissolved in acetone and an aqueous solution of potassium carbonate (2.84 g; 20.58 mmol) added followed by allyl bromide (1.55 g; 12.81 mmol). The reaction mixture was stirred for 18 h and then the acetone was substantially removed by evaporation under reduced pre...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Carboxylic acid
Ester
null
null
c1ccc2[nH]ccc2c1
HBr
CC(=O)C
null
18
C=CCBr.CC(C)(C)OC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)O>CC(=O)C>C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-275c3bd4a2eb43f196b2a4707e52cd1b
C=CCOC(=O)[C@H](N)Cc1c[nH]c2ccccc12.CC(C)(NC(=O)OCc1ccccc1)C(=O)O>>C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
F[P-](F)(F)(F)(F)F.N1(N=NC2=C1C=CC=C2)O[P+](N(C)C)(N(C)C)N(C)C.C(C=C)OC([C@H](N)CC1=CNC2=CC=CC=C12)=O.C(C)N(CC)CC.C(C1=CC=CC=C1)OC(=O)NC(C)(C(=O)O)C>>C(C1=CC=CC=C1)OC(=O)NC(C(=O)N[C@@H](C(=O)OCC=C)CC1=CNC2=CC=CC=C12)(C)C
[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][c:9]1[cH:10][nH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]12)[NH2:18].O[C:19](=[O:20])[C:21]([CH3:22])([CH3:23])[NH:24][C:25](=[O:26])[O:27][CH2:28][c:29]1[cH:30][cH:31][cH:32][cH:33][cH:34]1>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][c:9]1[cH:10][...
C=CCOC(=O)[C@H](N)Cc1c[nH]c2ccccc12.CC(C)(NC(=O)OCc1ccccc1)C(=O)O
C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
null
null
C(Cl)Cl.C(C)(=O)OCC
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CNC(=O)OCc1ccccc1)NCCc1c[nH]c2ccccc12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8].[C:9]-[C:10](-[NH2;D1;+0:11])-[C:12](=[O;D1;H0:13])-[#8:14]-[C:15]-[C:16]=[C;D1;H2:17]>>[C:9]-[C:10](-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#7:6]-[C:7]=[O;D1;H0:8])-[C:12](=[O;D1;H0:13])-[#8...
84.5
[{"value": 84.5, "product": "C(C1=CC=CC=C1)OC(=O)NC(C(=O)N[C@@H](C(=O)OCC=C)CC1=CNC2=CC=CC=C12)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.5, "product": "C(C1=CC=CC=C1)OC(=O)NC(C(=O)N[C@@H](C(=O)OCC=C)CC1=CNC2=CC=CC=C12)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
D-Tryptophan allyl ester (250 mg; 0.822 mmol), triethylamine (230 μl; 1.650 mmol) and N-benzyloxycarbonyl-α-methylalanine (167.9 mg; 0.826 mmol) were dissolved in dry methylene chloride (5 ml) and BOP (363.7 mg; 0.822 mmol) added. The reaction mixture was stirred at room temperature for 16 h and then the reaction quenc...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
C(Cl)Cl.C(C)(=O)OCC
null
16
C=CCOC(=O)[C@H](N)Cc1c[nH]c2ccccc12.CC(C)(NC(=O)OCc1ccccc1)C(=O)O>C(Cl)Cl.C(C)(=O)OCC>C=CCOC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C(C)(C)NC(=O)OCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e392efa1dd0c43839d8e3026d6f4b2ee
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>>CC(C)(CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
C(C1=CC=CC=C1)OC([C@H](N)CC1=CNC2=CC=CC=C12)=O.C(C)(C)(C)OC(=O)NC(CC(=O)O)(C)C>>C(C1=CC=CC=C1)OC([C@@H](CC1=CNC2=CC=CC=C12)NC(CC(C)(C)NC(=O)OC(C)(C)C)=O)=O
O[C:5]([CH2:4][C:2]([CH3:1])([CH3:3])[NH:29][C:30](=[O:31])[O:32][C:33]([CH3:34])([CH3:35])[CH3:36])=[O:6].[NH2:7][C@H:8]([CH2:9][c:10]1[cH:11][nH:12][c:13]2[cH:14][cH:15][cH:16][cH:17][c:18]12)[C:19](=[O:20])[O:21][CH2:22][c:23]1[cH:24][cH:25][cH:26][cH:27][cH:28]1>>[CH3:1][C:2]([CH3:3])([CH2:4][C:5](=[O:6])[NH:7][C@H...
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1
CC(C)(CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
null
null
null
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCc1c[nH]c2ccccc12)OCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9](-[C:10])-[NH2;D1;+0:11]>>[C:5]-[#8:6]-[C:7](=[O;D1;H0:8])-[C:9](-[C:10])-[NH;D2;+0:11]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4]
null
[]
null
null
null
null
Prepared from D-tryptophan benzyl ester (1 g; 3.40 mmol) and 3-t-butoxycarbonylamino-3-methylbutanoic acid (0.91 g; 4.19 mmol) by the procedure described in Example 6, Step C. The yield was 0.981 g (58%). Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccc2[nH]ccc2c1.c1ccccc1
HO-
null
null
null
CC(C)(CC(=O)O)NC(=O)OC(C)(C)C.N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1>>CC(C)(CC(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)OCc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-31a415ff907141efa27a3abe2528614f
CC(C)(C)OC(=O)NCc1ccccc1-c1ccc(CO)cc1.CCN>>CCNCc1ccc(-c2ccccc2CNC(=O)OC(C)(C)C)cc1
CS(=O)(=O)Cl.C(C)N(CC)CC.C(C)N.OCC1=CC=C(C=C1)C1=C(C=CC=C1)CNC(=O)OC(C)(C)C>>C(C)NCC1=CC=C(C=C1)C1=C(C=CC=C1)CNC(=O)OC(C)(C)C
O[CH2:4][c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[CH2:15][NH:16][C:17](=[O:18])[O:19][C:20]([CH3:21])([CH3:22])[CH3:23])[cH:24][cH:25]1.[CH3:1][CH2:2][NH2:3]>>[CH3:1][CH2:2][NH:3][CH2:4][c:5]1[cH:6][cH:7][c:8](-[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[CH2:15][NH:16][C:17](=[O:18])[O:19][C:20](...
CC(C)(C)OC(=O)NCc1ccccc1-c1ccc(CO)cc1.CCN
CCNCc1ccc(-c2ccccc2CNC(=O)OC(C)(C)C)cc1
null
null
CO.C(Cl)Cl.C(C)(=O)OCC
Heteroatom Alkylation and Arylation
Reductive amination with alcohol
80c5fffb5a6cd9bcf0b3d20ee51fe5f6574f02d4cb5ea6a4d33b4a9098b0e672
405fc0d288d595940df82750271ed5f4125713ca8b676b8ed83063765fec7c50
c1ccc(-c2ccccc2)cc1
O-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[C:6]-[NH2;D1;+0:7]>>[C;D1;H3:5]-[C:6]-[NH;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
68.2
[{"value": 68.0, "product": "C(C)NCC1=CC=C(C=C1)C1=C(C=CC=C1)CNC(=O)OC(C)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 68.2, "product": "C(C)NCC1=CC=C(C=C1)C1=C(C=CC=C1)CNC(=O)OC(C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
null
null
4-Hydroxymethyl-2'(t-butoxycarbonylaminomethyl)-1,1'-biphenyl (70 mg; 0.224 mmol) was dissolved in dry methylene chloride and stirred at 0° C. in an iced water bath and methanesulfonyl chloride (22 μl; 0.285 mmol) and triethylamine (39 μl; 0.280 mmol) added. The reaction mixture was stirred for 3 h at 0° C. and then 70...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary amine
Secondary amine
null
null
c1ccccc1.c1ccccc1
HO-
CO.C(Cl)Cl.C(C)(=O)OCC
0
null
CC(C)(C)OC(=O)NCc1ccccc1-c1ccc(CO)cc1.CCN>CO.C(Cl)Cl.C(C)(=O)OCC>CCNCc1ccc(-c2ccccc2CNC(=O)OC(C)(C)C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-36f08b8e5c0c4222ab2cf761a8e66449
C=CCO.CC(C)(C)OC(=O)N[C@H](COCc1ccccc1)C(=O)O>>C=CCOC(=O)[C@@H](COCc1ccccc1)NC(=O)OC(C)(C)C
C(C)(=O)OCC.C(C=C)O.C(C)(C)(C)OC(=O)N[C@H](COCC1=CC=CC=C1)C(=O)O.C(CCl)Cl>>C(C=C)OC([C@H](NC(=O)OC(C)(C)C)COCC1=CC=CC=C1)=O
O[CH2:3][CH:2]=[CH2:1].[OH:4][C:5](=[O:6])[C@@H:7]([CH2:8][O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[NH:17][C:18](=[O:19])[O:20][C:21]([CH3:22])([CH3:23])[CH3:24]>>[CH2:1]=[CH:2][CH2:3][O:4][C:5](=[O:6])[C@@H:7]([CH2:8][O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[NH:17][C:18](=[O:19])[O:20][...
C=CCO.CC(C)(C)OC(=O)N[C@H](COCc1ccccc1)C(=O)O
C=CCOC(=O)[C@@H](COCc1ccccc1)NC(=O)OC(C)(C)C
null
CN(C)C=1C=CN=CC1
C(Cl)Cl
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
3f9a9ace480b666da05fcfe5450d12b5c1ea5b0d435c195e1dd4bd20281604bb
dcbf04ec563ed0e9dfc79070490a028958024079a671c385858bb18cc8ec995a
c1ccccc1
O-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]>>[C:4]-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3]
null
[]
null
null
2.5
HOUR
N-(t-Butoxycarbonyl)-O-benzyl-D-serine (600 mg; 2.03 mmol) was dissolved in dry methylene chloride (5 ml), allyl alcohol (152 μl; 2.23 mmol) and DMAP (25 mg; 0.20 mmol) added and finally EDC (428.5 mg; 2.24 mmol) added to the acid. The reaction mixture was stirred at room temperature for 2.5 h and the resulting homogen...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
c1ccccc1
HO-
CN(C)C=1C=CN=CC1.C(Cl)Cl
null
2.5
C=CCO.CC(C)(C)OC(=O)N[C@H](COCc1ccccc1)C(=O)O>CN(C)C=1C=CN=CC1.C(Cl)Cl>C=CCOC(=O)[C@@H](COCc1ccccc1)NC(=O)OC(C)(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4973b5510ea745408780d7b531a293b6
CN(C(=O)[C@@H](CCc1ccccc1)NC(=O)OCC1c2ccccc2-c2ccccc21)c1ccc(-c2ccccc2[N+](=O)[O-])cc1>>CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2[N+](=O)[O-])cc1
C1=CC=CC=2C3=CC=CC=C3C(C12)COC(=O)N[C@@H](C(=O)N(C1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-])C)CCC1=CC=CC=C1.NCC1CCNCC1>>N[C@@H](C(=O)N(C1=CC=C(C=C1)C1=C(C=CC=C1)[N+](=O)[O-])C)CCC1=CC=CC=C1
O=C(OCC1c2ccccc2-c2ccccc21)[NH:6][C@@H:5]([C:3]([N:2]([CH3:1])[c:15]1[cH:16][cH:17][c:18](-[c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]2[N+:25](=[O:26])[O-:27])[cH:28][cH:29]1)=[O:4])[CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][N:2]([C:3](=[O:4])[C@H:5]([NH2:6])[CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12...
CN(C(=O)[C@@H](CCc1ccccc1)NC(=O)OCC1c2ccccc2-c2ccccc21)c1ccc(-c2ccccc2[N+](=O)[O-])cc1
CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2[N+](=O)[O-])cc1
null
null
C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
6b8c76d50ec667b483b13f7e325104eed6ba06fddb821da46e405c5dce0a3de5
4e549866ec1acadec4c84aaf8495992a28ec78d8ea5ef1b9f44dd843b0dcb7d4
O=C(CCCc1ccccc1)Nc1ccc(-c2ccccc2)cc1
O=C(-O-C-C1-c2:c:c:c:c:c:2-c2:c:c:c:c:c:2-1)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[#7:6](-[C;D1;H3:7])-[c:8]>>[C:3]-[C:2](-[NH2;D1;+0:1])-[C:4](=[O;D1;H0:5])-[#7:6](-[C;D1;H3:7])-[c:8]
null
[]
null
null
null
null
The FMOC amide from Step F (1.15 g; 1.88 mmol) was dissolved in methylene chloride (10 ml) and 4-(aminomethyl)piperidine (1 ml) added. The reaction mixture was stirred at room temperature. The reaction mixture was stirred for 15 minutes and then quenched by adding water. The methylene chloride phase was separated, drie...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether
Primary amine
c1ccc2c(c1)Cc1ccccc12
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
C(Cl)Cl
null
null
CN(C(=O)[C@@H](CCc1ccccc1)NC(=O)OCC1c2ccccc2-c2ccccc21)c1ccc(-c2ccccc2[N+](=O)[O-])cc1>C(Cl)Cl>CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2[N+](=O)[O-])cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f701c8034cd64527bb66e1cb9184c5a6
CNc1ccc(-c2ccccc2C#N)cc1.O=C(N[C@H](CCc1ccccc1)C(=O)O)OCC1c2ccccc2-c2ccccc21>>CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2C#N)cc1
C1=CC=CC=2C3=CC=CC=C3C(C12)COC(=O)N[C@@H](C(=O)O)CCC1=CC=CC=C1.CNC1=CC=C(C=C1)C1=C(C=CC=C1)C#N.C(C(=O)Cl)(=O)Cl.C(C)N(CC)CC>>N[C@@H](C(=O)N(C1=CC=C(C=C1)C1=C(C=CC=C1)C#N)C)CCC1=CC=CC=C1
[CH3:1][NH:2][c:15]1[cH:16][cH:17][c:18](-[c:19]2[cH:20][cH:21][cH:22][cH:23][c:24]2[C:25]#[N:26])[cH:27][cH:28]1.O=C(OCC1c2ccccc2-c2ccccc21)[NH:6][C@@H:5]([C:3](O)=[O:4])[CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][N:2]([C:3](=[O:4])[C@H:5]([NH2:6])[CH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][...
CNc1ccc(-c2ccccc2C#N)cc1.O=C(N[C@H](CCc1ccccc1)C(=O)O)OCC1c2ccccc2-c2ccccc21
CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2C#N)cc1
null
CN(C)C=O
C(Cl)Cl
Acylation
OtherReaction
1f3e78c052292d501d7437edb4bf22606988b28adaa781f40f6d3c5a3d2dcd8c
77a668978e69174334be4f36a3c7053272639f750105af3c4ac3ba22ece7f87c
O=C(CCCc1ccccc1)Nc1ccc(-c2ccccc2)cc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C:4])-[NH;D2;+0:5]-C(=O)-O-C-C1-c2:c:c:c:c:c:2-c2:c:c:c:c:c:2-1.[C;D1;H3:6]-[NH;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[C:4]-[C:3](-[NH2;D1;+0:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:7](-[C;D1;H3:6])-[c:8](:[c:9]):[c:10]
null
[]
null
null
2
HOUR
(R)-α-[N-(9-Fluorenylmethoxycarbonyl)amino]-benzenebutanoic acid (500 mg; 1.25 mmol), was converted into its corresponding acid chloride according to the procedure descibed in Example 33, Step F using 1 drop of DMF, oxalyl chloride (136 μl) in methylene chloride (2.5 ml). A yellow solid which was the acid chloride (525...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Carboxylic acid.Ether.Secondary amine
Tertiary amide.Primary amine
c1ccc2c(c1)Cc1ccccc12
null
c1ccccc1.c1ccccc1.c1ccccc1
HO-
CN(C)C=O.C(Cl)Cl
null
2
CNc1ccc(-c2ccccc2C#N)cc1.O=C(N[C@H](CCc1ccccc1)C(=O)O)OCC1c2ccccc2-c2ccccc21>CN(C)C=O.C(Cl)Cl>CN(C(=O)[C@H](N)CCc1ccccc1)c1ccc(-c2ccccc2C#N)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-51173d9d709c45cdbf8cf8891134c0bf
OCC(O)C(O)C(O)CO.OC[C@@H](O)[C@H](O)[C@@H](O)CO>>O=C(CO)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
C([C@H](O)[C@@H](O)[C@H](O)CO)O.C(C(C(C(CO)O)O)O)O.C([C@H](C([C@@H](CO)O)O)O)O>>O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.C([C@H](C([C@@H](CO)O)O)O)O.OCC(=O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO
[OH:1][CH:2]([CH2:3][OH:4])[CH:5]([OH:6])[CH:7]([OH:8])[CH2:9][OH:10].[OH:11][CH2:12][C@@H:13]([OH:14])[C@H:27]([OH:28])[C@@H:29]([OH:30])[CH2:31][OH:32]>>[O:1]=[C:2]([CH2:3][OH:4])[C@@H:5]([OH:6])[C@H:7]([OH:8])[CH2:9][OH:10].[O:11]=[CH:12][C@H:13]([OH:14])[C@@H:15]([OH:16])[C@H:17]([OH:18])[CH2:19][OH:20].[O:21]=[CH:...
OCC(O)C(O)C(O)CO.OC[C@@H](O)[C@H](O)[C@@H](O)CO
O=C(CO)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
null
null
null
Functional Group Addition
OtherReaction
cbb5e53a24f408b885543123031dd6b6da1e3b619b55409aacf6ea79017bf12e
a05ca77da51178ec59bb2b865241409ac5fa304d04a7a6acaf4ba97f90da5172
null
[C:1]-[C:2](-[O;D1;H1:3])-[C@H;D3;+0:4](-[O;D1;H1:5])-[C@@H;D3;+0:6](-[O;D1;H1:7])-[CH2;D2;+0:8]-[OH;D1;+0:9].[O;D1;H1:10]-[C:11]-[CH;D3;+0:12](-[O;D1;H1:13])-[CH;D3;+0:14](-[O;D1;H1:15])-[CH;D3;+0:16](-[OH;D1;+0:17])-[C:18]-[O;D1;H1:19]>>[C:20]-[C:21](-[O;D1;H1:22])-[C@@H;D3;+0:6](-[O;D1;H1:7])-[CH;D2;+0:8]=[O;H0;D1;+...
null
[]
null
null
null
null
It is known from European Patent No. 421,882, of which the Applicant is proprietor, to obtain xylitol syrups having a xylitol content of 80% to 90%, the remainder being essentially composed of D-arabitol, pentitol of the natural D series of sugars. These syrups, which are not very viscous and which are particularly wel...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
Aldehyde.Aldehyde.Ketone.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
null
null
null
Other
null
null
null
OCC(O)C(O)C(O)CO.OC[C@@H](O)[C@H](O)[C@@H](O)CO>>O=C(CO)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)CO.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9ba26a120c504949aabeae933256e0ed
O=P([O-])([O-])[O-].[NH4+].[NH4+]>>O=P([O-])([O-])O.O=P([O-])([O-])O.[NH4+].[NH4+].[NH4+]
P(=O)([O-])([O-])[O-].[NH4+].[NH4+].[NH4+].[Cl-].[Na+]>>P(=O)([O-])([O-])O.[NH4+].[Na+].[Cl-].[NH4+].P(=O)([O-])([O-])O.[NH4+].[NH4+]
[O-:1][P:2]([O-:3])(=[O:6])[O-:10].[NH4+:12].[NH4+:13]>>[O:1]=[P:2]([O-:3])([O-:4])[OH:5].[O:6]=[P:7]([O-:8])([O-:9])[OH:10].[NH4+:12].[NH4+:13].[NH4+:14]
O=P([O-])([O-])[O-].[NH4+].[NH4+]
O=P([O-])([O-])O.O=P([O-])([O-])O.[NH4+].[NH4+].[NH4+]
null
null
O
Functional Group Interconversion
OtherReaction
42af6cdfb86a130c92365e01a31b50705eea7bdf12f67dc370bf24402f7ceedc
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
null
[O-;H0;D1:1]-[P;H0;D4;+0:2](-[O-;H0;D1:3])(-[O;-;D1;H0:4])=[O;H0;D1;+0:5]>>[O;-;D1;H0:6]-[#15:7](-[O;-;D1;H0:8])(=[O;H0;D1;+0:5])-[OH;D1;+0:1].[O;-;D1;H0:4]-[P;H0;D4;+0:2](-[O;-;D1;H0:9])(-[O;D1;H1:10])=[O;H0;D1;+0:3]
null
[]
null
null
null
null
Sodium ammonium phosphate and ammonium chloride are prepared from an ammonium phosphate (e.g., diammonium phosphate) and sodium chloride in water. The crystallization of sodium ammonium phosphate may take place between -10° C. to 40° C. Using the present invention, technical grade sodium ammonium phosphate and ammonium...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O
null
null
O=P([O-])([O-])[O-].[NH4+].[NH4+]>O>O=P([O-])([O-])O.O=P([O-])([O-])O.[NH4+].[NH4+].[NH4+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-985d1723ff4d4b1298aaa363af9134e8
[Cl-].[Na+]>>[Cl-].[NH4+].[Na+]
[Cl-].[NH4+].S(=O)(=O)([O-])[O-].[Na+].[Na+]>>S(=O)(=O)([O-])[O-].[NH4+].[NH4+].[Na+].[Cl-]
[Cl-:6].[Na+:9]>>[Cl-:6].[NH4+:8].[Na+:9]
[Cl-].[Na+]
[Cl-].[NH4+].[Na+]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
null
null
It is also known that ammonium chloride and sodium sulphate can be produced from ammonium sulphate and salt (NaCl). According to this reaction, one would expect to produce disodium phosphate and ammonium chloride from sodium chloride and diammonium phosphate if the Na/P molar ratio is 2. Conditions: See reaction.notes....
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
null
null
null
[Cl-].[Na+]>>[Cl-].[NH4+].[Na+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c0cd0c63904c42eabebf3989bb71e6b3
O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1>>O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1
C1=CC=C(C=C1)C2=COC3(C2=O)C4=CC=CC=C4C(=O)O3.C1CC(CCC1CN2C(=O)C=CC2=O)C(=O)ON3C(=O)CC(C3=O)S(=O)(=O)[O-].[Na+].Cl.Cl.C(CN)N>>C(CN)N.C1CC(CCC1CN2C(=O)C=CC2=O)C(=O)ON3C(=O)CC(C3=O)S(=O)(=O)[O-].[Na+]
[O:5]=[C:6]([O:7][N:8]1[C:9](=[O:10])[CH2:11][CH:12]([S:13](=[O:14])(=[O:15])[O-:16])[C:17]1=[O:18])[CH:19]1[CH2:20][CH2:21][CH:22]([CH2:23][N:24]2[C:25](=[O:26])[CH:27]=[CH:28][C:29]2=[O:30])[CH2:31][CH2:32]1>>[O:5]=[C:6]([O:7][N:8]1[C:9](=[O:10])[CH2:11][CH:12]([S:13](=[O:14])(=[O:15])[O-:16])[C:17]1=[O:18])[CH:19]1[...
O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1
O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1
null
null
C(C)(=O)[O-].[Na+]
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
O=C(ON1C(=O)CCC1=O)C1CCC(CN2C(=O)C=CC2=O)CC1
null
null
[]
null
null
null
null
Sulfo-SMCC (1 eq.)(Pierce Chemical Co., Rockford, Ill.) is dissolved in sodium acetate buffer (pH 7) and ethylenediamine dihydrochloride (5 eq.) is added. The reaction is monitored by TLC visualized with fluorescamine. When reaction is complete the reaction mixture is applied directly to a C18 reverse-phase HPLC column...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
C1CC[NH]C1.C1CCCCC1.C1=CC[NH]C1
null
C(C)(=O)[O-].[Na+]
null
null
O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1>C(C)(=O)[O-].[Na+]>O=C(ON1C(=O)CC(S(=O)(=O)[O-])C1=O)C1CCC(CN2C(=O)C=CC2=O)CC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-32657578f2084976872d2cf3b47b25b7
CC(=O)SCC[N+](C)(C)C.N[C@@H](CS)C(=O)O>>CC(=O)N[C@@H](CS)C(=O)O.C[N+](C)(C)CCS
N[C@@H](CS)C(=O)O.C(C)(=O)SCC[N+](C)(C)C>>SCC[N+](C)(C)C.C(C)(=O)N[C@@H](CS)C(=O)O
[CH3:1][C:2](=[O:3])[S:17][CH2:16][CH2:15][N+:12]([CH3:11])([CH3:13])[CH3:14].[NH2:4][C@@H:5]([CH2:6][SH:7])[C:8](=[O:9])[OH:10]>>[CH3:1][C:2](=[O:3])[NH:4][C@@H:5]([CH2:6][SH:7])[C:8](=[O:9])[OH:10].[CH3:11][N+:12]([CH3:13])([CH3:14])[CH2:15][CH2:16][SH:17]
CC(=O)SCC[N+](C)(C)C.N[C@@H](CS)C(=O)O
CC(=O)N[C@@H](CS)C(=O)O.C[N+](C)(C)CCS
null
null
null
Acylation
OtherReaction
eadd48a08a1f1a35cc40325d486fb291670e6a7642c6207686313b68b53a9670
6543d3ccfa2e7364577832d8ac025f88ec72a87da9e0dea588fa48510f2b1d42
null
[C:1]-[C:2](-[NH2;D1;+0:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[C:7]-[C:8]-[S;H0;D2;+0:9]-[C;H0;D3;+0:10](-[C;D1;H3:11])=[O;D1;H0:12]>>[C:1]-[C:2](-[NH;D2;+0:3]-[C;H0;D3;+0:10](-[C;D1;H3:11])=[O;D1;H0:12])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6].[C:7]-[C:8]-[SH;D1;+0:9]
null
[]
null
null
null
null
reacting the cysteine with the acetylthiocholine to form thiocholine and N-acetylcysteine, each in a concentration of about 0.2 molar to about 3.0 molar and in a molar ratio of thiocholine to N-acetylcysteine of 1:1.2 to 1.2:1. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary amine.Carbo-thioester
Secondary amide.Aliphatic thiol
null
null
null
null
null
null
null
CC(=O)SCC[N+](C)(C)C.N[C@@H](CS)C(=O)O>>CC(=O)N[C@@H](CS)C(=O)O.C[N+](C)(C)CCS
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-987cbce73ecd44fa89c19bbd9f39470c
O=S([O-])[O-].[Na+]>>O=S(=O)([O-])CCS(=O)(=O)[O-].[Na+]
BrCCBr.S(=O)([O-])[O-].[Na+].[Na+]>>C(CS(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]
[O-:1][S:2]([O-:4])=[O:9].[Na+:12]>>[O:1]=[S:2](=[O:3])([O-:4])[CH2:5][CH2:6][S:7](=[O:8])(=[O:9])[O-:10].[Na+:12]
O=S([O-])[O-].[Na+]
O=S(=O)([O-])CCS(=O)(=O)[O-].[Na+]
null
null
O
Oxidation
OtherReaction
b34b58941ad31acdf479ae5ca981fe52f3be011f815cd9cc7ba4ddcb65f38c10
1eb7bb476006d502a02416eb81e7f131b3c53487adcd281911e6272706cdec95
null
[O-;H0;D1:1]-[S;H0;D3;+0:2](-[O;-;D1;H0:3])=[O;H0;D1;+0:4]>>[O;-;D1;H0:5]-[#16:6](=[O;D1;H0:7])(=[O;H0;D1;+0:4])-[C:8]-[C:9]-[S;H0;D4;+0:2](-[O;-;D1;H0:3])(=[O;D1;H0:10])=[O;H0;D1;+0:1]
65.1
[{"value": 65.1, "product": "C(CS(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 1,2-dibromoethane (37.6 g, 0.20 mol) and sodium sulfite (63.0 g, 0.5 mol) in water (225 mL) was heated at reflux temperature for 20 h. After the mixture was cooled in the refrigerator, crystals were collected. The crude product was repeatedly recrystallized from water-ethanol. The trace amount of inorganic...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonic acid.Sulfonic acid
null
null
null
null
O
null
null
O=S([O-])[O-].[Na+]>O>O=S(=O)([O-])CCS(=O)(=O)[O-].[Na+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b57c36d4bcc2495f859a14c585711e9b
BrCCCBr.O=S([O-])[O-].[Na+]>>O=S(=O)([O-])CCCS(=O)(=O)[O-].[Na+]
BrCCCBr.S(=O)([O-])[O-].[Na+].[Na+].C>>C(CCS(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]
Br[CH2:5][CH2:7][CH2:6]Br.[O-:1][S:2]([O-:4])=[O:10].[Na+:13]>>[O:1]=[S:2](=[O:3])([O-:4])[CH2:5][CH2:6][CH2:7][S:8](=[O:9])(=[O:10])[O-:11].[Na+:13]
BrCCCBr.O=S([O-])[O-].[Na+]
O=S(=O)([O-])CCCS(=O)(=O)[O-].[Na+]
null
null
O
Oxidation
OtherReaction
dfafa97ac1db18ed9885a8c9ddbde026679d862dea7cad49633322bc494b39ac
7c941e1ecba24481eaa2d98576388722e2302c88fba0b24ad34fbecf569e3576
null
Br-[CH2;D2;+0:1]-[CH2;D2;+0:2]-[CH2;D2;+0:3]-Br.[O-;H0;D1:4]-[S;H0;D3;+0:5](-[O;-;D1;H0:6])=[O;H0;D1;+0:7]>>[O;-;D1;H0:8]-[#16:9](=[O;D1;H0:10])(=[O;H0;D1;+0:7])-[CH2;D2;+0:2]-[CH2;D2;+0:3]-[CH2;D2;+0:1]-[S;H0;D4;+0:5](-[O;-;D1;H0:6])(=[O;D1;H0:11])=[O;H0;D1;+0:4]
85.6
[{"value": 85.6, "product": "C(CCS(=O)(=O)[O-])S(=O)(=O)[O-].[Na+].[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
This compound was prepared by a modification of the method described in Stone, G. C. H. (1936) J. Am. Chem. Soc., 58:488. 1,3-Dibromopropane (40.4 g, 0.20 mol) was treated with sodium sulfite (60.3 g, 0.50 mol) in water at reflux temperature for 48 h. Inorganic salts (sodium bromide and sodium sulfite) were removed by ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
Sulfonic acid.Sulfonic acid
null
null
null
Br-
O
null
null
BrCCCBr.O=S([O-])[O-].[Na+]>O>O=S(=O)([O-])CCCS(=O)(=O)[O-].[Na+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6ab0050d28734f3bbd40feed3cadae32
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O>>O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)CO)O)O)CO)O)O)O)O>>C([C@@H]1[C@H]([C@@H]([C@H](C(O1)O)O)O)O)O.O
OC[C@H]1O[C@@](C[OH:1])([O:7][C@H:6]2[O:5][C@H:4]([CH2:3][OH:2])[C@@H:12]([OH:13])[C@H:10]([OH:11])[C@H:8]2[OH:9])[C@@H](O)[C@@H]1O>>[OH2:1].[OH:2][CH2:3][C@H:4]1[O:5][CH:6]([OH:7])[C@H:8]([OH:9])[C@@H:10]([OH:11])[C@@H:12]1[OH:13]
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O
O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
null
null
O
Reduction
OtherReaction
4bdb706d436485c857e245c05b537da9c9d30893ed64af96235ac43136bb801d
3214caef4749dbf6b36c0350acd3bc28c8a03e3af74b1ea21fbc7730a8d65008
C1CCOCC1
null
null
[]
null
null
null
null
29 parts of liquid saccharose and 49 parts of water were mixed at 60° C. 0.2 parts of stabiliser formed by carrageenans and xanthan gum and 3.5 parts of glucose syrup were then added. 15.5 parts of apple puree, colouring agent and finally 2.1 parts of citric acid were then added thereto. After pasteurisation of the mix...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol
Secondary alcohol
C1CCOC1
null
C1CCOCC1
HO-
O
null
null
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O>O>O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-426a2c8a98564f41bccd59759d726727
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O>>O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
C([C@@H]1[C@H]([C@@H]([C@H]([C@H](O1)O[C@]2([C@H]([C@@H]([C@H](O2)CO)O)O)CO)O)O)O)O>>C([C@@H]1[C@H]([C@@H]([C@H](C(O1)O)O)O)O)O.O
OC[C@H]1O[C@@](C[OH:1])([O:7][C@H:6]2[O:5][C@H:4]([CH2:3][OH:2])[C@@H:12]([OH:13])[C@H:10]([OH:11])[C@H:8]2[OH:9])[C@@H](O)[C@@H]1O>>[OH2:1].[OH:2][CH2:3][C@H:4]1[O:5][CH:6]([OH:7])[C@H:8]([OH:9])[C@@H:10]([OH:11])[C@@H:12]1[OH:13]
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O
O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
null
null
O
Reduction
OtherReaction
4bdb706d436485c857e245c05b537da9c9d30893ed64af96235ac43136bb801d
3214caef4749dbf6b36c0350acd3bc28c8a03e3af74b1ea21fbc7730a8d65008
C1CCOCC1
null
null
[]
null
null
null
null
For this purpose, a composition was prepared by mixing 18.5 parts of liquid saccharose and 68 parts of water at 60° C. 0.2 parts of stabiliser formed by carrageenans and xanthan gum and 3.5 parts of glucose syrup were then added. 10 parts of apple puree and colouring agent were added and the mixture was pasteurised at ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Primary alcohol.Primary alcohol.Secondary alcohol.Secondary alcohol
Secondary alcohol
C1CCOC1
null
C1CCOCC1
HO-
O
null
null
OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O>O>O.OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a341d33ac8ca4d4dbeafbd8b5790110d
CC(C)=O.Cc1ccccc1.N#C[S-]>>C=Cc1ccc(CSC#N)cc1.C=Cc1ccccc1
[S-]C#N.[K+].CC(=O)C.C1(=CC=CC=C1)C>>C=CC1=CC=CC=C1.S(C#N)CC1=CC=C(C=C)C=C1
O=[C:12]([CH3:1])[CH3:14].[c:6]1([CH3:7])[cH:16][cH:17][cH:18][cH:19][cH:20]1.[S-:8][C:9]#[N:10]>>[CH2:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][S:8][C:9]#[N:10])[cH:11][cH:12]1.[CH2:13]=[CH:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1
CC(C)=O.Cc1ccccc1.N#C[S-]
C=Cc1ccc(CSC#N)cc1.C=Cc1ccccc1
null
null
CN(C)C=O
Aromatic Heterocycle Formation
OtherReaction
95f6b80107a2e3e1ea403a4587cde35cb6c99d517b7d5ad83528721b2e3acaa8
57a7b0b4cda119dfd964beeceb47d950936660c56ce34b88855dbb58b35e9241
c1ccccc1.c1ccccc1
O=[C;H0;D3;+0:1](-[CH3;D1;+0:2])-[CH3;D1;+0:3].[CH3;D1;+0:4]-[c;H0;D3;+0:5]1:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1.[N;D1;H0:11]#[C:12]-[S-;H0;D1:13]>>[C;D1;H2:14]=[CH;D2;+0:2]-[c:15]1:[cH;D2;+0:6]:[c:7]:[c:8]:[c:9]:[cH;D2;+0:10]:1.[CH2;D1;+0:3]=[C:16]-[c:17]1:[c:18]:[c:19]:[c;H0;D3;+0:5](-[CH2;D2;+0:4]-[S;H0;D...
null
[]
null
null
null
null
The desired terpolymer of styrene, 4-thiocyanatomethylstyrene, and vinyl benzyl polyethylene glycol was synthesized from the terpolymer of Step II as follows: 1.5 g of the terpolymer formed in Step II was mixed with 350 mL of toluene taken in a 500 mL flask and the contents stirred. To this mixture was added 1.2 g of p...
10.6084/m9.figshare.5104873.v1
null
Ketone
Monosulfide.Thiocyanate.Vinyl.Vinyl
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
null
CN(C)C=O
null
null
CC(C)=O.Cc1ccccc1.N#C[S-]>CN(C)C=O>C=Cc1ccc(CSC#N)cc1.C=Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-da3a70b3badd4e8da28a4299f8a4a21a
C#CCCOC1CCCCO1>>C#CCCCOC1CCCCO1
O.NN.[Li+].[AlH4-].C(CC#C)OC1OCCCC1.BrBr.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.OO.O1CCCC=C1.C(CCC)[Li].C1(=CC=C(C=C1)S(=O)(=O)Cl)C>>O1C(CCCC1)OCCCC#C
[CH:2]#[C:3][CH2:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1>>[CH:1]#[C:2][CH2:3][CH2:4][CH2:5][O:6][CH:7]1[CH2:8][CH2:9][CH2:10][CH2:11][O:12]1
C#CCCOC1CCCCO1
C#CCCCOC1CCCCO1
null
[N+](=O)([O-])[O-].[Ag+].[N+](=O)([O-])[O-].[Ag+]
null
Functional Group Interconversion
OtherReaction
717941f395a910361dbd079f0406c8739db3d600df9659ab84f995c3dd1e77a5
f5163dfbf670ee9f38d1be788eef0e0a983df5868f48fe01d48741d6a3f98157
C1CCOCC1
[C:1]-[C:2]-[C;H0;D2;+0:3]#[CH;D1;+0:4]>>[C:1]-[C:2]-[CH2;D2;+0:3]-[C;H0;D2;+0:4]#[C;D1;H1:5]
null
[]
null
null
null
null
Hydrazine hydrate and hydrogen peroxide (30 wt. % solution in water) were purchased from Mallinckrodt (Chesterfield, Mo.) and Fisher Chemical Co. (Fair Lawn, N.J.), respectively. Butyllithium (1.6M and 2.5M solutions in hexane), 2-(3-butynyloxy)tetrahydro-2H-pyran (1-(tetrahydopyran-2-yloxy)-3-butyne), lithium tetrahyd...
10.6084/m9.figshare.5104873.v1
null
Alkyne
Alkyne
null
null
C1CCOCC1
Other
[N+](=O)([O-])[O-].[Ag+].[N+](=O)([O-])[O-].[Ag+]
null
null
C#CCCOC1CCCCO1>[N+](=O)([O-])[O-].[Ag+].[N+](=O)([O-])[O-].[Ag+]>C#CCCCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6cc52ce6268b484891e547260b4cddbc
CCC#CCO.Cc1ccc(S(=O)(=O)Cl)cc1>>CCC#CCOS(=O)(=O)c1ccc(C)cc1
[OH-].[K+].C(C#CCC)O.C1(=CC=C(C=C1)S(=O)(=O)Cl)C>>C1(=CC=C(C=C1)S(=O)(=O)OCC#CCC)C
[CH3:1][CH2:2][C:3]#[C:4][CH2:5][OH:6].Cl[S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]1>>[CH3:1][CH2:2][C:3]#[C:4][CH2:5][O:6][S:7](=[O:8])(=[O:9])[c:10]1[cH:11][cH:12][c:13]([CH3:14])[cH:15][cH:16]1
CCC#CCO.Cc1ccc(S(=O)(=O)Cl)cc1
CCC#CCOS(=O)(=O)c1ccc(C)cc1
null
null
[Cl-].[Na+].O.C1CCOC1
Acylation
Formation of Sulfonic Esters
d05d91207659f8fa672c205a316a670adfe2b92492fc9adad2ee3f241e574fb9
a7748b0f3b0eba3868d0cf03ae67721db046202accaaea9cadb4edbc96ec8768
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]#[C:9]-[C:10]-[OH;D1;+0:11]>>[C:7]-[C:8]#[C:9]-[C:10]-[O;H0;D2;+0:11]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
76.4
[{"value": 76.4, "product": "C1(=CC=C(C=C1)S(=O)(=O)OCC#CCC)C", "details": "PERCENTYIELD", "is_desired": false}]
-10
CELSIUS
1.5
HOUR
A solution of 2-pentyn-1-ol (8.40 g, 100 mmol) in THF (60 mL) was treated with p-toluenesulfonyl chloride (23.9 g, 125 mmol) at -10° C., followed by pulverized KOH (11.3 g, 200 mmol) without allowing the temperature to exceed -5° C. After 1.5 hours of stirring at -10° C., 50 mL of saturated brine was added and the prod...
10.6084/m9.figshare.5104873.v1
null
Tosylate.Primary alcohol.Sulfonyl halide
Tosylate
null
null
c1ccccc1
HCl
[Cl-].[Na+].O.C1CCOC1
-10
1.5
CCC#CCO.Cc1ccc(S(=O)(=O)Cl)cc1>[Cl-].[Na+].O.C1CCOC1>CCC#CCOS(=O)(=O)c1ccc(C)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-20e7740b40a84d63aa989b9ae2ca2acc
BrBr.CCC=CCC=CCCCO>>CC/C=C\C/C=C\CCCBr
C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.BrBr.C(CCC=CCC=CCC)O.C(=O)(O)[O-].[Na+]>>BrCCC\C=C/C\C=C/CC
Br[Br:11].O[CH2:10][CH2:9][CH2:8][CH:7]=[CH:6][CH2:5][CH:4]=[CH:3][CH2:2][CH3:1]>>[CH3:1][CH2:2]/[CH:3]=[CH:4]\[CH2:5]/[CH:6]=[CH:7]\[CH2:8][CH2:9][CH2:10][Br:11]
BrBr.CCC=CCC=CCCCO
CC/C=C\C/C=C\CCCBr
null
null
C(Cl)Cl.O
Functional Group Interconversion
OtherReaction
bb752b9027dc4488ba075e5955118a819f80cabd751a7497b67c2eeb1db6b071
cbf41c7cf9fe6b47a243b1674d74ed5bf46a151f7f3a71d206e23176e158facf
null
Br-[Br;H0;D1;+0:1].O-[CH2;D2;+0:2]-[C:3]-[C:4]-[C:5]=[C:6]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:2]-[C:3]-[C:4]/[C:5]=[C:6]
32
[{"value": 32.0, "product": "BrCCC\\C=C/C\\C=C/CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
A solution of triphenylphosphine (20.9 g, 80 mmol) in CH2Cl2 (100 ml) was treated with Br2 (7.8 g, 49 mmol) in CH2Cl2 (15 mL, 0° C.) and the mixture was stirred at room temperature for 20 min. Into the slightly yellow suspension that formed, the crude mixture of 4 and 4Z,7Z)-4,7-decadien-1-ol (12.4 g) in CH2Cl2 (15 ml)...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Primary halide
null
null
null
HBr
C(Cl)Cl.O
null
0.333333
BrBr.CCC=CCC=CCCCO>C(Cl)Cl.O>CC/C=C\C/C=C\CCCBr
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1bd848ddd0dc4cfa834fa8dfc6a62227
C#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCBr>>CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1
BrCCC\C=C/C\C=C/CC.O1C(CCCC1)OCCC#C.CCCCCC.C(CCC)[Li]>>O1C(CCCC1)OCCC#CCCC\C=C/C\C=C/CC
[CH:11]#[C:12][CH2:13][CH2:14][O:15][CH:16]1[CH2:17][CH2:18][CH2:19][CH2:20][O:21]1.Br[CH2:10][CH2:9][CH2:8]/[CH:7]=[CH:6]\[CH2:5]/[CH:4]=[CH:3]\[CH2:2][CH3:1]>>[CH3:1][CH2:2]/[CH:3]=[CH:4]\[CH2:5]/[CH:6]=[CH:7]\[CH2:8][CH2:9][CH2:10][C:11]#[C:12][CH2:13][CH2:14][O:15][CH:16]1[CH2:17][CH2:18][CH2:19][CH2:20][O:21]1
C#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCBr
CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1
null
null
C1CCOC1
C-C Coupling
OtherReaction
a2902088eeffba8af7cde0e465024f8c5b6cd6239687cb7ab88d93a01519cd51
65c5c213019f4e08c3c32f7e1ced539ac3ff1efc4a39855e6d21bd16502eefc5
C1CCOCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3]/[C:4]=[C:5].[C:6]-[C:7]#[CH;D1;+0:8]>>[C:6]-[C:7]#[C;H0;D2;+0:8]-[CH2;D2;+0:1]-[C:2]-[C:3]/[C:4]=[C:5]
55
[{"value": 55.0, "product": "O1C(CCCC1)OCCC#CCCC\\C=C/C\\C=C/CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 1-(tetrahydropyran-2-yloxy)-3-butyne (2.25 g, 14 mmol) in dry THF (15 ml) was treated at -50° C. with n-butyllithium hexane solution (11 ml, 17.5 mmol). After 15 min at -30° C., the mixture was kept at room temperature for 30 min. The mixture was then treated at 0° C. with 5 (3.0 g, 13.8 mmol) dissolved i...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Alkyne
Alkyne
null
null
C1CCOCC1
HBr
C1CCOC1
null
0.25
C#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCBr>C1CCOC1>CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6ab5f2747c1246a3b5a9230c3b5b5892
CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1>>CC/C=C\C/C=C\CCCC#CCCO
O1C(CCCC1)OCCC#CCCC\C=C/C\C=C/CC>>C(CC#CCCC\C=C/C\C=C/CC)O
C1CCC([O:15][CH2:14][CH2:13][C:12]#[C:11][CH2:10][CH2:9][CH2:8]/[CH:7]=[CH:6]\[CH2:5]/[CH:4]=[CH:3]\[CH2:2][CH3:1])OC1>>[CH3:1][CH2:2]/[CH:3]=[CH:4]\[CH2:5]/[CH:6]=[CH:7]\[CH2:8][CH2:9][CH2:10][C:11]#[C:12][CH2:13][CH2:14][OH:15]
CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1
CC/C=C\C/C=C\CCCC#CCCO
null
null
CO
Reduction
Ether cleavage to primary alcohol
69ac283008defddd09d640f7879e86f66dd29371b5c835a2facf24163ef14e9f
a4561cbdd42f56679299e19ea8b11070a39a15f6a95fb8a877e677f11b7ff57f
null
[C:1]#[C:2]-[C:3]-[C:4]-[O;H0;D2;+0:5]-C1-C-C-C-C-O-1>>[C:1]#[C:2]-[C:3]-[C:4]-[OH;D1;+0:5]
83
[{"value": 83.0, "product": "C(CC#CCCC\\C=C/C\\C=C/CC)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 6 (2.2 g, 7.5 mmol) in methanol (50 mL) was stirred with DOWEX™ 50W-X8 (Dow Chemical, Midland, Mich.) ion exchange resin (2 g) and the formation of 7 was monitored by TLC. The resin was removed by filtration and washed with methanol (3×20 mL). The alcohol 7 was purified by flash chromatography (1.3 g, 83%...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Primary alcohol
C1CCOCC1
null
null
HO-
CO
null
null
CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1>CO>CC/C=C\C/C=C\CCCC#CCCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2b18349f92ab4ab2a31939346351aab8
CC/C=C\C/C=C\CCCBr.CC/C=C\C/C=C\CCCCCCCOC(C)=O>>CCCCC/C=C\CCC/C=C/CCOC(C)=O
BrCCC\C=C/C\C=C/CC.C(C)(=O)OCCCCCCC\C=C/C\C=C/CC.O1C(CCCC1)OCCC\C=C/C\C=C/CC>>C(C)(=O)OCC\C=C\CCC\C=C/CCCCC
Br[CH2:10][CH2:9][CH2:8]/[CH:7]=[CH:6]\[CH2:5]/[CH:4]=[CH:3]\[CH2:2][CH3:1].CC/C=C\C/C=C\CCC[CH2:11][CH2:12][CH2:13][CH2:14][O:15][C:16]([CH3:17])=[O:18]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5]/[CH:6]=[CH:7]\[CH2:8][CH2:9][CH2:10]/[CH:11]=[CH:12]/[CH2:13][CH2:14][O:15][C:16]([CH3:17])=[O:18]
CC/C=C\C/C=C\CCCBr.CC/C=C\C/C=C\CCCCCCCOC(C)=O
CCCCC/C=C\CCC/C=C/CCOC(C)=O
null
null
null
C-C Coupling
OtherReaction
15973705e8ad8fc52aace4e951dc2397c95f8af8fb2361e425388262f1895099
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
null
Br-[CH2;D2;+0:1]-[C:2]-[C:3]/[C:4]=[C:5]\[C:6]/[CH;D2;+0:7]=[CH;D2;+0:8]\[C:9]-[C;D1;H3:10].C-C/C=C\C/C=C\C-C-C-[CH2;D2;+0:11]-[CH2;D2;+0:12]-[C:13]-[C:14]>>[C:14]-[C:13]/[CH;D2;+0:12]=[CH;D2;+0:11]/[CH2;D2;+0:1]-[C:2]-[C:3]/[C:4]=[C:5]\[C:6]-[CH2;D2;+0:7]-[CH2;D2;+0:8]-[C:9]-[C;D1;H3:10]
null
[]
null
null
null
null
Dry THF (3 ml) was treated with trimethylsilyl iodide (260 mg, 185 μl, 1.30 mmol) at room temperature and stirred for 15 min to form 4-trimethylsiloxybutyl iodide (11). A solution of CuCN. (LiCl)2 in THF (1M, 100 μl) was added, and the mixture was cooled to -40° C. The above prepared solution of Grignard reagent 10, wa...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
null
HBr
null
null
null
CC/C=C\C/C=C\CCCBr.CC/C=C\C/C=C\CCCCCCCOC(C)=O>>CCCCC/C=C\CCC/C=C/CCOC(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9a6b921b6b9d454fb8489fe840ddec57
C#CCCCOC1CCCCO1.CCCCCBr>>CCCCCC#CCCCOC1CCCCO1
O1C(CCCC1)OCCCC#C.C(CCC)[Li].C(CCCC)Br.CCCCCC>>O1C(CCCC1)OCCCC#CCCCCC
[CH:6]#[C:7][CH2:8][CH2:9][CH2:10][O:11][CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16][O:17]1.Br[CH2:5][CH2:4][CH2:3][CH2:2][CH3:1]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][C:6]#[C:7][CH2:8][CH2:9][CH2:10][O:11][CH:12]1[CH2:13][CH2:14][CH2:15][CH2:16][O:17]1
C#CCCCOC1CCCCO1.CCCCCBr
CCCCCC#CCCCOC1CCCCO1
null
null
CN1CCCN(C1=O)C
C-C Coupling
OtherReaction
a2902088eeffba8af7cde0e465024f8c5b6cd6239687cb7ab88d93a01519cd51
65c5c213019f4e08c3c32f7e1ced539ac3ff1efc4a39855e6d21bd16502eefc5
C1CCOCC1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]#[CH;D1;+0:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D2;+0:6]#[C:5]-[C:4]
58
[{"value": 58.0, "product": "O1C(CCCC1)OCCCC#CCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
1-(Tetrahydopyran-2-yloxy)-4-pentyne (1) (0.66 g, 3.90 mmol) was metallated with n-butyllithium solution (2.5M) in hexane (1.87 ml, 1.2 eq.). Addition of a solution of n-pentyl bromide (0.725 ml, 1.5 eq.) in DMPU (2 ml) produced 0.54 g (58% yield) of the title compound (15). 1H NMR (200 MHz) δ: 4.60 (m, 1H, CH-2'), 3.6...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Alkyne
Alkyne
null
null
C1CCOCC1
HBr
CN1CCCN(C1=O)C
null
null
C#CCCCOC1CCCCO1.CCCCCBr>CN1CCCN(C1=O)C>CCCCCC#CCCCOC1CCCCO1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e5f31ed3fd4346d9967feec4d8f3e24d
CCCCCC#CCCCOC1CCCCO1.[Ni]>>CC(=O)[O-].CC(=O)[O-].[Ni+2]
O1C(CCCC1)OCCCC#CCCCCC.[Ni]>>C(C)(=O)[O-].[Ni+2].C(C)(=O)[O-]
CCCC[CH2:5][C:6]#CCCC[O:3][CH:2]1[CH2:1]CCC[O:4]1.[Ni:9]>>[CH3:1][C:2](=[O:3])[O-:4].[CH3:5][C:6](=[O:7])[O-:8].[Ni+2:9]
CCCCCC#CCCCOC1CCCCO1.[Ni]
CC(=O)[O-].CC(=O)[O-].[Ni+2]
null
null
C(C)O
Acylation
OtherReaction
2f340fbc5a4e453cff3d58cdbcd5df3c66d4c0ce7bc0561d47c0b4557350e1ce
cccf3c7b77140e050567e7c3d51d59570cf8b57c0909b466cc70b1284353b3a3
null
C-C-C-C-[CH2;D2;+0:1]-[C;H0;D2;+0:2]#C-C-C-C-[O;H0;D2;+0:3]-[CH;D3;+0:4]1-[CH2;D2;+0:5]-C-C-C-[O;H0;D2;+0:6]-1.[Ni;H0;D0;+0:7]>>[CH3;D1;+0:5]-[C;H0;D3;+0:4](-[O-;H0;D1:6])=[O;H0;D1;+0:3].[CH3;D1;+0:1]-[C;H0;D3;+0:2](-[O;-;D1;H0:8])=[O;D1;H0:9].[Ni+2;H0;D0:7]
null
[]
null
null
null
null
1-(Tetrahydropyran-2-yloxy)-4-decyne (15) (0.5 g, 2.1 mmol), prepared according to Example 13, was hydrogenated in ethanol (20 ml) over P2-Ni, formed from nickel acetate (75 mg) deactivated with ethylenediamine (0.2 ml) for 4 hr. After chromatography on silica gel, the product (16) (0.43 g) was obtained in 85% yield. G...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Alkyne
null
C1CCOCC1
null
null
Other
C(C)O
null
null
CCCCCC#CCCCOC1CCCCO1.[Ni]>C(C)O>CC(=O)[O-].CC(=O)[O-].[Ni+2]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-486cc915e99745379d961e1fc7268a73
BrBr.CCCCC/C=C\CCCOC1CCCCO1>>CCCCC/C=C\CCCBr
O1C(CCCC1)OCCC\C=C/CCCCC.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.BrBr>>BrCCC\C=C/CCCCC
Br[Br:11].C1CCC(O[CH2:10][CH2:9][CH2:8]/[CH:7]=[CH:6]\[CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])OC1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5]/[CH:6]=[CH:7]\[CH2:8][CH2:9][CH2:10][Br:11]
BrBr.CCCCC/C=C\CCCOC1CCCCO1
CCCCC/C=C\CCCBr
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
729729201dd51d0c8d3a04a278bc2364265bfb40acfeab8bf38c8b1c7b990e75
584f78421401c9ef21e71fadcbb76af4243eed60702b564d34493db8cfc1becb
null
Br-[Br;H0;D1;+0:1].[C:2]=[C:3]\[C:4]-[C:5]-[CH2;D2;+0:6]-O-C1-C-C-C-C-O-1>>[Br;H0;D1;+0:1]-[CH2;D2;+0:6]-[C:5]-[C:4]/[C:3]=[C:2]
90
[{"value": 90.0, "product": "BrCCC\\C=C/CCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To an ice-cool solution of triphenylphosphine (0.72 g, 2.74 mmol) and bromine (0.41 g, 2.6 mmol) in CH2Cl2, a solution of (4Z)-1-(tetrahydropyran-2-yloxy)-4-decene (16) (0.41 g, 1.71 mmol), prepared according to Example 16, in methylene chloride was added dropwise. Isolation and purification by conventional means affor...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Primary halide
C1CCOCC1
null
null
HBr
C(Cl)Cl
null
null
BrBr.CCCCC/C=C\CCCOC1CCCCO1>C(Cl)Cl>CCCCC/C=C\CCCBr
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2f15776952b34a539da4eb150087740b
CC/C=C\C/C=C\CCC/C=C/CCOC(C)=O.CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCCCCCO[Si](C)(C)C>>CC/C=C\CCCCCC/C=C/CCOC(C)=O
C#CCC.O1C(CCCC1)OCCC\C=C/CCCCC.O1C(CCCC1)OCCC#CCCC\C=C/C\C=C/CC.BrCCCCCCOC1OCCCC1.BrCCCCCCOC1OCCCC1.O1C(CCCC1)OCCC\C=C/CCCCC.C(C)(=O)OCC\C=C\CCC\C=C/CCCCC.C(C)(=O)OCC\C=C\CCC\C=C/C\C=C/CC.C[Si](OCCCCCCC\C=C/C\C=C/CC)(C)C>>C(C)(=O)OCC\C=C\CCCCCC\C=C/CC
CC/C=C\C/C=C\[CH2:8][CH2:9][CH2:10]/[CH:11]=[CH:12]/[CH2:13][CH2:14][O:15][C:16]([CH3:17])=[O:18].C(#CCCOC1CCCCO1)CCC/C=[CH:6]\[CH2:5]/[CH:4]=[CH:3]\[CH2:2][CH3:1].CC/C=C\C/C=C\CC[CH2:7]CCCCO[Si](C)(C)C>>[CH3:1][CH2:2]/[CH:3]=[CH:4]\[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10]/[CH:11]=[CH:12]/[CH2:13][CH2:14][O:15][C:16...
CC/C=C\C/C=C\CCC/C=C/CCOC(C)=O.CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCCCCCO[Si](C)(C)C
CC/C=C\CCCCCC/C=C/CCOC(C)=O
null
null
C(Cl)(Cl)(Cl)Cl
C-C Coupling
OtherReaction
110620469c9a1e347c8d5ae50f053bbfcd31236258cd6d2ed454593db79b15b6
9d9ee273c9321f51502caf23b61abf935b514d598fbf4ae5f4928d0a887c11ab
null
C-C/C=C\C/C=C\C-C-[CH2;D2;+0:1]-C-C-C-C-O-[Si](-C)(-C)-C.C-C/C=C\C/C=C\[CH2;D2;+0:2]-[C:3]-[C:4]/[C:5]=[C:6].[C:7]/[C:8]=[C:9]\[C:10]/[CH;D2;+0:11]=C\C-C-C-C#C-C-C-O-C1-C-C-C-C-O-1>>[C:6]=[C:5]/[C:4]-[C:3]-[CH2;D2;+0:2]-[CH2;D2;+0:1]-[CH2;D2;+0:11]-[C:10]/[C:9]=[C:8]\[C:7]
15
[{"value": 15.0, "product": "C(C)(=O)OCC\\C=C\\CCCCCC\\C=C/CC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
Starting from 1-butyne and 1-bromo-6-(tetrahydropyran-2-yloxy)-hexane (22), the (3E,11Z)-3,11-tetradecadien-1-yl acetate (30) was prepared by a synthetic route similar to that used for the preparation of (3E,8Z)-3,8-tetradecadien-1-yl acetate (21), as depicted in the following scheme. ##STR18## The yield was 15% [17 mg...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Alkyne.Silyl protective group
null
C1CCOCC1
null
null
HO-
C(Cl)(Cl)(Cl)Cl
null
null
CC/C=C\C/C=C\CCC/C=C/CCOC(C)=O.CC/C=C\C/C=C\CCCC#CCCOC1CCCCO1.CC/C=C\C/C=C\CCCCCCCO[Si](C)(C)C>C(Cl)(Cl)(Cl)Cl>CC/C=C\CCCCCC/C=C/CCOC(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-48e5492592614940b5cbab975adec0bb
O=P([O-])([O-])OP(=O)([O-])[O-].[Ca]>>O.O.O=P([O-])([O-])OP(=O)([O-])[O-].[Ca+2]
[Cl-].[Ca+2].[Cl-].[O-]P([O-])(=O)OP(=O)([O-])[O-].[Na+].[Na+].[Na+].[Na+].[Ca].[P]>>O.O.[O-]P([O-])(=O)OP(=O)([O-])[O-].[Ca+2].[Ca+2]
[O:1]=[P:4]([O-:5])([O-:6])[O:7][P:8](=[O:9])([O-:10])[O-:11].[Ca:12]>>[OH2:1].[OH2:2].[O:3]=[P:4]([O-:5])([O-:6])[O:7][P:8](=[O:9])([O-:10])[O-:11].[Ca+2:12]
O=P([O-])([O-])OP(=O)([O-])[O-].[Ca]
O.O.O=P([O-])([O-])OP(=O)([O-])[O-].[Ca+2]
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
[#15:1]-[#8:2]-[P;H0;D4;+0:3](-[O;-;D1;H0:4])(-[O;-;D1;H0:5])=[O;H0;D1;+0:6].[Ca;H0;D0;+0:7]>>[#15:1]-[#8:2]-[P;H0;D4;+0:3](-[O;-;D1;H0:4])(-[O;-;D1;H0:5])=[O;D1;H0:8].[Ca+2;H0;D0:7].[OH2;D0;+0:6]
null
[]
null
null
null
null
An aqueous calcium chloride solution and an aqueous sodium pyrophosphate solution were mixed together so that the calcium/phosphorus atomic ratio became 1:1, and the mixture was allowed to stand for a whole day to form calcium diphosphate dihydrate (Ca2P2O7.2H2O) crystals, which were then filtered off. The thus prepare...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
null
null
null
O=P([O-])([O-])OP(=O)([O-])[O-].[Ca]>>O.O.O=P([O-])([O-])OP(=O)([O-])[O-].[Ca+2]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1a28675e5d044056be5059476c8f3ce9
CS(=O)(=O)Cl>>CS(=O)(=O)O
C(C)N(CC)CC.C1(CCCCC1)C=1C(=CC(=C(C1)C(C1=CC(=C(C=C1)O)O)C1=C(C=C(C(=C1)C1CCCCC1)O)C)C)O.CS(=O)(=O)Cl>>C1(CCCCC1)C=1C(=CC(=C(C1)C(C1=CC(=C(C=C1)O)O)C1=C(C=C(C(=C1)C1CCCCC1)O)C)C)O.CS(=O)(=O)O
Cl[S:2]([CH3:1])(=[O:3])=[O:5]>>[CH3:1][S:2](=[O:3])(=[O:4])[OH:5]
CS(=O)(=O)Cl
CS(=O)(=O)O
null
null
O1CCOCC1
Functional Group Interconversion
OtherReaction
6c113db978119dd30ec9ac70e3a1ccab457b8adfa2d854ef650cc9d0d938808f
5664dc87dc3eea7f40384c1c98932c2b6f77a01ae2083f96843fa9d662971745
null
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;H0;D1;+0:4]>>[C;D1;H3:2]-[S;H0;D4;+0:1](=[O;D1;H0:3])(=[O;D1;H0:5])-[OH;D1;+0:4]
null
[]
null
null
null
null
Bis(5 -cyclohexyl-4-hydroxy-2-methylphenyl)-3,4-dihydroxyphenylmethane(1.0 mole), naphthoquinone-1,2-diazido-5-sulfonyl chloride (2.0 moles) and methanesulfonyl chloride(0.5 moles) were dissolved in dioxane (4,000 g). To the resulting solution, dioxane (1,500 g) having triethylamine (500 g) dissolved therein was added ...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonic acid
null
null
null
null
O1CCOCC1
null
null
CS(=O)(=O)Cl>O1CCOCC1>CS(=O)(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cf4091059f4c4259bc4581b2905f26f6
CS(=O)(=O)Cl>>CS(=O)(=O)O
OC1=CC=C(C=C1)C(C)(C)C1=CC=C(C=C1)C(C)(C1=CC=C(C=C1)O)C1=CC=C(C=C1)O.CS(=O)(=O)Cl.C(C)N(CC)CC>>OC1=CC=C(C=C1)C(C)(C)C1=CC=C(C=C1)C(C)(C1=CC=C(C=C1)O)C1=CC=C(C=C1)O.CS(=O)(=O)O
Cl[S:34]([CH3:33])(=[O:35])=[O:37]>>[CH3:33][S:34](=[O:35])(=[O:36])[OH:37]
CS(=O)(=O)Cl
CS(=O)(=O)O
null
null
O1CCOCC1
Functional Group Interconversion
OtherReaction
6c113db978119dd30ec9ac70e3a1ccab457b8adfa2d854ef650cc9d0d938808f
5664dc87dc3eea7f40384c1c98932c2b6f77a01ae2083f96843fa9d662971745
null
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;H0;D1;+0:4]>>[C;D1;H3:2]-[S;H0;D4;+0:1](=[O;D1;H0:3])(=[O;D1;H0:5])-[OH;D1;+0:4]
null
[]
null
null
null
null
One (1.0) mole of 1-[1-(4-hydroxyphenyl)isopropyl]-4-[1,1-bis(4-hydroxyphenyl)ethyl]benzene, naphthoquinone-1,2-diazido-5-sulfonyl chloride (2.0 moles) and methanesulfonyl chloride (0.5 moles) were dissolved in dioxane (4,000 g). To the resulting solution, dioxane (2,000 g) having triethylamine (500 g) dissolved therei...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonic acid
null
null
null
null
O1CCOCC1
null
null
CS(=O)(=O)Cl>O1CCOCC1>CS(=O)(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-34a870e6034145a8adf96361ff614be2
Ic1ccccc1.c1ccc(Nc2ccc3c4c(cccc24)CC3)cc1>>c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
NC1=CC=C2CCC=3C=CC=C1C32.IC1=CC=CC=C1.C([O-])([O-])=O.[K+].[K+].[N+](=O)([O-])C1=CC=CC=C1.C1(=CC=CC=C1)NC1=CC=C2CCC=3C=CC=C1C32>>C1(=CC=CC=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32
I[c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1.[cH:1]1[cH:2][cH:3][c:4]([NH:5][c:12]2[cH:13][cH:14][c:15]3[c:16]4[c:17]([cH:18][cH:19][cH:20][c:21]24)[CH2:22][CH2:23]3)[cH:24][cH:25]1>>[cH:1]1[cH:2][cH:3][c:4]([N:5]([c:6]2[cH:7][cH:8][cH:9][cH:10][cH:11]2)[c:12]2[cH:13][cH:14][c:15]3[c:16]4[c:17]([cH:18][cH:19][cH:20][c:21]2...
Ic1ccccc1.c1ccc(Nc2ccc3c4c(cccc24)CC3)cc1
c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
null
[Cu]
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
705933786518ece8447c3a260ed1708cc50b5b37b829540bc5bba9d6bb1dde91
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
I-[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:11]):[c:12]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:8](-[c:7](:[c:6]):[c:12])-[c:9](:[c:10]):[c:11]):[c:4]:[c:5]
75.7
[{"value": 75.7, "product": "C1(=CC=CC=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32", "details": "PERCENTYIELD", "is_desired": false}]
200
CELSIUS
26
HOUR
33.85 g (0.2 mol) of 5-aminoacenaphtthene was mixed with 102.1 g (0.5 mol) of iodo benzene, 1.3 g (0.02 mol) of copper powder, 34.5 g (0.25 mol) of anhydrous potassium carbonate and 100 ml of nitrobenzene, and the mixture was stirred at 200° C. for 26 hours. The reaction was determined to be finished when disappearance...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1cc2c3c(cccc3c1)CC2
HI
[Cu].C1(=CC=CC=C1)C
200
26
Ic1ccccc1.c1ccc(Nc2ccc3c4c(cccc24)CC3)cc1>[Cu].C1(=CC=CC=C1)C>c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c9df1b4f59204cf6ba44f7f63a8372d9
CN(C)C=O.c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1>>O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
C1(=CC=CC=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32.C1(=CC=CC=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32.[OH-].[Na+].CN(C=O)C.P(=O)(Cl)(Cl)Cl>>C(=O)C1=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32
CN(C)[CH:2]=[O:1].[cH:3]1[cH:4][cH:5][c:6]([N:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][cH:16][c:17]3[c:18]4[c:19]([cH:20][cH:21][cH:22][c:23]24)[CH2:24][CH2:25]3)[cH:26][cH:27]1>>[O:1]=[CH:2][c:3]1[cH:4][cH:5][c:6]([N:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14]2[cH:15][cH:16][c:17]3[c:18]4[c:...
CN(C)C=O.c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
null
null
O
C-C Coupling
OtherReaction
aae5f0134f66d7b9e3ae1bdd9b3a75c7cb29a8908ff53e1c4658205cbcae8547
f0bd75a0630092c31f21f61f4a015c77ae0dff14a0b742b4370d7a38fda490f7
c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
C-N(-C)-[CH;D2;+0:1]=[O;D1;H0:2].[c:3]:[c:4]:[cH;D2;+0:5]:[c:6]:[c:7]>>[O;D1;H0:2]=[CH;D2;+0:1]-[c;H0;D3;+0:5](:[c:4]:[c:3]):[c:6]:[c:7]
86.6
[{"value": 86.6, "product": "C(=O)C1=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
30
MINUTE
32.14 g (0.1 mol) of the above prepared 5-(N,N-diphenylamino)acenaphthene was dissolved in 300 ml of N,N-dimethylformamide, and 22.73 g (0.15 mol) of phosphorus oxychloride was dropwise added thereto at room temperature for 30 minutes. After raising the temperature to 50° C., the reaction mixture was stirred for 14 hou...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Aldehyde
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1cc2c3c(cccc3c1)CC2
Other
O
50
0.5
CN(C)C=O.c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1>O>O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b58f8f3df4214a82901f48cbd358ba6b
CC(C)(C)[O-].CO.O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1>>Cc1ccc(C=Cc2ccc(N(c3ccccc3)c3ccc4c5c(cccc35)CC4)cc2)cc1
CC(C)([O-])C.[K+].CO.O.C(=O)C1=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32>>CC1=CC=C(C=CC2=CC=C(C=C2)N(C2=CC=CC=C2)C2=CC=C3CCC=4C=CC=C2C43)C=C1
[O-][C:2]([CH3:1])([CH3:3])[CH3:34].O[CH3:6].O=[CH:7][c:8]1[cH:9][cH:10][c:11]([N:12]([c:13]2[cH:14][cH:15][cH:16][cH:17][cH:18]2)[c:19]2[cH:20][cH:21][c:22]3[c:23]4[c:24]([cH:25][cH:26][cH:27][c:28]24)[CH2:29][CH2:30]3)[cH:31][cH:32]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([CH:6]=[CH:7][c:8]2[cH:9][cH:10][c:11]([N:12]([c:13]...
CC(C)(C)[O-].CO.O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
Cc1ccc(C=Cc2ccc(N(c3ccccc3)c3ccc4c5c(cccc35)CC4)cc2)cc1
null
null
CN(C=O)C
C-C Coupling
OtherReaction
f0a0592b1a1e7c5334fb06381d02732361ab23bcea2e7f9781480ab4da02338a
916508af6de7b69ef7f25dc9a08aafad6db32342143032e3e6d5dcfab38f0b04
C(=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1)c1ccccc1
O-[CH3;D1;+0:1].O=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[C;H0;D4;+0:7](-[CH3;D1;+0:8])(-[CH3;D1;+0:9])-[O-]>>[C;D1;H3:6]-[c;H0;D3;+0:7]1:[cH;D2;+0:8]:[c:10]:[c:11](-[CH;D2;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]):[c:12]:[cH;D2;+0:9]:1
85
[{"value": 85.0, "product": "CC1=CC=C(C=CC2=CC=C(C=C2)N(C2=CC=CC=C2)C2=CC=C3CCC=4C=CC=C2C43)C=C1", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
20.96 g (0.06 mol) of 5-[N-(4-formylphenyl)-N-phenylamino]acenaphthene prepared in Preparation Example 1 and 17.44 g (0.072 mol) of diethyl 4-methylbenzyl phosphonate were dissolved in 300 ml of N,N-dimethylformamide, and 10.1 g (0.09 mol) of potassium-tert-butoxide was added thereto at room temperature for 20 minutes....
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Methanol
null
null
c1ccccc1
c1ccccc1.c1ccccc1.c1ccccc1.c1cc2c3c(cccc3c1)CC2
null
CN(C=O)C
null
0.333333
CC(C)(C)[O-].CO.O=Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1>CN(C=O)C>Cc1ccc(C=Cc2ccc(N(c3ccccc3)c3ccc4c5c(cccc35)CC4)cc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f7732a0ba48b458e9add51628a8da0ea
CC(=O)OC(C)=O.Nc1ccc2c3c(cccc13)CC2>>CC(=O)Nc1ccc2c3c(cccc13)CC2
NC1=CC=C2CCC=3C=CC=C1C32.C(C)(=O)OC(C)=O.NC1=CC=C2CCC=3C=CC=C1C32>>C(C)(=O)NC1=CC=C2CCC=3C=CC=C1C32
CC(=O)O[C:2]([CH3:1])=[O:3].[NH2:4][c:5]1[cH:6][cH:7][c:8]2[c:9]3[c:10]([cH:11][cH:12][cH:13][c:14]13)[CH2:15][CH2:16]2>>[CH3:1][C:2](=[O:3])[NH:4][c:5]1[cH:6][cH:7][c:8]2[c:9]3[c:10]([cH:11][cH:12][cH:13][c:14]13)[CH2:15][CH2:16]2
CC(=O)OC(C)=O.Nc1ccc2c3c(cccc13)CC2
CC(=O)Nc1ccc2c3c(cccc13)CC2
null
null
C(C)(=O)O
Acylation
Aminolysis of esters
87d35e51b477fc9a658a6f307eb56d84c8879182772c9dd3a42ec0d584fd2684
627cbc0550c9f51ad0105d9fcf46677e8c93bed87ee95bfe69292a82550c95b7
c1cc2c3c(cccc3c1)CC2
C-C(=O)-O-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[NH2;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[NH;D2;+0:4]-[c:5](:[c:6]):[c:7]
96.4
[{"value": 96.4, "product": "C(C)(=O)NC1=CC=C2CCC=3C=CC=C1C32", "details": "PERCENTYIELD", "is_desired": false}, {"value": 96.4, "product": "C(C)(=O)NC1=CC=C2CCC=3C=CC=C1C32", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
15
MINUTE
50 ml of glacial acetic acid was added to 6.77 g (0.04 mol) of 5-aminoacenaphthene and the mixture was stirred at 60° C. to dissolve, and 8.16 g (0.08 mol) acetic anhydride was dropwise added thereto for 15 minutes. After finishing the dropwise addition, the mixture was stirred at the same temperature for 2 hours. The ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Primary amine
Secondary amide
null
null
c1cc2c3c(cccc3c1)CC2
HO-
C(C)(=O)O
60
0.25
CC(=O)OC(C)=O.Nc1ccc2c3c(cccc13)CC2>C(C)(=O)O>CC(=O)Nc1ccc2c3c(cccc13)CC2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b70ac3636d7b43a287feb3a7f751e2d4
CC(=O)Nc1ccc2c3c(cccc13)CC2.Cc1ccc(I)cc1>>Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1
C(C)(=O)NC1=CC=C2CCC=3C=CC=C1C32.C(C)(=O)NC1=CC=C2CCC=3C=CC=C1C32.[OH-].[K+].IC1=CC=C(C=C1)C.C([O-])([O-])=O.[K+].[K+].[N+](=O)([O-])C1=CC=CC=C1>>C1(=CC=C(C=C1)NC1=CC=C2CCC=3C=CC=C1C32)C
CC(=O)[NH:6][c:7]1[cH:8][cH:9][c:10]2[c:11]3[c:12]([cH:13][cH:14][cH:15][c:16]13)[CH2:17][CH2:18]2.I[c:5]1[cH:4][cH:3][c:2]([CH3:1])[cH:20][cH:19]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH:6][c:7]2[cH:8][cH:9][c:10]3[c:11]4[c:12]([cH:13][cH:14][cH:15][c:16]24)[CH2:17][CH2:18]3)[cH:19][cH:20]1
CC(=O)Nc1ccc2c3c(cccc13)CC2.Cc1ccc(I)cc1
Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1
null
[Cu]
C(CC(C)C)O.O
Heteroatom Alkylation and Arylation
OtherReaction
4763e31bea43ae027a9f6a9b2dfaf0a863c582414461eb226c3255e1383821c8
1114ab2898bd0ea809755408ff9536c46f0d2f5958471cb24361706255b159ef
c1ccc(Nc2ccc3c4c(cccc24)CC3)cc1
C-C(=O)-[NH;D2;+0:1]-[c:2](:[c:3]):[c:4].I-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9]>>[c:3]:[c:2](-[NH;D2;+0:1]-[c;H0;D3;+0:5](:[c:6]:[c:7]):[c:8]:[c:9]):[c:4]
72.3
[{"value": 72.3, "product": "C1(=CC=C(C=C1)NC1=CC=C2CCC=3C=CC=C1C32)C", "details": "PERCENTYIELD", "is_desired": false}]
200
CELSIUS
6
HOUR
7.39 g (0.035 mol) of the above prepared 5-(N-acetylamino)acenaphthene was mixed with 10.91 g (0.05 mol) of p-iodo toluene, 0.32 g (0.005 mol) of copper powder, 5.52 g (0.04 mol) of anhydrous potassium carbonate and 10 ml of nitrobenzene, and the mixture was stirred at 200° C. for 6 hours. The reaction was determined t...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amide
Secondary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1cc2c3c(cccc3c1)CC2
HI
[Cu].C(CC(C)C)O.O
200
6
CC(=O)Nc1ccc2c3c(cccc13)CC2.Cc1ccc(I)cc1>[Cu].C(CC(C)C)O.O>Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a22b523213134b988e3fb268968dfa76
Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1.Ic1ccccc1>>Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
C1(=CC=C(C=C1)NC1=CC=C2CCC=3C=CC=C1C32)C.C1(=CC=C(C=C1)NC1=CC=C2CCC=3C=CC=C1C32)C.IC1=CC=CC=C1.C([O-])([O-])=O.[K+].[K+].[N+](=O)([O-])C1=CC=CC=C1>>C1(=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32)C
[CH3:1][c:2]1[cH:3][cH:4][c:5]([NH:6][c:13]2[cH:14][cH:15][c:16]3[c:17]4[c:18]([cH:19][cH:20][cH:21][c:22]24)[CH2:23][CH2:24]3)[cH:25][cH:26]1.I[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:13]2[cH:14][cH:15][c:16]3[c:17]4[c:18]([cH:19][cH:20]...
Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1.Ic1ccccc1
Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
null
[Cu]
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution amine
705933786518ece8447c3a260ed1708cc50b5b37b829540bc5bba9d6bb1dde91
b6b8e2cdb45054a35f5e8157d624f852c0601a09401556706e166b19536eb7a7
c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
I-[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:11]):[c:12]>>[c:3]:[c:2]:[c;H0;D3;+0:1](-[N;H0;D3;+0:8](-[c:7](:[c:6]):[c:12])-[c:9](:[c:10]):[c:11]):[c:4]:[c:5]
83.8
[{"value": 83.8, "product": "C1(=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32)C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
4.66 g (0.018 mol) of the above prepared 5-[N-(4-tolyl)amino]acenaphthene was mixed with 4.99 g (0.022 mol) of iodo benzene, 0.13 g (0.002 mol) of copper powder, 2.76 g (0.02 mol) of anhydrous potassium carbonate and 5 ml of nitrobenzene, and the resultant mixture was stirred at 200° C. for 25 hours. The reaction was d...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Secondary amine
Tertiary amine
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1cc2c3c(cccc3c1)CC2
HI
[Cu].C1(=CC=CC=C1)C
null
null
Cc1ccc(Nc2ccc3c4c(cccc24)CC3)cc1.Ic1ccccc1>[Cu].C1(=CC=CC=C1)C>Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-20078ac392344345839361b7b292e056
Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1.O=P(Cl)(Cl)Cl>>Cc1ccc(N(c2ccc(C=O)cc2)c2ccc3c4c(cccc24)CC3)cc1
C1(=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32)C.C1(=CC=C(C=C1)N(C1=CC=CC=C1)C1=CC=C2CCC=3C=CC=C1C32)C.[OH-].[Na+].CN(C=O)C.P(=O)(Cl)(Cl)Cl>>C(=O)C1=CC=C(C=C1)N(C1=CC=C(C=C1)C)C1=CC=C2CCC=3C=CC=C1C32
[CH3:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][cH:10][cH:13][cH:14]2)[c:15]2[cH:16][cH:17][c:18]3[c:19]4[c:20]([cH:21][cH:22][cH:23][c:24]24)[CH2:25][CH2:26]3)[cH:27][cH:28]1.ClP(Cl)(Cl)=[O:12]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]([N:6]([c:7]2[cH:8][cH:9][c:10]([CH:11]=[O:12])[cH:13][cH:14]2)[c:15]2[cH:16][cH:17][c...
Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1.O=P(Cl)(Cl)Cl
Cc1ccc(N(c2ccc(C=O)cc2)c2ccc3c4c(cccc24)CC3)cc1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
e3eb3563143a436a1b6dd1eadac83913d5a87e712b8ad652ab28367873285db5
be117abed4a0a0378ea43d3a5c1ccf903b86823ade7e92fcb09d68743e45d19a
c1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1
Cl-P(-Cl)(-Cl)=[O;H0;D1;+0:1].[c:2]:[c:3]:[cH;D2;+0:4]:[c:5]:[c:6]>>[O;H0;D1;+0:1]=[C:7]-[c;H0;D3;+0:4](:[c:3]:[c:2]):[c:5]:[c:6]
97.1
[{"value": 97.1, "product": "C(=O)C1=CC=C(C=C1)N(C1=CC=C(C=C1)C)C1=CC=C2CCC=3C=CC=C1C32", "details": "PERCENTYIELD", "is_desired": false}]
50
CELSIUS
10
MINUTE
4.7 g (0.014 mol) of the above prepared 5-[N-(4-tolyl)-N-phenylamino]acenaphthene was dissolved in 30 ml of N,N-dimethylformamide, and 3.22 g (0.021 mol) of phosphorus oxychloride was dropwise added thereto at room temperature for 10 minutes. After the temperature was raised to 50° C., and the mixture was stirred for 1...
10.6084/m9.figshare.5104873.v1
null
null
Aldehyde
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1.c1cc2c3c(cccc3c1)CC2
Other
O
50
0.166667
Cc1ccc(N(c2ccccc2)c2ccc3c4c(cccc24)CC3)cc1.O=P(Cl)(Cl)Cl>O>Cc1ccc(N(c2ccc(C=O)cc2)c2ccc3c4c(cccc24)CC3)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4a9ed02b548945d8a2465cef6a9abb9e
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]>>N#CCCCCC(N)=O
C(CCCCC#N)#N.[O-]P([O-])(=O)OP(=O)([O-])[O-]>>C(#N)CCCCC(=O)N
[N:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][C:7]#[N:8].O=P([O-])([O-])OP([O-])([O-])=[O:9]>>[N:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][C:7]([NH2:8])=[O:9]
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]
N#CCCCCC(N)=O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1d1793919e847ed86dcb16487e62464531560dbf4782f9a5875bfe7e0477a3ec
d6f9d146e8ef95e62f1a3ab55a7e3b4ceec8856a5f71b6dccd4ad850f945b658
null
O=P(-[O-])(-[O-])-O-P(-[O-])(-[O-])=[O;H0;D1;+0:1].[C:2]-[C:3]-[C;H0;D2;+0:4]#[N;H0;D1;+0:5]>>[C:2]-[C:3]-[C;H0;D3;+0:4](-[NH2;D1;+0:5])=[O;H0;D1;+0:1]
null
[]
5
CELSIUS
24
HOUR
Various Pseudomonas strains were grown on 10 mM adipontrile in PR Basal medium for 24 h and harvested by centrifugation. Wet cell pastes were frozen for storage. To test for biocatalyst reaction, 50 mg of frozen cell paste was resuspended in 1 mL of 50 mM pyrophosphate buffer, pH 7.5. Adiponitrile substrate was added t...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amide
null
null
null
Other
null
5
24
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]>>N#CCCCCC(N)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-62c80c03f0274ea6842044f298f2f2f0
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]>>N#CCCCCC(N)=O
C(CCCCC#N)#N.[O-]P([O-])(=O)OP(=O)([O-])[O-]>>C(#N)CCCCC(=O)N
[N:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][C:7]#[N:8].O=P([O-])([O-])OP([O-])([O-])=[O:9]>>[N:1]#[C:2][CH2:3][CH2:4][CH2:5][CH2:6][C:7]([NH2:8])=[O:9]
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]
N#CCCCCC(N)=O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
1d1793919e847ed86dcb16487e62464531560dbf4782f9a5875bfe7e0477a3ec
d6f9d146e8ef95e62f1a3ab55a7e3b4ceec8856a5f71b6dccd4ad850f945b658
null
O=P(-[O-])(-[O-])-O-P(-[O-])(-[O-])=[O;H0;D1;+0:1].[C:2]-[C:3]-[C;H0;D2;+0:4]#[N;H0;D1;+0:5]>>[C:2]-[C:3]-[C;H0;D3;+0:4](-[NH2;D1;+0:5])=[O;H0;D1;+0:1]
null
[]
30
CELSIUS
4
HOUR
In a 20 mL glass vial, 50 mg wet cell paste of 20-5-SBN-1b (ATCC 55735) was resuspended in 1 mL of 50 mM pyrophosphate buffer, pH 7.5. Adiponitrile was added to a final concentration of 400 mM and the reaction mixture was shaken at 200 rpm at 30° C. for 4 h on a rotary shaker. Cells were removed by centrifugation and t...
10.6084/m9.figshare.5104873.v1
null
Nitrile
Primary amide
null
null
null
Other
null
30
4
N#CCCCCC#N.O=P([O-])([O-])OP(=O)([O-])[O-]>>N#CCCCCC(N)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5b62ce49ffab4c1db9e358eac8f40d5a
C[C@@H](N)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O.O=C([O-])C(=O)Cc1ccccc1>>N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
N[C@@H](C)C(=O)O.N[C@@H](CC1=CC=CC=C1)C(=O)O.N[C@H](C)C(=O)O.C1(=CC=CC=C1)CC(C(=O)[O-])=O>>N[C@H](CC1=CC=CC=C1)C(=O)O.N[C@@H](CC1=CC=CC=C1)C(=O)O
C[C@@H:2]([NH2:1])[C:10](=[O:11])[OH:12].[NH2:13][C@@H:14]([CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[C:22](=[O:23])[OH:24].O=C([O-])C(=O)[CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1>>[NH2:1][C@@H:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12].[NH2:13][C@H:14]([CH2:15][c:16]1[cH:17][cH...
C[C@@H](N)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O.O=C([O-])C(=O)Cc1ccccc1
N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
null
null
null
C-C Coupling
OtherReaction
b47050f08d82e3e68de9d69580af9026f89fe179af05d47a7df8437aa12924dc
06a42e352cf517302d592bf38a2fd11b220014e39071074dc7becb6ee0bee4b2
c1ccccc1.c1ccccc1
C-[C@@H;D3;+0:1](-[N;D1;H2:2])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5].O=C(-[O-])-C(=O)-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9]>>[N;D1;H2:2]-[C@@H;D3;+0:1](-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9])-[C:3](=[O;D1;H0:4])-[O;D1;H1:5]
null
[]
null
null
null
null
Using cultures of recombinant cells of the present invention with the addition of D-, L-alanine and L-phenylalanine as additional sources of D-alanine and phenylpyruvate substrates for the D-aminotransferase gene product resulted in the production of 13.66 g/l of D-phenylalanine and 0.47 g/l of L-phenylalanine, a 94% e...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1.c1ccccc1
HO-
null
null
null
C[C@@H](N)C(=O)O.N[C@@H](Cc1ccccc1)C(=O)O.O=C([O-])C(=O)Cc1ccccc1>>N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ca050bcf3e3041878a46906ef366ed6a
C[C@H](N)C(=O)O.C[C@H](N)C(=O)O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO>>N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
N[C@@H](C)C(=O)O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.N[C@@H](C)C(=O)O>>N[C@H](CC1=CC=CC=C1)C(=O)O.N[C@@H](CC1=CC=CC=C1)C(=O)O
[NH2:1][C@H:2]([C:10](=[O:11])[OH:12])[CH3:17].[C:5]([C@@H:14]([NH2:13])[CH3:15])(=[O:23])[OH:24].O=[CH:3][C@H:4](O)[C@@H:9](O)[C@H:8](O)[C@H:7](O)[CH2:6]O>>[NH2:1][C@@H:2]([CH2:3][c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1)[C:10](=[O:11])[OH:12].[NH2:13][C@H:14]([CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1)[C:22](=[O...
C[C@H](N)C(=O)O.C[C@H](N)C(=O)O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO
N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
null
null
null
Aromatic Heterocycle Formation
OtherReaction
8788bca7db1c16f497c50d4ecbd4e7b6300043102b0ed8387a00a51db34dc368
eec4a41bd1d060d27fb2d966a546f07959e09f93c8e37af3aa50924ec628c32c
c1ccccc1.c1ccccc1
O-[CH2;D2;+0:1]-[C@@H;D3;+0:2](-O)-[C@@H;D3;+0:3](-O)-[C@H;D3;+0:4](-O)-[C@@H;D3;+0:5](-O)-[CH;D2;+0:6]=O.[CH3;D1;+0:7]-[C@H;D3;+0:8](-[N;D1;H2:9])-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[OH;D1;+0:12].[CH3;D1;+0:13]-[C@H;D3;+0:14](-[N;D1;H2:15])-[C:16](=[O;D1;H0:17])-[O;D1;H1:18]>>[N;D1;H2:15]-[C@@H;D3;+0:14](-[CH2;D2;+0:6]...
null
[]
null
null
12
HOUR
The amount of glucose fed was 2021 g over 52 hours. The fermentation medium included a D-, L-alanine feed whereby a total of 1400 mls of 167 g/l D-, L-alanine was fed at a rate of 1.9 ml/min starting 12 hrs from the beginning of the fermentation. In addition, L-phenylalanine was fed at the same concentration and rate a...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid.Primary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol.Secondary alcohol
Carboxylic acid
null
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
null
null
null
12
C[C@H](N)C(=O)O.C[C@H](N)C(=O)O.O=C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO>>N[C@@H](Cc1ccccc1)C(=O)O.N[C@H](Cc1ccccc1)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4e4527ef977240138a93b4260c881157
Nc1nc(=O)c2ncn([C@@H]3O[C@@H]4COP(=O)(O)O[C@H]4[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1O>>Nc1nc(=O)c2ncn([C@@H]3O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O
C=1N=C(C2=C(N1)N(C=N2)[C@H]3[C@@H]([C@H]4[C@H](O3)COP(=O)(O4)O)O)N.C1=NC2=C(N1[C@H]3[C@@H]([C@H]4[C@H](O3)COP(=O)(O4)O)O)NC(=NC2=O)N>>C1=NC2=C(C(=N1)N)N=CN2[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)(O)O)O)O.C1=NC2=C(N1[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)(O)O)O)O)NC(=NC2=O)N
[NH2:1][c:2]1[n:3][c:4](=[O:5])[c:6]2[n:7][cH:8][n:9]([C@@H:10]3[O:11][C@@H:12]4[CH2:13][O:14][P:15](=[O:16])([OH:17])[O:20][C@H:19]4[C@H:21]3[OH:22])[c:23]2[nH:24]1.[OH:18][P:40]1(=[O:41])[O:39][CH2:38][C@H:37]2[O:36][C@@H:35]([n:34]3[c:30]4[n:29][cH:28][n:27][c:26]([NH2:25])[c:31]4[n:32][cH:33]3)[C@H:46]([OH:47])[C@@...
Nc1nc(=O)c2ncn([C@@H]3O[C@@H]4COP(=O)(O)O[C@H]4[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1O
Nc1nc(=O)c2ncn([C@@H]3O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O
null
null
null
Miscellaneous
OtherReaction
aa17667f8b741130e83d131d323d153ef4079e376eeaacc64ab5d0dd33c5cd61
97340401e708c23011c193957a1863de6b8895607cc7ceebe54b6a3b81ea560d
O=c1nc[nH]c2c1ncn2[C@H]1CCCO1.c1ncc2ncn([C@H]3CCCO3)c2n1
[#8:1]-[C:2]1-[C:3]-[#8:4]-[P;H0;D4;+0:5](=[O;D1;H0:6])(-[O;D1;H1:7])-[O;H0;D2;+0:8]-[C:9]-1-[C:10].[#8:11]-[C:12]1-[C:13]-[#8:14]-[P;H0;D4;+0:15](=[O;D1;H0:16])(-[OH;D1;+0:17])-[O;H0;D2;+0:18]-[C:19]-1-[C:20]>>[#8:11]-[C:12](-[C:13]-[#8:14]-[P;H0;D4;+0:15](=[O;D1;H0:16])(-[O;D1;H1:21])-[O;D1;H1:22])-[C:19](-[OH;D1;+0:...
null
[]
null
null
null
null
The enzyme of the present invention isolated and purified from rat cerebral cortex in Example was acted on [8-3H] cAMP and [8-3H] cGMP as substrates to form [8-3H] 5'-AMP and [8-3H] 5'-GMP, respectively. The products were reacted with 5'-nucleotidase to form [8-3H] adenosine and [8-3H] guanosine, respectively. These pr...
10.6084/m9.figshare.5104873.v1
null
null
Secondary alcohol.Secondary alcohol.Phosphate ester.Phosphate ester
C1C[C@@H]2O[P]OC[C@H]2O1.C1C[C@@H]2O[P]OC[C@H]2O1
null
c1ncc2[nH]cnc2n1.C1CCOC1.c1ncnc2nc[nH]c12.C1CCOC1
Other
null
null
null
Nc1nc(=O)c2ncn([C@@H]3O[C@@H]4COP(=O)(O)O[C@H]4[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@@H]2COP(=O)(O)O[C@H]2[C@H]1O>>Nc1nc(=O)c2ncn([C@@H]3O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]3O)c2[nH]1.Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dd6d1a78ee72419a8409d1047d1e9c38
C1CO1.CCCCCCCCCCCCCCCCCCNC>>CCCCCCCCCCCCCCCCCCN(C)CCO
CNCCCCCCCCCCCCCCCCCC.C1CO1>>OCCN(C)CCCCCCCCCCCCCCCCCC
[CH2:21]1[CH2:22][O: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][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][NH:19][CH3:20]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][CH2:18][N:19]([...
C1CO1.CCCCCCCCCCCCCCCCCCNC
CCCCCCCCCCCCCCCCCCN(C)CCO
null
null
null
Heteroatom Alkylation and Arylation
Ring opening of epoxide with amine
7de6cb7ffc33700c22d0ce54ea22e03fc1bea9a639db7a130c2c399ea3700642
128400f60196a90df2be08c769daa326293f26a6f70a086568a2c266322e372f
null
[C:1]-[C:2]-[NH;D2;+0:3]-[C;D1;H3:4].[C:5]1-[CH2;D2;+0:6]-[O;H0;D2;+0:7]-1>>[C:1]-[C:2]-[N;H0;D3;+0:3](-[C;D1;H3:4])-[CH2;D2;+0:6]-[C:5]-[OH;D1;+0:7]
86.6
[{"value": 86.6, "product": "OCCN(C)CCCCCCCCCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
160
CELSIUS
null
null
An autoclave provided with a stirrer, a thermometer, a pressure gauge and a pressure dropping funnel was charged with 250 g of N-methyloctadecylamine and heated to 160° C. Then 45 g of ethylene oxide was occasionally added dropwise thereto under a pressure of 0 to 6 kg/cm2G. Three hours were required for completing the...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine
Primary alcohol.Tertiary amine
C1CO1
null
null
null
null
160
null
C1CO1.CCCCCCCCCCCCCCCCCCNC>>CCCCCCCCCCCCCCCCCCN(C)CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d450d9a3b4314144865c4274817143d7
CCCCCCCCCCCCCCCCCC(=O)O.CCCCCCCCCCCCCCCCCCN(C)CCO>>CCCCCCCCCCCCCCCCCCN(C)CCOC(=O)CCCCCCCCCCCCCCCCC
OCCN(C)CCCCCCCCCCCCCCCCCC.C(CCCCCCCCCCCCCCCCC)(=O)O>>C(CCCCCCCCCCCCCCCCC)(=O)OCCN(C)CCCCCCCCCCCCCCCCCC
[OH:23][C:24](=[O:25])[CH2:26][CH2:27][CH2:28][CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH2:34][CH2:35][CH2:36][CH2:37][CH2:38][CH2:39][CH2:40][CH2:41][CH3:42].O[CH2:22][CH2:21][N:19]([CH2:18][CH2:17][CH2:16][CH2:15][CH2:14][CH2:13][CH2:12][CH2:11][CH2:10][CH2:9][CH2:8][CH2:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[...
CCCCCCCCCCCCCCCCCC(=O)O.CCCCCCCCCCCCCCCCCCN(C)CCO
CCCCCCCCCCCCCCCCCCN(C)CCOC(=O)CCCCCCCCCCCCCCCCC
null
null
null
Heteroatom Alkylation and Arylation
Esterification of Carboxylic Acids
3f9a9ace480b666da05fcfe5450d12b5c1ea5b0d435c195e1dd4bd20281604bb
dcbf04ec563ed0e9dfc79070490a028958024079a671c385858bb18cc8ec995a
null
O-[CH2;D2;+0:1]-[C:2]-[#7:3].[C:4]-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]>>[#7:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:7]-[C:5](-[C:4])=[O;D1;H0:6]
96.5
[{"value": 96.5, "product": "C(CCCCCCCCCCCCCCCCC)(=O)OCCN(C)CCCCCCCCCCCCCCCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
180
CELSIUS
null
null
A four-neck flask provided with a stirrer, a thermometer and a dehydrating tube was charged with 200 g of the N-(2-hydroxyethyl)-N-methyloctadecylamine and 174 g of octadecanoic acid. The mixture was heated to 180° C. and maintained at this temperature for 12 hours while distilling off the water thus formed. Thus 350 g...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary alcohol
Ester
null
null
null
HO-
null
180
null
CCCCCCCCCCCCCCCCCC(=O)O.CCCCCCCCCCCCCCCCCCN(C)CCO>>CCCCCCCCCCCCCCCCCCN(C)CCOC(=O)CCCCCCCCCCCCCCCCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c4fd97650ffa477c91c1528e59316f4a
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.O=C(OO)c1cccc(Cl)c1>>C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl
ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC=C.C([O-])([O-])=O.[Na+].[Na+].ClC=1C=C(C(=O)OO)C=CC1>>ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC1CO1
[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]([CH2:11][CH2:12][CH:13]=[CH2:14])[nH:16][c:17]2=[O:18])[c:19]([Cl:20])[cH:21][c:22]1[Cl:23].O=C(O[OH:15])c1cccc(Cl)c1>>[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]([CH2:11][CH2:12][CH:13]3[CH2:14][O:15]3)[nH:16][c:17]2=[O:18])[c:19]([Cl:20])[c...
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.O=C(OO)c1cccc(Cl)c1
C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl
null
null
ClCCl
Heteroatom Alkylation and Arylation
OtherReaction
fa67e488c6e215faf3f8ba92b55089cf5ac738315c63f0805edf5ac603aa4c40
8f36f0953871bb4e46b1272823a9df5d866ec11318b28272136c57016b5bffba
O=c1[nH]c(CCC2CO2)nn1-c1ccccc1
Cl-c1:c:c:c:c(-C(=O)-O-[OH;D1;+0:1]):c:1.[C:2]-[C:3]-[CH;D2;+0:4]=[CH2;D1;+0:5]>>[C:2]-[C:3]-[CH;D3;+0:4]1-[CH2;D2;+0:5]-[O;H0;D2;+0:1]-1
95.4
[{"value": 95.4, "product": "ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC1CO1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 500 mg (1.48 mmol) of 2-[2,4-dichloro-5-(2-propynyloxy)-phenyl]-2,4-dihydro-5-(3-butenyl)-3H- 1,2,4-triazol-3-one in 20 mL of dichloromethane was added 172 mg (1.63 mmol) of sodium carbonate and 970 mg of m-chloroperoxybenzoic acid (50-60%, 2.81 mmol) in an ice bath. The reaction mixture was stirred at...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Peroxide.Allyl
Ether
c1ccccc1
C1CO1
c1ccccc1.c1nc[nH]n1.C1CO1
HCl
ClCCl
null
24
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.O=C(OO)c1cccc(Cl)c1>ClCCl>C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2736e404c5764e36926699eef871adb6
C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl>>C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl
ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC1CO1.C([O-])([O-])=O.[K+].[K+]>>ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CC(CC2)O)C1=O
[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]([CH2:18][CH2:17][CH:15]3[CH2:14][O:16]3)[nH:11][c:12]2=[O:13])[c:19]([Cl:20])[cH:21][c:22]1[Cl:23]>>[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]3[n:11]([c:12]2=[O:13])[CH2:14][CH:15]([OH:16])[CH2:17][CH2:18]3)[c:19]([Cl:20])[cH:21][c:22]1[Cl:2...
C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl
C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl
null
null
C(C)#N
Miscellaneous
OtherReaction
8a1e2ba333438ec4bf65f5dde9fc2657ecc85bcbc203e7f6c36e36567619a509
816a42e4e92b4becc10e09218671f2e2a7942c9348b22e40d965e6444e589265
O=c1n(-c2ccccc2)nc2n1CCCC2
[O;D1;H0:1]=[c:2]1:[nH;D2;+0:3]:[c:4](-[C:5]-[C:6]-[C:7]2-[CH2;D2;+0:8]-[O;H0;D2;+0:9]-2):[#7;a:10]:[#7;a:11]:1-[c:12]>>[O;D1;H0:1]=[c:2]1:[#7;a:11](-[c:12]):[#7;a:10]:[c:4]2:[n;H0;D3;+0:3]:1-[CH2;D2;+0:8]-[C:7](-[OH;D1;+0:9])-[C:6]-[C:5]-2
36.8
[{"value": 36.8, "product": "ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CC(CC2)O)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 500 mg (1.41 mmol) of 2-[2,4-dichloro-5-(2-propynyloxy)-phenyl]-2,4-dihydro-5-(3,4-epoxybutyl)-3H-1,2,4-triazol-3-one and 563 mg (4.08 mmol) of potassium carbonate in 20 mL of acetonitrile was warmed at reflux for 2h. The mixture was cooled to room temperature and filtered. The filtrate was evaporated in v...
10.6084/m9.figshare.5104873.v1
null
Ether
Secondary alcohol
c1nc[nH]n1.C1CO1
c1nnc2n1CCCC2
c1ccccc1.c1nnc2n1CCCC2
null
C(C)#N
null
null
C#CCOc1cc(-n2nc(CCC3CO3)[nH]c2=O)c(Cl)cc1Cl>C(C)#N>C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9634d1d63f934be6bfca6b1b336ece9e
C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl.CCN(CC)S(F)(F)F>>C#CCOc1cc(-n2nc3n(c2=O)CC(F)CC3)c(Cl)cc1Cl
ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CC(CC2)O)C1=O.C(C)N(CC)S(F)(F)F>>ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CC(CC2)F)C1=O
O[CH:15]1[CH2:14][n:11]2[c:10]([n:9][n:8](-[c:7]3[cH:6][c:5]([O:4][CH2:3][C:2]#[CH:1])[c:22]([Cl:23])[cH:21][c:19]3[Cl:20])[c:12]2=[O:13])[CH2:18][CH2:17]1.CCN(CC)S(F)(F)[F:16]>>[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]3[n:11]([c:12]2=[O:13])[CH2:14][CH:15]([F:16])[CH2:17][CH2:18]3)[c:19]([Cl:20])[cH...
C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl.CCN(CC)S(F)(F)F
C#CCOc1cc(-n2nc3n(c2=O)CC(F)CC3)c(Cl)cc1Cl
null
null
ClCCl
Functional Group Interconversion
OtherReaction
d8fbab1d02e1efd4596161d3c366fdb64771eeec247c936cd515b9bbca4f09d5
2e01f8a2520bb2c01521f4c10ab406a1b29fe14554ff1fda976238a9b96e671b
O=c1n(-c2ccccc2)nc2n1CCCC2
C-C-N(-C-C)-S(-F)(-F)-[F;H0;D1;+0:1].O-[CH;D3;+0:2]1-[C:3]-[#7;a:4]2:[c:5]:[#7;a:6]:[#7;a:7]:[c:8]:2-[C:9]-[C:10]-1>>[F;H0;D1;+0:1]-[CH;D3;+0:2]1-[C:3]-[#7;a:4]2:[c:5]:[#7;a:6]:[#7;a:7]:[c:8]:2-[C:9]-[C:10]-1
37.7
[{"value": 37.7, "product": "ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CC(CC2)F)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
1
HOUR
To a solution of 169 mg (0.477 mmol) of 5,6,7,8-tetrahydro-2-[2,4-dichloro-5-(2-propynyloxy)phenyl]-6-hydroxy-1,2,4-triazolo[4,3-a]pyridin-3(2H)-one in 5 mL of dichloromethane was added 76 μl (0.573 mmol) of diethylaminosulfur trifluoride (DAST) at 0° C. The reaction mixture was stirred at 0° C. for 1h. The mixture was...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Tertiary amine
Secondary halide
c1nnc2n1CCCC2
c1nnc2n1CCCC2
c1ccccc1.c1nnc2n1CCCC2
HF
ClCCl
0
1
C#CCOc1cc(-n2nc3n(c2=O)CC(O)CC3)c(Cl)cc1Cl.CCN(CC)S(F)(F)F>ClCCl>C#CCOc1cc(-n2nc3n(c2=O)CC(F)CC3)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64c534178a4a4c3f822722a59b57a089
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.[O-][I+3]([O-])([O-])[O-]>>C#CCOc1cc(-n2nc(CCC=O)[nH]c2=O)c(Cl)cc1Cl
ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC=C.I(=O)(=O)(=O)[O-].[Na+]>>ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC=O
C=[CH:13][CH2:12][CH2:11][c:10]1[n:9][n:8](-[c:7]2[cH:6][c:5]([O:4][CH2:3][C:2]#[CH:1])[c:21]([Cl:22])[cH:20][c:18]2[Cl:19])[c:16](=[O:17])[nH:15]1.[O-][I+3]([O-])([O-])[O-:14]>>[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]([CH2:11][CH2:12][CH:13]=[O:14])[nH:15][c:16]2=[O:17])[c:18]([Cl:19])[cH:20][c:21]...
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.[O-][I+3]([O-])([O-])[O-]
C#CCOc1cc(-n2nc(CCC=O)[nH]c2=O)c(Cl)cc1Cl
null
[Os](=O)(=O)(=O)=O
O.O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
b16cdbf18e0a0961ab3e2390d6e4aee8b329f7136e9bd1c8a4c806ff7a76d090
c8848c7c3d9cc0904f82fae046e80cc577adb0f636b4d050e73f85888c0c7f1d
O=c1[nH]cnn1-c1ccccc1
C=[CH;D2;+0:1]-[C:2]-[C:3].[O-;H0;D1:4]-[I+3](-[O-])(-[O-])-[O-]>>[C:3]-[C:2]-[CH;D2;+0:1]=[O;H0;D1;+0:4]
92.2
[{"value": 92.2, "product": "ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C(NC1=O)CCC=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 500 mg (1.48 mmol) of 2-[2,4-dichloro-5-(2-propynyloxy)phenyl]-2,4-dihydro-5-(3-butenyl)-3H-1,2,4-triazol-3-one in a mixture of 10 mL of tetrahydrofuran and 10 mL of water was added 696 mg (3.25 mmol) of sodium periodate and 167 mL of 0.18M aqueous solution of osmium tetroxide at room temperature. The ...
10.6084/m9.figshare.5104873.v1
null
Allyl
Aldehyde
null
null
c1ccccc1.c1nc[nH]n1
HI
[Os](=O)(=O)(=O)=O.O.O1CCCC1
null
null
C#CCOc1cc(-n2nc(CCC=C)[nH]c2=O)c(Cl)cc1Cl.[O-][I+3]([O-])([O-])[O-]>[Os](=O)(=O)(=O)=O.O.O1CCCC1>C#CCOc1cc(-n2nc(CCC=O)[nH]c2=O)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8a4b58ae25a9460d8b441c80118dd2e8
CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3)c(Cl)cc1Cl.O=C1CCC(=O)N1Br>>CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3Br)c(Cl)cc1Cl
C(C)(=O)OC=1C(=CC(=C(C1)N1N=C2N(CCCC2)C1=O)Cl)Cl.BrN1C(CCC1=O)=O>>C(C)(=O)OC=1C(=CC(=C(C1)N1N=C2N(CCCC2Br)C1=O)Cl)Cl
[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]3[n:11]([c:12]2=[O:13])[CH2:14][CH2:15][CH2:16][CH2:17]3)[c:19]([Cl:20])[cH:21][c:22]1[Cl:23].O=C1CCC(=O)N1[Br:18]>>[CH3:1][C:2](=[O:3])[O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]3[n:11]([c:12]2=[O:13])[CH2:14][CH2:15][CH2:16][CH:17]3[Br:18])[c:19]([Cl:20])[cH:...
CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3)c(Cl)cc1Cl.O=C1CCC(=O)N1Br
CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3Br)c(Cl)cc1Cl
null
null
C(Cl)(Cl)(Cl)Cl
Functional Group Interconversion
Wohl-Ziegler bromination benzyl secondary
865273dafce70d025fe5f37b7c3b9e9a944136dd18628bfe5f064e092d7013a4
d425bc7fa712969b9477dfeabb5ca2470f442214b30503c51715e13a06c60154
O=c1n(-c2ccccc2)nc2n1CCCC2
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[c:2]-[#7;a:3]1:[#7;a:4]:[c:5]2:[#7;a:6](:[c:7]:1)-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-2>>[Br;H0;D1;+0:1]-[CH;D3;+0:11]1-[C:10]-[C:9]-[C:8]-[#7;a:6]2:[c:7]:[#7;a:3](-[c:2]):[#7;a:4]:[c:5]:2-1
93.6
[{"value": 93.6, "product": "C(C)(=O)OC=1C(=CC(=C(C1)N1N=C2N(CCCC2Br)C1=O)Cl)Cl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 3.55 g (10.4 mmol) of 5,6,7,8-tetrahydro-2-(5-acetyloxy-2,4-dichlorophenyl)-1,2,4-triazolo[4,3-α]pyridin-3(2H)-one in 100 mL of carbon tetrachloride was added 2.03 g (11.4 mmol) of N-bromosuccinimide at room temperature. The mixture was warmed under reflux by irradiating with a sun lamp for 3h. The mix...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Secondary halide
c1nnc2n1CCCC2.C1CCNC1
c1nnc2n1CCCC2
c1ccccc1.c1nnc2n1CCCC2
HO-
C(Cl)(Cl)(Cl)Cl
null
null
CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3)c(Cl)cc1Cl.O=C1CCC(=O)N1Br>C(Cl)(Cl)(Cl)Cl>CC(=O)Oc1cc(-n2nc3n(c2=O)CCCC3Br)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-04601f04a9e04e4b899149b8d86a04b2
C#CCOc1cc(-n2nc3n(c2=O)CCCC3O)c(Cl)cc1Cl.CCN(CC)S(F)(F)F>>C#CCOc1cc(-n2nc3n(c2=O)CCCC3F)c(Cl)cc1Cl
ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CCCC2O)C1=O.C(C)N(CC)S(F)(F)F>>ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CCCC2F)C1=O
O[CH:17]1[c:10]2[n:9][n:8](-[c:7]3[cH:6][c:5]([O:4][CH2:3][C:2]#[CH:1])[c:22]([Cl:23])[cH:21][c:19]3[Cl:20])[c:12](=[O:13])[n:11]2[CH2:14][CH2:15][CH2:16]1.CCN(CC)S(F)(F)[F:18]>>[CH:1]#[C:2][CH2:3][O:4][c:5]1[cH:6][c:7](-[n:8]2[n:9][c:10]3[n:11]([c:12]2=[O:13])[CH2:14][CH2:15][CH2:16][CH:17]3[F:18])[c:19]([Cl:20])[cH:2...
C#CCOc1cc(-n2nc3n(c2=O)CCCC3O)c(Cl)cc1Cl.CCN(CC)S(F)(F)F
C#CCOc1cc(-n2nc3n(c2=O)CCCC3F)c(Cl)cc1Cl
null
null
ClCCl
Functional Group Interconversion
OtherReaction
d8fbab1d02e1efd4596161d3c366fdb64771eeec247c936cd515b9bbca4f09d5
2e01f8a2520bb2c01521f4c10ab406a1b29fe14554ff1fda976238a9b96e671b
O=c1n(-c2ccccc2)nc2n1CCCC2
C-C-N(-C-C)-S(-F)(-F)-[F;H0;D1;+0:1].O-[CH;D3;+0:2]1-[C:3]-[C:4]-[C:5]-[#7;a:6]2:[c:7]:[#7;a:8](-[c:9]):[#7;a:10]:[c:11]:2-1>>[F;H0;D1;+0:1]-[CH;D3;+0:2]1-[C:3]-[C:4]-[C:5]-[#7;a:6]2:[c:7]:[#7;a:8](-[c:9]):[#7;a:10]:[c:11]:2-1
90.2
[{"value": 90.2, "product": "ClC1=C(C=C(C(=C1)Cl)OCC#C)N1N=C2N(CCCC2F)C1=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-78
CELSIUS
4
HOUR
To a solution of 300 mg (0.847 mmol) of 5,6,7,8-tetrahydro-2-[2,4-dichloro-5-(2-propynyloxy)phenyl]-8-hydroxy-1,2,4-triazolo[4,3-α]pyridin-3(2H)-one in 10 mL of dichloromethane was added 123 mL (0.930 mmol) of diethylaminosulfur trifluoride (DAST) at -78° C. The reaction mixture was stirred at -78° C. for 4h. The mixtu...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Tertiary amine
Secondary halide
c1nnc2n1CCCC2
c1nnc2n1CCCC2
c1ccccc1.c1nnc2n1CCCC2
HF
ClCCl
-78
4
C#CCOc1cc(-n2nc3n(c2=O)CCCC3O)c(Cl)cc1Cl.CCN(CC)S(F)(F)F>ClCCl>C#CCOc1cc(-n2nc3n(c2=O)CCCC3F)c(Cl)cc1Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2169f1be862948a3a9409a68450a60e7
CCOC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>>CCOP(=O)(OCC)C(CC(=O)O)P(=O)(OCC)OCC
[OH-].[Na+].C(C)OP(=O)(C(CC(=O)OCC)P(=O)(OCC)OCC)OCC>>O(CC)P(=O)(C(CC(=O)O)P(=O)(OCC)OCC)OCC
CC[O:13][C:11]([CH2:10][CH:9]([P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:6][CH2:7][CH3:8])[P:14](=[O:15])([O:16][CH2:17][CH3:18])[O:19][CH2:20][CH3:21])=[O:12]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][C:11](=[O:12])[OH:13])[P:14](=[O:15])([O:16][CH2:17][CH3:18])[O:19][CH2:20][CH3:21]
CCOC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
CCOP(=O)(OCC)C(CC(=O)O)P(=O)(OCC)OCC
null
null
CCO.O
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
null
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
96
[{"value": 96.0, "product": "O(CC)P(=O)(C(CC(=O)O)P(=O)(OCC)OCC)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 95.6, "product": "O(CC)P(=O)(C(CC(=O)O)P(=O)(OCC)OCC)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
80
CELSIUS
null
null
A solution of NaOH (4.00 g, 100 mmol) in water (50 ml) was added to a solution of ethyl 3,3-bis(diethoxyphosphinyl)propionate (32.6 g, 87 mmol) in EtOH (100 ml), and heated at 80° C. for 1 hour. After cooling, the EtOH was evaporated, and the residue was acidified to methyl orange with 12N HCl. The product was extracte...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
null
Other
CCO.O
80
null
CCOC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>CCO.O>CCOP(=O)(OCC)C(CC(=O)O)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64a7cfe6196c4bb8ae1073b5f5bdac47
CCCN(CCC)C(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>>CCCN(CCC)CCC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
C(CC)N(C(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O)CCC.B.CSC.Cl>>C(C)OP(OCC)(=O)C(CCN(CCC)CCC)P(OCC)(=O)OCC
O=[C:8]([N:4]([CH2:3][CH2:2][CH3:1])[CH2:5][CH2:6][CH3:7])[CH2:9][CH:10]([P:11](=[O:12])([O:13][CH2:14][CH3:15])[O:16][CH2:17][CH3:18])[P:19](=[O:20])([O:21][CH2:22][CH3:23])[O:24][CH2:25][CH3:26]>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[CH2:8][CH2:9][CH:10]([P:11](=[O:12])([O:13][CH2:14][CH3:15])[O:16][CH2:1...
CCCN(CCC)C(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
CCCN(CCC)CCC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
null
null
C1CCOC1
Reduction
Reduction of tertiary amides to amines
f74c5a050b269ec4da3871c266f01344b7447381f47cda744f8b1e9c225ae62d
c8f3c617792f7a4fae96b8a97dc0ce23461ab85d8a738fe6caacff776ef51ffa
null
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[#7:4](-[C:5])-[C:6]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[#7:4](-[C:5])-[C:6]
60
[{"value": 60.0, "product": "C(C)OP(OCC)(=O)C(CCN(CCC)CCC)P(OCC)(=O)OCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.9, "product": "C(C)OP(OCC)(=O)C(CCN(CCC)CCC)P(OCC)(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
20
MINUTE
A solution of N,N-dipropyl-3,3-bis(diethoxyphosphinyl)propionamide (1.25 g, 2.9 mmol) in THF (7.1 ml) was cooled to 0° C., and borane-methylsulfide (0.71 ml, 7.1 mmol) was added via syringe. The reaction was stirred at 0° C. for 20 minutes, then warmed at 65 C. for 3 hours. The reaction mixture was cooled to 0° C. and ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
null
null
null
null
Other
C1CCOC1
0
0.333333
CCCN(CCC)C(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>C1CCOC1>CCCN(CCC)CCC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-513ee407692540e49f626f2d20b712d3
CCOP(=O)(OCC)C(CC(=O)N(C)OC)P(=O)(OCC)OCC>>CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC
CON(C(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O)C.[H-].[Na+].C1CCOC1.C1CCOC1.[H-]>>O=C(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CC
CON([C:11]([CH2:10][CH:9]([P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:6][CH2:7][CH3:8])[P:15](=[O:16])([O:17][CH2:18][CH3:19])[O:20][CH2:21][CH3:22])=[O:12])[CH3:14]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][C:11](=[O:12])[CH2:13][CH3:14])[P:15](=[O:16])([O:17][CH2:18][CH3:19])[O:20][CH2:21][CH3:22...
CCOP(=O)(OCC)C(CC(=O)N(C)OC)P(=O)(OCC)OCC
CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC
null
null
null
Functional Group Interconversion
OtherReaction
0e1b501f4aadb0e84ffc93b33216cc37dfe617cb6c3e325779c58539a7f5c4e4
af85307a4412ed48cedcfde84079732215472ffbe274bdc1dc12e9979d5c5e06
null
C-O-N(-[CH3;D1;+0:1])-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:4]-[C:5]>>[C:5]-[C:4]-[C;H0;D3;+0:2](=[O;D1;H0:3])-[C:6]-[CH3;D1;+0:1]
54
[{"value": 54.0, "product": "O=C(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CC", "details": "PERCENTYIELD", "is_desired": false}]
-78
CELSIUS
null
null
A solution of N-methoxy-N-methyl-3,3-bis(diethoxyphosphinyl)propionamide (1.00 g, 2.6 mmol) in THF (5 ml) was slowly added to a slurry of 80% sodium hydride (80 mg, 2.7 mmol) in THF (10 ml) at 0° C. Stirring was continued until all of the hydride was consumed (~20 minutes). The solution was cooled to -78° C. and ethylm...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide
Ketone
null
null
null
HO-
null
-78
null
CCOP(=O)(OCC)C(CC(=O)N(C)OC)P(=O)(OCC)OCC>>CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ea7684e9a71040288dbea5e299a3c7d7
CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC.NCc1ccccc1>>CCOP(=O)(OCC)C(CC(CC)NCc1ccccc1)P(=O)(OCC)OCC
[BH3-]C#N.[Na+].O=C(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CC.CC1=C(C(=C(C=C1C2(C3=CC=CC=C3S(=O)(=O)O2)C4=CC(=C(C(=C4C)Br)O)C(C)C)C(C)C)O)Br.C(C1=CC=CC=C1)N.[BH3-]C#N.[Na+]>>C(C1=CC=CC=C1)NC(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CC
O=[C:11]([CH2:10][CH:9]([P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:6][CH2:7][CH3:8])[P:22](=[O:23])([O:24][CH2:25][CH3:26])[O:27][CH2:28][CH3:29])[CH2:12][CH3:13].[NH2:14][CH2:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][CH:11]([CH2:12][CH3:13])[NH:14][C...
CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC.NCc1ccccc1
CCOP(=O)(OCC)C(CC(CC)NCc1ccccc1)P(=O)(OCC)OCC
null
null
C(C)(=O)O.CO
Heteroatom Alkylation and Arylation
Reductive amination with ketone
4940e8ed9a0db9bde699fdcdc3aff2cff0409c19478aa0ed1acfd98213338adf
07faf85ffe990e88a1de7fd04a339bf226f78d8bfae9712ea59eebd76bb54b9f
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C;D1;H3:5].[NH2;D1;+0:6]-[C:7]-[c:8]>>[C:3]-[C:2]-[CH;D3;+0:1](-[C:4]-[C;D1;H3:5])-[NH;D2;+0:6]-[C:7]-[c:8]
null
[]
null
null
4
DAY
To a stirred solution of tetraethyl 3-oxopentane-1,1-bisphosphonate (0.50 g, 1.4 mmol) in methanol (5 ml) was added a small amount of bromothymol blue and benzylamine (0.75 g, 7.0 mmol). Acetic acid was added dropwise until the solution turned yellow (pH=6), and NaCNBH3 (57 mg, 0.9 mmol) was added. The resulting yellow...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Secondary amine
null
null
c1ccccc1
Other
C(C)(=O)O.CO
null
96
CCOP(=O)(OCC)C(CC(=O)CC)P(=O)(OCC)OCC.NCc1ccccc1>C(C)(=O)O.CO>CCOP(=O)(OCC)C(CC(CC)NCc1ccccc1)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0d06fa7cb400433aac9523d5cb4e75c0
CCCCNC(=O)CCl.CCOP(=O)(CP(=O)(OCC)OCC)OCC>>CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
C(CCC)NC(CCl)=O.[I-].[K+].[Cl-].[Na+].C(P(OCC)(OCC)=O)P(OCC)(OCC)=O.[H-].[Na+].[H-]>>C(CCC)NC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O
Cl[CH2:8][C:6]([NH:5][CH2:4][CH2:3][CH2:2][CH3:1])=[O:7].[CH2:9]([P:10](=[O:11])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17])[P:18](=[O:19])([O:20][CH2:21][CH3:22])[O:23][CH2:24][CH3:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][C:6](=[O:7])[CH2:8][CH:9]([P:10](=[O:11])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17])[P:18](...
CCCCNC(=O)CCl.CCOP(=O)(CP(=O)(OCC)OCC)OCC
CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
null
null
C1CCOC1
C-C Coupling
OtherReaction
15973705e8ad8fc52aace4e951dc2397c95f8af8fb2361e425388262f1895099
f5e5e22797736d188bba28deb76a4cee8e4fee4dca04fe24f733d2ee68a23361
null
Cl-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5].[#8:6]-[#15:7](-[#8:8])(=[O;D1;H0:9])-[CH2;D2;+0:10]-[#15:11](-[#8:12])(-[#8:13])=[O;D1;H0:14]>>[#8:6]-[#15:7](-[#8:8])(=[O;D1;H0:9])-[CH;D3;+0:10](-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[#7:4]-[C:5])-[#15:11](-[#8:12])(-[#8:13])=[O;D1;H0:14]
70
[{"value": 70.0, "product": "C(CCC)NC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 69.8, "product": "C(CCC)NC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Tetraethyl methylenebisphosphonate (1.44 g, 5.0 mmol) in THF (1 mL) was added to a slurry of 80% sodium hydride (150 mg, 5.0 mmol) in THF (4 mL) at 0° C. The reaction was warmed to room temperature and stirred until all of the hydride was consumed. A solution of N-butyl-2-chloroacetamide (0.75 g, 5.0 mmol) in THF (1 ml...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
null
HCl
C1CCOC1
null
null
CCCCNC(=O)CCl.CCOP(=O)(CP(=O)(OCC)OCC)OCC>C1CCOC1>CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3f7c12ece3d5427682be4ea183c9152d
CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>>CCCCNCCC(P(=O)(O)O)P(=O)(O)O
C(CCC)NC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)=O.B.CSC.Cl>>C(CCC)NCCC(P(O)(=O)O)P(O)(=O)O
CC[O:11][P:9]([CH:8]([CH2:7][C:6](=O)[NH:5][CH2:4][CH2:3][CH2:2][CH3:1])[P:13](=[O:14])([O:15]CC)[O:16]CC)(=[O:10])[O:12]CC>>[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH:8]([P:9](=[O:10])([OH:11])[OH:12])[P:13](=[O:14])([OH:15])[OH:16]
CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
CCCCNCCC(P(=O)(O)O)P(=O)(O)O
null
null
C1CCOC1
Reduction
OtherReaction
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
null
C-C-[O;H0;D2;+0:1]-[#15:2](=[O;D1;H0:3])(-[O;H0;D2;+0:4]-C-C)-[C:5](-[C:6]-[C;H0;D3;+0:7](=O)-[#7:8]-[C:9])-[#15:10](=[O;D1;H0:11])(-[O;H0;D2;+0:12]-C-C)-[O;H0;D2;+0:13]-C-C>>[C:9]-[#7:8]-[CH2;D2;+0:7]-[C:6]-[C:5](-[#15:10](=[O;D1;H0:11])(-[OH;D1;+0:12])-[OH;D1;+0:13])-[#15:2](=[O;D1;H0:3])(-[OH;D1;+0:1])-[OH;D1;+0:4]
109
[{"value": 109.0, "product": "C(CCC)NCCC(P(O)(=O)O)P(O)(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
5
MINUTE
A solution of N-butyl-3,3-bis(diethoxyphosphinyl)propionamide (1.40 g, 3.5 mmol) in THF (9 mL) was cooled to 0° C., and borane-methyl sulfide (0.90 ml, 9.0 mmol) was added via syringe. The reaction was stirred at 0° C. for 5 minutes, then warmed to 65° C. for 3 hours. The reaction mixture was cooled to 0° C. and 6N HCl...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
null
HO-
C1CCOC1
0
0.083333
CCCCNC(=O)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>C1CCOC1>CCCCNCCC(P(=O)(O)O)P(=O)(O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-18119a89941c4368a7ad288ebe54d59f
CCOP(=O)(OCC)C(CCCCN)P(=O)(OCC)OCC.O=C(Cl)c1ccccc1>>CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC
C(C1=CC=CC=C1)(=O)Cl.NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC.C(C)N(CC)CC>>C(C1=CC=CC=C1)(=O)NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC
[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][CH2:11][CH2:12][CH2:13][NH2:14])[P:23](=[O:24])([O:25][CH2:26][CH3:27])[O:28][CH2:29][CH3:30].Cl[C:15](=[O:16])[c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][CH2:11][CH2:12][CH2:13][NH...
CCOP(=O)(OCC)C(CCCCN)P(=O)(OCC)OCC.O=C(Cl)c1ccccc1
CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC
null
null
ClCCl
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccccc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c: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]
30.7
[{"value": 30.7, "product": "C(C1=CC=CC=C1)(=O)NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of benzoyl chloride (0.73 g, 5.0 mmol) in dichloromethane was added slowly to a solution of tetraethyl 5-aminopentane-1,1-bisphosphonate (1.50 g, 4.5 mmol) from Example 11, part A, and triethylamine (0.76 mL, 5.5 mmol) in dichloromethane at 0° C. After warming to room temperature for 30 minutes, the reaction...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccccc1
HCl
ClCCl
null
null
CCOP(=O)(OCC)C(CCCCN)P(=O)(OCC)OCC.O=C(Cl)c1ccccc1>ClCCl>CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-861d1c5c6eb14e7f813a68ed25b21881
CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC>>CCOP(=O)(OCC)C(CCCCNCc1ccccc1)P(=O)(OCC)OCC
C(C1=CC=CC=C1)(=O)NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC.CSC.B.Cl>>C(C1=CC=CC=C1)NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC
O=[C:15]([NH:14][CH2:13][CH2:12][CH2:11][CH2:10][CH:9]([P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:6][CH2:7][CH3:8])[P:22](=[O:23])([O:24][CH2:25][CH3:26])[O:27][CH2:28][CH3:29])[c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([O:6][CH2:7][CH3:8])[CH:9]([CH2:10][CH2:11][CH2:12][CH2:13][NH:14][CH2:...
CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC
CCOP(=O)(OCC)C(CCCCNCc1ccccc1)P(=O)(OCC)OCC
null
null
C1CCOC1
Reduction
Reduction of secondary amides to amines
85b757f1833edc9e5c6365ee6b904683f414e7b9a5f9bfcfd7addca401447058
ab40188eef2f825df7003af0ffae31d0ce53d126542122535627d3d354cbc9fe
c1ccccc1
O=[C;H0;D3;+0:1](-[#7:2]-[C:3])-[c:4](:[c:5]):[c:6]>>[C:3]-[#7:2]-[CH2;D2;+0:1]-[c:4](:[c:5]):[c:6]
45.8
[{"value": 45.8, "product": "C(C1=CC=CC=C1)NCCCCC(P(OCC)(=O)OCC)P(OCC)(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
0
CELSIUS
20
MINUTE
A solution of tetraethyl N-benzoyl-5-aminopentane-1,1-bisphosphonate (0.63 g, 1.36 mmol) in THF (3.4 mL) was cooled to 0° C., and borane methylsulfide (0.34 ml, 3.4 mmol) was added via syringe. The reaction was stirred at 0° C. for 20 minutes, then warmed to 65° C. for 2.5 hours. The reaction mixture was cooled to 0° C...
10.6084/m9.figshare.5104873.v1
null
Secondary amide
null
null
null
c1ccccc1
Other
C1CCOC1
0
0.333333
CCOP(=O)(OCC)C(CCCCNC(=O)c1ccccc1)P(=O)(OCC)OCC>C1CCOC1>CCOP(=O)(OCC)C(CCCCNCc1ccccc1)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6f9159e7c4774638b827a4db2641898a
CCCCCC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)[N+](=O)[O-]>>CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
C(=O)[O-].[NH4+].[N+](=O)([O-])C(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CCCCC.C(=O)[O-].[NH4+]>>NC(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CCCCC
O=[N+:7]([O-])[CH:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[CH2:8][CH:9]([P:10](=[O:11])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17])[P:18](=[O:19])([O:20][CH2:21][CH3:22])[O:23][CH2:24][CH3:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]([NH2:7])[CH2:8][CH:9]([P:10](=[O:11])([O:12][CH2:13][CH3:14])[O:15][CH2:16][CH3:17...
CCCCCC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)[N+](=O)[O-]
CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
null
[Pd].[Pd]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
null
O=[N+;H0;D3:1](-[O-])-[C:2](-[C:3])-[C:4]>>[C:3]-[C:2](-[C:4])-[NH2;D1;+0:1]
95
[{"value": 95.0, "product": "NC(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CCCCC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 92.3, "product": "NC(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a stirred solution of tetraethyl 3-nitrooctane-1,1-bisphosphonate (0.70 g, 1.62 mmol) in methanol (4 mL) was added ammonium formate (0.45 g, 6.9 mmol) and 10% palladium on carbon (0.070 g). After 24 hours, more 10% palladium on carbon (0.035 g) and ammonium formate (0.45 g, 6.9 mmol) were added. After stirring for a...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
null
Other
[Pd].[Pd].CO
null
24
CCCCCC(CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC)[N+](=O)[O-]>[Pd].[Pd].CO>CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-66715e3038e443c89124069570855fa8
CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>>CCCCCC(N)CC(P(=O)([O-])[O-])P(=O)([O-])O.[NH4+].[NH4+].[NH4+]
NC(CC(P(OCC)(=O)OCC)P(OCC)(=O)OCC)CCCCC.Br[Si](C)(C)C>>[NH4+].[NH4+].[NH4+].NC(CC(P([O-])(=O)[O-])P(O)(=O)[O-])CCCCC
CC[O:12][P:10]([CH:9]([CH2:8][CH:6]([CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[NH2:7])[P:14](=[O:15])([O:16]CC)[O:17]CC)(=[O:11])[O:13]CC>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH:6]([NH2:7])[CH2:8][CH:9]([P:10](=[O:11])([O-:12])[O-:13])[P:14](=[O:15])([O-:16])[OH:17].[NH4+:18].[NH4+:19].[NH4+:20]
CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC
CCCCCC(N)CC(P(=O)([O-])[O-])P(=O)([O-])O.[NH4+].[NH4+].[NH4+]
null
null
ClCCl
Functional Group Interconversion
OtherReaction
42af6cdfb86a130c92365e01a31b50705eea7bdf12f67dc370bf24402f7ceedc
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
null
C-C-[O;H0;D2;+0:1]-[#15:2](=[O;D1;H0:3])(-[C:4]-[#15:5](=[O;D1;H0:6])(-[O;H0;D2;+0:7]-C-C)-[O;H0;D2;+0:8]-C-C)-[O;H0;D2;+0:9]-C-C>>[O-;H0;D1:1]-[#15:2](-[O-;H0;D1:9])(=[O;D1;H0:3])-[C:4]-[#15:5](-[O-;H0;D1:7])(=[O;D1;H0:6])-[OH;D1;+0:8]
419.8
[{"value": 419.8, "product": "[NH4+].[NH4+].[NH4+].NC(CC(P([O-])(=O)[O-])P(O)(=O)[O-])CCCCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of tetraethyl 3-aminooctane-1,1-bisphosphonate (0.45 g, 1.12 mmol) in dry dichloromethane (1.1 mL) was added bromotrimethylsilane (1.05 mL, 7.85 mmol) via syringe. After 18 hours, the mixture was concentrated under vacuum. To the residue was added 3N NH4OH (8 mL) which was stirred for 30 minutes at room t...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
Other
ClCCl
null
18
CCCCCC(N)CC(P(=O)(OCC)OCC)P(=O)(OCC)OCC>ClCCl>CCCCCC(N)CC(P(=O)([O-])[O-])P(=O)([O-])O.[NH4+].[NH4+].[NH4+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-73770e6874334f60888ff4ce1f4e06f1
CO.Cc1ccc(OCC(=O)O)cc1.O=Cc1ccccc1S(=O)(=O)O.[Na].c1ccc([PH+](c2ccccc2)c2ccccc2)cc1>>COC(=O)c1ccc(/C=C/c2cccc[c]2[Na])c(S(=O)(=O)O)c1
C1(=CC=CC=C1)[PH+](C1=CC=CC=C1)C1=CC=CC=C1.C(=O)(O)COC1=CC=C(C=C1)C.C(=O)C1=C(C=CC=C1)S(=O)(=O)O.[Na].CO.C[O-].[Na+]>>[Na]C1=C(/C=C/C2=C(C=C(C=C2)C(=O)OC)S(=O)(=O)O)C=CC=C1
O[CH3:1].c1[c:8]([CH3:9])[cH:7][cH:6]c(O[CH2:5][C:3]([OH:2])=[O:4])[cH:23]1.O=[CH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][c:18]1[S:19](=[O:20])(=[O:21])[OH:22].[Na:17].c1ccc([PH+](c2ccccc2)c2cccc[cH:16]2)cc1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8](/[CH:9]=[CH:10]/[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[Na:1...
CO.Cc1ccc(OCC(=O)O)cc1.O=Cc1ccccc1S(=O)(=O)O.[Na].c1ccc([PH+](c2ccccc2)c2ccccc2)cc1
COC(=O)c1ccc(/C=C/c2cccc[c]2[Na])c(S(=O)(=O)O)c1
null
CS(=O)(=O)O
null
Heteroatom Alkylation and Arylation
OtherReaction
a5892bc718af7fd687d0891e151f9bacf978b68c56679fea314853496fdb59cb
a88642547a8d0b18ebe5827c60bfffb7fd0e6760c9bffb376aaf721018ea99e5
C(=C/c1ccccc1)\c1ccccc1
O-[CH3;D1;+0:1].O=[CH;D2;+0:2]-[c;H0;D3;+0:3]1:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:[c;H0;D3;+0:8]:1-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[O;D1;H1:12].[CH3;D1;+0:13]-[c;H0;D3;+0:14]1:[c:15]:[cH;D2;+0:16]:c(-O-[CH2;D2;+0:17]-[C:18](=[O;D1;H0:19])-[OH;D1;+0:20]):[cH;D2;+0:21]:c:1.[Na;H0;D0;+0:22].[cH;D2;+0:23]1:c:c:c:c:c:1-[P...
null
[]
null
null
null
null
To 146 gm (0.327 mol) of the adduct prepared in Example 10 in a 2 L, three-neck round bottom flask equipped with a magnetic stirring bar, condenser, addition funnel, and thermometer connected to a temperature controlling device (Thermowatch, I2R), is added 2-formylbenzenesulfonic acid, sodium salt, hydrate (Aldrich, 80...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid.Ether.Methanol
Ester
c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
HO-
CS(=O)(=O)O
null
null
CO.Cc1ccc(OCC(=O)O)cc1.O=Cc1ccccc1S(=O)(=O)O.[Na].c1ccc([PH+](c2ccccc2)c2ccccc2)cc1>CS(=O)(=O)O>COC(=O)c1ccc(/C=C/c2cccc[c]2[Na])c(S(=O)(=O)O)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0a27e3faf3c24930a2eeef0ff4a98ee9
COC.COc1cccc(-c2oc3ccccc3c2C)c1.COc1cccc(-c2oc3ccccc3c2C)c1.O>>Cc1c(-c2cccc(O)c2)oc2ccccc12.Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
O.COC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2.COC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2.Cl.N1=CC=CC=C1.COC>>OC(COC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2)CO.OC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2
[CH3:28][O:29][CH3:30].C[O:9][c:8]1[cH:7][cH:6][cH:5][c:4](-[c:3]2[c:2]([CH3:1])[c:17]3[c:12]([o:11]2)[cH:13][cH:14][cH:15][cH:16]3)[cH:10]1.[CH3:18][c:19]1[c:20](-[c:21]2[cH:22][cH:23][cH:24][c:25]([O:26][CH3:27])[cH:32]2)[o:33][c:34]2[cH:35][cH:36][cH:37][cH:38][c:39]12.[OH2:31]>>[CH3:1][c:2]1[c:3](-[c:4]2[cH:5][cH:6...
COC.COc1cccc(-c2oc3ccccc3c2C)c1.COc1cccc(-c2oc3ccccc3c2C)c1.O
Cc1c(-c2cccc(O)c2)oc2ccccc12.Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
null
[Ti](Cl)(Cl)(Cl)Cl.[Zn]
O1CCOCC1
Heteroatom Alkylation and Arylation
OtherReaction
7787e927eda04892d51ea69720338113e3a470222203566827db92b9f1cbe895
65ac6f7cf6ec095bf5a4e40cc6a8549e6c1b4a5d53d05b78aaa58078db8ffa96
c1ccc(-c2cc3ccccc3o2)cc1.c1ccc(-c2cc3ccccc3o2)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4].[CH3;D1;+0:5]-[#8:6]-[c:7].[CH3;D1;+0:8]-[O;H0;D2;+0:9]-[CH3;D1;+0:10].[OH2;D0;+0:11]>>[OH;D1;+0:9]-[CH;D3;+0:8](-[CH2;D2;+0:5]-[#8:6]-[c:7])-[CH2;D2;+0:10]-[OH;D1;+0:11].[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
The ester which results from the condensation of 2'-hydroxyacetophenone and m-anisic acid is converted to 2-(3-methoxyphenyl)-3-methylbenzofuran by reductive cyclization in dioxane with a titanium tetrachloride/zinc metal catalyst according to the method of Banerji and Nayak, J. Chem. Soc., Chem. Comm., (1990), 150. Th...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether
Ether.Primary alcohol.Secondary alcohol.Aromatic alcohol
null
null
c1ccccc1.c1ccc2occc2c1.c1ccccc1.c1ccc2occc2c1
Other
[Ti](Cl)(Cl)(Cl)Cl.[Zn].O1CCOCC1
null
null
COC.COc1cccc(-c2oc3ccccc3c2C)c1.COc1cccc(-c2oc3ccccc3c2C)c1.O>[Ti](Cl)(Cl)(Cl)Cl.[Zn].O1CCOCC1>Cc1c(-c2cccc(O)c2)oc2ccccc12.Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5dd2c77bb7de45af8bd5e3455820ca7e
Cc1c(-c2cccc(O)c2)oc2ccccc12.OCC1CO1>>Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
CS(=O)(=O)O.C[O-].[Na+].OC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2.C1C(O1)CO>>OC(COC=1C=C(C=CC1)C=1OC2=C(C1C)C=CC=C2)CO
[CH3:1][c:2]1[c:3](-[c:4]2[cH:5][cH:6][cH:7][c:8]([OH:9])[cH:15]2)[o:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12.[CH2:10]1[CH:11]([CH2:13][OH:14])[O:12]1>>[CH3:1][c:2]1[c:3](-[c:4]2[cH:5][cH:6][cH:7][c:8]([O:9][CH2:10][CH:11]([OH:12])[CH2:13][OH:14])[cH:15]2)[o:16][c:17]2[cH:18][cH:19][cH:20][cH:21][c:22]12
Cc1c(-c2cccc(O)c2)oc2ccccc12.OCC1CO1
Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
c8f37de1487a64e5d0f374942194fdf1fb5ee79a4a7c0eead7f4385797f6a345
d65f28c52f0777a08a008cfdcfc030aaa24bdbbd95c8114c9f5ad2abd4641bd1
c1ccc(-c2cc3ccccc3o2)cc1
[C:1]-[C:2]1-[CH2;D2;+0:3]-[O;H0;D2;+0:4]-1.[OH;D1;+0:5]-[c:6](:[c:7]):[c:8]>>[C:1]-[C:2](-[OH;D1;+0:4])-[CH2;D2;+0:3]-[O;H0;D2;+0:5]-[c:6](:[c:7]):[c:8]
null
[]
200
CELSIUS
null
null
The ester which results from the condensation of 2'-hydroxyacetophenone and m-anisic acid is converted to 2-(3-methoxyphenyl)-3-methylbenzofuran by reductive cyclization in dioxane with a titanium tetrachloride/zinc metal catalyst according to the method of Banerji and Nayak, J. Chem. Soc., Chem. Comm., (1990), 150. Th...
10.6084/m9.figshare.5104873.v1
null
Ether.Aromatic alcohol
Ether.Secondary alcohol
C1CO1
null
c1ccccc1.c1ccc2occc2c1
null
CO
200
null
Cc1c(-c2cccc(O)c2)oc2ccccc12.OCC1CO1>CO>Cc1c(-c2cccc(OCC(O)CO)c2)oc2ccccc12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-19b4002a336d4a0c990cd5217402dc7e
O=S(=O)(O)CCO.OCC(O)CO.[Na]>>O=S(=O)([O-])CCOCC(O)CO.[Na+]
S(=O)(=O)(O)CCO.[Na].[OH-].[Na+].OCC(O)CO.P(=O)([O-])([O-])[O-].[K+].[K+].[K+]>>OC(COCCS(=O)(=O)[O-])CO.[Na+]
[O:1]=[S:2](=[O:3])([OH:4])[CH2:5][CH2:6][OH:7].O[CH2:8][CH:9]([OH:10])[CH2:11][OH:12].[Na:13]>>[O:1]=[S:2](=[O:3])([O-:4])[CH2:5][CH2:6][O:7][CH2:8][CH:9]([OH:10])[CH2:11][OH:12].[Na+:13]
O=S(=O)(O)CCO.OCC(O)CO.[Na]
O=S(=O)([O-])CCOCC(O)CO.[Na+]
null
null
O
Functional Group Interconversion
OtherReaction
e8fb1027e56e3c54291c20a3c526ee1e94fc86a9ca345d4e7c58af742e7a29e9
72e2e67028b40f6270954d8b22bd8a0c5a3a0929b41d153aa51c47f0d73fd934
null
O-[CH2;D2;+0:1]-[C:2](-[C:3])-[O;D1;H1:4].[Na;H0;D0;+0:5].[O;D1;H0:6]=[#16:7](=[O;D1;H0:8])(-[OH;D1;+0:9])-[C:10]-[C:11]-[OH;D1;+0:12]>>[C:3]-[C:2](-[O;D1;H1:4])-[CH2;D2;+0:1]-[O;H0;D2;+0:12]-[C:11]-[C:10]-[#16:7](-[O-;H0;D1:9])(=[O;D1;H0:6])=[O;D1;H0:8].[Na+;H0;D0:5]
null
[]
200
CELSIUS
null
null
To a 500 mL, three neck, round bottom flask equipped with a magnetic stirring bar, modified Claisen head, condenser (set for distillation), thermometer, and temperature controller (Therm-O-Watch®, I2R) was added isethionic acid, sodium salt (Aldrich, 50.0 gm, 0.338 mol), sodium hydroxide (2.7 g, 0.0675 mol), and glycer...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Primary alcohol
Ether
null
null
null
HO-
O
200
null
O=S(=O)(O)CCO.OCC(O)CO.[Na]>O>O=S(=O)([O-])CCOCC(O)CO.[Na+]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-929810e1bbe644d497f54844a1a40378
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O>>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]32)C1
C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC=C4[C@@]3(CC[C@@H](C4)O)C.N1=CC=CC=C1.O>>C(C)(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@]2(CC1)C)=O
[OH:4][C@H:5]1[CH2:6][CH2:7][C@@:8]2([CH3:9])[C:10](=[CH:11][CH2:12][C@@H:13]3[C@@H:14]2[CH2:15][CH2:16][C@:17]2([CH3:18])[C:19](=[O:20])[CH2:21][CH2:22][C@@H:23]32)[CH2:24]1.[OH2:3]>>[CH3:1][C:2](=[O:3])[O:4][C@H:5]1[CH2:6][CH2:7][C@@:8]2([CH3:9])[C:10](=[CH:11][CH2:12][C@@H:13]3[C@@H:14]2[CH2:15][CH2:16][C@:17]2([CH3...
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O
CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]32)C1
null
null
null
Acylation
OtherReaction
959a87fd7ff99d445b5957c6cdcb595e35c7aeec865dcf9e1912a4cdfcb738f9
37f9d0c402085ae7a53dbce85561bce6850cbef4177e39b629509223b5de2bec
O=C1CC[C@@H]2C1CC[C@@H]1C3CCCCC3=CC[C@@H]21
[C:1]=[C:2]-[C:3]-[C:4](-[OH;D1;+0:5])-[C:6].[OH2;D0;+0:7]>>[C:1]=[C:2]-[C:3]-[C:4](-[O;H0;D2;+0:5]-[C:8](-[C;D1;H3:9])=[O;H0;D1;+0:7])-[C:6]
null
[]
null
null
16
HOUR
Dehydroepiandrosterone (2.88 g, 10 mmol) is dissolved in a mixture (100 ml) of anhydride acetic and pyridine (1:1 v/v) and left at room temperature for 16 h. The mixture is then poured carefully into iced water and after 16 h, crystals are filtered and dried in vacuo. Conditions: See reaction.notes.procedure_details. W...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Ester
null
null
C1=C2CCCC[C@@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
Other
null
null
16
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O>>CC(=O)O[C@H]1CC[C@@]2(C)C(=CC[C@@H]3[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]32)C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1079585e7a194106a0429ed7ca89727f
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O=C(Cl)OCc1ccccc1>>C[C@]12CC[C@H](OC(=O)OCc3ccccc3)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC=C4[C@@]3(CC[C@@H](C4)O)C.C(C1=CC=CC=C1)OC(=O)Cl>>C(C1=CC=CC=C1)OC(=O)O[C@@H]1CC2=CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@]2(CC1)C)=O
[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]([OH:6])[CH2:17][C:18]1=[CH:19][CH2:20][C@@H:21]1[C@@H:22]2[CH2:23][CH2:24][C@:25]2([CH3:26])[C:27](=[O:28])[CH2:29][CH2:30][C@@H:31]12.Cl[C:7](=[O:8])[O:9][CH2:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][C@:2]12[CH2:3][CH2:4][C@H:5]([O:6][C:7](=[O:8])[O:9][CH2:10][c:11]3...
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O=C(Cl)OCc1ccccc1
C[C@]12CC[C@H](OC(=O)OCc3ccccc3)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
null
null
C(Cl)Cl
Acylation
Schotten-Baumann to ester
16a18aa130cea39a3a662ee8b6057b54f71a5546be78b0c40ff9ad2c1213d664
75f277925c316017cfa5d00758bde92cc568ffecb2651aae6fab24b6daa74c11
O=C(OCc1ccccc1)O[C@H]1CCC2C(=CC[C@H]3[C@@H]4CCC(=O)C4CC[C@H]23)C1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[C:5]=[C:6]-[C:7]-[C:8](-[OH;D1;+0:9])-[C:10]>>[C:4]-[#8:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:9]-[C:8](-[C:10])-[C:7]-[C:6]=[C:5]
null
[]
null
null
30
MINUTE
To a stirred solution of dehydroepiandrosterone (2.88 % 10 mmol) in methylene chloride (100 mL) is added dropwise benzylchloroformate, over a period of 30 min following the known procedure (F. Reber and T. Reichstein, Helv. Chim. Acta, 28, 1164, 1945). After stirring for 3 h, the mixture is washed with water and evapor...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Secondary alcohol
Carbonic Ester
null
null
c1ccccc1.C1=C2CCCC[C@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
HCl
C(Cl)Cl
null
0.5
C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12.O=C(Cl)OCc1ccccc1>C(Cl)Cl>C[C@]12CC[C@H](OC(=O)OCc3ccccc3)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6642d755fcb048beb2e3a7e3e3b838c6
C=O.CC(=O)OCCl.C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12>>CC(=O)O.C[C@]12CC[C@H](OCO)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
C(C)(=O)OCCl.C(C)(=O)Cl.C=O.C[C@]12CC[C@H]3[C@H]([C@@H]1CCC2=O)CC=C4[C@@]3(CC[C@@H](C4)O)C.[H-].[Na+].[H-].[Na+]>>C(C)(=O)O.OCO[C@@H]1CC2=CC[C@H]3[C@@H]4CCC([C@@]4(C)CC[C@@H]3[C@]2(CC1)C)=O
[CH2:11]=[O:12].ClC[O:4][C:2]([CH3:1])=[O:3].[CH3:5][C@:6]12[CH2:7][CH2:8][C@H:9]([OH:10])[CH2:13][C:14]1=[CH:15][CH2:16][C@@H:17]1[C@@H:18]2[CH2:19][CH2:20][C@:21]2([CH3:22])[C:23](=[O:24])[CH2:25][CH2:26][C@@H:27]12>>[CH3:1][C:2](=[O:3])[OH:4].[CH3:5][C@:6]12[CH2:7][CH2:8][C@H:9]([O:10][CH2:11][OH:12])[CH2:13][C:14]1...
C=O.CC(=O)OCCl.C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
CC(=O)O.C[C@]12CC[C@H](OCO)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
null
[Cl-].[Cl-].[Zn+2]
C1CCOC1.O
Heteroatom Alkylation and Arylation
OtherReaction
1a9395c10ca76090517f98be345a719f76251743a8a92b7bc57bfb61a8b1655b
7e58f7e56164cfb063118065627b0f677475303dc2b8ba84dacb11f878913aed
O=C1CC[C@@H]2C1CC[C@@H]1C3CCCCC3=CC[C@@H]21
Cl-C-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].[CH2;D1;+0:5]=[O;H0;D1;+0:6].[C:7]=[C:8]-[C:9]-[C:10](-[OH;D1;+0:11])-[C:12]>>[C;D1;H3:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1].[C:7]=[C:8]-[C:9]-[C:10](-[O;H0;D2;+0:11]-[CH2;D2;+0:5]-[OH;D1;+0:6])-[C:12]
null
[]
null
null
null
null
To a solution of dehydroepiandrosterone (2.88 g, 10 mmol) in THF (100 mL) is added sodium hydride (11 mmol, 60% in oil) at room temperature under an argon atmosphere. When all the sodium hydride has reacted, chloromethyl acetate (prepared from acetyl chloride and formaldehyde (or derivative) using ZnCl2 as catalyst) is...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Formaldehyde.Ester.Secondary alcohol
Carboxylic acid.Ether.Primary alcohol
null
null
C1=C2CCCC[C@H]2[C@H]2CC[C@@H]3CCC[C@H]3[C@@H]2C1
HCl
[Cl-].[Cl-].[Zn+2].C1CCOC1.O
null
null
C=O.CC(=O)OCCl.C[C@]12CC[C@H](O)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12>[Cl-].[Cl-].[Zn+2].C1CCOC1.O>CC(=O)O.C[C@]12CC[C@H](OCO)CC1=CC[C@@H]1[C@@H]2CC[C@]2(C)C(=O)CC[C@@H]12
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-126b62e8f9c14b19bd96ee46b744d0b7
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
CN1C(=O)N(C=2N=CNC2C1=O)C.ClCCCCP(OCC)(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>CN1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C
Cl[CH2:9][CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:23][CH2:24][CH3:25].[nH:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH3:18])[c:19](=[O:20])[n:21]2[CH3:22]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH3:18])[c:19](=[...
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O
CCOP(=O)(CCCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[nH;D2;+0:12]:[c:13]:2:[c:14]:1=[O;D1;H0:15]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9]2:[#7;a:7](-[C;D1;H3:8]):[c:6]:[#7;a:5](-[C;D1;H3:4]):[c:14](=[O;D1;H0:15]):[c:13]:2:1
null
[]
70
CELSIUS
null
null
10.9 g (0.05 mol) of 1,3-dimethylxanthine were suspended in 150 ml of DMF, treated with 13.7 g (0.06 mol) of diethyl 4-chlorobutanephosphonate and 7.0 g (0.05 mol) of activated potassium carbonate and heated at 70° C. for approximately 4 hours. The solid was then filtered off, the filtrate was concentrated under reduce...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HCl
CN(C)C=O
70
null
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O>CN(C)C=O>CCOP(=O)(CCCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0e2048f259f14c369c409d485f3d1e95
BrCCCBr.CCBr.CCOP(OCC)OCC>>CCOP(=O)(CCCBr)OCC
BrCCCBr.P(OCC)(OCC)OCC.BrCC>>BrCCCP(OCC)(=O)OCC
Br[CH2:6][CH2:7][CH2:8][Br:9].Br[CH2:2][CH3:1].CC[O:3][P:4]([O:5]CC)[O:10][CH2:11][CH3:12]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][Br:9])[O:10][CH2:11][CH3:12]
BrCCCBr.CCBr.CCOP(OCC)OCC
CCOP(=O)(CCCBr)OCC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
e746a4bbdeb1bd93cf6f9b604439d9c6c63bcf906752fdb4eb1d1aaca7f7c595
1bf8450aa85de8176950624f95531e53b97b1bac759bf7a1510546cbfef8b9d1
null
Br-[CH2;D2;+0:1]-[C;D1;H3:2].Br-[CH2;D2;+0:3]-[C:4]-[C:5].C-C-[O;H0;D2;+0:6]-[P;H0;D3;+0:7](-[#8:8]-[C:9])-[O;H0;D2;+0:10]-C-C>>[C:9]-[#8:8]-[P;H0;D4;+0:7](=[O;H0;D1;+0:10])(-[CH2;D2;+0:3]-[C:4]-[C:5])-[O;H0;D2;+0:6]-[CH2;D2;+0:1]-[C;D1;H3:2]
null
[]
130
CELSIUS
null
null
A mixture of 605 g (3.0 mol) of 1,3-dibromopropane and 250 g (1.5 mol) of triethyl phosphite was heated at an oil bath temperature of 130° C., while stirring and passing in nitrogen, for approximately 5 hours until approximately 154 g (1.5 mol) of bromoethane distilled over into a strongly ice-cooled receiver. The reac...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide
null
null
null
null
HBr
null
130
null
BrCCCBr.CCBr.CCOP(OCC)OCC>>CCOP(=O)(CCCBr)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d7d7141538f0422c85b05b45f2b6979e
CCOCOCC.Cn1c(=O)[nH]c(=O)c2[nH]cnc21>>CCOCn1cnc2c1c(=O)[nH]c(=O)n2C
CN1C(NC(C=2NC=NC12)=O)=O.C(C)OCOCC.C1(=CC=C(C=C1)S(=O)(=O)Cl)C.C(C)(=O)[O-].[Na+]>>C(C)OCN1C=NC=2N(C(NC(C12)=O)=O)C
CCO[CH2:4][O:3][CH2:2][CH3:1].[nH:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[nH:12][c:13](=[O:14])[n:15]2[CH3:16]>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[nH:12][c:13](=[O:14])[n:15]2[CH3:16]
CCOCOCC.Cn1c(=O)[nH]c(=O)c2[nH]cnc21
CCOCn1cnc2c1c(=O)[nH]c(=O)n2C
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
82589f00df7347b300983ffcf7e3ab490c8226c85728ef746198e8f397b81806
ccc058ecd89f692c39a92bd6db91fb86578428d38b5955a659e0a2343eccf0fd
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
C-C-O-[CH2;D2;+0:1]-[#8:2]-[C:3].[C;D1;H3:4]-[#7;a:5]1:[c:6]:[#7;a:7]:[c:8](=[O;D1;H0:9]):[c:10]2:[nH;D2;+0:11]:[c:12]:[#7;a:13]:[c:14]:1:2>>[C:3]-[#8:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:11]1:[c:12]:[#7;a:13]:[c:14]2:[#7;a:5](-[C;D1;H3:4]):[c:6]:[#7;a:7]:[c:8](=[O;D1;H0:9]):[c:10]:2:1
null
[]
90
CELSIUS
null
null
52.5 g (0.28 mol) of p-toluenesulfonyl chloride were initially introduced into 50 ml of dimethylformamide and 22.6 g (0.29 mol) of sodium acetate were introduced with stirring and ice-cooling. The mixture was subsequently stirred for one hour, treated with 39.1 g of formaldehyde diethyl acetal and again subsequently st...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether
Ether
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HO-
CN(C=O)C
90
null
CCOCOCC.Cn1c(=O)[nH]c(=O)c2[nH]cnc21>CN(C=O)C>CCOCn1cnc2c1c(=O)[nH]c(=O)n2C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d7603175462343e28fe8ca12d8b33976
BrCc1ccccc1.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C>>CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C
C(C1=CC=CC=C1)Br.C(C)OCN1C=NC=2N(C(NC(C12)=O)=O)C.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)N1C(=O)N(C=2N=CN(C2C1=O)COCC)C
Br[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[CH3:1][CH2:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[nH:12][c:20](=[O:21])[n:22]2[CH3:23]>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[n:12]([CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1)[c:20](=[O:21])[n:22]2[CH3:2...
BrCc1ccccc1.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C
CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c2nc[nH]c2c(=O)n1Cc1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[#7;a:6]1:[c:7]:[#7;a:8]:[c:9]2:[#7;a:10](-[C;D1;H3:11]):[c:12](=[O;D1;H0:13]):[nH;D2;+0:14]:[c:15](=[O;D1;H0:16]):[c:17]:1:2>>[C:5]-[#7;a:6]1:[c:7]:[#7;a:8]:[c:9]2:[#7;a:10](-[C;D1;H3:11]):[c:12](=[O;D1;H0:13]):[n;H0;D3;+0:14](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:15](=[O;D1...
null
[]
90
CELSIUS
8
HOUR
205 g (1.2 mol) of benzyl bromide were added to a suspension of 224 g (1 mol) of 7-ethoxymethyl-3-methylxanthine and 165 g of potassium carbonate in 1000 ml of dimethylformamide and the mixture was then stirred overnight at 90° C. The reaction solution was filtered hot, the filtrate was concentrated under reduced press...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1.c1ccccc1
HBr
CN(C=O)C
90
8
BrCc1ccccc1.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C>CN(C=O)C>CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a7e91768d4c487cad45cb6ac939a6f7
CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C>>Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21
C(C1=CC=CC=C1)N1C(=O)N(C=2N=CN(C2C1=O)COCC)C.Cl>>Cl.C(C1=CC=CC=C1)N1C(=O)N(C=2N=CNC2C1=O)C
CCOC[n:17]1[c:16]2[c:14](=[O:15])[n:6]([CH2:7][c:8]3[cH:9][cH:10][cH:11][cH:12][cH:13]3)[c:4](=[O:5])[n:3]([CH3:2])[c:20]2[n:19][cH:18]1>>[CH3:2][n:3]1[c:4](=[O:5])[n:6]([CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)[c:14](=[O:15])[c:16]2[nH:17][cH:18][n:19][c:20]12
CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C
Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21
null
null
null
Reduction
OtherReaction
8d95695d3b7944b0963f4887dc50bd8cf245d5b3d94bbee056f9862d4eeae931
84394d34c591024a84d9393eb3e8adb8ada5a6225c3abafc4dae9aedd4568be4
O=c1[nH]c2nc[nH]c2c(=O)n1Cc1ccccc1
C-C-O-C-[n;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4]2:[#7;a:5](-[C;D1;H3:6]):[c:7]:[#7;a:8](-[C:9]):[c:10](=[O;D1;H0:11]):[c:12]:2:1>>[C:9]-[#7;a:8]1:[c:7]:[#7;a:5](-[C;D1;H3:6]):[c:4]2:[#7;a:3]:[c:2]:[nH;D2;+0:1]:[c:12]:2:[c:10]:1=[O;D1;H0:11]
null
[]
60
CELSIUS
6
HOUR
The unpurified 1-benzyl-7-ethoxymethyl-3-methylxanthine was treated with 1000 ml of 5N hydrochloric acid and stirred at 60° C. for 6 hours. The precipitated solid was filtered off with suction, washed with ethanol and dried under reduced pressure (164 g). It was possible from the mother liquor, after concentrating to a...
10.6084/m9.figshare.5104873.v1
null
Ether
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ccccc1.c1ncc2[nH]cnc2n1
HO-
null
60
6
CCOCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C>>Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1b88eb8cb6094a9a8d87846b4529cb21
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC
Cl.C(C1=CC=CC=C1)N1C(=O)N(C=2N=CNC2C1=O)C.ClCCCCP(OCC)(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)N1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C
Cl[CH2:9][CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:29][CH2:30][CH3:31].[nH:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH2:18][c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1)[c:25](=[O:26])[n:27]2[CH3:28]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:1...
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21
CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c2nc[nH]c2c(=O)n1Cc1ccccc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[nH;D2;+0:12]:[c:13]:2:[c:14]:1=[O;D1;H0:15]>>[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[n;H0;D3;+0:12](-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:13]:2:[c:14]:1=[O;D1;H0:15]
null
[]
70
CELSIUS
6
HOUR
20 g (0.078 mol) of 1-benzyl-3-methylxanthine hydrochloride, 21.4 g (0.094 mol) of diethyl 4-chlorobutanephosphonate and 26 g (0.2 mol) of potassium carbonate were suspended in 400 ml of dimethylformamide and stirred at 70° C. for 6 hours. The solution was filtered hot and the dimethylformamide was evaporated under red...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1.c1ccccc1
HCl
CN(C=O)C
70
6
CCOP(=O)(CCCCCl)OCC.Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21>CN(C=O)C>CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7770e21bea004978a0779f7b92547672
CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC>>CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC
C(C1=CC=CC=C1)N1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C.N>>CN1C(NC(C=2N(C=NC12)CCCCP(OCC)(OCC)=O)=O)=O
c1ccc(C[n:17]2[c:15](=[O:16])[c:14]3[n:10]([CH2:9][CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:22][CH2:23][CH3:24])[cH:11][n:12][c:13]3[n:20]([CH3:21])[c:18]2=[O:19])cc1>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[nH:17][c:18](=[O:19])[n:2...
CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC
CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC
null
[Pd]
C(C)O
Deprotection
OtherReaction
3d9a5ab3644944bc89314c4573926012058c142eafe4129eb62ce309eab26216
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
[C:1]-[#7;a:2]1:[c:3]:[#7;a:4]:[c:5]2:[#7;a:6](-[C;D1;H3:7]):[c:8](=[O;D1;H0:9]):[n;H0;D3;+0:10](-C-c3:c:c:c:c:c:3):[c:11](=[O;D1;H0:12]):[c:13]:1:2>>[C:1]-[#7;a:2]1:[c:3]:[#7;a:4]:[c:5]2:[#7;a:6](-[C;D1;H3:7]):[c:8](=[O;D1;H0:9]):[nH;D2;+0:10]:[c:11](=[O;D1;H0:12]):[c:13]:1:2
null
[]
null
null
48
HOUR
13 g (0.03 mol) of diethyl [4-(1-benzyl-3-methylxanthin-7-yl)-butyl]phosphonate were suspended in 150 ml of ethanol with 2 g of palladium on activated carbon (10%) and, after addition of 3 ml of concentrated ammonia solution, hydrogenated with shaking at 1.5 bar in the course of 48 hours. The catalyst was filtered off,...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1.c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
Other
[Pd].C(C)O
null
48
CCOP(=O)(CCCCn1cnc2c1c(=O)n(Cc1ccccc1)c(=O)n2C)OCC>[Pd].C(C)O>CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-841b9089cd1f4520ba61b48f730e5eeb
CCI.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C>>CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C
C(C)OCN1C=NC=2N(C(NC(C12)=O)=O)C.C(C)I.C([O-])([O-])=O.[K+].[K+]>>C(C)OCN1C=NC=2N(C(N(C(C12)=O)CC)=O)C
I[CH2:13][CH3:14].[CH3:1][CH2:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[nH:12][c:15](=[O:16])[n:17]2[CH3:18]>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[cH:6][n:7][c:8]2[c:9]1[c:10](=[O:11])[n:12]([CH2:13][CH3:14])[c:15](=[O:16])[n:17]2[CH3:18]
CCI.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C
CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
I-[CH2;D2;+0:1]-[C;D1;H3:2].[C:3]-[#7;a:4]1:[c:5]:[#7;a:6]:[c:7]2:[#7;a:8](-[C;D1;H3:9]):[c:10](=[O;D1;H0:11]):[nH;D2;+0:12]:[c:13](=[O;D1;H0:14]):[c:15]:1:2>>[C:3]-[#7;a:4]1:[c:5]:[#7;a:6]:[c:7]2:[#7;a:8](-[C;D1;H3:9]):[c:10](=[O;D1;H0:11]):[n;H0;D3;+0:12](-[CH2;D2;+0:1]-[C;D1;H3:2]):[c:13](=[O;D1;H0:14]):[c:15]:1:2
null
[]
70
CELSIUS
5
HOUR
30 g (0.134 mol) of 7-ethoxymethyl-3-methylxanthine were suspended in 500 ml of absolute DMF with 25 g (0.161 mol) of ethyl iodide and 22.2 g (0.161 mol) of potassium carbonate and the mixture was stirred at 70° C. for 5 hours. The solution was filtered and the residue which remained was crystallized in diisopropyl eth...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HI
CN(C)C=O
70
5
CCI.CCOCn1cnc2c1c(=O)[nH]c(=O)n2C>CN(C)C=O>CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-1e4a1fe78dd64b49acf4eb3616e08f35
CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C>>CCn1c(=O)c2[nH]cnc2n(C)c1=O
C(C)OCN1C=NC=2N(C(N(C(C12)=O)CC)=O)C.Cl>>C(C)N1C(=O)N(C=2N=CNC2C1=O)C
CCOC[n:7]1[c:6]2[c:4](=[O:5])[n:3]([CH2:2][CH3:1])[c:13](=[O:14])[n:11]([CH3:12])[c:10]2[n:9][cH:8]1>>[CH3:1][CH2:2][n:3]1[c:4](=[O:5])[c:6]2[nH:7][cH:8][n:9][c:10]2[n:11]([CH3:12])[c:13]1=[O:14]
CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C
CCn1c(=O)c2[nH]cnc2n(C)c1=O
null
null
C(C)O
Reduction
OtherReaction
8d95695d3b7944b0963f4887dc50bd8cf245d5b3d94bbee056f9862d4eeae931
84394d34c591024a84d9393eb3e8adb8ada5a6225c3abafc4dae9aedd4568be4
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
C-C-O-C-[n;H0;D3;+0:1]1:[c:2]:[#7;a:3]:[c:4]2:[#7;a:5](-[C;D1;H3:6]):[c:7]:[#7;a:8](-[C:9]):[c:10](=[O;D1;H0:11]):[c:12]:2:1>>[C:9]-[#7;a:8]1:[c:7]:[#7;a:5](-[C;D1;H3:6]):[c:4]2:[#7;a:3]:[c:2]:[nH;D2;+0:1]:[c:12]:2:[c:10]:1=[O;D1;H0:11]
null
[]
null
null
null
null
28.7 g (0.11 mol) of 7-ethoxymethyl-1-ethyl-3-methylxanthine were stirred at 60° C. for 60 hours in a solution of 200 ml of 5N hydrochloric acid and 200 ml of ethanol. The reaction mixture was concentrated to dryness and the residue which remained was crystallized in ethyl acetate/diisopropyl ether. Conditions: See rea...
10.6084/m9.figshare.5104873.v1
null
Ether
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HO-
C(C)O
null
null
CCOCn1cnc2c1c(=O)n(CC)c(=O)n2C>C(C)O>CCn1c(=O)c2[nH]cnc2n(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-66898f10be454898bdbc10dabbccc95a
CCCC(Cl)P(=O)(OCC)OCC.CCn1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(CC)c(=O)n2C)OCC
C(C)N1C(=O)N(C=2N=CNC2C1=O)C.ClC(CCC)P(OCC)(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>C(C)N1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C
Cl[CH:6]([P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:24][CH2:25][CH3:26])[CH2:7][CH2:8][CH3:9].[nH:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH2:18][CH3:19])[c:20](=[O:21])[n:22]2[CH3:23]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH2:18][...
CCCC(Cl)P(=O)(OCC)OCC.CCn1c(=O)c2[nH]cnc2n(C)c1=O
CCOP(=O)(CCCCn1cnc2c1c(=O)n(CC)c(=O)n2C)OCC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
d2d10e0bf3282dbee093e452ce5b563e0a690db4b22dcbf64e79bd3aa60743f8
3456c966f3f7e7d410f206842ab08ae4d1cfab4368ca2a0de7a6ad251462e6f4
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH;D3;+0:1](-[C:2]-[C:3]-[CH3;D1;+0:4])-[#15:5](-[#8:6])(-[#8:7])=[O;D1;H0:8].[C:9]-[#7;a:10]1:[c:11]:[#7;a:12](-[C;D1;H3:13]):[c:14]2:[#7;a:15]:[c:16]:[nH;D2;+0:17]:[c:18]:2:[c:19]:1=[O;D1;H0:20]>>[#8:6]-[#15:5](-[#8:7])(=[O;D1;H0:8])-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[n;H0;D3;+0:17]1:[c:16]:[#7;a:15]:[c:14]...
null
[]
null
null
null
null
9.7 g (0.05 mol) of 1-ethyl-3-methylxanthine were stirred at 70° C. for 6 hours with 12.7 g (0.06 mol) of diethyl chlorobutanephosphonate and 8.3 g of potassium carbonate. The solution was filtered, the solvent was evaporated, and the residue which remained was chromatographed (eluent: ethyl acetate/methanol 10: 1) and...
10.6084/m9.figshare.5104873.v1
null
Secondary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HCl
null
null
null
CCCC(Cl)P(=O)(OCC)OCC.CCn1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(CC)c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2b41b35df72e44c4adc18e6e041d2837
ClCc1ccccc1.Cn1c(=O)[nH]c(=O)c2[nH]cnc21>>Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1
C(C1=CC=CC=C1)Cl.[H-].[Na+].CN1C(NC(C=2NC=NC12)=O)=O.[H][H]>>C(C1=CC=CC=C1)N1C=NC=2N(C(NC(C12)=O)=O)C
Cl[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[CH3:1][n:2]1[c:3](=[O:4])[nH:5][c:6](=[O:7])[c:8]2[c:9]1[n:10][cH:11][nH:12]2>>[CH3:1][n:2]1[c:3](=[O:4])[nH:5][c:6](=[O:7])[c:8]2[c:9]1[n:10][cH:11][n:12]2[CH2:13][c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
ClCc1ccccc1.Cn1c(=O)[nH]c(=O)c2[nH]cnc21
Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1
null
null
CN(C=O)C.O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2c(ncn2Cc2ccccc2)[nH]1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[#7;a:6]1:[c:7]:[#7;a:8]:[c:9](=[O;D1;H0:10]):[c:11]2:[nH;D2;+0:12]:[c:13]:[#7;a:14]:[c:15]:1:2>>[C;D1;H3:5]-[#7;a:6]1:[c:7]:[#7;a:8]:[c:9](=[O;D1;H0:10]):[c:11]2:[c:15]:1:[#7;a:14]:[c:13]:[n;H0;D3;+0:12]:2-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
100
CELSIUS
1
HOUR
16.8 g (0.7 mol) of sodium hydride were introduced in portions with stirring into a suspension of 99.6 g (0.6 mol) of 3-methylxanthine in 1.5 l of dimethylformamide. After evolution of hydrogen had ended, the mixture was heated to 100° C., treated dropwise with 76 g (0.6 mol) of benzyl chloride and heated at 120° C. fo...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1.c1ccccc1
HCl
CN(C=O)C.O
100
1
ClCc1ccccc1.Cn1c(=O)[nH]c(=O)c2[nH]cnc21>CN(C=O)C.O>Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eadaded2a68a4a4683c2b0691e2f1aa0
CCOCCl.Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1>>CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O
C(C1=CC=CC=C1)N1C=NC=2N(C(NC(C12)=O)=O)C.C(C)OCCl.C([O-])([O-])=O.[K+].[K+]>>C(C1=CC=CC=C1)N1C=NC=2N(C(N(C(C12)=O)COCC)=O)C
Cl[CH2:4][O:3][CH2:2][CH3:1].[nH:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][n:12]2[CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[n:20]([CH3:21])[c:22]1=[O:23]>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][n:12]2[CH2:13][c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[n:20]([CH3:21])[c:22]1=[O...
CCOCCl.Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1
CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
f1a41fa8f82aa77600cb200025b462ea732d1b9362867647d4b1c004bfdafb56
969a4609e178674696657c590a647839ca01abd1f90b8f0c9e475b1d6507651b
O=c1[nH]c(=O)c2c(ncn2Cc2ccccc2)[nH]1
Cl-[CH2;D2;+0:1]-[#8:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7]:[c:8]2:[#7;a:9](-[C;D1;H3:10]):[c:11](=[O;D1;H0:12]):[nH;D2;+0:13]:[c:14](=[O;D1;H0:15]):[c:16]:1:2>>[C:4]-[#7;a:5]1:[c:6]:[#7;a:7]:[c:8]2:[#7;a:9](-[C;D1;H3:10]):[c:11](=[O;D1;H0:12]):[n;H0;D3;+0:13](-[CH2;D2;+0:1]-[#8:2]-[C:3]):[c:14](=[O;D1;H0:15]):[c:16]:...
null
[]
null
null
null
null
20 g (0.078 mol) of 7-benzyl-3-methylxanthine were stirred at 80° C. for 6 hours with 8.8 g (0.094 mol) of ethoxymethyl chloride and 13 g of potassium carbonate in 500 ml of absolute dimethylformamide, the mixture was filtered and concentrated, and the residue which remained was chromatographed (eluent: dichloromethane...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1.c1ccccc1
HCl
CN(C=O)C
null
null
CCOCCl.Cn1c(=O)[nH]c(=O)c2c1ncn2Cc1ccccc1>CN(C=O)C>CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8274ed2fb34e4d4d9f44b77cbe179a49
CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O>>CCOCn1c(=O)c2[nH]cnc2n(C)c1=O
C(C1=CC=CC=C1)N1C=NC=2N(C(N(C(C12)=O)COCC)=O)C>>C(C)OCN1C(=O)N(C=2N=CNC2C1=O)C
c1ccc(C[n:9]2[c:8]3[c:6](=[O:7])[n:5]([CH2:4][O:3][CH2:2][CH3:1])[c:15](=[O:16])[n:13]([CH3:14])[c:12]3[n:11][cH:10]2)cc1>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[nH:9][cH:10][n:11][c:12]2[n:13]([CH3:14])[c:15]1=[O:16]
CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O
CCOCn1c(=O)c2[nH]cnc2n(C)c1=O
null
[Pd]
C(C)O
Deprotection
OtherReaction
3d9a5ab3644944bc89314c4573926012058c142eafe4129eb62ce309eab26216
30a26bc929988d0041b9998cdccd1d65eb125114a78065ed35d40f50c965c0a7
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
[C:1]-[#7;a:2]1:[c:3]:[#7;a:4](-[C;D1;H3:5]):[c:6]2:[#7;a:7]:[c:8]:[n;H0;D3;+0:9](-C-c3:c:c:c:c:c:3):[c:10]:2:[c:11]:1=[O;D1;H0:12]>>[C:1]-[#7;a:2]1:[c:3]:[#7;a:4](-[C;D1;H3:5]):[c:6]2:[#7;a:7]:[c:8]:[nH;D2;+0:9]:[c:10]:2:[c:11]:1=[O;D1;H0:12]
null
[]
null
null
null
null
17.5 g (0.056 mol) of 7-benzyl-1-ethoxymethyl-3-methylxanthine were hydrogenated over 1.8 g of palladium (10%) on activated carbon at room temperature for 8 hours in 500 ml of ethanol. The catalyst was filtered off and the filtrate was concentrated to dryness and crystallized from dimethylformamide/diisopropyl ether. C...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccccc1.c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
Other
[Pd].C(C)O
null
null
CCOCn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O>[Pd].C(C)O>CCOCn1c(=O)c2[nH]cnc2n(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8750cc7ad61a432da65104ddaeebb4b3
CCCC(Cl)P(=O)(OCC)OCC.CCOCn1c(=O)[nH]c2nc[nH]c2c1=O>>CCOCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O
C(C)OCN1C(=O)NC=2N=CNC2C1=O.C([O-])([O-])=O.[K+].[K+].ClC(CCC)P(OCC)(=O)OCC>>C(C)OCN1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C
Cl[CH:16]([CH2:15][CH2:14][CH3:13])[P:17](=[O:18])([O:19][CH2:20][CH3:21])[O:22][CH2:23][CH3:24].[CH3:1][CH2:2][O:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][nH:12]2)[nH:25][c:27]1=[O:28]>>[CH3:1][CH2:2][O:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][n:12]2[CH2:13][CH2:14][CH2:15][CH2:16][P:17](=[O:1...
CCCC(Cl)P(=O)(OCC)OCC.CCOCn1c(=O)[nH]c2nc[nH]c2c1=O
CCOCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
945badfe62d08793a7a77e1f7911213401b8f39f60cb6469278838440322098e
3456c966f3f7e7d410f206842ab08ae4d1cfab4368ca2a0de7a6ad251462e6f4
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH;D3;+0:1](-[C:2]-[C:3]-[CH3;D1;+0:4])-[#15:5](-[#8:6])(-[#8:7])=[O;D1;H0:8].[C:9]-[#7;a:10]1:[c:11](=[O;D1;H0:12]):[nH;D2;+0:13]:[c:14]2:[#7;a:15]:[c:16]:[nH;D2;+0:17]:[c:18]:2:[c:19]:1=[O;D1;H0:20]>>[#8:6]-[#15:5](-[#8:7])(=[O;D1;H0:8])-[CH2;D2;+0:1]-[C:2]-[C:3]-[CH2;D2;+0:4]-[n;H0;D3;+0:17]1:[c:16]:[#7;a:15]:[c...
null
[]
null
null
null
null
4 g (0.018 mol) of 1-ethoxymethylxanthine were stirred at 70° C. for 6 hours with 3 g of potassium carbonate and 4.9 g (0.0214 mol) of diethyl chlorobutanephosphonate. The solution was filtered and concentrated, and the residue which remained was chromatographed (eluent: dichloromethane/methanol 20:1). Conditions: See ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
null
null
null
null
CCCC(Cl)P(=O)(OCC)OCC.CCOCn1c(=O)[nH]c2nc[nH]c2c1=O>>CCOCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c12104568b5442eda2e049aa7fbffb8a
CCOP(=O)(CCCCCl)OCC.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC>>CCOP(=O)(CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O)OCC
C(C)OP(=O)(OCC)CCCCN1C=NC=2N(C(NC(C12)=O)=O)C.ClCCCCP(OCC)(=O)OCC.C([O-])([O-])=O.[K+].[K+]>>C(C)OP(=O)(OCC)CCCCN1C=NC=2N(C(N(C(C12)=O)CCCCP(OCC)(OCC)=O)=O)C
Cl[CH2:9][CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:34][CH2:35][CH3:36].[nH:10]1[c:11](=[O:12])[c:13]2[c:14]([n:15][cH:16][n:17]2[CH2:18][CH2:19][CH2:20][CH2:21][P:22](=[O:23])([O:24][CH2:25][CH3:26])[O:27][CH2:28][CH3:29])[n:30]([CH3:31])[c:32]1=[O:33]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH...
CCOP(=O)(CCCCCl)OCC.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC
CCOP(=O)(CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O)OCC
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7]:[c:8]2:[#7;a:9](-[C;D1;H3:10]):[c:11](=[O;D1;H0:12]):[nH;D2;+0:13]:[c:14](=[O;D1;H0:15]):[c:16]:1:2>>[C:4]-[#7;a:5]1:[c:6]:[#7;a:7]:[c:8]2:[#7;a:9](-[C;D1;H3:10]):[c:11](=[O;D1;H0:12]):[n;H0;D3;+0:13](-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:14](=[O;D1;H0:15]):[c:16]:1:...
null
[]
70
CELSIUS
null
null
8 g (0.022 mol) of 7-(4-diethylphosphonobutyl)-3-methylxanthine (according to Example 24) were suspended in 100 ml of DMF, treated with 6.13 g (0.027 mol) of diethyl 4-chlorobutanephosphonate and 3.7 g (0.028 mol) of activated potassium carbonate and heated at 70° C. for 4 hours. The product was then filtered, the filt...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HCl
CN(C)C=O
70
null
CCOP(=O)(CCCCCl)OCC.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC>CN(C)C=O>CCOP(=O)(CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(C)c1=O)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a8fa17d9b69648f1b64d1468e8fdce34
CCOP(=O)(CCCBr)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
CN1C(=O)N(C=2N=CNC2C1=O)C.BrCCCP(OCC)(=O)OCC>>CN1C(=O)N(C=2N=CN(C2C1=O)CCCP(OCC)(OCC)=O)C
Br[CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:22][CH2:23][CH3:24].[nH:9]1[cH:10][n:11][c:12]2[c:13]1[c:14](=[O:15])[n:16]([CH3:17])[c:18](=[O:19])[n:20]2[CH3:21]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][n:9]1[cH:10][n:11][c:12]2[c:13]1[c:14](=[O:15])[n:16]([CH3:17])[c:18](=[O:19])[n:20]2[CH...
CCOP(=O)(CCCBr)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O
CCOP(=O)(CCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H3:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[nH;D2;+0:12]:[c:13]:2:[c:14]:1=[O;D1;H0:15]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:12]1:[c:11]:[#7;a:10]:[c:9]2:[#7;a:7](-[C;D1;H3:8]):[c:6]:[#7;a:5](-[C;D1;H3:4]):[c:14](=[O;D1;H0:15]):[c:13]:2:1
null
[]
null
null
null
null
The title substance was prepared from 1,3-dimethylxanthine and diethyl 3-bromopropanephosphonate analogously to Example 1. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HBr
null
null
null
CCOP(=O)(CCCBr)OCC.Cn1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCn1cnc2c1c(=O)n(C)c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-37d510efe3de46df8fb8264294561f22
CCCn1c(=O)c2[nH]cnc2n(CCC)c1=O.CCOP(=O)(CCCBr)OCC>>CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
C(CC)N1C(=O)N(C=2N=CNC2C1=O)CCC.BrCCCP(OCC)(=O)OCC>>C(CC)N1C(=O)N(C=2N=CN(C2C1=O)CCCP(OCC)(OCC)=O)CCC
[CH3:1][CH2:2][CH2:3][n:4]1[c:5](=[O:6])[c:7]2[c:8]([n:9][cH:10][nH:11]2)[n:23]([CH2:24][CH2:25][CH3:26])[c:27]1=[O:28].Br[CH2:12][CH2:13][CH2:14][P:15](=[O:16])([O:17][CH2:18][CH3:19])[O:20][CH2:21][CH3:22]>>[CH3:1][CH2:2][CH2:3][n:4]1[c:5](=[O:6])[c:7]2[c:8]([n:9][cH:10][n:11]2[CH2:12][CH2:13][CH2:14][P:15](=[O:16])(...
CCCn1c(=O)c2[nH]cnc2n(CCC)c1=O.CCOP(=O)(CCCBr)OCC
CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]2:[nH;D2;+0:12]:[c:13]:[#7;a:14]:[c:15]:1:2>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:12]1:[c:13]:[#7;a:14]:[c:15]2:[#7;a:5](-[C:4]):[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]:2:1
null
[]
null
null
null
null
The title substance was prepared from 1,3-dipropylxanthine and diethyl 3-bromopropanephosphonate analogously to Example 1 and chromatographed on silica gel (eluent: ethyl acetate/methanol 20:1). Conditions: See reaction.notes.procedure_details. Workup: chromatographed on silica gel (eluent: ethyl acetate/methanol 20:1)
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HBr
null
null
null
CCCn1c(=O)c2[nH]cnc2n(CCC)c1=O.CCOP(=O)(CCCBr)OCC>>CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8d917ed641af4aa08c8cf5aa6c47bd70
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCBr)OCC>>CCCCn1c(=O)c2c(ncn2CCCCCP(=O)(OCC)OCC)n(CCCC)c1=O
C(CCC)N1C(=O)N(C=2N=CNC2C1=O)CCCC.BrCCCCCP(OCC)(=O)OCC>>C(CCC)N1C(=O)N(C=2N=CN(C2C1=O)CCCCCP(OCC)(OCC)=O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][nH:12]2)[n:26]([CH2:27][CH2:28][CH2:29][CH3:30])[c:31]1=[O:32].Br[CH2:13][CH2:14][CH2:15][CH2:16][CH2:17][P:18](=[O:19])([O:20][CH2:21][CH3:22])[O:23][CH2:24][CH3:25]>>[CH3:1][CH2:2][CH2:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][n:12]2...
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCBr)OCC
CCCCn1c(=O)c2c(ncn2CCCCCP(=O)(OCC)OCC)n(CCCC)c1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]2:[nH;D2;+0:12]:[c:13]:[#7;a:14]:[c:15]:1:2>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:12]1:[c:13]:[#7;a:14]:[c:15]2:[#7;a:5](-[C:4]):[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]:2:1
null
[]
null
null
null
null
The title substance was prepared from 1,3-dibutylxanthine and diethyl 5-bromopentanephosphonate analogously to Example 9. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HBr
null
null
null
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCBr)OCC>>CCCCn1c(=O)c2c(ncn2CCCCCP(=O)(OCC)OCC)n(CCCC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-02d09630ce874394bc3b749bf3745493
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCl)OCC>>CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(CCCC)c1=O
C(CCC)N1C(=O)N(C=2N=CNC2C1=O)CCCC.ClCCCCP(OCC)(=O)OCC>>C(CCC)N1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)CCCC
[CH3:1][CH2:2][CH2:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][nH:12]2)[n:25]([CH2:26][CH2:27][CH2:28][CH3:29])[c:30]1=[O:31].Cl[CH2:13][CH2:14][CH2:15][CH2:16][P:17](=[O:18])([O:19][CH2:20][CH3:21])[O:22][CH2:23][CH3:24]>>[CH3:1][CH2:2][CH2:3][CH2:4][n:5]1[c:6](=[O:7])[c:8]2[c:9]([n:10][cH:11][n:12]2[CH2:13]...
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCl)OCC
CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(CCCC)c1=O
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]2:[nH;D2;+0:12]:[c:13]:[#7;a:14]:[c:15]:1:2>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:12]1:[c:13]:[#7;a:14]:[c:15]2:[#7;a:5](-[C:4]):[c:6]:[#7;a:7](-[C:8]):[c:9](=[O;D1;H0:10]):[c:11]:2:1
null
[]
null
null
null
null
The title substance was prepared from 1,3-dibutylxanthine and diethyl 4-chlorobutanephosphonate analogously to Example 9. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HCl
null
null
null
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCCCl)OCC>>CCCCn1c(=O)c2c(ncn2CCCCP(=O)(OCC)OCC)n(CCCC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aa87420356fe4ddca1dff1d5942c9cf8
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCBr)OCC>>CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
C(CCC)N1C(=O)N(C=2N=CNC2C1=O)CCCC.BrCCCP(OCC)(=O)OCC>>C(CC)N1C(=O)N(C=2N=CN(C2C1=O)CCCP(OCC)(OCC)=O)CCC
C[CH2:1][CH2:2][CH2:3][n:4]1[c:5](=[O:6])[c:7]2[c:8]([n:9][cH:10][nH:11]2)[n:23]([CH2:24][CH2:25][CH2:26]C)[c:27]1=[O:28].Br[CH2:12][CH2:13][CH2:14][P:15](=[O:16])([O:17][CH2:18][CH3:19])[O:20][CH2:21][CH3:22]>>[CH3:1][CH2:2][CH2:3][n:4]1[c:5](=[O:6])[c:7]2[c:8]([n:9][cH:10][n:11]2[CH2:12][CH2:13][CH2:14][P:15](=[O:16]...
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCBr)OCC
CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
453c185c7ca08f316f04eb7765c2f018ec3b56836368f5fa1ad0e7a49cf724d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].C-[CH2;D2;+0:4]-[C:5]-[C:6]-[#7;a:7]1:[c:8]:[#7;a:9](-[C:10]-[C:11]-[CH2;D2;+0:12]-C):[c:13]2:[#7;a:14]:[c:15]:[nH;D2;+0:16]:[c:17]:2:[c:18]:1=[O;D1;H0:19]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[n;H0;D3;+0:16]1:[c:15]:[#7;a:14]:[c:13]2:[#7;a:9](-[C:10]-[C:11]-[CH3;D1;+0:12]):[c:8]:[#7;a:7](-[C:6]-[C:5...
null
[]
null
null
null
null
The title substance was prepared from 1,3-dibutylxanthine and diethyl 3-bromopropanephosphonate analogously to Example 9. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
c1ncc2nc[nH]c2n1
HBr
null
null
null
CCCCn1c(=O)c2[nH]cnc2n(CCCC)c1=O.CCOP(=O)(CCCBr)OCC>>CCCn1c(=O)c2c(ncn2CCCP(=O)(OCC)OCC)n(CCC)c1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7fae1dd89d25493ea4ac31663986c9df
CCOP(=O)(CCCCCl)OCC.COC(C)n1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(C(C)OC)c(=O)n2C)OCC
COC(C)N1C(=O)N(C=2N=CNC2C1=O)C.ClCCCCP(OCC)(=O)OCC>>COC(C)N1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C
Cl[CH2:9][CH2:8][CH2:7][CH2:6][P:4]([O:3][CH2:2][CH3:1])(=[O:5])[O:26][CH2:27][CH3:28].[nH:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n:17]([CH:18]([CH3:19])[O:20][CH3:21])[c:22](=[O:23])[n:24]2[CH3:25]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[n...
CCOP(=O)(CCCCCl)OCC.COC(C)n1c(=O)c2[nH]cnc2n(C)c1=O
CCOP(=O)(CCCCn1cnc2c1c(=O)n(C(C)OC)c(=O)n2C)OCC
null
null
null
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[nH;D2;+0:12]:[c:13]:2:[c:14]:1=[O;D1;H0:15]>>[C:4]-[#7;a:5]1:[c:6]:[#7;a:7](-[C;D1;H3:8]):[c:9]2:[#7;a:10]:[c:11]:[n;H0;D3;+0:12](-[CH2;D2;+0:1]-[C:2]-[C:3]):[c:13]:2:[c:14]:1=[O;D1;H0:15]
null
[]
null
null
null
null
The title substance was prepared from 1-methoxyethyl-3-methylxanthine and diethyl 4-chlorobutanephosphonate analogously to Example 4 and crystallized from diisopropyl ether. Conditions: See reaction.notes.procedure_details. Workup: crystallized from diisopropyl ether
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HCl
null
null
null
CCOP(=O)(CCCCCl)OCC.COC(C)n1c(=O)c2[nH]cnc2n(C)c1=O>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(C(C)OC)c(=O)n2C)OCC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-54829741e0d340c6aeb01d34861de329
CCC(C)CCl.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(CCC(C)C)c(=O)n2C)OCC
CN1C(NC(C=2N(C=NC12)CCCCP(OCC)(OCC)=O)=O)=O.CC(CCl)CC>>CC(CCN1C(=O)N(C=2N=CN(C2C1=O)CCCCP(OCC)(OCC)=O)C)C
Cl[CH2:19][CH:20]([CH2:21][CH3:18])[CH3:22].[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[O:16])[nH:17][c:23](=[O:24])[n:25]2[CH3:26])[O:27][CH2:28][CH3:29]>>[CH3:1][CH2:2][O:3][P:4](=[O:5])([CH2:6][CH2:7][CH2:8][CH2:9][n:10]1[cH:11][n:12][c:13]2[c:14]1[c:15](=[...
CCC(C)CCl.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC
CCOP(=O)(CCCCn1cnc2c1c(=O)n(CCC(C)C)c(=O)n2C)OCC
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
0a7aa46051d8e94ebdb6aa279b8d844c1e6c7142c7648fe909b83533b33d80d8
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1[nH]c(=O)c2[nH]cnc2[nH]1
Cl-[CH2;D2;+0:1]-[C:2](-[C;D1;H3:3])-[CH2;D2;+0:4]-[CH3;D1;+0:5].[C:6]-[#7;a:7]1:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11](-[C;D1;H3:12]):[c:13](=[O;D1;H0:14]):[nH;D2;+0:15]:[c:16](=[O;D1;H0:17]):[c:18]:1:2>>[C:6]-[#7;a:7]1:[c:8]:[#7;a:9]:[c:10]2:[#7;a:11](-[C;D1;H3:12]):[c:13](=[O;D1;H0:14]):[n;H0;D3;+0:15](-[CH2;D2;+0:5]-[CH2...
null
[]
null
null
null
null
The title substance was prepared from diethyl [4-(3-methylxanthin-7-yl)-butyl]phosphonate and 2-methylbutyl chloride analogously to Example 1 and chromatographed on silica gel (eluent: dichloromethane/methanol 10:1) Conditions: See reaction.notes.procedure_details. Workup: chromatographed on silica gel (eluent: dichlor...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
c1ncc2[nH]cnc2n1
HCl
null
null
null
CCC(C)CCl.CCOP(=O)(CCCCn1cnc2c1c(=O)[nH]c(=O)n2C)OCC>>CCOP(=O)(CCCCn1cnc2c1c(=O)n(CCC(C)C)c(=O)n2C)OCC