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-c34472859da14a81bfe0f74e60f15c43
ord-cb4a46d648dd4f1a83720a3d3f18dc4c
COc1c[n+]([O-])c(C)c(C)c1OC>>COc1cnc(CO)c(C)c1OC
COC1=C(C(=[N+](C=C1OC)[O-])C)C.C(C)(=O)OC(C)=O>>OCC1=NC=C(C(=C1C)OC)OC
[CH3:1][O:2][c:3]1[cH:4][n+:5]([O-:8])[c:6]([CH3:7])[c:9]([CH3:10])[c:11]1[O:12][CH3:13]>>[CH3:1][O:2][c:3]1[cH:4][n:5][c:6]([CH2:7][OH:8])[c:9]([CH3:10])[c:11]1[O:12][CH3:13]
COc1c[n+]([O-])c(C)c(C)c1OC
COc1cnc(CO)c(C)c1OC
null
null
null
Miscellaneous
OtherReaction
7e561d7afee9600ed6bdb2a097e47ef139bafb1884a12ad7f91414ba01df7b33
0607ce9ac404b7f992b14bf13602ccd36eb29bd5911f2b79cc25c0bfd203a764
c1ccncc1
[CH3;D1;+0:1]-[c:2](:[c:3]):[n+;H0;D3:4](-[O-;H0;D1:5]):[c:6]:[c:7]>>[OH;D1;+0:5]-[CH2;D2;+0:1]-[c:2](:[c:3]):[n;H0;D2;+0:4]:[c:6]:[c:7]
89
[{"value": 89.0, "product": "OCC1=NC=C(C(=C1C)OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
80
CELSIUS
2
HOUR
4.5 of 4,5-dimethoxy-2,3-dimethylpyridine 1-oxide are warmed to 110° C. in 20 ml of acetic anhydride in the course of 30 minutes and the mixture is then concentrated on a rotary evaporator. The oily residue, which consists of the intemediate 2-acetoxymethyl-4,5-dimethoxy-3-methylpyridine, is stirred in 30 ml of 3N sodi...
10.6084/m9.figshare.5104873.v1
null
null
Primary alcohol
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1
null
null
80
2
COc1c[n+]([O-])c(C)c(C)c1OC>>COc1cnc(CO)c(C)c1OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-63bcfa1627524035ab17caa52c67434b
COc1cnc(C)c(C)c1OC>>COc1c[n+]([O-])c(C)c(C)c1OC
COC1=C(C(=NC=C1OC)C)C.ClC=1C=C(C(=O)OO)C=CC1.[OH-].[Na+]>>COC1=C(C(=[N+](C=C1OC)[O-])C)C
[CH3:1][O:2][c:3]1[cH:4][n:5][c:7]([CH3:8])[c:9]([CH3:10])[c:11]1[O:12][CH3:13]>>[CH3:1][O:2][c:3]1[cH:4][n+:5]([O-:6])[c:7]([CH3:8])[c:9]([CH3:10])[c:11]1[O:12][CH3:13]
COc1cnc(C)c(C)c1OC
COc1c[n+]([O-])c(C)c(C)c1OC
null
null
C(Cl)Cl
Functional Group Interconversion
OtherReaction
54415aed4bb61f76efee9ed140374352608210a9fed7c372975c12eb7023cea2
f1bbf9aa3c82f5e49be9f6d53533b6bb152f359232b6d32090c168949766aa71
c1cc[nH+]cc1
[C;D1;H3:1]-[c:2](:[c:3]):[n;H0;D2;+0:4]:[c:5]:[c:6]>>[C;D1;H3:1]-[c:2](:[c:3]):[n+;H0;D3:4](-[O;-;D1;H0:7]):[c:5]:[c:6]
66.6
[{"value": 66.0, "product": "COC1=C(C(=[N+](C=C1OC)[O-])C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 66.6, "product": "COC1=C(C(=[N+](C=C1OC)[O-])C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
20
CELSIUS
2
HOUR
6.3 g of 4,5-dimethoxy-2,3-dimethylpyridine are dissolved in 120 ml of methylene chloride, 20 g of m-chloroperoxybenzoic acid are added successively and the mixture is stirred first at 20° C. for 2 hours and then at 40° C. for 4 hours. After addition of 20 ml of 5N sodium hydroxide solution, the mixture is washed three...
10.6084/m9.figshare.5104873.v1
null
null
null
c1ccncc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
null
C(Cl)Cl
20
2
COc1cnc(C)c(C)c1OC>C(Cl)Cl>COc1c[n+]([O-])c(C)c(C)c1OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f635efdd0db543148499f921950620e1
COc1ccnc(COC(C)=O)c1OC>>COc1ccnc(CO)c1OC
[OH-].[Na+].C(C)(=O)OCC1=NC=CC(=C1OC)OC>>OCC1=NC=CC(=C1OC)OC
CC(=O)[O:9][CH2:8][c:7]1[n:6][cH:5][cH:4][c:3]([O:2][CH3:1])[c:10]1[O:11][CH3:12]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH2:8][OH:9])[c:10]1[O:11][CH3:12]
COc1ccnc(COC(C)=O)c1OC
COc1ccnc(CO)c1OC
null
null
null
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccncc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2]-[c:3]:[#7;a:4]>>[#7;a:4]:[c:3]-[C:2]-[OH;D1;+0:1]
96
[{"value": 96.0, "product": "OCC1=NC=CC(=C1OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 93.6, "product": "OCC1=NC=CC(=C1OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
After adding 15 ml of 2N sodium hydroxide solution, 4.8 g of 2-acetoxymethyl-3,4-dimethoxypyridine are stirred vigorously at 80° C., whereupon a homogeneous solution forms from the initial two-phase mixture. After 2 hours, the solution is allowed to cool and is extracted five times with 30 ml of methylene chloride each...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccncc1
HO-
null
null
2
COc1ccnc(COC(C)=O)c1OC>>COc1ccnc(CO)c1OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c54f61d1844b40efaf008bcca8fff9bf
CC(=O)OC(C)=O.COc1cc[n+]([O-])c(C)c1OC>>COc1ccnc(COC(C)=O)c1OC
COC=1C(=[N+](C=CC1OC)[O-])C.C(C)(=O)OC(C)=O>>C(C)(=O)OCC1=NC=CC(=C1OC)OC
CC(=O)[O:9][C:10]([CH3:11])=[O:12].[O-][n+:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[c:13]([O:14][CH3:15])[c:7]1[CH3:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH2:8][O:9][C:10]([CH3:11])=[O:12])[c:13]1[O:14][CH3:15]
CC(=O)OC(C)=O.COc1cc[n+]([O-])c(C)c1OC
COc1ccnc(COC(C)=O)c1OC
null
null
null
Protection
OtherReaction
f4e85b633bf4e79d1b81c036d2f4e246a93c2eb8ec0202f93c45d73e710e4f0d
dd0b9e5a615173b1d6c9fe991a352f69d24fef80f4bf0eeab7c46667d446dcd0
c1ccncc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].[CH3;D1;+0:5]-[c:6](:[c:7]):[n+;H0;D3:8](-[O-]):[c:9]:[c:10]>>[C;D1;H3:3]-[C:2](=[O;D1;H0:4])-[O;H0;D2;+0:1]-[CH2;D2;+0:5]-[c:6](:[c:7]):[n;H0;D2;+0:8]:[c:9]:[c:10]
90
[{"value": 90.0, "product": "C(C)(=O)OCC1=NC=CC(=C1OC)OC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
4.8 g (28 mmol) of 3,4-dimethoxy-2-methylpyridine 1-oxide are metered into 25 ml of acetic anhydride at 85° C. in the course of one hour, the mixture is stirred at the same temperature for one hour and concentrated completely in vacuo and the brown oily residue is distilled in a bulb type still under 1 Pa. 5.3 g (90% o...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Ester
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1
HO-
null
null
1
CC(=O)OC(C)=O.COc1cc[n+]([O-])c(C)c1OC>>COc1ccnc(COC(C)=O)c1OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-7c86e719293c4a85964d03812b201ded
COc1c([N+](=O)[O-])cc[n+]([O-])c1C.C[O-]>>COc1cc[n+]([O-])c(C)c1OC
COC=1C(=[N+](C=CC1[N+](=O)[O-])[O-])C.C[O-].[Na+].S(O)(O)(=O)=O>>COC=1C(=[N+](C=CC1OC)[O-])C
O=[N+]([O-])[c:3]1[cH:4][cH:5][n+:6]([O-:7])[c:8]([CH3:9])[c:10]1[O:11][CH3:12].[CH3:1][O-:2]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n+:6]([O-:7])[c:8]([CH3:9])[c:10]1[O:11][CH3:12]
COc1c([N+](=O)[O-])cc[n+]([O-])c1C.C[O-]
COc1cc[n+]([O-])c(C)c1OC
null
null
CO
Functional Group Interconversion
OtherReaction
27f99d080b738ed3c11247d992420b7c028ad8e0895bb75728d6435304986321
5d154e9342b990e3d7c4ce2c6f7cc039bc2f1990cb4cb06dbac9dbddc28572dc
c1cc[nH+]cc1
O=[N+](-[O-])-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#7;a;+:4](-[O;-;D1;H0:5]):[c:6](-[C;D1;H3:7]):[c:8]:1-[#8:9].[C;D1;H3:10]-[O-;H0;D1:11]>>[#8:9]-[c:8]1:[c:6](-[C;D1;H3:7]):[#7;a;+:4](-[O;-;D1;H0:5]):[c:3]:[c:2]:[c;H0;D3;+0:1]:1-[O;H0;D2;+0:11]-[C;D1;H3:10]
88
[{"value": 88.0, "product": "COC=1C(=[N+](C=CC1OC)[O-])C", "details": "PERCENTYIELD", "is_desired": false}]
40
CELSIUS
16
HOUR
4.5 g (25 mmol) of 3-methoxy-2-methyl-4-nitropyridine 1-oxide are stirred at 40° C. in 75 ml of dry methanol, after addition of 4.7 ml of 30% strength sodium methylate solution, for 16 hours. The mixture is then cooled, brought to pH 7 with concentrated sulphuric acid, filtered and concentrated completely in vacuo, the...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Ether
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
Other
CO
40
16
COc1c([N+](=O)[O-])cc[n+]([O-])c1C.C[O-]>CO>COc1cc[n+]([O-])c(C)c1OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-561c4e56cfd54777a4013971762f0f41
COc1ccc[n+]([O-])c1C.O=[N+]([O-])O>>COc1c([N+](=O)[O-])cc[n+]([O-])c1C
[OH-].[Na+].[N+](=O)(O)[O-].COC=1C(=[N+](C=CC1)[O-])C.[N+](=O)(O)[O-]>>COC=1C(=[N+](C=CC1[N+](=O)[O-])[O-])C
[CH3:1][O:2][c:3]1[cH:4][cH:8][cH:9][n+:10]([O-:11])[c:12]1[CH3:13].O[N+:5](=[O:6])[O-:7]>>[CH3:1][O:2][c:3]1[c:4]([N+:5](=[O:6])[O-:7])[cH:8][cH:9][n+:10]([O-:11])[c:12]1[CH3:13]
COc1ccc[n+]([O-])c1C.O=[N+]([O-])O
COc1c([N+](=O)[O-])cc[n+]([O-])c1C
null
null
C(C)(=O)O
Functional Group Addition
Aromatic nitration with HNO3
ca5f1190ddada94452e11b52ea1eb215875524fe8173f14c45d3608500a1c3bf
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1cc[nH+]cc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[#8:4]-[c:5]1:[cH;D2;+0:6]:[c:7]:[c:8]:[#7;a;+:9](-[O;-;D1;H0:10]):[c:11]:1-[C;D1;H3:12]>>[#8:4]-[c:5]1:[c:11](-[C;D1;H3:12]):[#7;a;+:9](-[O;-;D1;H0:10]):[c:8]:[c:7]:[c;H0;D3;+0:6]:1-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]
null
[]
null
null
8
HOUR
8 ml of concentrated nitric acid are added in four portions of 2 ml each to 5.4 g of 3-methoxy-2-methylpyridine 1-oxide in 12 ml of glacial acetic acid at 80° C. in the course of 6 hours, the mixture is stirred at the same temperature overnight, a further 8 ml of nitric acid are added in three portions in the course of...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
HO-
C(C)(=O)O
null
8
COc1ccc[n+]([O-])c1C.O=[N+]([O-])O>C(C)(=O)O>COc1c([N+](=O)[O-])cc[n+]([O-])c1C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4408d181f6a54f72929cd29a06522ab8
COc1cccnc1C.OO>>COc1ccc[n+]([O-])c1C
COC=1C(=NC=CC1)C.OO>>COC=1C(=[N+](C=CC1)[O-])C
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][n:7][c:9]1[CH3:10].O[OH:8]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][n+:7]([O-:8])[c:9]1[CH3:10]
COc1cccnc1C.OO
COc1ccc[n+]([O-])c1C
null
null
C(C)(=O)O
Functional Group Interconversion
OtherReaction
d7f3c84fb751fef5567bc0e84a2e7c0afb271257e8dfb17aa871e038ff1a84c7
bf536f3bf8ed7b8faf08cf1c004ccd0a5e7fe59339402dd73ac837bb4a52f2ba
c1cc[nH+]cc1
O-[OH;D1;+0:1].[C;D1;H3:2]-[c:3](:[c:4]):[n;H0;D2;+0:5]:[c:6]:[c:7]>>[C;D1;H3:2]-[c:3](:[c:4]):[n+;H0;D3:5](-[O-;H0;D1:1]):[c:6]:[c:7]
60
[{"value": 60.0, "product": "COC=1C(=[N+](C=CC1)[O-])C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
15.3 g (0.124 mol) of 3-methoxy-2-methylpyridine are dissolved in 100 ml of glacial acetic acid, and 40 ml of 30% strength hydrogen peroxide are added in 4 portions at 80° C. in the course of 6 hours. The mixture is stirred for a further 3 hours and then concentrated in vacuo (1.5 kPa), and two 50 ml portions of acetic...
10.6084/m9.figshare.5104873.v1
null
Peroxide
null
c1ccncc1
C1=CC=[NH+]C=C1
C1=CC=[NH+]C=C1
HO-
C(C)(=O)O
null
3
COc1cccnc1C.OO>C(C)(=O)O>COc1ccc[n+]([O-])c1C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d9e9a77157924c8592aec16db23141ed
COc1ccnc(C(C)O)c1.O=S(Cl)Cl>>COc1ccnc(C(C)Cl)c1.Cl
S(=O)(Cl)Cl.COC1=CC(=NC=C1)C(C)O.C1(=CC=CC=C1)C>>Cl.ClC(C)C1=NC=CC(=C1)OC
O[CH:8]([c:7]1[n:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:11]1)[CH3:9].O=S([Cl:10])[Cl:12]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH:8]([CH3:9])[Cl:10])[cH:11]1.[ClH:12]
COc1ccnc(C(C)O)c1.O=S(Cl)Cl
COc1ccnc(C(C)Cl)c1.Cl
null
null
ClCCl
Functional Group Interconversion
Alcohol to chloride_SOCl2
ed0947fcf0a870fa4568d74e29e264525d0acf781c20c116470537e8cf1d911a
495868b18ac37eabad313a8861412e57f019fb3569a2b2e50afa3ee29413ec02
c1ccncc1
O-[CH;D3;+0:1](-[C;D1;H3:2])-[c:3](:[c:4]):[#7;a:5]:[c:6].O=S(-[Cl;H0;D1;+0:7])-[Cl;H0;D1;+0:8]>>[C;D1;H3:2]-[CH;D3;+0:1](-[Cl;H0;D1;+0:7])-[c:3](:[c:4]):[#7;a:5]:[c:6].[ClH;D0;+0:8]
null
[]
null
null
null
null
36 ml of thionyl chloride are added dropwise to a cooled suspension of 57 g of (±)-1-[4-methoxy-2-pyridyl]ethanol in 400 ml of dichloromethane, in such a way that the internal temperature does not exceed 15° C. The mixture is then heated under reflux for 2.5 h, treated with 300 ml of toluene and concentrated to 150 ml....
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Secondary halide
null
null
c1ccncc1
Other
ClCCl
null
null
COc1ccnc(C(C)O)c1.O=S(Cl)Cl>ClCCl>COc1ccnc(C(C)Cl)c1.Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-30efe7987615405c8b41b1f3ee99935c
COc1ccnc(C(C)OC(C)=O)c1>>COc1ccnc(C(C)O)c1
C(C)(=O)OC(C)C1=NC=CC(=C1)OC.[OH-].[Na+]>>COC1=CC(=NC=C1)C(C)O
CC(=O)[O:10][CH:8]([c:7]1[n:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:11]1)[CH3:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH:8]([CH3:9])[OH:10])[cH:11]1
COc1ccnc(C(C)OC(C)=O)c1
COc1ccnc(C(C)O)c1
null
null
null
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
d7acfb2397f2b5b2a83b3bebf3698d6d984dd716982297f62a944222c79ce234
19dd58e0f83625e74b4b1375d88cb4c813ee60f593d812516d14eafc4ab68dc7
c1ccncc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])-[c:4]:[#7;a:5]>>[#7;a:5]:[c:4]-[C:2](-[C;D1;H3:3])-[OH;D1;+0:1]
null
[]
75
CELSIUS
2
HOUR
114 g of (+)-1-[4-methoxy-2-pyridyl]-ethyl acetate are added dropwise at 70° C. to 220 ml of 4N sodium hydroxide solution. The mixture is then stirred for a further 2 h at 75° C., cooled and extracted with four times 200 ml of dichloromethane. The organic phase is washed with 2N sodium hydroxide solution and water, dri...
10.6084/m9.figshare.5104873.v1
null
Ester
Secondary alcohol
null
null
c1ccncc1
HO-
null
75
2
COc1ccnc(C(C)OC(C)=O)c1>>COc1ccnc(C(C)O)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-500050d121a64feabe3a407461393efa
CC(=O)OC(C)=O.CCc1cc(OC)cc[n+]1[O-]>>COc1ccnc(C(C)OC(C)=O)c1
C(C)C1=[N+](C=CC(=C1)OC)[O-].C(C)(=O)OC(C)=O.C(C)(=O)OC(C)=O>>C(C)(=O)OC(C)C1=NC=CC(=C1)OC
CC(=O)[O:10][C:11]([CH3:12])=[O:13].[O-][n+:6]1[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:14][c:7]1[CH2:8][CH3:9]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][n:6][c:7]([CH:8]([CH3:9])[O:10][C:11]([CH3:12])=[O:13])[cH:14]1
CC(=O)OC(C)=O.CCc1cc(OC)cc[n+]1[O-]
COc1ccnc(C(C)OC(C)=O)c1
null
null
null
Protection
OtherReaction
f4e85b633bf4e79d1b81c036d2f4e246a93c2eb8ec0202f93c45d73e710e4f0d
dd0b9e5a615173b1d6c9fe991a352f69d24fef80f4bf0eeab7c46667d446dcd0
c1ccncc1
C-C(=O)-[O;H0;D2;+0:1]-[C:2](-[C;D1;H3:3])=[O;D1;H0:4].[C;D1;H3:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[n+;H0;D3:9](-[O-]):[c:10]:[c:11]>>[C;D1;H3:3]-[C:2](=[O;D1;H0:4])-[O;H0;D2;+0:1]-[CH;D3;+0:6](-[C;D1;H3:5])-[c:7](:[c:8]):[n;H0;D2;+0:9]:[c:10]:[c:11]
78
[{"value": 78.0, "product": "C(C)(=O)OC(C)C1=NC=CC(=C1)OC", "details": "PERCENTYIELD", "is_desired": false}]
90
CELSIUS
2.5
HOUR
171 g of 2-ethyl-4-methoxy-pyridine N-oxide are added dropwise within 3 h to 312 ml of acetic anhydride heated to 90° C., in such a way that the internal temperature does not exceed 115° C. The mixture is then left to stand for a further 2.5 h at 100° C., and excess acetic anhydride is stripped off. Distillation of the...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Ester
C1=CC=[NH+]C=C1
c1ccncc1
c1ccncc1
HO-
null
90
2.5
CC(=O)OC(C)=O.CCc1cc(OC)cc[n+]1[O-]>>COc1ccnc(C(C)OC(C)=O)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-aa2d9d186baa4dec80079d17c6497e03
Nc1cc(F)c(OC(F)F)cc1[N+](=O)[O-]>>Cl.Nc1cc(F)c(OC(F)F)cc1N
FC(OC1=CC(=C(N)C=C1F)[N+](=O)[O-])F.FC(OC1=CC(=C(C=C1F)NC(C)=O)[N+](=O)[O-])F.[N+](=O)(O)[O-].Cl>>Cl.Cl.FC(OC1=CC(=C(C=C1F)N)N)F
O=[N+:15]([O-])[c:14]1[c:4]([NH2:3])[cH:5][c:6]([F:7])[c:8]([O:9][CH:10]([F:11])[F:12])[cH:13]1>>[ClH:2].[NH2:3][c:4]1[cH:5][c:6]([F:7])[c:8]([O:9][CH:10]([F:11])[F:12])[cH:13][c:14]1[NH2:15]
Nc1cc(F)c(OC(F)F)cc1[N+](=O)[O-]
Cl.Nc1cc(F)c(OC(F)F)cc1N
null
null
ClCCl.C1CCCCC1.CO
Functional Group Interconversion
Reduction of nitro groups to amines
5c1ea979989295c14f1f65f49e58974d5c524451abca65fc2e6cec44e3d0784f
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
85
[{"value": 85.0, "product": "Cl.Cl.FC(OC1=CC(=C(C=C1F)N)N)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
15
HOUR
22.5 ml of 100% nitric acid are added dropwise at 20° C. within 30 min. to 20 g of the above compound in 200 ml of dichloromethane, and the mixture is stirred for a further 15 h at room temperature. Analogously to Example B7c, this gives N-(4-difluoromethoxy-5-fluoro-2-nitrophenyl)acetamide of m.p. 72°-74° C. (from cyc...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
ClCCl.C1CCCCC1.CO
null
15
Nc1cc(F)c(OC(F)F)cc1[N+](=O)[O-]>ClCCl.C1CCCCC1.CO>Cl.Nc1cc(F)c(OC(F)F)cc1N
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-afc1b28b948743f0ab162dbe3eb3f56e
Nc1c([N+](=O)[O-])ccc2c1OC(F)(F)O2>>Cl.Nc1ccc2c(c1N)OC(F)(F)O2
NC1=C(C=CC=2OC(OC21)(F)F)[N+](=O)[O-].Cl>>Cl.Cl.FC1(OC=2C(O1)=CC=C(C2N)N)F
O=[N+:3]([O-])[c:4]1[cH:5][cH:6][c:7]2[c:8]([c:9]1[NH2:10])[O:11][C:12]([F:13])([F:14])[O:15]2>>[ClH:2].[NH2:3][c:4]1[cH:5][cH:6][c:7]2[c:8]([c:9]1[NH2:10])[O:11][C:12]([F:13])([F:14])[O:15]2
Nc1c([N+](=O)[O-])ccc2c1OC(F)(F)O2
Cl.Nc1ccc2c(c1N)OC(F)(F)O2
null
[Pd]
CO
Functional Group Interconversion
Reduction of nitro groups to amines
5c1ea979989295c14f1f65f49e58974d5c524451abca65fc2e6cec44e3d0784f
10b8579fd1662beac4350d758bc16e1f45ee6ea295ff9572db62110c9e2a77db
c1ccc2c(c1)OCO2
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
97
[{"value": 97.0, "product": "Cl.Cl.FC1(OC=2C(O1)=CC=C(C2N)N)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
30 g of 4-amino-2,2-difluoro-5-nitro-1,3-benzodioxole are hydrogenated in 300 ml of methanol on 0.5 g of 10% palladium-on-carbon in a circulating hydrogenation apparatus under atmospheric pressure and at room temperature, 2.5 equivalents of methanolic hydrogen chloride solution are added, the mixture is filtered, the s...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2c(c1)OCO2
Other
[Pd].CO
null
null
Nc1c([N+](=O)[O-])ccc2c1OC(F)(F)O2>[Pd].CO>Cl.Nc1ccc2c(c1N)OC(F)(F)O2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-0b49246c61754d2eb5f40629087f96d0
COc1cccc(O)c1OC.FC(F)Cl.O=[N+]([O-])O>>COc1cc([N+](=O)[O-])cc(OC(F)F)c1OC
COC1=C(C=CC=C1OC)O.ClC(F)F.[N+](=O)(O)[O-].[OH-].[K+]>>FC(OC1=C(C(=CC(=C1)[N+](=O)[O-])OC)OC)F
[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:9][c:10]([OH:11])[c:15]1[O:16][CH3:17].Cl[CH:12]([F:13])[F:14].O[N+:6](=[O:7])[O-:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[cH:9][c:10]([O:11][CH:12]([F:13])[F:14])[c:15]1[O:16][CH3:17]
COc1cccc(O)c1OC.FC(F)Cl.O=[N+]([O-])O
COc1cc([N+](=O)[O-])cc(OC(F)F)c1OC
null
CC1=CC2=C(C=C1C)N(C=N2)[C@@H]3C(C([C@@H](O3)CO)OP(=O)([O-])O[C@H](C)CNC(=O)CC[C@@]\4([C@H]([C@@H]5[C@]6([C@@]([C@@H](C(=N6)/C(=C\7/[C@@]([C@@H](C(=N7)/C=C\8/C([C@@H](C(=N8)/C(=C4\[N-]5)/C)CCC(=O)N)(C)C)CCC(=O)N)(C)CC(=O)N)/C)CCC(=O)N)(C)CC(=O)N)C)CC(=O)N)C)O.O.[Co+2]
C1CCCCC1.C(C)(=O)OCC.O1CCOCC1.O
Heteroatom Alkylation and Arylation
OtherReaction
2edee3a90d086e0c6aecabbbb84387827a7cfa69a1985004a8e5da1b9462ed39
88e41d56e95ada653e6c3e7bd29bcb9c274826b2a35bc97c304754c936ddd589
c1ccccc1
Cl-[CH;D3;+0:1](-[F;D1;H0:2])-[F;D1;H0:3].O-[N+;H0;D3:4](-[O;-;D1;H0:5])=[O;D1;H0:6].[OH;D1;+0:7]-[c:8]1:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:[c:13]:1>>[F;D1;H0:2]-[CH;D3;+0:1](-[F;D1;H0:3])-[O;H0;D2;+0:7]-[c:8]1:[c:9]:[c:10]:[c:11]:[c;H0;D3;+0:12](-[N+;H0;D3:4](-[O;-;D1;H0:5])=[O;D1;H0:6]):[c:13]:1
48
[{"value": 48.0, "product": "FC(OC1=C(C(=CC(=C1)[N+](=O)[O-])OC)OC)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
50 g of 2,3-dimethoxyphenol are reacted analogously to Example B12a with 80 g of potassium hydroxide and chlorodifluoromethane in dioxane/water. The mixture is extracted with diisopropyl ether by shaking, the extract is washed with sodium hydroxide solution and 35 g of a product (b.p. 70°-74° C./0.3 mbar) are obtained ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Secondary halide.Nitrate.Aromatic alcohol
Secondary halide.Secondary halide.Ether.Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HCl
CC1=CC2=C(C=C1C)N(C=N2)[C@@H]3C(C([C@@H](O3)CO)OP(=O)([O-])O[C@H](C)CNC(=O)CC[C@@]\4([C@H]([C@@H]5[C@]6([C@@]([C@@H](C(=N6)/C(=C\7/[C@@]([C@@H](C(=N7)/C=C\8/C([C@@H](C(=N8)/C(=C4\[N-]5)/C)CCC(=O)N)(C)C)CCC(=O)N)(C)CC(=O)N)/C)CCC(=O)N)(C)CC(=O)N)C)CC(=O)N)C)O.O.[Co+2].C1CCCCC1.C(C)(=O)OCC.O1CCOCC1.O
null
null
COc1cccc(O)c1OC.FC(F)Cl.O=[N+]([O-])O>CC1=CC2=C(C=C1C)N(C=N2)[C@@H]3C(C([C@@H](O3)CO)OP(=O)([O-])O[C@H](C)CNC(=O)CC[C@@]\4([C@H]([C@@H]5[C@]6([C@@]([C@@H](C(=N6)/C(=C\7/[C@@]([C@@H](C(=N7)/C=C\8/C([C@@H](C(=N8)/C(=C4\[N-]5)/C)CCC(=O)N)(C)C)CCC(=O)N)(C)CC(=O)N)/C)CCC(=O)N)(C)CC(=O)N)C)CC(=O)N)C)O.O.[Co+2].C1CCCCC1.C(C)(...
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b146a08d4e884b7fbc08bcc79a0d1f24
CC(=O)C(C)C.ClCc1ccc(Cl)cc1>>CC(=O)C(C)(C)Cc1ccc(Cl)cc1
[OH-].[K+].ClC1=CC=C(CCl)C=C1.C(C)(C)C(=O)C>>ClC1=CC=C(C=C1)CC(C(C)=O)(C)C
[CH3:1][C:2](=[O:3])[CH:4]([CH3:5])[CH3:6].Cl[CH2:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1>>[CH3:1][C:2](=[O:3])[C:4]([CH3:5])([CH3:6])[CH2:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
CC(=O)C(C)C.ClCc1ccc(Cl)cc1
CC(=O)C(C)(C)Cc1ccc(Cl)cc1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
e8b75e5efb691ecf3c9116420e15918cdd0fda7b899536fb179ed39cbdad1bc2
836e0f77354d9f44b98dde88e343d5cebbf81f14d452aa51d1e50ec699999492
c1ccccc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[CH;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
87
[{"value": 87.0, "product": "ClC1=CC=C(C=C1)CC(C(C)=O)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.9, "product": "ClC1=CC=C(C=C1)CC(C(C)=O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
85
CELSIUS
3
HOUR
254.4 g (4 mols) of powdered technical grade potassium hydroxide (88% strength) are suspended in 1 liter of toluene, 40 g of tetrabutylammonium bromide are added, and a mixture of 644 g (4 mols) of 4-chlorobenzyl chloride and 430 g (5 mols) of methyl isopropyl ketone is then slowly added dropwise at 85° C. To complete ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
null
null
c1ccccc1
HCl
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)C
85
3
CC(=O)C(C)C.ClCc1ccc(Cl)cc1>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)C>CC(=O)C(C)(C)Cc1ccc(Cl)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-51cb3e7d23ad4c4bb41ea2033ba73586
C=CCCl.CC(=O)C(C)C>>C=CCC(C)(C)C(C)=O
C1(=CC=CC=C1)C.[OH-].[K+].C(C=C)Cl.C(C)(C)C(=O)C>>CC(CC=C)(C(C)=O)C
Cl[CH2:3][CH:2]=[CH2:1].[CH:4]([CH3:5])([CH3:6])[C:7]([CH3:8])=[O:9]>>[CH2:1]=[CH:2][CH2:3][C:4]([CH3:5])([CH3:6])[C:7]([CH3:8])=[O:9]
C=CCCl.CC(=O)C(C)C
C=CCC(C)(C)C(C)=O
null
[Cl-].C(CCCCCCC)[NH+](CCCCCCCC)CCCCCCCC
null
C-C Coupling
OtherReaction
cd9c61577f3b1e4398b200b69dbc22378f11d930d200a7cd1fe8916ac61b33c7
f5ccd90096c3201115eb6510107831f398bf8f80381c3ea6084a10b0ebb25a81
null
Cl-[CH2;D2;+0:1]-[C:2]=[C;D1;H2:3].[C;D1;H3:4]-[CH;D3;+0:5](-[C;D1;H3:6])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]>>[C;D1;H2:3]=[C:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:5](-[C;D1;H3:4])(-[C;D1;H3:6])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
76
[{"value": 76.0, "product": "CC(CC=C)(C(C)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
70
CELSIUS
4
HOUR
63.6 g (1 mol) of powdered technical grade potassium hydroxide (88% strength) are suspended in 200 ml of toluene, and 10 g of trioctylammonium chloride are added. A mixture of 76.5 g (1 mol) of allyl chloride and 129 g (1.5 mols) of methyl isopropyl ketone is then added dropwise so that the temperature does not exceed ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone.Allyl
null
null
null
HCl
[Cl-].C(CCCCCCC)[NH+](CCCCCCCC)CCCCCCCC
70
4
C=CCCl.CC(=O)C(C)C>[Cl-].C(CCCCCCC)[NH+](CCCCCCCC)CCCCCCCC>C=CCC(C)(C)C(C)=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-9a4daa9ae65a4e5fadbc80d78186f469
C#CCBr.CC(=O)C(C)C>>C#CCC(C)(C)C(C)=O
C(C#C)Br.C(C)(C)C(=O)C.[OH-].[K+].C1(=CC=CC=C1)C>>CC(CC#C)(C(C)=O)C
Br[CH2:3][C:2]#[CH:1].[CH:4]([CH3:5])([CH3:6])[C:7]([CH3:8])=[O:9]>>[CH:1]#[C:2][CH2:3][C:4]([CH3:5])([CH3:6])[C:7]([CH3:8])=[O:9]
C#CCBr.CC(=O)C(C)C
C#CCC(C)(C)C(C)=O
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
null
C-C Coupling
OtherReaction
e8b75e5efb691ecf3c9116420e15918cdd0fda7b899536fb179ed39cbdad1bc2
836e0f77354d9f44b98dde88e343d5cebbf81f14d452aa51d1e50ec699999492
null
Br-[CH2;D2;+0:1]-[C:2]#[C;D1;H1:3].[C;D1;H3:4]-[CH;D3;+0:5](-[C;D1;H3:6])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]>>[C;D1;H1:3]#[C:2]-[CH2;D2;+0:1]-[C;H0;D4;+0:5](-[C;D1;H3:4])(-[C;D1;H3:6])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
54
[{"value": 54.0, "product": "CC(CC#C)(C(C)=O)C", "details": "PERCENTYIELD", "is_desired": false}]
45
CELSIUS
12
HOUR
70 g (1.1 mols) of powdered technical grade potassium hydroxide (88% strength) and 10 g of tetrabutylammonium bromide in 250 ml of toluene are initially introduced. A mixture if 119 g (1 mol) of propargyl bromide and 103.2 g (1.2 mols) of methyl isopropyl ketone is then added dropwise so that the temperature does not e...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
null
null
null
HBr
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
45
12
C#CCBr.CC(=O)C(C)C>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC>C#CCC(C)(C)C(C)=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-0e9e073cc57d485fad6ab38501ccba80
CC(=O)C(C)C.ClCc1ccccc1>>CC(=O)C(C)(C)Cc1ccccc1
O.C(C)(C)C(=O)C.C(C1=CC=CC=C1)Cl.[OH-].[K+]>>CC(C(C)=O)(CC1=CC=CC=C1)C
[CH3:1][C:2](=[O:3])[CH:4]([CH3:5])[CH3:6].Cl[CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][C:2](=[O:3])[C:4]([CH3:5])([CH3:6])[CH2:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1
CC(=O)C(C)C.ClCc1ccccc1
CC(=O)C(C)(C)Cc1ccccc1
null
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC
C1(=CC=CC=C1)C
C-C Coupling
OtherReaction
e8b75e5efb691ecf3c9116420e15918cdd0fda7b899536fb179ed39cbdad1bc2
836e0f77354d9f44b98dde88e343d5cebbf81f14d452aa51d1e50ec699999492
c1ccccc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[CH;D3;+0:8](-[C;D1;H3:9])-[C;D1;H3:10]>>[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[C;H0;D4;+0:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]
47.9
[{"value": 47.9, "product": "CC(C(C)=O)(CC1=CC=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
12
HOUR
516 g (6 mols) of methyl isopropyl ketone, 759 g (6 mols) of benzyl chloride and 60 g (0.186 mol) of tetrabutylammonium bromide are dissolved in 1 liter of toluene, and the solution is heated to 100° C. 420 g (7.49 mols) of powered potassium hydroxide are slowly metered in at this temperature. The reaction mixture is s...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
null
null
c1ccccc1
HCl
[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)C
100
12
CC(=O)C(C)C.ClCc1ccccc1>[Br-].C(CCC)[N+](CCCC)(CCCC)CCCC.C1(=CC=CC=C1)C>CC(=O)C(C)(C)Cc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2f4f64a7a9604d9cb15c5894dbbdf971
BrBr.CC(=O)C(C)(C)Cc1ccccc1>>CC(C)(Cc1ccccc1)C(=O)CBr
CC(C(C)=O)(CC1=CC=CC=C1)C.BrBr>>BrCC(C(CC1=CC=CC=C1)(C)C)=O
Br[Br:14].[CH3:1][C:2]([CH3:3])([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C:11](=[O:12])[CH3:13]>>[CH3:1][C:2]([CH3:3])([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C:11](=[O:12])[CH2:13][Br:14]
BrBr.CC(=O)C(C)(C)Cc1ccccc1
CC(C)(Cc1ccccc1)C(=O)CBr
null
null
C(Cl)(Cl)Cl
Functional Group Interconversion
Bromination
97ca6720945af5a02c450d33ec56e946521050f9771c27f9cfcb85f3477593f6
cb3e14519230141aa015a4cf9c960def3e60f01997e61621f62506924bfa15de
c1ccccc1
Br-[Br;H0;D1;+0:1].[C:2]-[C:3](-[CH3;D1;+0:4])=[O;D1;H0:5]>>[Br;H0;D1;+0:1]-[CH2;D2;+0:4]-[C:3](-[C:2])=[O;D1;H0:5]
100
[{"value": 100.0, "product": "BrCC(C(CC1=CC=CC=C1)(C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
100 g (0.57 mol) of 3,3-dimethyl-4-phenylbutan-2-one (Example 5) are dissolved in 0.8 liter of chloroform, and 29 ml (91.9 g; 1.14 mols) of bromine are added slowly at room temperature. The mixture is stirred for a further hour at room temperature and is concentrated. 145.5 g (quantitative) of 1-bromo-3,3-dimethyl-4-ph...
10.6084/m9.figshare.5104873.v1
null
Ketone
Primary halide
null
null
c1ccccc1
HBr
C(Cl)(Cl)Cl
null
null
BrBr.CC(=O)C(C)(C)Cc1ccccc1>C(Cl)(Cl)Cl>CC(C)(Cc1ccccc1)C(=O)CBr
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a4036584ea9043a3bc1ad0d617585e2e
CC(C)(Cc1ccccc1)C(=O)CBr.c1nc[nH]n1>>CC(C)(Cc1ccccc1)C(=O)Cn1cncn1
BrCC(C(CC1=CC=CC=C1)(C)C)=O.N1N=CN=C1.C([O-])([O-])=O.[K+].[K+]>>CC(C(CN1N=CN=C1)=O)(CC1=CC=CC=C1)C
Br[CH2:13][C:11]([C:2]([CH3:1])([CH3:3])[CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)=[O:12].[nH:14]1[cH:15][n:16][cH:17][n:18]1>>[CH3:1][C:2]([CH3:3])([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C:11](=[O:12])[CH2:13][n:14]1[cH:15][n:16][cH:17][n:18]1
CC(C)(Cc1ccccc1)C(=O)CBr.c1nc[nH]n1
CC(C)(Cc1ccccc1)C(=O)Cn1cncn1
null
null
CC(=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
5fd537c1811b5d927630316f1d8d0b895550dd6e0a23faad4b2f0cac2b65c9fb
0844e813fd6aa8a6f803ffd9d05cd5ff5272ddf69396b8c87d384d86e0562add
O=C(CCc1ccccc1)Cn1cncn1
Br-[CH2;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[#7;a:5]1:[c:6]:[nH;D2;+0:7]:[#7;a:8]:[c:9]:1>>[C:3]-[C:2](=[O;D1;H0:4])-[CH2;D2;+0:1]-[n;H0;D3;+0:7]1:[#7;a:8]:[c:9]:[#7;a:5]:[c:6]:1
48.4
[{"value": 48.4, "product": "CC(C(CN1N=CN=C1)=O)(CC1=CC=CC=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 48.3, "product": "CC(C(CN1N=CN=C1)=O)(CC1=CC=CC=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
74 g (0.29 mol) of 1-bromo-3,3-dimethyl-4-phenylbutan-2-one, 40 g (0.58 mol) of 1,2,4-triazole and 80 g of potassium carbonate are dissolved in 700 ml of acetone, and the solution is heated under reflux for 3 hours. Thereafter, it is allowed to cool and is filtered off under suction from the inorganic residue, and the ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
c1nc[nH]n1
c1nc[nH]n1
c1ccccc1.c1nc[nH]n1
HBr
CC(=O)C
null
null
CC(C)(Cc1ccccc1)C(=O)CBr.c1nc[nH]n1>CC(=O)C>CC(C)(Cc1ccccc1)C(=O)Cn1cncn1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6ff56abd36cd489b8cb4b6495cf0458f
CC(C)(Cc1ccccc1)C(=O)Cn1cncn1.ClCc1ccccc1>>CC(C)(Cc1ccccc1)C(=O)C(Cc1ccccc1)n1cncn1
CC(C(CN1N=CN=C1)=O)(CC1=CC=CC=C1)C.C(C1=CC=CC=C1)Cl.[OH-].[K+]>>C1(=CC=CC=C1)CC(C(C(CC1=CC=CC=C1)N1N=CN=C1)=O)(C)C
[CH3:1][C:2]([CH3:3])([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C:11](=[O:12])[CH2:13][n:21]1[cH:22][n:23][cH:24][n:25]1.Cl[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][C:2]([CH3:3])([CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C:11](=[O:12])[CH:13]([CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][cH:2...
CC(C)(Cc1ccccc1)C(=O)Cn1cncn1.ClCc1ccccc1
CC(C)(Cc1ccccc1)C(=O)C(Cc1ccccc1)n1cncn1
null
null
O.CS(=O)C
C-C Coupling
OtherReaction
e8b75e5efb691ecf3c9116420e15918cdd0fda7b899536fb179ed39cbdad1bc2
836e0f77354d9f44b98dde88e343d5cebbf81f14d452aa51d1e50ec699999492
O=C(CCc1ccccc1)C(Cc1ccccc1)n1cncn1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[C:5]-[C:6](=[O;D1;H0:7])-[CH2;D2;+0:8]-[#7;a:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1>>[C:5]-[C:6](=[O;D1;H0:7])-[CH;D3;+0:8](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4])-[#7;a:9]1:[#7;a:10]:[c:11]:[#7;a:12]:[c:13]:1
81.8
[{"value": 81.8, "product": "C1(=CC=CC=C1)CC(C(C(CC1=CC=CC=C1)N1N=CN=C1)=O)(C)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 81.7, "product": "C1(=CC=CC=C1)CC(C(C(CC1=CC=CC=C1)N1N=CN=C1)=O)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
8
HOUR
48.6 g (0.2 mol) of 3,3-dimethyl-4-phenyl-1-(1,2,4-triazol-1-yl)-butan-2-one, 27.9 g (0.22 mol) of benzyl chloride and 12.3 g (0.22 mol) of potassium hydroxide in 15 ml of water are dissolved in 300 ml of dimethylsulphoxide. The reaction mixture is stirred for a further 8 hours at 50° C. and then poured onto water. The...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ketone
null
null
c1ccccc1.c1ccccc1.c1nc[nH]n1
HCl
O.CS(=O)C
50
8
CC(C)(Cc1ccccc1)C(=O)Cn1cncn1.ClCc1ccccc1>O.CS(=O)C>CC(C)(Cc1ccccc1)C(=O)C(Cc1ccccc1)n1cncn1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a9bc5be1b5fe444bb0b94e7222020b44
COC(=O)CC(O)CCl.NCC(N)=O>>NC(=O)CN1CC(O)CC1=O
Cl.NCC(=O)N.C([O-])([O-])=O.[Na+].[Na+].ClCC(CC(=O)OC)O>>C1C(CN(C1=O)CC(=O)N)O
CO[C:10]([CH2:9][CH:7]([CH2:6]Cl)[OH:8])=[O:11].[NH2:1][C:2](=[O:3])[CH2:4][NH2:5]>>[NH2:1][C:2](=[O:3])[CH2:4][N:5]1[CH2:6][CH:7]([OH:8])[CH2:9][C:10]1=[O:11]
COC(=O)CC(O)CCl.NCC(N)=O
NC(=O)CN1CC(O)CC1=O
null
null
C(C)O
Acylation
OtherReaction
819e3f2b7868adc1c1b9de9bb195abc43156b28c3cf194597f96cec7ac859f91
0eb062b0407fca631aebf8550994dc507c145d19ea7e1f961f104337865aa8f4
O=C1CCCN1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[O;D1;H1:5])-[CH2;D2;+0:6]-Cl.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[C:10]-[NH2;D1;+0:11]>>[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[C:10]-[N;H0;D3;+0:11]1-[CH2;D2;+0:6]-[C:4](-[O;D1;H1:5])-[C:3]-[C;H0;D3;+0:1]-1=[O;D1;H0:2]
75
[{"value": 75.0, "product": "C1C(CN(C1=O)CC(=O)N)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
In 10 ml of ethanol, 1.11 g (10 m.moles) of glycinamide hydrochloride, 1.06 g (10 m.moles) of sodium carbonate, and 1.53 g (10 m.moles) of methyl 4-chloro-3-hydroxybutyrate were stirred and refluxed simultaneously for 20 hours. After completion of the reaction, the warm reaction mixture was filtered to expel inorganic ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester.Primary amine
Tertiary amide
null
C1CC[NH]C1
C1CC[NH]C1
HCl
C(C)O
null
null
COC(=O)CC(O)CCl.NCC(N)=O>C(C)O>NC(=O)CN1CC(O)CC1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4f322b0df7884eecbb913acbcc3a95a3
CCOC(=O)c1cc(NC(C)=O)c([N+](=O)[O-])cc1OCC>>CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC
C(C)(=O)NC=1C(=CC(=C(C(=O)OCC)C1)OCC)[N+](=O)[O-].S(O)(O)(=O)=O>>NC=1C(=CC(=C(C(=O)OC)C1)OCC)[N+](=O)[O-]
CC(=O)[NH:11][c:10]1[c:6]([N+:7](=[O:8])[O-:9])[cH:5][c:4]([O:3][CH2:2][CH3:1])[c:13]([C:14](=[O:15])[O:16][CH2:17]C)[cH:12]1>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][c:6]([N+:7](=[O:8])[O-:9])[c:10]([NH2:11])[cH:12][c:13]1[C:14](=[O:15])[O:16][CH3:17]
CCOC(=O)c1cc(NC(C)=O)c([N+](=O)[O-])cc1OCC
CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC
null
null
null
Reduction
OtherReaction
4a88b9d891ba339b9f646daf4454983fe862101e27f3f81079d77433b43c2a4d
0f81e8b234be8a24e6ae74926d0948198849f4c90af528e8f6929d1a30a9bbd7
c1ccccc1
C-[CH2;D2;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]:[c:7](-[NH;D2;+0:8]-C(-C)=O):[c:9]>>[CH3;D1;+0:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6]:[c:7](-[NH2;D1;+0:8]):[c:9]
null
[]
null
null
null
null
A suspension of 1 5 g of ethyl 5-acetylamino-2-ethoxy-4-nitrobenzoate in 50 ml of 5 % (v/v) sulfuric acid methanolic solution was refluxed for 4 hours After cooling, the reaction solution was poured into an ice water, the resulting crystals were collected by filtration and recrystallized from methanol to give the title...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amide
Ester.Primary amine
null
null
c1ccccc1
HO-
null
null
null
CCOC(=O)c1cc(NC(C)=O)c([N+](=O)[O-])cc1OCC>>CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-080db1e1911245f1a72773b25eb51c23
CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC>>CCOc1cc(N)c(N)cc1C(=O)OC
NC=1C(=CC(=C(C(=O)OC)C1)OCC)[N+](=O)[O-]>>NC1=CC(=C(C(=O)OC)C=C1N)OCC
O=[N+:7]([O-])[c:6]1[cH:5][c:4]([O:3][CH2:2][CH3:1])[c:11]([C:12](=[O:13])[O:14][CH3:15])[cH:10][c:8]1[NH2:9]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][c:6]([NH2:7])[c:8]([NH2:9])[cH:10][c:11]1[C:12](=[O:13])[O:14][CH3:15]
CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC
CCOc1cc(N)c(N)cc1C(=O)OC
null
[C].[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A suspension of 873 mg of methyl 5-amino-2-ethoxy-4-nitrobenzoate and 50 mg of 10 % palladium carbon in 50 ml of ethanol was stirred at room temperature under a hydrogen atmosphere. After the absorption of hydrogen was completed, the catalyst was removed by filtration, and the filtrate was evaporated to dryness under r...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[C].[Pd].C(C)O
null
null
CCOc1cc([N+](=O)[O-])c(N)cc1C(=O)OC>[C].[Pd].C(C)O>CCOc1cc(N)c(N)cc1C(=O)OC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-891c1c61ec8840a4be4dcb49b477b3d6
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOc1cc(N)c(N)cc1C(=O)OC>>CCOC(=O)c1c(O)c2ccccc2c2nc3cc(OCC)c(C(=O)OC)cc3nc12
C(C)O.NC1=CC(=C(C(=O)OC)C=C1N)OCC.OC1=C(C(C2=CC=CC=C2C1=O)=O)C(=O)OCC>>C(C)OC=1C(=CC2=NC3=C(C(=C4C(=C3N=C2C1)C=CC=C4)O)C(=O)OCC)C(=O)OC
O=[C:15]1[c:14]2[c:9]([cH:10][cH:11][cH:12][cH:13]2)[C:7](=[O:8])[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[C:31]1O.[NH2:16][c:17]1[cH:18][c:19]([O:20][CH2:21][CH3:22])[c:23]([C:24](=[O:25])[O:26][CH3:27])[cH:28][c:29]1[NH2:30]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[c:7]([OH:8])[c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[...
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOc1cc(N)c(N)cc1C(=O)OC
CCOC(=O)c1c(O)c2ccccc2c2nc3cc(OCC)c(C(=O)OC)cc3nc12
null
null
CN(C=O)C
Aromatic Heterocycle Formation
OtherReaction
0f37fd42aea68cadbedb11d01c9c5ebfd4f7677147d66d48c8da29ffeb8db436
db2db5c11675d0fa08e932d30f06638472b18a8a17601e3ea92d2edabfa89b7b
c1ccc2c(c1)ccc1nc3ccccc3nc12
O-[C;H0;D3;+0:1]1=[C;H0;D3;+0:2](-[C:3](=[O;D1;H0:4])-[#8:5]-[C:6])-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9](:[c:10]):[c:11](:[c:12])-[C;H0;D3;+0:13]-1=O.[NH2;D1;+0:14]-[c:15](:[c:16]):[c:17](-[NH2;D1;+0:18]):[c:19]>>[C:6]-[#8:5]-[C:3](=[O;D1;H0:4])-[c;H0;D3;+0:2]1:[c;H0;D3;+0:1]2:[n;H0;D2;+0:18]:[c:17](:[c:19]):[c:15](:[...
null
[]
null
null
2
HOUR
To a solution of 895 mg of ethyl 3-hydroxy-1,4-dihydro1,4-dioxo-2-naphthoate in 10 ml of N,N-dimethylformamide was added 620 mg of N,N'-carbonyldiimidazole, and the mixture was stirred at room temperature for 2 hours. To the mixture was added the crude methyl 4,5-diamino-2-ethoxybenzoate in 10 ml of N,N-dimethyl-formam...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ketone.Ester.Enol.Primary amine.Primary amine
Ester.Aromatic alcohol
C1=CCc2ccccc2C1.c1ccccc1
c1ccc2c(c1)ccc1nc3ccccc3nc12
c1ccc2c(c1)ccc1nc3ccccc3nc12
HO-
CN(C=O)C
null
2
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOc1cc(N)c(N)cc1C(=O)OC>CN(C=O)C>CCOC(=O)c1c(O)c2ccccc2c2nc3cc(OCC)c(C(=O)OC)cc3nc12
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a170a4be891f44c2bc90932bb1a45f78
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC>>COc1cc([N+](=O)[O-])c(N)cc1C(=O)O
NC=1C(=CC(=C(C(=O)OC)C1)OC)[N+](=O)[O-].[OH-].[K+].Cl>>NC=1C(=CC(=C(C(=O)O)C1)OC)[N+](=O)[O-]
C[O:15][C:13]([c:12]1[c:3]([O:2][CH3:1])[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11]1)=[O:14]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11][c:12]1[C:13](=[O:14])[OH:15]
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC
COc1cc([N+](=O)[O-])c(N)cc1C(=O)O
null
null
O1CCOCC1.O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
null
null
To a suspension of 13.57 g of methyl 5-amino-2-methoxy-4-nitrobenzoate in 250 ml of dioxane was added a solution of 4.36 g of potassium hydroxide in 25 ml of water, and the mixture was refluxed for 4 hours. To the reaction solution was added 7 ml of concentrated hydrochloric acid. The solvent was evaporated under reduc...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1
Other
O1CCOCC1.O
null
null
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC>O1CCOCC1.O>COc1cc([N+](=O)[O-])c(N)cc1C(=O)O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-bcfdfddfae3a43ad965c1d4f29ef6011
C1CCNC1.COc1cc([N+](=O)[O-])c(N)cc1C(=O)O>>COc1cc([N+](=O)[O-])c(N)cc1C(=O)N1CCCC1
N1CCCC1.NC=1C(=CC(=C(C(=O)O)C1)OC)[N+](=O)[O-]>>NC=1C(=CC(=C(C(=O)N2CCCC2)C1)OC)[N+](=O)[O-]
[NH:15]1[CH2:16][CH2:17][CH2:18][CH2:19]1.O[C:13]([c:12]1[c:3]([O:2][CH3:1])[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11]1)=[O:14]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11][c:12]1[C:13](=[O:14])[N:15]1[CH2:16][CH2:17][CH2:18][CH2:19]1
C1CCNC1.COc1cc([N+](=O)[O-])c(N)cc1C(=O)O
COc1cc([N+](=O)[O-])c(N)cc1C(=O)N1CCCC1
null
null
CN(C=O)C
Acylation
Acylation of Nitrogen Nucleophiles by Carboxylic Acids
a590d96426a2fbaed42913d9daf8a16471a16de4978200f1d35a30a10009ebe7
c5e4172490b2731ba9322b68af56376edadc31ce0bb9a3dfdea23a1817a852fd
O=C(c1ccccc1)N1CCCC1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C:6]1-[C:7]-[C:8]-[C:9]-[NH;D2;+0:10]-1>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[N;H0;D3;+0:10]1-[C:6]-[C:7]-[C:8]-[C:9]-1)-[c:3](:[c:4]):[c:5]
null
[]
null
null
30
MINUTE
To a solution of 4.24 g of 5-amino-2-methoxy-4-nitrobenzoic acid in 30 ml of N,N-dimethylformamide was added 3.24 g of N,N'-carbonyldiimidazole at room temperature. After 30 minutes, 5 ml of pyrrolidine was added, and the mixture was stirred for 2 hours. The solvent was evaporated under reduced pressure, and the residu...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Secondary amine
Tertiary amide
C1CCNC1
C1CC[NH]C1
c1ccccc1.C1CC[NH]C1
HO-
CN(C=O)C
null
0.5
C1CCNC1.COc1cc([N+](=O)[O-])c(N)cc1C(=O)O>CN(C=O)C>COc1cc([N+](=O)[O-])c(N)cc1C(=O)N1CCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f895edc41e134a04912976c873e74c91
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC.N>>COc1cc([N+](=O)[O-])c(N)cc1C(N)=O
NC=1C(=CC(=C(C(=O)OC)C1)OC)[N+](=O)[O-].O.N>>NC=1C(=CC(=C(C(=O)N)C1)OC)[N+](=O)[O-]
CO[C:13]([c:12]1[c:3]([O:2][CH3:1])[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11]1)=[O:15].[NH3:14]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11][c:12]1[C:13]([NH2:14])=[O:15]
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC.N
COc1cc([N+](=O)[O-])c(N)cc1C(N)=O
null
null
O1CCOCC1
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
c1ccccc1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[NH3;D0;+0:6]>>[NH2;D1;+0:6]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
40
HOUR
To a solution of 5.66 g of methyl 5-amino-2-methoxy-4-nitrobenzoate in 200 ml of dioxane was added 50 ml of 28 % ammonia water, and then the mixture was allowed to stand at room temperature for 40 hours. The solvent was evaporated under reduced pressure, and the residue was recrystallized from dioxane to give the title...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1ccccc1
HO-
O1CCOCC1
null
40
COC(=O)c1cc(N)c([N+](=O)[O-])cc1OC.N>O1CCOCC1>COc1cc([N+](=O)[O-])c(N)cc1C(N)=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b3e0e8b3d9e24c10a6b7e68172cefca4
COc1cc([N+](=O)[O-])c(N)cc1C(=O)O>>COc1cc([N+](=O)[O-])c(N)cc1C(=O)Oc1ccccc1
NC=1C(=CC(=C(C(=O)O)C1)OC)[N+](=O)[O-].S(=O)(Cl)Cl>>NC=1C(=CC(=C(C(=O)OC2=CC=CC=C2)C1)OC)[N+](=O)[O-]
[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11][c:12]1[C:13](=[O:14])[OH:15]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([N+:6](=[O:7])[O-:8])[c:9]([NH2:10])[cH:11][c:12]1[C:13](=[O:14])[O:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
COc1cc([N+](=O)[O-])c(N)cc1C(=O)O
COc1cc([N+](=O)[O-])c(N)cc1C(=O)Oc1ccccc1
null
null
C1=CC=CC=C1
Aromatic Heterocycle Formation
OtherReaction
2640b6d528093b776d79d942911e114b3490be6981cb7ca8e05a8b09997b8c38
2544f5a75f58466594e8a458c4167bc85e6ab94e6608e9185a9356c6df8260b8
O=C(Oc1ccccc1)c1ccccc1
[O;D1;H0:1]=[C:2](-[OH;D1;+0:3])-[c:4]>>[O;D1;H0:1]=[C:2](-[c:4])-[O;H0;D2;+0:3]-[c:5](:[c:6]):[c:7]
null
[]
null
null
30
MINUTE
To a suspension of 5.55 g of 5-amino-2-methoxy-4-nitrobenzoic acid in 40 ml of benzene was added 40 ml of thionyl chloride, and the mixture was refluxed for 4 hours. Subsequently, an excess amount of the thionyl chloride and the solvent were evaporated, the residue was dissolved in 40 ml of benzene, and then 12.3 g of ...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
c1ccccc1
c1ccccc1.c1ccccc1
Other
C1=CC=CC=C1
null
0.5
COc1cc([N+](=O)[O-])c(N)cc1C(=O)O>C1=CC=CC=C1>COc1cc([N+](=O)[O-])c(N)cc1C(=O)Oc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-491a4f8f742343318b3697e3cf01bfb4
COc1cc([N+](=O)[O-])c(N)cc1C(N)=O>>COc1cc(N)c(N)cc1C(N)=O
NC=1C(=CC(=C(C(=O)N)C1)OC)[N+](=O)[O-]>>NC1=CC(=C(C(=O)N)C=C1N)OC
O=[N+:6]([O-])[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:10]([C:11]([NH2:12])=[O:13])[cH:9][c:7]1[NH2:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([NH2:8])[cH:9][c:10]1[C:11]([NH2:12])=[O:13]
COc1cc([N+](=O)[O-])c(N)cc1C(N)=O
COc1cc(N)c(N)cc1C(N)=O
null
[C].[Pd]
CO
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
60
CELSIUS
null
null
A suspension of 3.04 g of 5-amino-2-methoxy-4-nitrobenzamide and 110 mg of 10 % palladium carbon in 300 ml of methanol was stirred at 60° C. under a hydrogen atmosphere. After absorption of hydrogen was completed, the catalyst was removed by filtration, and the filtrate was concentrated to give the title compound, m.p....
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[C].[Pd].CO
60
null
COc1cc([N+](=O)[O-])c(N)cc1C(N)=O>[C].[Pd].CO>COc1cc(N)c(N)cc1C(N)=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-645d23f56c494813b02511252ba424b5
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOC(=O)Cl>>CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O
OC1=C(C(C2=CC=CC=C2C1=O)=O)C(=O)OCC.C(C)N(CC)CC.ClC(=O)OCC>>C(C)OC(=O)OC1=C(C(C2=CC=CC=C2C1=O)=O)C(=O)OCC
[OH:6][C:7]1=[C:8]([C:9](=[O:10])[O:11][CH2:12][CH3:13])[C:14](=[O:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[C:22]1=[O:23].Cl[C:4]([O:3][CH2:2][CH3:1])=[O:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[O:6][C:7]1=[C:8]([C:9](=[O:10])[O:11][CH2:12][CH3:13])[C:14](=[O:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2[C:22]1=[O:2...
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOC(=O)Cl
CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O
null
null
O1CCCC1
Acylation
Schotten-Baumann to ester
5c9831da69657409ba7bd0a3096162b750678f7e141d35459e83185367325ab9
0e42a6e697573ca10503dcf2b634671b9afcb1038f77ae84d0feab55946900a5
O=C1C=CC(=O)c2ccccc21
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4].[#8:5]-[C:6](=[O;D1;H0:7])-[C:8](=[C:9](-[OH;D1;+0:10])-[C:11](=[O;D1;H0:12])-[c:13])-[C:14]=[O;D1;H0:15]>>[#8:5]-[C:6](=[O;D1;H0:7])-[C:8](=[C:9](-[O;H0;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#8:3]-[C:4])-[C:11](=[O;D1;H0:12])-[c:13])-[C:14]=[O;D1;H0:15]
null
[]
null
null
2
HOUR
To a solution of 2.48 g of ethyl 3-hydroxy-1,4-dihydro1,4-dioxo-2-naphthoate and 1.5 ml of triethylamine in 10 ml of dry tetrahydrofuran was added dropwise 1 ml of ethyl chloroformate at 5° C. or below, and the mixture was stirred at room temperature for 2 hours. The resulting solid was removed by filtration, and the f...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Enol
Carbonic Ester
null
null
C1=CCc2ccccc2C1
HCl
O1CCCC1
null
2
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O.CCOC(=O)Cl>O1CCCC1>CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-25d717c20516453d9c35a1cb80195294
COc1cc([N+](=O)[O-])c(N)cc1C(=O)N(C)C>>COc1cc(N)c(N)cc1C(=O)N(C)C
CN(C(C1=C(C=C(C(=C1)N)[N+](=O)[O-])OC)=O)C>>CN(C(C1=C(C=C(C(=C1)N)N)OC)=O)C
O=[N+:6]([O-])[c:5]1[cH:4][c:3]([O:2][CH3:1])[c:10]([C:11](=[O:12])[N:13]([CH3:14])[CH3:15])[cH:9][c:7]1[NH2:8]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([NH2:6])[c:7]([NH2:8])[cH:9][c:10]1[C:11](=[O:12])[N:13]([CH3:14])[CH3:15]
COc1cc([N+](=O)[O-])c(N)cc1C(=O)N(C)C
COc1cc(N)c(N)cc1C(=O)N(C)C
null
[C].[Pd]
C(C)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
A suspension of 3.62 g of N,N-dimethyl 5-amino-2-methoxy4-nitrobenzamide and 150 mg of 10 % palladium carbon in 140 ml of ethanol was stirred at 70°-80° C. under a hydrogen atmosphere. After the absorption of hydrogen was completed, the catalyst was removed by filtration, and the filtrate was evaporated to dryness to g...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
[C].[Pd].C(C)O
null
null
COc1cc([N+](=O)[O-])c(N)cc1C(=O)N(C)C>[C].[Pd].C(C)O>COc1cc(N)c(N)cc1C(=O)N(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-669afe21a6c94457b614431828ff5378
CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O>>CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O
C(C)OC(=O)OC1=C(C(C2=CC=CC=C2C1=O)=O)C(=O)OCC>>OC1=C(C(C2=CC=CC=C2C1=O)=O)C(=O)OCC
CCOC(=O)[O:8][C:7]1=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[C:17](=[O:18])[c:16]2[c:11]([cH:12][cH:13][cH:14][cH:15]2)[C:9]1=[O:10]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6]1=[C:7]([OH:8])[C:9](=[O:10])[c:11]2[cH:12][cH:13][cH:14][cH:15][c:16]2[C:17]1=[O:18]
CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O
CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O
null
null
O1CCCC1
Reduction
Hydrolysis or Hydrogenolysis of Carboxylic Esters or Thioesters
1f127acc721d58b85f26233246e4bb998945459af6b424dde9f17c27128b810d
fde344b61345cfd3921c83775cd6c5b93b7c81dba5b2fd728b3eb5fd56fc77ae
O=C1C=CC(=O)c2ccccc21
C-C-O-C(=O)-[O;H0;D2;+0:1]-[C:2](=[C:3](-[C:4](-[#8:5])=[O;D1;H0:6])-[C:7]=[O;D1;H0:8])-[C:9](=[O;D1;H0:10])-[c:11]>>[#8:5]-[C:4](=[O;D1;H0:6])-[C:3](=[C:2](-[OH;D1;+0:1])-[C:9](=[O;D1;H0:10])-[c:11])-[C:7]=[O;D1;H0:8]
null
[]
null
null
null
null
To the tetrahydrofuran solution under water cooling was added a solution of ethyl 3-ethoxycarbonyloxy-1,4-dihydro-1,4-dioxo-2-naphthoate, obtained by the procedure of Referential Example 22(1) using 3.41 g of ethyl 3-hydroxy-1,4-dihydro-1,4-dioxo-2-naphthoate, in 10 ml of tetrahydrofuran. The mixture was stirred at roo...
10.6084/m9.figshare.5104873.v1
null
Carbonic Ester
Enol
null
null
C1=CCc2ccccc2C1
HO-
O1CCCC1
null
null
CCOC(=O)OC1=C(C(=O)OCC)C(=O)c2ccccc2C1=O>O1CCCC1>CCOC(=O)C1=C(O)C(=O)c2ccccc2C1=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-5cc48f0a138a4dc4bcee162880e6a771
C=CC#N.C=CC(CCCCCCCCC)=NO>>C=C(C#N)CCCCCCCCC
C(C=C)#N.CC=1C=CC=CC1C.C(CCCCCCCC)C(C=C)=NO>>C(CCCCCCCC)C(C#N)=C
[CH2:1]=[CH:2][C:3]#[N:4].C=CC(=NO)[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH3:13]>>[CH2:1]=[C:2]([C:3]#[N:4])[CH2:5][CH2:6][CH2:7][CH2:8][CH2:9][CH2:10][CH2:11][CH2:12][CH3:13]
C=CC#N.C=CC(CCCCCCCCC)=NO
C=C(C#N)CCCCCCCCC
null
C(C)C(C(=O)[O-])CCCC.[Cu+2].C(C)C(C(=O)[O-])CCCC
null
C-C Coupling
OtherReaction
fd79b1593b2906913d9dceb9488c568dd9acd9840935e9931bf8c9c472997196
a259f45a344da3183e96d62de08419dd5868237740e0b89dd258fcbc666488fd
null
C=C-C(=N-O)-[CH2;D2;+0:1]-[C:2]-[C:3].[C;D1;H2:4]=[CH;D2;+0:5]-[C:6]#[N;D1;H0:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D3;+0:5](=[C;D1;H2:4])-[C:6]#[N;D1;H0:7]
89
[{"value": 89.0, "product": "C(CCCCCCCC)C(C#N)=C", "details": "PERCENTYIELD", "is_desired": false}]
115
CELSIUS
10
MINUTE
A solution of 80.7 g of acrylonitrile and 5.3 g of copper(II) 2-ethylhexanoate in 250 g or o-xylene was heated to the boil (97° C.), after which 151.5 g of 99% pure alpha-nonylacrolein oxime were added dropwise in the course of 15 minutes, the temperature increasing to 115° C. during the addition. When the addition was...
10.6084/m9.figshare.5104873.v1
null
Vinyl.Vinyl.Oxime
Vinyl
null
null
null
HO-
C(C)C(C(=O)[O-])CCCC.[Cu+2].C(C)C(C(=O)[O-])CCCC
115
0.166667
C=CC#N.C=CC(CCCCCCCCC)=NO>C(C)C(C(=O)[O-])CCCC.[Cu+2].C(C)C(C(=O)[O-])CCCC>C=C(C#N)CCCCCCCCC
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c71aa7c41c254ef8940038a9e76a0288
CN(C)c1ccc(C=NO)cc1>>CN(C)c1ccc(C#N)cc1
C(C=C)#N.CN(C1=CC=C(C=NO)C=C1)C>>CN(C1=CC=C(C#N)C=C1)C
O[N:9]=[CH:8][c:7]1[cH:6][cH:5][c:4]([N:2]([CH3:1])[CH3:3])[cH:11][cH:10]1>>[CH3:1][N:2]([CH3:3])[c:4]1[cH:5][cH:6][c:7]([C:8]#[N:9])[cH:10][cH:11]1
CN(C)c1ccc(C=NO)cc1
CN(C)c1ccc(C#N)cc1
null
C(C)(=O)[O-].[Cu+2].C(C)(=O)[O-]
CC=1C=CC=CC1C
Functional Group Interconversion
OtherReaction
17f476cc256704e312f02cdb730538a4d2e78e129aaed9ef4aa555a9b052c890
9ad4e779dba60265752423413bc1b61ff9562539f91b24f3b3d9205e4bb46232
c1ccccc1
O-[N;H0;D2;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5]>>[N;H0;D1;+0:1]#[C;H0;D2;+0:2]-[c:3](:[c:4]):[c:5]
90.4
[{"value": 90.0, "product": "CN(C1=CC=C(C#N)C=C1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 90.4, "product": "CN(C1=CC=C(C#N)C=C1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
135
CELSIUS
8
HOUR
A solution of 53 g of acrylonitrile and 1.0 g of copper(II) acetate in 100 g of o-xylene was heated to the boil (85° C.), after which a solution of 82 g of p-dimethylaminobenzaldoxime in 110 g of o-xylene was added dropwise by heating further. During the addition, the boiling point of the reaction mixture increased to ...
10.6084/m9.figshare.5104873.v1
null
Oxime
Nitrile
null
null
c1ccccc1
HO-
C(C)(=O)[O-].[Cu+2].C(C)(=O)[O-].CC=1C=CC=CC1C
135
8
CN(C)c1ccc(C=NO)cc1>C(C)(=O)[O-].[Cu+2].C(C)(=O)[O-].CC=1C=CC=CC1C>CN(C)c1ccc(C#N)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-32ae5c7ca03e4dc381e964a85ea45d07
CCCCCCOc1ccc(CCC(=O)Cl)cc1.Oc1ccc(-c2ccc(F)cc2)cc1>>CCCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(F)cc3)cc2)cc1
OC1=CC=C(C=C1)C1=CC=C(C=C1)F.N1=CC=CC=C1.C(CCCCC)OC1=CC=C(C=C1)CCC(=O)Cl>>CC(C(=O)OC1=CC=C(C=C1)C1=CC=C(C=C1)F)CC1=CC=C(C=C1)OCCCCCC
Cl[C:15]([CH2:13][CH2:12][c:11]1[cH:10][cH:9][c:8]([O:7][CH2:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:32][cH:31]1)=[O:16].[OH:17][c:18]1[cH:19][cH:20][c:21](-[c:22]2[cH:23][cH:24][c:25]([F:26])[cH:27][cH:28]2)[cH:29][cH:30]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][O:7][c:8]1[cH:9][cH:10][c:11]([CH2:12][CH:13]([CH3...
CCCCCCOc1ccc(CCC(=O)Cl)cc1.Oc1ccc(-c2ccc(F)cc2)cc1
CCCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(F)cc3)cc2)cc1
null
null
O
Acylation
OtherReaction
1cda078f55e64d9385e544d1067595d5e7672bbd1eff542e7a341817a2d8c4d5
6439fc27f97ee9ed7c11ef9b5032d9493d05f28a7bbb50d256a2d54d035fbfb2
O=C(CCc1ccccc1)Oc1ccc(-c2ccccc2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[C:4]-[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[C;D1;H3:10]-[CH;D3;+0:3](-[C:4]-[c:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
48
[{"value": 48.0, "product": "CC(C(=O)OC1=CC=C(C=C1)C1=CC=C(C=C1)F)CC1=CC=C(C=C1)OCCCCCC", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
4-Hydroxy-4'-fluorobiphenyl (2.1 g, 0.012 mol) was dissolved in pyridine (10 ml), and to the solution was added β-(4-hexyloxyphenyl)propionic acid chloride (3.0 g, 0.01 mol) with sufficient shaking, followed by allowing the resulting reaction solution to stand overnight, thereafter pouring it in water (100 ml), extract...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccccc1.c1ccccc1
null
O
null
8
CCCCCCOc1ccc(CCC(=O)Cl)cc1.Oc1ccc(-c2ccc(F)cc2)cc1>O>CCCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(F)cc3)cc2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-149cf621368447ca9478e75c0d11594b
CCCCCOc1ccc(CCC(=O)Cl)cc1.CCCc1ccc(-c2ccc(O)cc2)cc1>>CCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(CCC)cc3)cc2)cc1
OC1=CC=C(C=C1)C1=CC=C(C=C1)CCC.N1=CC=CC=C1.C(CCCC)OC1=CC=C(C=C1)CCC(=O)Cl>>CC(C(=O)OC1=CC=C(C=C1)C1=CC=C(C=C1)CCC)CC1=CC=C(C=C1)OCCCCC
Cl[C:14]([CH2:12][CH2:11][c:10]1[cH:9][cH:8][c:7]([O:6][CH2:5][CH2:4][CH2:3][CH2:2][CH3:1])[cH:33][cH:32]1)=[O:15].[OH:16][c:17]1[cH:18][cH:19][c:20](-[c:21]2[cH:22][cH:23][c:24]([CH2:25][CH2:26][CH3:27])[cH:28][cH:29]2)[cH:30][cH:31]1>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][O:6][c:7]1[cH:8][cH:9][c:10]([CH2:11][CH:12]([C...
CCCCCOc1ccc(CCC(=O)Cl)cc1.CCCc1ccc(-c2ccc(O)cc2)cc1
CCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(CCC)cc3)cc2)cc1
null
null
O
Acylation
OtherReaction
1cda078f55e64d9385e544d1067595d5e7672bbd1eff542e7a341817a2d8c4d5
6439fc27f97ee9ed7c11ef9b5032d9493d05f28a7bbb50d256a2d54d035fbfb2
O=C(CCc1ccccc1)Oc1ccc(-c2ccccc2)cc1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH2;D2;+0:3]-[C:4]-[c:5].[OH;D1;+0:6]-[c:7](:[c:8]):[c:9]>>[C;D1;H3:10]-[CH;D3;+0:3](-[C:4]-[c:5])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:6]-[c:7](:[c:8]):[c:9]
null
[]
null
null
8
HOUR
4-Hydroxy-4'-propylbiphenyl (2.5 g, 0.012 mol) was dissolved in pyridine (10 ml) and to the solution was added β-(4-pentyloxyphenyl)propionic acid chloride (2.5 g, 0.01 mol) with sufficient shaking, followed by allowing the resulting reaction solution to stand overnight, pouring it in water (100 ml), extracting the res...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Aromatic alcohol
Ester
null
null
c1ccccc1.c1ccccc1.c1ccccc1
null
O
null
8
CCCCCOc1ccc(CCC(=O)Cl)cc1.CCCc1ccc(-c2ccc(O)cc2)cc1>O>CCCCCOc1ccc(CC(C)C(=O)Oc2ccc(-c3ccc(CCC)cc3)cc2)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-872ec79cdd2e42ecb9a3d4b0e647897d
BrCCc1cccc(Br)c1Br>>BrC(Br)=Cc1ccccc1
BrCCC=1C(=C(C=CC1)Br)Br.[OH-].[Na+].[Br-].C(C)[N+](CCCCC)(CC)CC>>BrC(=CC1=CC=CC=C1)Br
Br[c:9]1[cH:8][cH:7][cH:6][c:5]([CH2:4][CH2:2][Br:1])[c:10]1[Br:3]>>[Br:1][C:2]([Br:3])=[CH:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1
BrCCc1cccc(Br)c1Br
BrC(Br)=Cc1ccccc1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
84b153b3b69ebce5def9af64ea344141980bb8d9e401ce4573d6e309559af488
5b120c389fcf30b9aa92d3fab7f855f7a7447308c566c8fdec7d2a54cd05faa5
c1ccccc1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5](-[CH2;D2;+0:6]-[CH2;D2;+0:7]-[Br;D1;H0:8]):[c;H0;D3;+0:9]:1-[Br;H0;D1;+0:10]>>[Br;D1;H0:8]-[C;H0;D3;+0:7](-[Br;H0;D1;+0:10])=[CH;D2;+0:6]-[c:5]1:[c:4]:[c:3]:[c:2]:[cH;D2;+0:1]:[cH;D2;+0:9]:1
null
[]
null
null
null
null
A solution of 147.90 g. (0.431 mole) of 2-bromoethyldibromobenzene in 250 ml. of methylene chloride was stirred for 7 ks (2 hours) at 5 Hz (300 rpm) at 313 K. (40° C.) with 150 g (2.25 mole) of 60 percent sodium hydroxide solution and 3.12 g. (0.0124 mole) of triethylpentyl ammonium bromide. The product was washed with...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aromatic halide.Primary halide
Alkenyl halide.Alkenyl halide
c1ccccc1
c1ccccc1
c1ccccc1
HBr
C(Cl)Cl
null
null
BrCCc1cccc(Br)c1Br>C(Cl)Cl>BrC(Br)=Cc1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d281ede4768c447887f8d1e077b75f5f
CC(=O)CCCCO[Si](C)(C)C(C)(C)C.CC1(C)OCC(CC=O)O1>>CC1(C)OCC(CC(O)CC(=O)CCCCO[Si](C)(C)C(C)(C)C)O1
C(CCC)[Li].CCCCCC.C(C)(C)NC(C)C.[Si](C)(C)(C(C)(C)C)OCCCCC(C)=O.CC1(OCC(O1)CC=O)C>>[Si](C)(C)(C(C)(C)C)OCCCCC(CC(CC1OC(OC1)(C)C)O)=O
[CH3:10][C:11](=[O:12])[CH2:13][CH2:14][CH2:15][CH2:16][O:17][Si:18]([CH3:19])([CH3:20])[C:21]([CH3:22])([CH3:23])[CH3:24].[CH3:1][C:2]1([CH3:3])[O:4][CH2:5][CH:6]([CH2:7][CH:8]=[O:9])[O:25]1>>[CH3:1][C:2]1([CH3:3])[O:4][CH2:5][CH:6]([CH2:7][CH:8]([OH:9])[CH2:10][C:11](=[O:12])[CH2:13][CH2:14][CH2:15][CH2:16][O:17][Si:...
CC(=O)CCCCO[Si](C)(C)C(C)(C)C.CC1(C)OCC(CC=O)O1
CC1(C)OCC(CC(O)CC(=O)CCCCO[Si](C)(C)C(C)(C)C)O1
null
null
O.C1CCOC1
C-C Coupling
OtherReaction
d08eb7b2615717189cce315501bb2cfa7ee3668e6d8eaa24218b092d1454a850
7d7139092067ff475e8e8a4ad6adb4833600ca969e282ed08dc56c016dccb864
C1COCO1
[#8:1]-[C:2]-[C:3]-[CH;D2;+0:4]=[O;H0;D1;+0:5].[C:6]-[C:7](-[CH3;D1;+0:8])=[O;D1;H0:9]>>[#8:1]-[C:2]-[C:3]-[CH;D3;+0:4](-[OH;D1;+0:5])-[CH2;D2;+0:8]-[C:7](-[C:6])=[O;D1;H0:9]
null
[]
null
null
20
MINUTE
A solution of n-butyl lithium in hexane (119 ml, 1.6M, 0.19 mol) is added dropwise to a solution of diisopropylamine (19.3 g, 0.191 mol) in THF (100 ml) cooled in an ice bath. After the addition, the mixture is stirred for 20 minutes then cooled to -78°. A solution of 6-t-butyldimethylsilyloxy-hexan-2-one (40.0 g, 0.17...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Ketone
Ketone.Secondary alcohol
null
null
C1COCO1
null
O.C1CCOC1
null
0.333333
CC(=O)CCCCO[Si](C)(C)C(C)(C)C.CC1(C)OCC(CC=O)O1>O.C1CCOC1>CC1(C)OCC(CC(O)CC(=O)CCCCO[Si](C)(C)C(C)(C)C)O1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b1c8ce92ad7041c4bfcaac9c619c0317
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1>>C/C(=C\O)CCC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
CC(C)C[AlH]CC(C)C.CC(C)(C)[SiH2]OC1CC(OC2(C1)OCCCC2)C/C=C(/C(=O)OCC)\C.C(C)(=O)OCC.CCCCCC.CO>>CC(C)(C)[SiH2]OC1CC(OC2(C1)OCCCC2)CC/C(=C/O)/C
CCO[C:3](/[C:2]([CH3:1])=[CH:5]/[CH2:6][CH:7]1[CH2:8][CH:9]([O:10][SiH2:11][C:12]([CH3:13])([CH3:14])[CH3:15])[CH2:16][C:17]2([CH2:18][CH2:19][CH2:20][CH2:21][O:22]2)[O:23]1)=[O:4]>>[CH3:1]/[C:2](=[CH:3]\[OH:4])[CH2:5][CH2:6][CH:7]1[CH2:8][CH:9]([O:10][SiH2:11][C:12]([CH3:13])([CH3:14])[CH3:15])[CH2:16][C:17]2([CH2:18]...
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
C/C(=C\O)CCC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
null
null
C(Cl)Cl
Miscellaneous
OtherReaction
376e540652952c6e822fc93ca8a82f0b5972de8286f641931ad175283484e914
7b120640ba088dcf1d992af005dc3b1a94f9ed638ceed084bca0b30ee3d1d840
C1CCC2(CCCCO2)OC1
C-C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])/[C;H0;D3;+0:3](-[C;D1;H3:4])=[CH;D2;+0:5]/[C:6]-[C:7]-[#8:8]>>[#8:8]-[C:7]-[C:6]-[CH2;D2;+0:5]/[C;H0;D3;+0:3](-[C;D1;H3:4])=[CH;D2;+0:1]/[OH;D1;+0:2]
null
[]
null
null
null
null
A solution of 1M DIBAL (155 ml; 155 mmoles) is added dropwise to a solution of ethyl 4-[4-[(1,1-dimethylethyl)silyl]oxy-1,7-dioxaspiro[5.5]undec-2-yl]-2-methyl-2E-butenoate, (29.0 g; 70.3 mmoles) in methylene chloride (350 ml) with stirring under nitrogen at -78°. Upon completion of the addition, the reaction mixture i...
10.6084/m9.figshare.5104873.v1
null
Ester
Enol
null
null
C1CCC2(CCCCO2)OC1
HO-
C(Cl)Cl
null
null
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1>C(Cl)Cl>C/C(=C\O)CCC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-97558f66ea4445e291a3e8e538aec74a
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1>>C/C(C=O)=C\CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
CC(C)(C)[SiH2]OC1CC(OC2(C1)OCCCC2)C/C=C(/C(=O)OCC)\C.[Cr](=O)(=O)([O-])Cl.[NH+]1=CC=CC=C1>>CC(C)(C)[SiH2]OC1CC(OC2(C1)OCCCC2)C/C=C(/C=O)\C
CCO[C:3](/[C:2]([CH3:1])=[CH:5]/[CH2:6][CH:7]1[CH2:8][CH:9]([O:10][SiH2:11][C:12]([CH3:13])([CH3:14])[CH3:15])[CH2:16][C:17]2([CH2:18][CH2:19][CH2:20][CH2:21][O:22]2)[O:23]1)=[O:4]>>[CH3:1]/[C:2]([CH:3]=[O:4])=[CH:5]\[CH2:6][CH:7]1[CH2:8][CH:9]([O:10][SiH2:11][C:12]([CH3:13])([CH3:14])[CH3:15])[CH2:16][C:17]2([CH2:18][...
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
C/C(C=O)=C\CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
null
null
CCOCC.C(Cl)Cl
Reduction
OtherReaction
ec1c6c64dd9be73981e5a6c952ab740869d298b20e87e097e88e1179cc5bc6dc
33ddc7b9457742ba0a376f08a972e4f33779267f6f1fe15e3be786427ae9f4ec
C1CCC2(CCCCO2)OC1
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](-[C;D1;H3:4])=[C:5]/[C:6]-[C:7]-[#8:8]>>[#8:8]-[C:7]-[C:6]/[C:5]=[C:3](\[C;D1;H3:4])-[CH;D2;+0:1]=[O;D1;H0:2]
null
[]
null
null
null
null
To a solution of ethyl 4-[4-[(1,1-dimethylethyl)silyl]oxy-1,7-dioxaspiro[5.5]undec-2-yl]-2-methyl-2E-butenoate, (10.0 g; 27.0 mmoles) in methylene chloride (160 ml) is added finely powdered pyridinium chlorochromate (PCC; 8.7 g; 40.5 mmoles) in a single portion with stirring under nitrogen at 25°. After twenty minutes ...
10.6084/m9.figshare.5104873.v1
null
Ester
Aldehyde
null
null
C1CCC2(CCCCO2)OC1
HO-
CCOCC.C(Cl)Cl
null
null
CCOC(=O)/C(C)=C/CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1>CCOCC.C(Cl)Cl>C/C(C=O)=C\CC1CC(O[SiH2]C(C)(C)C)CC2(CCCCO2)O1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-af9b398431b84c62bf61834b7fe891d4
O=C(NCCCC[C@H](OP(=O)(O)C(Cc1ccccc1)OC(=O)c1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1)OCc1ccccc1>>O=C(OCc1ccccc1)[C@@H]1CCCN1
C(C1=CC=CC=C1)(=O)OC(CC1=CC=CC=C1)P(=O)(O[C@H](C(=O)N1[C@H](C(=O)OCC2=CC=CC=C2)CCC1)CCCCNC(=O)OCC1=CC=CC=C1)O.ClCCC(C(=O)[O-])(C)C.ClCCC(C(=O)[O-])(C)C.C([O-])([O-])=O.[K+].[K+]>>N1[C@H](C(=O)OCC2=CC=CC=C2)CCC1
O=C(NCCCC[C@H](OP(=O)(O)C(Cc1ccccc1)OC(=O)c1ccccc1)C(=O)[N:15]1[C@H:11]([C:2](=[O:1])[O:3][CH2:4][c:5]2[cH:6][cH:7][cH:8][cH:9][cH:10]2)[CH2:12][CH2:13][CH2:14]1)OCc1ccccc1>>[O:1]=[C:2]([O:3][CH2:4][c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1)[C@@H:11]1[CH2:12][CH2:13][CH2:14][NH:15]1
O=C(NCCCC[C@H](OP(=O)(O)C(Cc1ccccc1)OC(=O)c1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1)OCc1ccccc1
O=C(OCc1ccccc1)[C@@H]1CCCN1
null
null
CN(C=O)C.C(C)(=O)OCC
Reduction
Hydrogenolysis of tertiary amines
f88b1249c2b143fc5d85cf9dcec02127d48320f42bb4a811327e633d965756da
0149663aa25bdac246afd8acdcdc0f22a7ea1635947435099953c93482349ddc
O=C(OCc1ccccc1)[C@@H]1CCCN1
O-P(=O)(-O-[C@H](-C-C-C-C-N-C(=O)-O-C-c1:c:c:c:c:c:1)-C(=O)-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[C:4]-[C:5]-1-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9])-C(-C-c1:c:c:c:c:c:1)-O-C(=O)-c1:c:c:c:c:c:1>>[C:9]-[#8:8]-[C:6](=[O;D1;H0:7])-[C:5]1-[C:4]-[C:3]-[C:2]-[NH;D2;+0:1]-1
null
[]
null
null
8
HOUR
1-[(S)-2-[[[1-(Benzoyloxy)-2-phenylethyl]hydroxyphosphinyl]oxy]-1-oxo-6-[[(phenylmethoxy)carbonyl]amino]hexyl]-L-proline, phenylmethyl ester from Example 5(d) is suspended in dry dimethylformamide and treated with chloromethylpivalate. After several hours, additional chloromethylpivalate and anhydrous potassium carbona...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ester.Ether.Tertiary amide
Secondary amine
c1ccccc1.c1ccccc1.C1CC[NH]C1.c1ccccc1
C1CCNC1
c1ccccc1.C1CCNC1
HO-
CN(C=O)C.C(C)(=O)OCC
null
8
O=C(NCCCC[C@H](OP(=O)(O)C(Cc1ccccc1)OC(=O)c1ccccc1)C(=O)N1CCC[C@H]1C(=O)OCc1ccccc1)OCc1ccccc1>CN(C=O)C.C(C)(=O)OCC>O=C(OCc1ccccc1)[C@@H]1CCCN1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6bd97a4a77f74b30bd8dfa2238b52eb2
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C1=CC=CC=C1)=O.C(CCC)[Li].C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.Cl>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.[CH:13](=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
CCCCCC.COCCOC.C(C)OCC
C-C Coupling
OtherReaction
3ebd6f16ba89cc360449fd30ab34ced1781fbed4a414d9e59bcf754777378132
2f319ce34b90d24c5ffbe402ed9c6fde7375d736dd872cea5121694203d4c1fd
[CH]=C(CC1CCCCC1)c1ccccc1
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]):c(-C(-C)-C):c:1.[O;H0;D1;+0:8]=[CH;D2;+0:9]-[c;H0;D3;+0:10]1:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:1>>[#7:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[CH;D3;+0:9](-[OH;D1;+0:8])-[CH;D3;+0...
null
[]
0
CELSIUS
15
MINUTE
A 1.5M solution (29 cc) of n-butyllithium in hexane is added to a solution of β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (9.15 g) in 1,2-dimethoxyethane (100 cc) kept under a nitrogen atmosphere at a temperature in the region of -75° C. The orange solution obtained is then stirred for 15 m...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
CCCCCC.COCCOC.C(C)OCC
0
0.25
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1>CCCCCC.COCCOC.C(C)OCC>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-834831151d84462eb2ebc4e92790c02c
CCN(CC)CCC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(CC)CC)C1=CC=CC=C1.C(C1=CC=CC=C1)=O>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH2:1]C)[CH2:3]C)[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.[CH:13](=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH...
CCN(CC)CCC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
3ebd6f16ba89cc360449fd30ab34ced1781fbed4a414d9e59bcf754777378132
2f319ce34b90d24c5ffbe402ed9c6fde7375d736dd872cea5121694203d4c1fd
[CH]=C(CC1CCCCC1)c1ccccc1
C-[CH2;D2;+0:1]-[#7:2](-[C:3]-[CH2;D2;+0:4]-[C;H0;D3;+0:5](=N-N-S(=O)(=O)-c1:c(-C(-C)-C):c:c(-C(-C)-C):c:c:1-C(-C)-C)-[c:6](:[c:7]):[c:8])-[CH2;D2;+0:9]-C.[O;H0;D1;+0:10]=[CH;D2;+0:11]-[c;H0;D3;+0:12]1:[cH;D2;+0:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:1>>[CH3;D1;+0:1]-[#7:2](-[CH3;D1;+0:9])-[C:3]-[C...
null
[]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-diethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (30 g) and benzaldehyde (6.9 cc), 4-diethylamino-1,2-diphenyl-2-buten-1-ol (Z) hydrochloride (3.2 g) is obtained, after recrystallisation from acetone, in the form of whit...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
null
null
null
CCN(CC)CCC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3db90bb8ed7d4a83b2cd6d140be26831
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN2CCCC2)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN1CCCC1)C1=CC=CC=C1.C(C1=CC=CC=C1)=O>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]2[CH2:1]CC[CH2:3]2)[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.[CH:13](=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN2CCCC2)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
c45b75d201fa0fc63b5af89abaf2e5cd11b5109f3038ca7df05c17bfe01224db
2f319ce34b90d24c5ffbe402ed9c6fde7375d736dd872cea5121694203d4c1fd
[CH]=C(CC1CCCCC1)c1ccccc1
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4]2-[CH2;D2;+0:5]-C-C-[CH2;D2;+0:6]-2)-[c:7](:[c:8]):[c:9]):c(-C(-C)-C):c:1.[O;H0;D1;+0:10]=[CH;D2;+0:11]-[c;H0;D3;+0:12]1:[cH;D2;+0:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:1>>[CH3;D1;+0:5]-[#7:4](-[CH3;D1;+0:6])-[C:3]...
null
[]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-(1-pyrrolidinyl)propiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g), and benzaldehyde (4.6 cc), 1,2-diphenyl-4-(1-pyrrolidinyl)-2-buten-1-ol (Z) hydrochloride (9.9 g) is obtained, after recrystallisation from a mixture of 2-prop...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde
Secondary alcohol
c1ccccc1.C1CC[NH]C1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN2CCCC2)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-48017fd73a1c4f57ad670594cebf5361
CNC1C=C(c2ccccc2)C(c2ccccc2)O1.CO>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
[BH4-].[Na+].C1(=CC=CC=C1)C1OC(C=C1C1=CC=CC=C1)NC.CO>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
[CH3:1][NH:2][CH:4]1[CH:5]=[C:6]([c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[CH:13]([c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[O:14]1.O[CH3:3]>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]1
CNC1C=C(c2ccccc2)C(c2ccccc2)O1.CO
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
ac9840b6515733b11f214a4630f191bc01cc9e09bc9ae80f0e97909cad33ebfc
6ef7e83d526b7eb20c61e46462d34cb565cd38bffa4c0faa2c98debacd425740
[CH]=C(CC1CCCCC1)c1ccccc1
O-[CH3;D1;+0:1].[C;D1;H3:2]-[NH;D2;+0:3]-[CH;D3;+0:4]1-[C:5]=[C:6](-[c:7])-[C:8](-[c;H0;D3;+0:9]2:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:2)-[O;H0;D2;+0:15]-1>>[C;D1;H3:2]-[N;H0;D3;+0:3](-[CH3;D1;+0:1])-[CH2;D2;+0:4]-[C:5]=[C:6](-[c:7])-[C:8](-[OH;D1;+0:15])-[CH;D3;+0:9]1-[CH2;D2;+0:10]-[C...
null
[]
20
CELSIUS
18
HOUR
Sodium borohydride (10.3 g) is added over approximately 30 minutes at a temperature in the region of 5° C. to a solution of 2,3-diphenyl-5-methylamino-2,5-dihydrofuran (9.7 g) in methanol (90 cc) and distilled water (10 cc). The reaction mixture is then stirred for 18 hours at a temperature in the region of 20° C., and...
10.6084/m9.figshare.5104873.v1
null
Ether.Secondary amine.Methanol
Secondary alcohol.Tertiary amine
C1=CCOC1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
Other
null
20
18
CNC1C=C(c2ccccc2)C(c2ccccc2)O1.CO>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-475f9554de1148c0944b4557eb4b3965
Cl>>Cl
C1(=CC=CC=C1)C1OC(C=C1C1=CC=CC=C1)NC.[H-].[Na+].Cl.C1(=CC=CC=C1)C(=O)C(O)C1=CC=CC=C1.CN=CCP(OCC)(OCC)=O>>Cl.C1(=CC=CC=C1)C1OC(C=C1C1=CC=CC=C1)NC
[ClH:20]>>[ClH:20]
Cl
Cl
null
null
O1CCCC1.O.C(C)(=O)OCC.C(C)OCC
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
20
CELSIUS
30
MINUTE
2,3-Diphenyl-5-methylamino-2,5-dihydrofuran can be prepared as follows: benzoin (29.7 g) dissolved in tetrahydrofuran (400 cc) is added to a suspension of sodium hydride (3.4 g) in tetrahydrofuran (50 cc) kept under a nitrogen atmosphere at a temperature in the region of 0° C., and the reaction mixture is stirred for 3...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
O1CCCC1.O.C(C)(=O)OCC.C(C)OCC
20
0.5
Cl>O1CCCC1.O.C(C)(=O)OCC.C(C)OCC>Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2bec0db7777d45418f92d4f32b0400dd
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
P(=O)(Cl)(Cl)Cl.CN(C=CC(=O)C1=CC=CC=C1)C.C1(=CC=CC=C1)S.[OH-].[Na+].C(#N)[BH3-].[Na+].Cl>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]1
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
O.C(C)N(CC)CC.C(Cl)(Cl)Cl.CO.C(Cl)Cl.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
d3753080378e8b20b0eab8cb0647dcbd1c690dba65847cdc72439e586f418fa6
7190e6f5f02f53d96c757c88d1ed0b3f7706d003dbd95bb86d4860d15fd3d555
[CH]=C(CC1CCCCC1)c1ccccc1
S-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:1.[C;D1;H3:7]-[#7:8](-[C;D1;H3:9])-[CH;D2;+0:10]=[CH;D2;+0:11]-[C;H0;D3;+0:12](=[O;H0;D1;+0:13])-[c:14](:[c:15]):[c:16]>>[C;D1;H3:7]-[#7:8](-[C;D1;H3:9])-[CH2;D2;+0:10]-[CH;D2;+0:11]=[C;H0;D3;+0:12](-[C:17](-[OH;D1;+0:13])-[CH;D3;+0:1]1-...
null
[]
0
CELSIUS
15
MINUTE
Phosphorus oxychloride (2.5 cc) dissolved in methylene chloride (6 cc) is added dropwise at 0° C. to a solution of 3-dimethylaminoacrylophenone (5 g) in methylene chloride (16 cc). After stirring for 15 minutes at 0° C. and then 30 minutes at 20° C., the temperature is again brought down to 0° C. The precipitate formed...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Aromatic thiol
Secondary alcohol
c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
null
O.C(C)N(CC)CC.C(Cl)(Cl)Cl.CO.C(Cl)Cl.C(C)OCC
0
0.25
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1>O.C(C)N(CC)CC.C(Cl)(Cl)Cl.CO.C(Cl)Cl.C(C)OCC>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4d74cf0142914f1a99f632065fe19ea0
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1>>CN(C)CC=C(Sc1ccccc1)c1ccccc1
CN(C=CC(=O)C1=CC=CC=C1)C.C1(=CC=CC=C1)S.C(#N)[BH3-].[Na+]>>CN(CC=C(SC1=CC=CC=C1)C1=CC=CC=C1)C
O=[C:6]([CH:5]=[CH:4][N:2]([CH3:1])[CH3:3])[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1.[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][cH:17][cH:18][cH:19]1
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1
CN(C)CC=C(Sc1ccccc1)c1ccccc1
null
null
P(=O)(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
4762356a283a4dd15b9c6c402bec2a8d06b05d6260a2333b5a6b92e7043303a0
102db1557e8988ecf5e34231cc3ffb434e574fba60712f7d6b62030e75389393
[CH]=C(Sc1ccccc1)c1ccccc1
O=[C;H0;D3;+0:1](-[CH;D2;+0:2]=[CH;D2;+0:3]-[#7:4](-[C;D1;H3:5])-[C;D1;H3:6])-[c:7](:[c:8]):[c:9].[SH;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C;D1;H3:5]-[#7:4](-[C;D1;H3:6])-[CH2;D2;+0:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[S;H0;D2;+0:10]-[c:11](:[c:12]):[c:13])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (80 g), phosphorus oxychloride (40 cc), thiophenol (50.3 cc) and sodium cyanoborohydride (16 g), and crystallising the (Z)-isomer, a yellow solid is isolated after evaporation of the mother liquors under reduced pr...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Aromatic thiol
Monosulfide
null
null
c1ccccc1.c1ccccc1
Other
P(=O)(Cl)(Cl)Cl
null
null
CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1>P(=O)(Cl)(Cl)Cl>CN(C)CC=C(Sc1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-76c9e3d8f8064427b92e1694b802ac91
CCO.CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Cl)cc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(#N)[BH3-].[Na+].C(C)O.CN(C=CC(=O)C1=CC=CC=C1)C.P(=O)(Cl)(Cl)Cl.Cl.ClC1=CC=C(C=C1)S>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
O[CH2:17][CH3:16].[CH3:1][N:2]([CH3:3])[CH:5]=[CH:6][C:13](=[O:14])[c:15]1[cH:12][cH:11][cH:10][cH:9][cH:20]1.S[c:7]1cc[c:18](Cl)[cH:19][cH:8]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]1
CCO.CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Cl)cc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
405a039f51659caa1e8c43958e23f806a037c4c59238574dcd8dcbc4faa45ced
54947926ef1b05f1c941996ef79177c8404f5f26356adf51e3a232e3b2392eab
[CH]=C(CC1CCCCC1)c1ccccc1
Cl-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[c;H0;D3;+0:4](-S):c:c:1.O-[CH2;D2;+0:5]-[CH3;D1;+0:6].[C;D1;H3:7]-[N;H0;D3;+0:8](-[C;D1;H3:9])-[CH;D2;+0:10]=[CH;D2;+0:11]-[C;H0;D3;+0:12](=[O;H0;D1;+0:13])-[c;H0;D3;+0:14]1:[cH;D2;+0:15]:[c:16]:[c:17]:[cH;D2;+0:18]:[cH;D2;+0:19]:1>>[C;D1;H3:7]-[N;H0;D3;+0:8](-[C;D1;H3:9])-...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (5 g), phosphorus oxychloride (2.5 cc), p-chlorothiophenol (4.13 g) and sodium cyanoborohydride (1 g), and after evaporating the reaction mixture under reduced pressure (2.7 kPa) at 40° C., a residue is obtained, w...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone.Primary alcohol.Aromatic thiol
Secondary alcohol.Tertiary amine
c1ccccc1.c1ccccc1
c1ccccc1.C1CCCCC1
c1ccccc1.C1CCCCC1
Other
C(C)OCC
null
null
CCO.CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Cl)cc1>C(C)OCC>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-f4d74320692a4dfaa4096e7c39523c9c
CN(C)C=CC(=O)c1ccccc1.Sc1ccncc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(#N)[BH3-].[Na+].P(=O)(Cl)(Cl)Cl.SC1=CC=NC=C1.Cl.CN(C=CC(=O)C1=CC=CC=C1)C.C(C(=O)O)(=O)O>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:15]1[cH:16][cH:17]n[cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]1
CN(C)C=CC(=O)c1ccccc1.Sc1ccncc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
O.C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
da58b9b01ed6d9c6b3cf459555d1b76f311474cd5082f582d3af10df6ccbb5b8
7190e6f5f02f53d96c757c88d1ed0b3f7706d003dbd95bb86d4860d15fd3d555
[CH]=C(CC1CCCCC1)c1ccccc1
S-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:n:[cH;D2;+0:4]:[cH;D2;+0:5]:1.[C;D1;H3:6]-[#7:7](-[C;D1;H3:8])-[CH;D2;+0:9]=[CH;D2;+0:10]-[C;H0;D3;+0:11](=[O;H0;D1;+0:12])-[c:13](:[c:14]):[c:15]>>[C;D1;H3:6]-[#7:7](-[C;D1;H3:8])-[CH2;D2;+0:9]-[CH;D2;+0:10]=[C;H0;D3;+0:11](-[C:16](-[OH;D1;+0:12])-[CH;D3;+0:1]1-[CH2;D2;+0:2]...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (10 g), phosphorus oxychloride (5 cc), 4-mercaptopyridine (6.35 g) and sodium cyanoborohydride (2 g), a chestnut-coloured residue is obtained which is taken up in water (100 cc). The solution is acidified to pH 2 b...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Aromatic thiol
Secondary alcohol
c1ccncc1
C1CCCCC1
c1ccccc1.C1CCCCC1
null
O.C(C)O
null
null
CN(C)C=CC(=O)c1ccccc1.Sc1ccncc1>O.C(C)O>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3065eef9ebf54707a979828bb3decf18
CN(C)C=CC(=O)c1ccc(F)cc1.Sc1ccccc1>>CN(C)CC=C(Sc1ccccc1)c1ccc(F)cc1
FC1=CC=C(C=C1)C(C=CN(C)C)=O.Cl.[OH-].[Na+].C1(=CC=CC=C1)S.C(#N)[BH3-].[Na+].P(=O)(Cl)(Cl)Cl>>CN(CC=C(SC1=CC=CC=C1)C1=CC=C(C=C1)F)C
O=[C:6]([CH:5]=[CH:4][N:2]([CH3:1])[CH3:3])[c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1.[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][c:17]([F:18])[cH:19][cH:20]1
CN(C)C=CC(=O)c1ccc(F)cc1.Sc1ccccc1
CN(C)CC=C(Sc1ccccc1)c1ccc(F)cc1
null
null
C(Cl)(Cl)Cl.C(C)(C)O.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
4762356a283a4dd15b9c6c402bec2a8d06b05d6260a2333b5a6b92e7043303a0
102db1557e8988ecf5e34231cc3ffb434e574fba60712f7d6b62030e75389393
[CH]=C(Sc1ccccc1)c1ccccc1
O=[C;H0;D3;+0:1](-[CH;D2;+0:2]=[CH;D2;+0:3]-[#7:4](-[C;D1;H3:5])-[C;D1;H3:6])-[c:7](:[c:8]):[c:9].[SH;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C;D1;H3:5]-[#7:4](-[C;D1;H3:6])-[CH2;D2;+0:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[S;H0;D2;+0:10]-[c:11](:[c:12]):[c:13])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 1-(4-fluorophenyl)-3-dimethylamino-2-propen-1-one (10 g), phosphorus oxychloride (4.76 cc), thiophenol (5.57 cc) and sodium cyanoborohydride (1.92 g), a residue is obtained which is taken up in chloroform. The solution is then adjusted to pH 1...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Aromatic thiol
Monosulfide
null
null
c1ccccc1.c1ccccc1
Other
C(Cl)(Cl)Cl.C(C)(C)O.C(C)OCC
null
null
CN(C)C=CC(=O)c1ccc(F)cc1.Sc1ccccc1>C(Cl)(Cl)Cl.C(C)(C)O.C(C)OCC>CN(C)CC=C(Sc1ccccc1)c1ccc(F)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-cf43cabef56e42ff831c0043b831c695
CN(C)C=CC(=O)c1ccc(Br)cc1.Sc1ccccc1>>CN(C)CC=C(Sc1ccccc1)c1ccc(Br)cc1
BrC1=CC=C(C=C1)C(C=CN(C)C)=O.[OH-].[Na+].C1(=CC=CC=C1)S.C(#N)[BH3-].[Na+].Cl.P(=O)(Cl)(Cl)Cl>>BrC1=CC=C(C=C1)C(=CCN(C)C)SC1=CC=CC=C1
O=[C:6]([CH:5]=[CH:4][N:2]([CH3:1])[CH3:3])[c:14]1[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]1.[SH:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([S:7][c:8]1[cH:9][cH:10][cH:11][cH:12][cH:13]1)[c:14]1[cH:15][cH:16][c:17]([Br:18])[cH:19][cH:20]1
CN(C)C=CC(=O)c1ccc(Br)cc1.Sc1ccccc1
CN(C)CC=C(Sc1ccccc1)c1ccc(Br)cc1
null
null
CCOCC.C(Cl)(Cl)Cl.C(C)(C)O
Heteroatom Alkylation and Arylation
OtherReaction
4762356a283a4dd15b9c6c402bec2a8d06b05d6260a2333b5a6b92e7043303a0
102db1557e8988ecf5e34231cc3ffb434e574fba60712f7d6b62030e75389393
[CH]=C(Sc1ccccc1)c1ccccc1
O=[C;H0;D3;+0:1](-[CH;D2;+0:2]=[CH;D2;+0:3]-[#7:4](-[C;D1;H3:5])-[C;D1;H3:6])-[c:7](:[c:8]):[c:9].[SH;D1;+0:10]-[c:11](:[c:12]):[c:13]>>[C;D1;H3:5]-[#7:4](-[C;D1;H3:6])-[CH2;D2;+0:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[S;H0;D2;+0:10]-[c:11](:[c:12]):[c:13])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 1-(4-bromophenyl)-3-dimethylamino-2-propen-1-one (10 g), phosphorus oxychloride (3.64 g), thiophenol (4.2 cc) and sodium cyanoborohydride (1.47 g), a residue is obtained which is taken up in chloroform. The solution is adjusted to pH 10 by add...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Aromatic thiol
Monosulfide
null
null
c1ccccc1.c1ccccc1
Other
CCOCC.C(Cl)(Cl)Cl.C(C)(C)O
null
null
CN(C)C=CC(=O)c1ccc(Br)cc1.Sc1ccccc1>CCOCC.C(Cl)(Cl)Cl.C(C)(C)O>CN(C)CC=C(Sc1ccccc1)c1ccc(Br)cc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-437d9ff9e7c043fe95a9f0b8da7e0249
CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Br)cc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
CN(C=CC(=O)C1=CC=CC=C1)C.[OH-].[Na+].BrC1=CC=C(C=C1)S.C(#N)[BH3-].[Na+].Cl.P(=O)(Cl)(Cl)Cl>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:15]1[cH:16][cH:17][c:18](Br)[cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:19][CH2:20]1
CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Br)cc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
CCOCC.C(Cl)(Cl)Cl.C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
1e537e83cebfd43b146ccf8ea392cf5d3050879ecbe689f3ec93b9cce50b64c2
ddd1516ad43f47fa7b86b0594e44d52ec4b102fdedd9f20b49005145737c746a
[CH]=C(CC1CCCCC1)c1ccccc1
Br-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[c;H0;D3;+0:4](-S):[cH;D2;+0:5]:[cH;D2;+0:6]:1.[C;D1;H3:7]-[#7:8](-[C;D1;H3:9])-[CH;D2;+0:10]=[CH;D2;+0:11]-[C;H0;D3;+0:12](=[O;H0;D1;+0:13])-[c:14](:[c:15]):[c:16]>>[C;D1;H3:7]-[#7:8](-[C;D1;H3:9])-[CH2;D2;+0:10]-[CH;D2;+0:11]=[C;H0;D3;+0:12](-[C:17](-[OH;D1;+0:13])-[CH;D3;...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (5 g), phosphorus oxychloride (2.47 cc), 4-bromothiophenol (5.39 g) and sodium cyanoborohydride (1 g), a chestnut-coloured residue is obtained which is taken up in chloroform. The solution is made alkaline to pH 10...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone.Aromatic thiol
Secondary alcohol
c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
Br-
CCOCC.C(Cl)(Cl)Cl.C(C)O
null
null
CN(C)C=CC(=O)c1ccccc1.Sc1ccc(Br)cc1>CCOCC.C(Cl)(Cl)Cl.C(C)O>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d9922a320104492598aad6f7450006e5
CCN(CC)CC.CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1.CO.[OH-]>>CCOC(=O)OC(C(=CCN)c1ccccc1)c1ccccc1
[OH-].[Na+].C(C)N(CC)CC.C(CCS)S.C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O.CO>>NCC=C(C(OC(=O)OCC)C1=CC=CC=C1)C1=CC=CC=C1
CCN(CC)[CH2:2][CH3:1].C[N:11](C)[CH2:10][CH:9]=[C:8]([CH:7]([OH:6])[CH:18]1[CH2:19][CH2:20][CH2:21][CH2:22][CH2:23]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[OH:3][CH3:4].[OH-:5]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[O:6][CH:7]([C:8](=[CH:9][CH2:10][NH2:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1)[c:18]1[cH:19][cH:...
CCN(CC)CC.CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1.CO.[OH-]
CCOC(=O)OC(C(=CCN)c1ccccc1)c1ccccc1
null
null
O
Aromatic Heterocycle Formation
OtherReaction
623b1b8dd75701180f14d12f6469fe8fa4bef224afaf799df33b41aafa681763
3189d70a09073085feb5c65a6b0c23cebbe2ad41207a23d57ad58e1eb3599814
[CH]=C(Cc1ccccc1)c1ccccc1
C-C-N(-C-C)-[CH2;D2;+0:1]-[C;D1;H3:2].C-[N;H0;D3;+0:3](-C)-[C:4]-[C:5]=[C:6](-[c:7])-[C:8](-[OH;D1;+0:9])-[CH;D3;+0:10]1-[CH2;D2;+0:11]-[CH2;D2;+0:12]-[CH2;D2;+0:13]-[CH2;D2;+0:14]-[CH2;D2;+0:15]-1.[CH3;D1;+0:16]-[OH;D1;+0:17].[OH-;D0:18]>>[C;D1;H3:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:17]-[C;H0;D3;+0:16](=[O;H0;D1;+0:18])-[O;H...
null
[]
null
null
18
HOUR
Triethylamine (1.05 cc) and 1,3-propanedithiol (0.74 cc) are added to a solution of 4-azido-1,2-diphenyl-1-ethoxycarbonyloxy-2-butene (Z) (0.5 g) in methanol (7.5 cc). The mixture is stirred under a nitrogen atmosphere for 18 hours at ambient temperature. The reaction mixture is then poured into water (10 cc), adjusted...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Tertiary amine.Tertiary amine.Methanol
Carbonic Ester.Primary amine
C1CCCCC1
c1ccccc1
c1ccccc1.c1ccccc1
Other
O
null
18
CCN(CC)CC.CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1.CO.[OH-]>O>CCOC(=O)OC(C(=CCN)c1ccccc1)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-bafaf1cd37ff4a9e9438a2f3b095ad7f
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1F>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.FC1=C(C=O)C=CC=C1>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.F[c:20]1[c:15]([CH:13]=[O:14])[cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1F
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
e9d48bb333e25370f39508268f8fab0013d8c9d2216ebb4925f8d09549804f1a
05339c96fb0a21edb48547dfb79b5c1cd719c10814e28a0fe9b4657ab6ae568d
[CH]=C(CC1CCCCC1)c1ccccc1
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]):c(-C(-C)-C):c:1.F-[c;H0;D3;+0:8]1:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[CH;D2;+0:14]=[O;H0;D1;+0:15]>>[#7:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[CH;D3;+0:14](-[OH;D1;+0:15])-[CH...
null
[]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (10 g) and 2-fluorobenzaldehyde (2.6 cc), 4-dimethylamino-1-(2-fluorophenyl)-2-phenyl-2-buten-1-ol (Z) hydrochloride (3.5 g) is obtained in the form of a white powder mel...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aromatic halide.Aldehyde
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HF
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1ccccc1F>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e8cacf0dd8e14469911f26b32ae1fd9e
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1cccc(Br)c1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.BrC=1C=C(C=O)C=CC1>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.Br[c:19]1[cH:18][cH:17][cH:16][c:15]([CH:13]=[O:14])[cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1cccc(Br)c1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
e9d48bb333e25370f39508268f8fab0013d8c9d2216ebb4925f8d09549804f1a
05339c96fb0a21edb48547dfb79b5c1cd719c10814e28a0fe9b4657ab6ae568d
[CH]=C(CC1CCCCC1)c1ccccc1
Br-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:[cH;D2;+0:3]:[cH;D2;+0:4]:[c;H0;D3;+0:5](-[CH;D2;+0:6]=[O;H0;D1;+0:7]):[cH;D2;+0:8]:1.C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:9](-[CH2;D2;+0:10]-[C:11]-[#7:12])-[c:13](:[c:14]):[c:15]):c(-C(-C)-C):c:1>>[#7:12]-[C:11]-[CH;D2;+0:10]=[C;H0;D3;+0:9](-[CH;D3;+0:6](-[OH;D1;+0:7])...
null
[]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g) and 3-bromobenzaldehyde (5.6 cc), 1-(3-bromophenyl)-4dimethylamino-2-phenyl-2-buten-1-ol (Z) hydrochloride (11.3 g ) is obtained in the form of a white solid melti...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aromatic halide.Aldehyde
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HBr
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=Cc1cccc(Br)c1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1119c717db4a4fe39ded8a3d3c1e6c12
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.Cc1ccccc1C=O>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.C=1(C(=CC=CC1)C=O)C>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.C[c:20]1[c:15]([CH:13]=[O:14])[cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2:...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.Cc1ccccc1C=O
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
3ebd6f16ba89cc360449fd30ab34ced1781fbed4a414d9e59bcf754777378132
2f319ce34b90d24c5ffbe402ed9c6fde7375d736dd872cea5121694203d4c1fd
[CH]=C(CC1CCCCC1)c1ccccc1
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]):c(-C(-C)-C):c:1.C-[c;H0;D3;+0:8]1:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[CH;D2;+0:14]=[O;H0;D1;+0:15]>>[#7:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[CH;D3;+0:14](-[OH;D1;+0:15])-[CH...
85.4
[{"value": 85.4, "product": "C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g) and from o-tolualdehyde (5.78 g), 4-dimethylamino-1-(2-methylphenyl)-2-phenyl-2-buten-1-ol (Z) hydrochloride (10.2 g) is obtained in the form of a white powder mel...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.Cc1ccccc1C=O>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c08a21ca488a4c3cba0c0cc8ce71679a
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.COc1ccccc1C=O>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.C(C=1C(=CC=CC1)OC)=O>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.CO[c:20]1[c:15]([CH:13]=[O:14])[cH:16][cH:17][cH:18][cH:19]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.COc1ccccc1C=O
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
dbdcade79204e0a56ee5dd8ca835909d31858cdd25556e93a2e48c42de6cfc67
a6ca4bb4b6273366d3220f5e21425d37f94d720df0cf6fa944abf75c839397d5
[CH]=C(CC1CCCCC1)c1ccccc1
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]):c(-C(-C)-C):c:1.C-O-[c;H0;D3;+0:8]1:[cH;D2;+0:9]:[cH;D2;+0:10]:[cH;D2;+0:11]:[cH;D2;+0:12]:[c;H0;D3;+0:13]:1-[CH;D2;+0:14]=[O;H0;D1;+0:15]>>[#7:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[CH;D3;+0:14](-[OH;D1;+0:15])-[...
60.3
[{"value": 60.3, "product": "C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g) and from o-anisaldehyde (6.5 g), 4-dimethylamino-1-(2-methoxyphenyl)-2-phenyl-2-buten-1-ol (Z) (7.2 g) is obtained in the form of a white powder melting at 77° C. ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde.Ether
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.COc1ccccc1C=O>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-db19edbbd8e3453fbede5bf34086d2cf
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CC(OC)N(C)C)C1=CC=CC=C1.C(C1=CC=CC=C1)=O>>C1(CCCCC1)C(C(=CCN(C)C)C1=CC=CC=C1)O
CO[CH:4]([N:2]([CH3:1])[CH3:3])[CH2:5][C:6](=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)[c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1.[CH:13](=[O:14])[c:15]1[cH:16][cH:17][cH:18][cH:19][cH:20]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[CH:13]([OH:14])[CH:15]1[CH2:16][CH2:17][CH2:18][CH2...
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.O=Cc1ccccc1
CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
null
null
null
C-C Coupling
OtherReaction
dbdcade79204e0a56ee5dd8ca835909d31858cdd25556e93a2e48c42de6cfc67
a6ca4bb4b6273366d3220f5e21425d37f94d720df0cf6fa944abf75c839397d5
[CH]=C(CC1CCCCC1)c1ccccc1
C-O-[CH;D3;+0:1](-[CH2;D2;+0:2]-[C;H0;D3;+0:3](=N-N-S(=O)(=O)-c1:c(-C(-C)-C):c:c(-C(-C)-C):c:c:1-C(-C)-C)-[c:4](:[c:5]):[c:6])-[#7:7](-[C;D1;H3:8])-[C;D1;H3:9].[O;H0;D1;+0:10]=[CH;D2;+0:11]-[c;H0;D3;+0:12]1:[cH;D2;+0:13]:[cH;D2;+0:14]:[cH;D2;+0:15]:[cH;D2;+0:16]:[cH;D2;+0:17]:1>>[C;D1;H3:8]-[#7:7](-[C;D1;H3:9])-[CH2;D2...
null
[]
null
null
null
null
By using a method similar to that described in Example 22, but starting from β-dimethylamino-3-methoxypropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (21.7 g) and from benzaldehyde (5.4 cc), 4-dimethylamino-2-(3-methoxyphenyl)-1-phenyl-2-buten-1-ol (Z) hydrochloride (11.9 g) is obtained in the form of a white...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde.Ether
Secondary alcohol
c1ccccc1.c1ccccc1
C1CCCCC1
c1ccccc1.C1CCCCC1
HO-
null
null
null
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C(O)C1CCCCC1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-09f2dc9bd7e647de8c42509b9a2f23f0
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.COC(CC(=O)c1ccccc1)N(C)C>>COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C
Cl.CN(C(CC(=O)C1=CC=CC=C1)OC)C.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CC(OC)N(C)C)C1=CC=CC=C1.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN>>Cl.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CC(OC)N(C)C)C1=CC=CC=C1
COC(CC(c1ccccc1)=[N:6][NH:7][S:8](=[O:9])(=[O:10])[c:11]1[c:12]([CH:13]([CH3:14])[CH3:15])[cH:16][c:17]([CH:18]([CH3:19])[CH3:20])[cH:21][c:22]1[CH:23]([CH3:24])[CH3:25])N(C)C.O=[C:5]([CH2:4][CH:3]([O:2][CH3:1])[N:32]([CH3:33])[CH3:34])[c:26]1[cH:27][cH:28][cH:29][cH:30][cH:31]1>>[CH3:1][O:2][CH:3]([CH2:4][C:5](=[N:6][...
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.COC(CC(=O)c1ccccc1)N(C)C
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
0c2b5a2a8b3a7ec9ac4dc44d972abcaaa626b1aa98d94ffc0bbb0902425de6b3
27a0181f8ce20ba7c73a6073a00fbe45a31cc81b202698f805c5c59d0572138b
O=S(=O)(NN=Cc1ccccc1)c1ccccc1
C-O-C(-C-C(=[N;H0;D2;+0:1]-[#7:2]-[#16:3])-c1:c:c:c:c:c:1)-N(-C)-C.O=[C;H0;D3;+0:4](-[C:5]-[C:6])-[c:7](:[c:8]):[c:9]>>[#16:3]-[#7:2]-[N;H0;D2;+0:1]=[C;H0;D3;+0:4](-[C:5]-[C:6])-[c:7](:[c:8]):[c:9]
null
[]
null
null
null
null
β-Dimethylamino-3-methoxypropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone can be prepared by a method similar to that described in Example 22 for the preparation of β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone, but starting from 2,4,6-triisopropylbenzenesulphonylhydrazine (25.3 g) a...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ether.Tertiary amine
Hydrazone
c1ccccc1
null
c1ccccc1.c1ccccc1
HO-
null
null
null
COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C.COC(CC(=O)c1ccccc1)N(C)C>>COC(CC(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1)N(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-057736d84dce4583ac2843e145deeba9
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCc2ccccc21>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.C1CC2=CC=CC=C2C(=O)C1>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c(C(C)C)c1.[C:13]1(=[O:14])[CH2:15][CH2:16][CH2:17][c:18]2[cH:19][cH:20][cH:21][cH:22][c:23]21>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCc2ccccc21
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
null
C-C Coupling
OtherReaction
962f47f6f8a0ba8f5776d76748b695cc760c3fd02e61302b9e486bc76a80ee92
be7df71ea82e782c3aad2bcb7c0413b1294333bcd0b030726d2fd5180ffb4746
[CH]=C(c1ccccc1)C1CCCc2ccccc21
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH2;D2;+0:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]):c(-C(-C)-C):c:1.[C:8]-[C:9]-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[c:12](:[c:13]):[c:14]>>[#7:4]-[C:3]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[c:5](:[c:6]):[c:7])-[C;H0;D4;+0:10](-[OH;D1;+0:11])(-[C:9]-[C:8])-[c:12](:[c:13]):[c...
null
[]
null
null
null
null
By using a method similar to that described in Example 22 but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g) and from α-tetralone (6.4 cc), 1-(1-hydroxy-1,2,3,4-tetrahydro-1-naphthyl)-3-dimethylamino-1-phenyl-1-propene (Z) (3.8 g) is obtained in the form of a white powder ...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Ketone
Tertiary alcohol
c1ccccc1.c1ccc2c(c1)CCCC2
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCc2ccccc21>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dd5c9bc449b941468df29aa629851196
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCCC1>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CCN(C)C)C1=CC=CC=C1.C1(CCCCC1)=O>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
CC(C)c1c[c:22](C(C)C)[c:23](S(=O)(=O)NN=[C:6]([CH2:5][CH2:4][N:2]([CH3:1])[CH3:3])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[c:18](C(C)C)[cH:17]1.[C:13]1(=[O:14])[CH2:15][CH2:16][CH2:21][CH2:20][CH2:19]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:16][C...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCCC1
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
null
C-C Coupling
OtherReaction
a261bd99a8a92a2d89f9c3684f105c3de74eb8d4a99c9cfa511931cd4e34c000
be7df71ea82e782c3aad2bcb7c0413b1294333bcd0b030726d2fd5180ffb4746
[CH]=C(c1ccccc1)C1CCCc2ccccc21
C-C(-C)-[c;H0;D3;+0:1]1:[cH;D2;+0:2]:c(-C(-C)-C):c:[c;H0;D3;+0:3](-C(-C)-C):[c;H0;D3;+0:4]:1-S(=O)(=O)-N-N=[C;H0;D3;+0:5](-[CH2;D2;+0:6]-[C:7]-[#7:8])-[c:9](:[c:10]):[c:11].[O;H0;D1;+0:12]=[C;H0;D3;+0:13]1-[C:14]-[CH2;D2;+0:15]-[CH2;D2;+0:16]-[CH2;D2;+0:17]-[CH2;D2;+0:18]-1>>[#7:8]-[C:7]-[CH;D2;+0:6]=[C;H0;D3;+0:5](-[c...
null
[]
null
null
null
null
By using a procedure similar to that described in Example 22 but starting from β-dimethylaminopropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (20 g) and from cyclohexanone (5 cc), 1-(1-hydroxy-1-cyclohexyl)-3-dimethylamino-1-phenyl-1-propene (Z) hydrochloride (6 g) is obtained in the form of a white powder me...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Ketone
Tertiary alcohol
c1ccccc1.C1CCCCC1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CCN(C)C)c2ccccc2)c(C(C)C)c1.O=C1CCCCC1>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e86a3e9ff2604fdf978a729dc5841fcf
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN)c(C(C)C)c1.CN1CCCC1CC(=O)c1ccccc1>>CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CC2CCCN2C)c2ccccc2)c(C(C)C)c1
C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CC1N(CCC1)C)C1=CC=CC=C1.CN(CCC(=O)C1=CC=CC=C1)C.Cl.CN1C(CCC1)CC(=O)C1=CC=CC=C1>>Cl.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(CC1N(CCC1)C)C1=CC=CC=C1
[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][c:6]([CH:7]([CH3:8])[CH3:9])[c:10]([S:11](=[O:12])(=[O:13])[NH:14][NH2:15])[c:30]([CH:31]([CH3:32])[CH3:33])[cH:34]1.O=[C:16]([CH2:17][CH:18]1[CH2:19][CH2:20][CH2:21][N:22]1[CH3:23])[c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][c:6]([CH:7]([CH3:8])[CH...
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN)c(C(C)C)c1.CN1CCCC1CC(=O)c1ccccc1
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CC2CCCN2C)c2ccccc2)c(C(C)C)c1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
83882590079d324612170330ec542715e8ce71411b1b2946e5f0d75ea75ad4dd
16267fcabf9e555e6c245927fd3675c621f876db12f50a1b3e8576a12e06a1cf
O=S(=O)(NN=C(CC1CCCN1)c1ccccc1)c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7].[#16:8]-[#7:9]-[NH2;D1;+0:10]>>[#16:8]-[#7:9]-[N;H0;D2;+0:10]=[C;H0;D3;+0:1](-[C:2]-[C:3]-[#7:4])-[c:5](:[c:6]):[c:7]
null
[]
null
null
null
null
α-(1-Methyl-2-pyrrolidinyl)acetophenone 2,4,6-triisopropylbenzenesulphonylhydrazone can be prepared by a method similar to that described in Example 22 for the preparation of β-dimethylaminopropiophenone, 2,4,6-triisopropylbenzenesulphonylhydrazone, but starting from 2,4,6-triisopropylbenzenesulphonylhydrazine (30.6 g)...
10.6084/m9.figshare.5104873.v1
null
Hydrazine.Ketone
Hydrazone
null
null
c1ccccc1.C1CC[NH]C1.c1ccccc1
HO-
null
null
null
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN)c(C(C)C)c1.CN1CCCC1CC(=O)c1ccccc1>>CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=C(CC2CCCN2C)c2ccccc2)c(C(C)C)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e523d3bf6d6f4be7aaccce500d9e3658
CC(CN(C)C)C(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(C1=CC=CC=C1)=O.C(C)(C)(C)[Li].C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(C(CN(C)C)C)C1=CC=CC=C1.Cl.Cl>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
CC(C)c1cc(C(C)C)c(S(=O)(=O)NN=[C:6]([CH:5]([CH2:4][N:2]([CH3:1])[CH3:3])[CH3:15])[c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)c([CH:17](C)[CH3:16])c1.[CH:13](=[O:14])[c:18]1[cH:19][cH:20][cH:21][cH:22][cH:23]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:16...
CC(CN(C)C)C(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
O.CCCCC.CC(=O)C.COCCOC.C(C)OCC
C-C Coupling
OtherReaction
1cbd32a051eafbbb080795e8a663b5e7083fd4b13a4460c3abba6e7e78ec81ce
993855a2ea4c79485046a4d8ea0ca7051719a1c4ea0d6f63d12db845ee36cf08
[CH]=C(c1ccccc1)C1CCCc2ccccc21
C-C(-C)-c1:c:c(-C(-C)-C):c(-S(=O)(=O)-N-N=[C;H0;D3;+0:1](-[CH;D3;+0:2](-[CH3;D1;+0:3])-[C:4]-[#7:5])-[c:6](:[c:7]):[c:8]):c(-[CH;D3;+0:9](-C)-[CH3;D1;+0:10]):c:1.[O;H0;D1;+0:11]=[CH;D2;+0:12]-[c;H0;D3;+0:13]1:[c:14]:[c:15]:[c:16]:[c:17]:[cH;D2;+0:18]:1>>[#7:5]-[C:4]-[CH;D2;+0:2]=[C;H0;D3;+0:1](-[c:6](:[c:7]):[c:8])-[C;...
null
[]
15
CELSIUS
20
MINUTE
A 1.9M solution (30.4 cc) of tert-butyllithium in pentane is added to a solution of β-dimethylamino-α-methylpropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone (10.9 g) in 1,2-dimethoxyethane (109 cc), kept under nitrogen atmosphere at a temperature in the region of -75° C. Once the addition has been completed th...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Hydrazone.Aldehyde
Tertiary alcohol
c1ccccc1.c1ccccc1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HO-
O.CCCCC.CC(=O)C.COCCOC.C(C)OCC
15
0.333333
CC(CN(C)C)C(=NNS(=O)(=O)c1c(C(C)C)cc(C(C)C)cc1C(C)C)c1ccccc1.O=Cc1ccccc1>O.CCCCC.CC(=O)C.COCCOC.C(C)OCC>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-cad463dd5b794184bd05ea983ee11d4c
Cl>>Cl
O.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(C(CN(C)C)C)C1=CC=CC=C1.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN.Cl.CC(C(=O)C1=CC=CC=C1)CN(C)C>>Cl.C(C)(C)C1=C(C(=CC(=C1)C(C)C)C(C)C)S(=O)(=O)NN=C(C(CN(C)C)C)C1=CC=CC=C1
[ClH:34]>>[ClH:34]
Cl
Cl
null
null
C(C)(=O)O.C(Cl)Cl
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
null
null
null
[]
null
null
24
HOUR
β-Dimethylamino-α-methylpropiophenone 2,4,6-triisopropylbenzenesulphonylhydrazone can be prepared as follows: 2,4,6-triisopropylbenzenesulphonylhydrazine (23.8 g) is added to α-methyl-β-dimethylaminopropiophenone hydrochloride (16.3 g) dissolved in methylene chloride (150 cc) and acetic acid (5 cc). The solution is sti...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
C(C)(=O)O.C(Cl)Cl
null
24
Cl>C(C)(=O)O.C(Cl)Cl>Cl
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-0cce6a139615472cb7594067073fa6a4
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1Cl>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(#N)[BH3-].[Na+].C(C)(C)O.CN(C=CC(=O)C1=CC=CC=C1)C.P(=O)(Cl)(Cl)Cl.Cl.ClC1=C(C=CC=C1)S>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
O[CH:13]([CH3:15])[CH3:17].[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:18]1[cH:19][cH:20][cH:21][cH:22][c:23]1Cl>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:16][CH2:17][c:18]2[cH:19][cH:20][cH:21][cH:22]...
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1Cl
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
8d83f6ca45ac827a93af4e5a9762e2536a73a6aa8fbe03ff6c989f700c3a6d78
4c02746a7bcb3f60b9410fd6f58e28fd8dc6dcef087ecf59d23b8c4d87859c2b
[CH]=C(c1ccccc1)C1CCCc2ccccc21
Cl-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6]:1-S.O-[CH;D3;+0:7](-[CH3;D1;+0:8])-[CH3;D1;+0:9].[C;D1;H3:10]-[#7:11](-[C;D1;H3:12])-[CH;D2;+0:13]=[CH;D2;+0:14]-[C;H0;D3;+0:15](=[O;H0;D1;+0:16])-[c:17](:[c:18]):[c:19]>>[C;D1;H3:10]-[#7:11](-[C;D1;H3:12])-[CH2;D2;+0:13]-[CH;D2;+0:14]=[C;H0;D3;+0:15](-[c:17](:[...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (6.1 g), phosphorus oxychloride (3 cc), 2-chlorothiophenol (5 g) and sodium cyanoborohydride (1.3 g), and after evaporating the organic phase to dryness under reduced pressure (2.7 kPa) at 40° C., a yellow oil is o...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone.Secondary alcohol.Aromatic thiol
Tertiary alcohol
c1ccccc1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
HCl
C(C)OCC
null
null
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Sc1ccccc1Cl>C(C)OCC>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-afe170f81add48948f8c1aa954ce0259
CC(C)=O.CN(C)C=CC(=O)c1ccccc1.Sc1cccc(Cl)c1>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(#N)[BH3-].[Na+].CC(=O)C.CN(C=CC(=O)C1=CC=CC=C1)C.P(=O)(Cl)(Cl)Cl.Cl.ClC=1C=C(C=CC1)S>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
O=[C:13]([CH3:22])[CH3:23].[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:20]1[cH:15][cH:16][cH:17][c:18](Cl)[cH:19]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:16][CH2:17][c:18]2[cH:19][cH:20][cH:21][cH:2...
CC(C)=O.CN(C)C=CC(=O)c1ccccc1.Sc1cccc(Cl)c1
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
C(C)OCC
Aromatic Heterocycle Formation
OtherReaction
5d4fb066042b9c0d5a9632ed89dde9c7ca52f374909b06d95f813f88e3166c0a
d283927a0205aa30e926eea5d70f92cd65ba9dc33533b37bc72d16ef464b4bee
[CH]=C(c1ccccc1)C1CCCc2ccccc21
Cl-[c;H0;D3;+0:1]1:[c:2]:[c;H0;D3;+0:3](-S):[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:1.O=[C;H0;D3;+0:7](-[CH3;D1;+0:8])-[CH3;D1;+0:9].[C;D1;H3:10]-[#7:11](-[C;D1;H3:12])-[CH;D2;+0:13]=[CH;D2;+0:14]-[C;H0;D3;+0:15](=[O;H0;D1;+0:16])-[c:17](:[c:18]):[c:19]>>[C;D1;H3:10]-[#7:11](-[C;D1;H3:12])-[CH2;D2;+0:13]-[CH;D2;+0:14]=[...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (5 g), phosphorus oxychloride (2.5 cc), 3-chlorothiophenol (4.13 g) and sodium cyanoborohydride (1 g), and after evaporating the organic phase to dryness under reduced pressure (2.7 kPa) at 40° C., a residue is obt...
10.6084/m9.figshare.5104873.v1
null
Enamine.Aromatic halide.Ketone.Ketone.Aromatic thiol
Tertiary alcohol
c1ccccc1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
Other
C(C)OCC
null
null
CC(C)=O.CN(C)C=CC(=O)c1ccccc1.Sc1cccc(Cl)c1>C(C)OCC>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3d6a0a5566b347cb9e82ee1e43eb1bee
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Cc1ccc(S)cc1>>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
C(#N)[BH3-].[Na+].C(C)(C)O.CN(C=CC(=O)C1=CC=CC=C1)C.P(=O)(Cl)(Cl)Cl.Cl.CC1=CC=C(C=C1)S>>OC1(CCCC2=CC=CC=C12)C(=CCN(C)C)C1=CC=CC=C1
O[CH:20]([CH3:19])[CH3:21].[CH3:1][N:2]([CH3:3])[CH:4]=[CH:5][C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)=[O:14].S[c:23]1[cH:13][cH:15][c:16]([CH3:17])[cH:18][cH:22]1>>[CH3:1][N:2]([CH3:3])[CH2:4][CH:5]=[C:6]([c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]1([OH:14])[CH2:15][CH2:16][CH2:17][c:18]2[cH:19][cH:20][cH:21...
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Cc1ccc(S)cc1
CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
null
null
C(C)OCC
Aromatic Heterocycle Formation
OtherReaction
3c273c4d6d071f4bac60c71def7bc310168d971792cc9dc702b87a6eb4b960d8
434d667421f49e168b0a4474941b0a4a16434d6ae30c3f3d228a76739210d470
[CH]=C(c1ccccc1)C1CCCc2ccccc21
O-[CH;D3;+0:1](-[CH3;D1;+0:2])-[CH3;D1;+0:3].S-[c;H0;D3;+0:4]1:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7](-[CH3;D1;+0:8]):[cH;D2;+0:9]:[cH;D2;+0:10]:1.[C;D1;H3:11]-[#7:12](-[C;D1;H3:13])-[CH;D2;+0:14]=[CH;D2;+0:15]-[C;H0;D3;+0:16](=[O;H0;D1;+0:17])-[c:18](:[c:19]):[c:20]>>[C;D1;H3:11]-[#7:12](-[C;D1;H3:13])-[CH2;D2;+0:14...
null
[]
null
null
null
null
By using a method similar to that described in Example 35, but starting from 3-dimethylaminoacrylophenone (5 g), phosphorus oxychloride (2.47 cc), 4-methylthiophenol (3.55 g) and sodium cyanoborohydride (1 g), and after evaporating the organic phase to dryness under reduced pressure (2.7 kPa) at 40° C., an orange oil i...
10.6084/m9.figshare.5104873.v1
null
Enamine.Ketone.Secondary alcohol.Aromatic thiol
Tertiary alcohol
c1ccccc1
c1ccc2c(c1)CCCC2
c1ccccc1.c1ccc2c(c1)CCCC2
Other
C(C)OCC
null
null
CC(C)O.CN(C)C=CC(=O)c1ccccc1.Cc1ccc(S)cc1>C(C)OCC>CN(C)CC=C(c1ccccc1)C1(O)CCCc2ccccc21
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-2b42240b607b49ddbd42f80892057fb4
C=Cc1ccccc1.CC(C)c1ccccc1>>CC(C)c1ccccc1C(C)c1ccccc1
C1(=CC=CC=C1)C(C)C.C=CC1=CC=CC=C1>>C1(=CC=CC=C1)C(C)C1=C(C=CC=C1)C(C)C
[CH:10](=[CH2:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1.[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][cH:9]1>>[CH3:1][CH:2]([CH3:3])[c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[CH:10]([CH3:11])[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
C=Cc1ccccc1.CC(C)c1ccccc1
CC(C)c1ccccc1C(C)c1ccccc1
null
S(O)(O)(=O)=O
null
C-C Coupling
Friedel-Crafts alkylation
f6021e53f57d07d48a856391b21137517c9bd669381174a55381b6219a6afd68
48297e5b607b4624d5b08506879ba8f9dd47fb272c10888542fa01ef83829ef2
c1ccc(Cc2ccccc2)cc1
[CH2;D1;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[c:5].[C:6]-[c:7](:[c:8]):[cH;D2;+0:9]:[c:10]:[c:11]>>[C:6]-[c:7](:[c:8]):[c;H0;D3;+0:9](-[CH;D3;+0:2](-[CH3;D1;+0:1])-[c:3](:[c:4]):[c:5]):[c:10]:[c:11]
null
[]
null
null
null
null
Aralkylation of cumene with styrene was carried out in the presence of sulfuric acid catalyst. From the reaction product, a fraction mainly containing 1-phenyl-1-(isopropylphenyl)ethane was obtained by distillation. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Vinyl
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccccc1
null
S(O)(O)(=O)=O
null
null
C=Cc1ccccc1.CC(C)c1ccccc1>S(O)(O)(=O)=O>CC(C)c1ccccc1C(C)c1ccccc1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-dd05b8f1b2c540f8a6f6e96280a71fb4
CCCCN(CCCC)C(=O)c1cccc(OC(C)=O)c1>>CCCCN(CCCC)Cc1cccc(O)c1
S(=O)(=O)([O-])[O-].[Mg+2].[OH-].[Na+].C(C)(=O)OC=1C=C(C(=O)N(CCCC)CCCC)C=CC1.[H-].[Al+3].[Li+].[H-].[H-].[H-]>>OC=1C=C(CN(CCCC)CCCC)C=CC1
CC(=O)[O:16][c:15]1[cH:14][cH:13][cH:12][c:11]([C:10](=O)[N:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][CH2:8][CH3:9])[cH:17]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH3:9])[CH2:10][c:11]1[cH:12][cH:13][cH:14][c:15]([OH:16])[cH:17]1
CCCCN(CCCC)C(=O)c1cccc(OC(C)=O)c1
CCCCN(CCCC)Cc1cccc(O)c1
null
null
O.CCOCC
Reduction
OtherReaction
9abc997e012ed9d8d834b9a3f63bfe3454f23ced03bff048e83e49d30af1132c
9f208a8b94e5538e117d755d0b06e07196757bf445f80a083aafb16ca1eb9d6a
c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]:[c:5](-[C;H0;D3;+0:6](=O)-[#7:7](-[C:8])-[C:9]):[c:10]>>[C:8]-[#7:7](-[C:9])-[CH2;D2;+0:6]-[c:5](:[c:10]):[c:4]:[c:2](-[OH;D1;+0:1]):[c:3]
null
[]
null
null
null
null
A mixture of 33.0 g (0.133 m) of 3-acetoxy-N,N-dibutylbenzamide in 400 ml of ether was slowly added over one half hour to a suspension of 5.0 (0.133 m) grams of lithium aluminum hydride (LAH) in 300 ml of ether. The mixture was heated to reflux for 2 hours. The mixture was slowly treated with 5.0 ml of water, 5.0 ml of...
10.6084/m9.figshare.5104873.v1
null
Ester.Tertiary amide
Aromatic alcohol
null
null
c1ccccc1
Other
O.CCOCC
null
null
CCCCN(CCCC)C(=O)c1cccc(OC(C)=O)c1>O.CCOCC>CCCCN(CCCC)Cc1cccc(O)c1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-8a6119e32beb49ab984ec47353dcc123
CCCCI.CCCCN(CCCC)Cc1cccc(O)c1>>CCCC[N+](CCCC)(CCCC)Cc1cccc(O)c1.[I-]
OC=1C=C(CN(CCCC)CCCC)C=CC1.C(CCC)I>>[I-].C(CCC)[N+](CCCC)(CCCC)CC1=CC(=CC=C1)O
[CH3:1][CH2:2][CH2:3][CH2:4][I:22].[N:5]([CH2:6][CH2:7][CH2:8][CH3:9])([CH2:10][CH2:11][CH2:12][CH3:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][c:19]([OH:20])[cH:21]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N+:5]([CH2:6][CH2:7][CH2:8][CH3:9])([CH2:10][CH2:11][CH2:12][CH3:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][c:19]([OH:20])[cH:21...
CCCCI.CCCCN(CCCC)Cc1cccc(O)c1
CCCC[N+](CCCC)(CCCC)Cc1cccc(O)c1.[I-]
null
null
C(C)#N
Functional Group Interconversion
OtherReaction
cf95568d208ea67162a1e8aa2ffc7c679479f5b8aaab2573599ff5258836e869
3d861fb9efedfc352e8049eef974a995ad6d89e50a2cf826c8f45bd07b1b8172
c1ccccc1
[C:1]-[C:2]-[CH2;D2;+0:3]-[I;H0;D1;+0:4].[C:5]-[C:6]-[N;H0;D3;+0:7](-[C:8]-[c:9])-[C:10]-[C:11]>>[C:5]-[C:6]-[N+;H0;D4:7](-[C:8]-[c:9])(-[C:10]-[C:11])-[CH2;D2;+0:3]-[C:2]-[C:1].[I-;H0;D0:4]
null
[]
null
null
null
null
A mixture was prepared containing 10 g (0.042 m) of 3-hydroxy N,N-dibutylbenzylamine, 15 g (0.082 m) of butyliodide and 25 ml of acetonitrile. The mixture was heated to reflux overnight. The completion of the reaction was determined by high pressure liquid chromatography. After completion, the solvent was removed and t...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Tertiary amine
null
null
null
c1ccccc1
null
C(C)#N
null
null
CCCCI.CCCCN(CCCC)Cc1cccc(O)c1>C(C)#N>CCCC[N+](CCCC)(CCCC)Cc1cccc(O)c1.[I-]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-0c0178a0dfca4667947a0499d672e7af
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1cc(Cl)nc(N)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(N)cc(Cl)n1
NC1=NC(=CC(=N1)N)Cl.C(=O)(OC)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>NC1=NC(=NC(=C1)Cl)NC(=O)NS(=O)(=O)C1=C(C(=O)OC)C=CC=C1
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([NH2:21])[cH:22][c:23]([Cl:24])[n:25]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:20]([NH2:21])[...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1cc(Cl)nc(N)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(N)cc(Cl)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
4
DAY
To a warmed mixture containing 1.4 g (0.01 mole) 2,4-diamino-6-chloropyrimidine in 50 ml acetonitrile is added 2.4 g (0.01 mole) 2-carbomethoxybenzenesulfonylisocyanate. The reaction mixture was stirred at room temperature for four days. The reaction mixture was filtered and the precipitate washed with ether. The filte...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(C)#N
null
96
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1cc(Cl)nc(N)n1>C(C)#N>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(N)cc(Cl)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1aa257d84f0a42fc9e249dbfb9ff3317
COC(=O)c1cccc([N+](=O)[O-])c1C.O=C1CCC(=O)N1Br>>COC(=O)c1cccc([N+](=O)[O-])c1CBr
ClCCCC.C1CCCCC1.CC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-].BrN1C(CCC1=O)=O.C(Cl)(Cl)(Cl)Cl>>BrCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-]
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[CH3:14].O=C1CCC(=O)N1[Br:15]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[CH2:14][Br:15]
COC(=O)c1cccc([N+](=O)[O-])c1C.O=C1CCC(=O)N1Br
COC(=O)c1cccc([N+](=O)[O-])c1CBr
null
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O
CCOCC
Functional Group Interconversion
Wohl-Ziegler bromination benzyl primary
45c0aca0d63a96f0092e6dded9c888827eaf6379dac179e1cefc99293896300a
08f5e7e34d3f321cce3e85421b38226d6240cca0939494ae61032d4f8405cf22
c1ccccc1
O=C1-C-C-C(=O)-N-1-[Br;H0;D1;+0:1].[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](-[CH3;D1;+0:7]):[c:8]>>[#8:2]-[C:3](=[O;D1;H0:4])-[c:5]:[c:6](-[CH2;D2;+0:7]-[Br;H0;D1;+0:1]):[c:8]
52.6
[{"value": 52.6, "product": "BrCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
A mixture of 100.0 g of methyl 2-methyl-3-nitrobenzoate, 100.0 g of N-bromosuccinimide, 3.0 g of dibenzoyl peroxide and 1000 ml of carbon tetrachloride was refluxed for 24 hours. The reaction mixture was cooled, 3.0 g of dibenzoyl peroxide added, and refluxing continued an additional 24 hours. The reaction mixture was ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Tertiary amide
Primary halide
C1CCNC1
null
c1ccccc1
HO-
C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.CCOCC
null
24
COC(=O)c1cccc([N+](=O)[O-])c1C.O=C1CCC(=O)N1Br>C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.C(C1=CC=CC=C1)(=O)OOC(C1=CC=CC=C1)=O.CCOCC>COC(=O)c1cccc([N+](=O)[O-])c1CBr
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-16231784b9784304b58199bd7c4f5769
COC(=O)c1cccc([N+](=O)[O-])c1CBr>>O=C1OCc2c1cccc2[N+](=O)[O-]
BrCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-]>>[N+](=O)([O-])C1=CC=CC=2C(OCC21)=O
C[O:3][C:2](=[O:1])[c:6]1[c:5]([CH2:4]Br)[c:10]([N+:11](=[O:12])[O-:13])[cH:9][cH:8][cH:7]1>>[O:1]=[C:2]1[O:3][CH2:4][c:5]2[c:6]1[cH:7][cH:8][cH:9][c:10]2[N+:11](=[O:12])[O-:13]
COC(=O)c1cccc([N+](=O)[O-])c1CBr
O=C1OCc2c1cccc2[N+](=O)[O-]
null
null
O1CCOCC1.O
Heteroatom Alkylation and Arylation
OtherReaction
aea24383edbe96de2d472a5cab034365c9438019ff5020199b3fcfad09fd8a38
6007d70cc3173f3039a472489995dad2781e8d749be1f1aa209b0bf2f190a4b4
O=C1OCc2ccccc21
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-C>>[O;D1;H0:6]=[C:5]1-[O;H0;D2;+0:7]-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-1
59.7
[{"value": 59.7, "product": "[N+](=O)([O-])C1=CC=CC=2C(OCC21)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 54.8 g of methyl 2-bromomethyl-3-nitrobenzoate in a mixture of 200 ml dioxane and 45 ml water was refluxed for 72 hours. The reaction solution was cooled and concentrated in vacuo. The resulting solid was slurried in water, collected, washed with water and dried. Recrystallization from 1-chlorobutane gave...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ester
Ester
null
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
HBr
O1CCOCC1.O
null
null
COC(=O)c1cccc([N+](=O)[O-])c1CBr>O1CCOCC1.O>O=C1OCc2c1cccc2[N+](=O)[O-]
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b9aaf99d87f6452baa0b885bec5e43ab
O=C1OCc2c1cccc2[N+](=O)[O-]>>O=[N+]([O-])c1cccc2c1COC2
[N+](=O)([O-])C1=CC=CC=2C(OCC21)=O>>[N+](=O)([O-])C1=CC=CC=2COCC21
O=[C:12]1[c:8]2[cH:7][cH:6][cH:5][c:4]([N+:2](=[O:1])[O-:3])[c:9]2[CH2:10][O:11]1>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][c:8]2[c:9]1[CH2:10][O:11][CH2:12]2
O=C1OCc2c1cccc2[N+](=O)[O-]
O=[N+]([O-])c1cccc2c1COC2
null
null
B(F)(F)F.CCOCC
Reduction
OtherReaction
fe61f926af1f03b39ab4264cfb4b79e476d6001758cdd7c373343d5ebadbb2b1
827848a04fae177f236c29c6caa2fc79931c8d66451736910cacf959ca644e0e
c1ccc2c(c1)COC2
O=[C;H0;D3;+0:1]1-[#8:2]-[C:3]-[c:4]:[c:5]-1:[c:6]>>[c:6]:[c:5]1:[c:4]-[C:3]-[#8:2]-[CH2;D2;+0:1]-1
85.7
[{"value": 85.7, "product": "[N+](=O)([O-])C1=CC=CC=2COCC21", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 19.5 g of 1,3-dihydro-4-nitrobenzo[c]furan-1-one in 100 ml of boron trifluoride etherate was cooled to 0°-5° under nitrogen. 125 ml of a 1M solution of borane-tetrahydrofuran complex was added dropwise below 10°. The orange suspension was allowed to warm to ambient temperature (H2 evolution), and the re...
10.6084/m9.figshare.5104873.v1
null
Ester
Ether
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
Other
B(F)(F)F.CCOCC
null
null
O=C1OCc2c1cccc2[N+](=O)[O-]>B(F)(F)F.CCOCC>O=[N+]([O-])c1cccc2c1COC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1648cd82d5bd4d05bf80b3d180ec237b
Cl.Nc1cccc2c1COC2.O=S=O>>O=S(=O)(Cl)c1cccc2c1COC2
N(=O)[O-].[Na+].C1OCC2=C1C=CC=C2N.Cl.S(=O)=O.N(=O)[O-].[Na+].Cl>>C1OCC2=C1C=CC=C2S(=O)(=O)Cl
[ClH:4].N[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[CH2:11][O:12][CH2:13]2.[O:1]=[S:2]=[O:3]>>[O:1]=[S:2](=[O:3])([Cl:4])[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[CH2:11][O:12][CH2:13]2
Cl.Nc1cccc2c1COC2.O=S=O
O=S(=O)(Cl)c1cccc2c1COC2
null
O.O.[Cu](Cl)Cl
O.C(C)(=O)O
Heteroatom Alkylation and Arylation
OtherReaction
298b7523df104b16c2f933c319292577559cdcf41a184e06cb1ebbdbb03d5eca
49dcc8f7b4471977f8fe724b4dd774612c303d853f75a373d5b25cc7ccd4c205
c1ccc2c(c1)COC2
N-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](:[c:5])-[C:6]-[#8:7].[ClH;D0;+0:8].[O;D1;H0:9]=[S;H0;D2;+0:10]=[O;D1;H0:11]>>[#8:7]-[C:6]-[c:4](:[c:5]):[c;H0;D3;+0:1](-[S;H0;D4;+0:10](-[Cl;H0;D1;+0:8])(=[O;D1;H0:9])=[O;D1;H0:11]):[c:2]:[c:3]
null
[]
null
null
1
HOUR
A suspension of 22.1 g of the crude hydrochloride salt prepared in Example 2 in a mixture of 30 ml of concentrated hydrochloric acid and 30 ml acetic acid was cooled to 0°-5°. A solution of 6.2 g of sodium nitrite in 15 ml water was added dropwise at 0°-5°. The thick suspension was diluted with 19 ml of concentrated hy...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonyl halide
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
Other
O.O.[Cu](Cl)Cl.O.C(C)(=O)O
null
1
Cl.Nc1cccc2c1COC2.O=S=O>O.O.[Cu](Cl)Cl.O.C(C)(=O)O>O=S(=O)(Cl)c1cccc2c1COC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1b8604044755497b8d713cda5a70a3fa
C1CCOC1.O=S(=O)(Cl)Cl.[NH4+].[OH-]>>NS(=O)(=O)c1cccc2c1COC2
S(=O)(=O)(Cl)Cl.O1CCCC1.[OH-].[NH4+]>>C1OCC2=C1C=CC=C2S(=O)(=O)N
O1[CH2:5][CH2:8][CH2:9][CH2:10]1.Cl[S:2](Cl)(=[O:3])=[O:4].[NH4+:1].[OH-:12]>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[CH2:11][O:12][CH2:13]2
C1CCOC1.O=S(=O)(Cl)Cl.[NH4+].[OH-]
NS(=O)(=O)c1cccc2c1COC2
null
null
null
Aromatic Heterocycle Formation
OtherReaction
977d8c666e412a53b664075ea73d0125eeefc2947eddbd1499ee7c191988d0bc
d239650332f2cf8d0af06622e2859ddb0cf4ecc1f38f84ddc5e28b00f2af42d8
c1ccc2c(c1)COC2
Cl-[S;H0;D4;+0:1](-Cl)(=[O;D1;H0:2])=[O;D1;H0:3].O1-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[CH2;D2;+0:7]-1.[NH4+;D0:8].[OH-;D0:9]>>[NH2;D1;+0:8]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c;H0;D3;+0:7]1:[c:10]:[c:11]:[cH;D2;+0:6]:[c;H0;D3;+0:5]2:[c;H0;D3;+0:4]:1-[C:12]-[O;H0;D2;+0:9]-[C:13]-2
null
[]
null
null
0.5
HOUR
A solution of 9.8 g of the sulfonyl chloride, prepared in Part A, in 150 ml tetrahydrofuran was cooled to approximately 5°, and 6.6 ml of concentrated ammonium hydroxide was added dropwise. The resulting yellow suspension was allowed to warm to ambient temperature and stirred 0.5 hour; thin-layer chromatography showed ...
10.6084/m9.figshare.5104873.v1
null
Ether
Sulfonamide.Ether
C1CCOC1
c1ccc2c(c1)COC2
c1ccc2c(c1)COC2
HCl
null
null
0.5
C1CCOC1.O=S(=O)(Cl)Cl.[NH4+].[OH-]>>NS(=O)(=O)c1cccc2c1COC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-cc092392aa584ae0992038eb02f92cc7
CCCCN=C=O.NS(=O)(=O)c1cccc2c1COC2>>O=C=NS(=O)(=O)c1cccc2c1COC2
C(=O)(Cl)Cl.C1OCC2=C1C=CC=C2S(=O)(=O)N.C(CCC)N=C=O.C1CN2CCN1CC2.C(=O)(Cl)Cl>>C1OCC2=C1C=CC=C2S(=O)(=O)N=C=O
CCCCN=[C:2]=[O:1].[NH2:3][S:4](=[O:5])(=[O:6])[c:7]1[cH:8][cH:9][cH:10][c:11]2[c:12]1[CH2:13][O:14][CH2:15]2>>[O:1]=[C:2]=[N:3][S:4](=[O:5])(=[O:6])[c:7]1[cH:8][cH:9][cH:10][c:11]2[c:12]1[CH2:13][O:14][CH2:15]2
CCCCN=C=O.NS(=O)(=O)c1cccc2c1COC2
O=C=NS(=O)(=O)c1cccc2c1COC2
null
null
C=1(C(=CC=CC1)C)C
Functional Group Interconversion
OtherReaction
d6c69f89b87c5c421a628563544ee2b8b0164ec4561bcd29a2cbba0dce4075ac
5df9e857f75ada60baf9e936007533a18389016451154bd1ed26e91b5babd844
c1ccc2c(c1)COC2
C-C-C-C-N=[C;H0;D2;+0:1]=[O;D1;H0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[O;D1;H0:2]=[C;H0;D2;+0:1]=[N;H0;D2;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]
null
[]
null
null
null
null
A mixture of 7.0 g of 1,3-dihydrobenzo[c]furan-4-sulfonamide, 4.0 ml of butyl isocyanate, 0.1 g of DABCO® and 150 ml xylene was heated to reflux. Phosgene (3.1 ml) was added in small portions to the reaction mixture while maintaining the reaction temperature <130°. When addition of phosgene was complete, the reaction m...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
null
null
null
c1ccc2c(c1)COC2
Other
C=1(C(=CC=CC1)C)C
null
null
CCCCN=C=O.NS(=O)(=O)c1cccc2c1COC2>C=1(C(=CC=CC1)C)C>O=C=NS(=O)(=O)c1cccc2c1COC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-9807506e1fd84e8989ff7c4a88a76aeb
CC(C)(C)S.COC(=O)c1cccc([N+](=O)[O-])c1CBr>>COC(=O)c1cccc([N+](=O)[O-])c1CSC(C)(C)C
BrCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-].C[O-].[Na+].CC(C)(S)C>>CC(C)(SCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-])C
[SH:15][C:16]([CH3:17])([CH3:18])[CH3:19].Br[CH2:14][c:13]1[c:5]([C:3]([O:2][CH3:1])=[O:4])[cH:6][cH:7][cH:8][c:9]1[N+:10](=[O:11])[O-:12]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]([N+:10](=[O:11])[O-:12])[c:13]1[CH2:14][S:15][C:16]([CH3:17])([CH3:18])[CH3:19]
CC(C)(C)S.COC(=O)c1cccc([N+](=O)[O-])c1CBr
COC(=O)c1cccc([N+](=O)[O-])c1CSC(C)(C)C
null
null
CO
Heteroatom Alkylation and Arylation
thioether_nucl_sub
77cd742b5ba20df0e225494f6e5f3d958ee82ce9a1b16fd99a2d9f8350b4fdc8
b05f7dda7dad719ae1868a84c33eeaf5bf649036fc64173cf4774a5eb4d70181
c1ccccc1
Br-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]-[C:5](-[#8:6])=[O;D1;H0:7].[C;D1;H3:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[SH;D1;+0:12]>>[#8:6]-[C:5](=[O;D1;H0:7])-[c:4]:[c:2](-[CH2;D2;+0:1]-[S;H0;D2;+0:12]-[C:9](-[C;D1;H3:8])(-[C;D1;H3:10])-[C;D1;H3:11]):[c:3]
92
[{"value": 92.0, "product": "CC(C)(SCC1=C(C(=O)OC)C=CC=C1[N+](=O)[O-])C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 34.7 g of sodium methoxide in 600 ml methanol was added 57.9 g of 1,1-dimethylethanethiol below 25°. The resulting solution was stirred one hour before the portionwise addition of 172.7 g of methyl 2-bromomethyl-3-nitrobenzoate. The resulting suspension was refluxed two hours. The mixture was cooled, a...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aliphatic thiol
Monosulfide
null
null
c1ccccc1
HBr
CO
null
null
CC(C)(C)S.COC(=O)c1cccc([N+](=O)[O-])c1CBr>CO>COC(=O)c1cccc([N+](=O)[O-])c1CSC(C)(C)C
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-05a324f4402741408c24e634cccd45e7
O=C1SCc2c1cccc2[N+](=O)[O-]>>Nc1cccc2c1CSC2=O
[N+](=O)([O-])C1=CC=CC=2C(SCC21)=O.Cl>>Cl.O=C1SCC2=C1C=CC=C2N
O=[N+:2]([O-])[c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[CH2:9][S:10][C:11]2=[O:12]>>[NH2:2][c:3]1[cH:4][cH:5][cH:6][c:7]2[c:8]1[CH2:9][S:10][C:11]2=[O:12]
O=C1SCc2c1cccc2[N+](=O)[O-]
Nc1cccc2c1CSC2=O
null
null
null
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
O=C1SCc2ccccc21
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
4-Nitrobenzo[c]thiophene-1(3H)-one (38.1 g) was added portionwise to a solution of 146.0 g of stannous chloride dihydrate in 325 ml concentrated hydrochloric acid. A slow exotherm from 18° to 42° occurred and the reaction mixture was maintained at 40°-45° by cooling. When the exotherm subsided, the suspension was stirr...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccc2c(c1)CSC2
Other
null
null
null
O=C1SCc2c1cccc2[N+](=O)[O-]>>Nc1cccc2c1CSC2=O
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-5f3a1c1934ff44819208f12cf8073b61
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2=O>>CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2
B(F)(F)F.CCOCC.CC(C)(C)NS(=O)(=O)C1=CC=CC=2C(SCC21)=O>>CC(C)(C)NS(=O)(=O)C1=CC=CC=2CSCC21
O=[C:17]1[c:13]2[cH:12][cH:11][cH:10][c:9]([S:6]([NH:5][C:2]([CH3:1])([CH3:3])[CH3:4])(=[O:7])=[O:8])[c:14]2[CH2:15][S:16]1>>[CH3:1][C:2]([CH3:3])([CH3:4])[NH:5][S:6](=[O:7])(=[O:8])[c:9]1[cH:10][cH:11][cH:12][c:13]2[c:14]1[CH2:15][S:16][CH2:17]2
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2=O
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2
null
null
O1CCCC1
Reduction
OtherReaction
d43898b8eaf7ddd83b2ce67a1416e7f6a7945d083cd3daf5ffa5f056080cba6b
2ca05ab8de5156f6c61f18ec42bac575d94b50ddbeffeb0dbed053d2d8fdb54d
c1ccc2c(c1)CSC2
O=[C;H0;D3;+0:1]1-[#16:2]-[C:3]-[c:4]:[c:5]-1:[c:6]>>[c:6]:[c:5]1:[c:4]-[C:3]-[#16:2]-[CH2;D2;+0:1]-1
47.3
[{"value": 47.3, "product": "CC(C)(C)NS(=O)(=O)C1=CC=CC=2CSCC21", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
A suspension of 8.0 g of 1,3-dihydro-N-(1,1-dimethylethyl)-1-oxobenzo[c]thiophene-4-sulfonamide in a mixture of 15 ml of tetrahydrofuran, 25 ml of boron trifluoride etherate was cooled to 10° under N2, and 56 ml of a 1M solution of borane tetrahydrofuran complex was added dropwise at approximately 10°. The reaction mix...
10.6084/m9.figshare.5104873.v1
null
Carbo-thioester
Monosulfide
c1ccc2c(c1)CSC2
c1ccc2c(c1)CSC2
c1ccc2c(c1)CSC2
Other
O1CCCC1
null
8
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2=O>O1CCCC1>CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-c00937995bdd4e3994a23e4c6555f433
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2>>NS(=O)(=O)c1cccc2c1CSC2
CC(C)(C)NS(=O)(=O)C1=CC=CC=2CSCC21>>C1SCC2=C1C=CC=C2S(=O)(=O)N
CC(C)(C)[NH:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[CH2:11][S:12][CH2:13]2>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][c:9]2[c:10]1[CH2:11][S:12][CH2:13]2
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2
NS(=O)(=O)c1cccc2c1CSC2
null
null
CCCCCC.C(C)(=O)OCC.FC(C(=O)O)(F)F
Deprotection
Tert-butyl deprotection of amine
f7e1da1b4c254f1e6d5afbf8cb56733a4fabd145b80e971e3b7e31007de9e7d6
278d0fb11b582c058ac903379d7fbe11ab8c395937a204965031cf0c344845a9
c1ccc2c(c1)CSC2
C-C(-C)(-C)-[NH;D2;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]>>[NH2;D1;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]
58.8
[{"value": 58.8, "product": "C1SCC2=C1C=CC=C2S(=O)(=O)N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of 3.0 g of 1,3-dihydro-N-(1,1-dimethylethyl)benzo[c]thiophene-4-sulfonamide in 50 ml of trifluoroacetic acid was stirred at ambient temperature for 4 hours. The brown solution was concentrated in vacuo. 1-Chlorobutane was added to the resulting brown oil and the mixture concentrated in vacuo. Repeating this...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonamide
null
null
c1ccc2c(c1)CSC2
Other
CCCCCC.C(C)(=O)OCC.FC(C(=O)O)(F)F
null
null
CC(C)(C)NS(=O)(=O)c1cccc2c1CSC2>CCCCCC.C(C)(=O)OCC.FC(C(=O)O)(F)F>NS(=O)(=O)c1cccc2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-e1893475f31044b7b7638714ac2306e2
CCCCN=C=O.NS(=O)(=O)c1cccc2c1CSC2>>O=C=NS(=O)(=O)c1cccc2c1CSC2
C(=O)(Cl)Cl.C1SCC2=C1C=CC=C2S(=O)(=O)N.C(CCC)N=C=O.C1CN2CCN1CC2.C(=O)(Cl)Cl>>C1SCC2=C1C=CC=C2S(=O)(=O)N=C=O
CCCCN=[C:2]=[O:1].[NH2:3][S:4](=[O:5])(=[O:6])[c:7]1[cH:8][cH:9][cH:10][c:11]2[c:12]1[CH2:13][S:14][CH2:15]2>>[O:1]=[C:2]=[N:3][S:4](=[O:5])(=[O:6])[c:7]1[cH:8][cH:9][cH:10][c:11]2[c:12]1[CH2:13][S:14][CH2:15]2
CCCCN=C=O.NS(=O)(=O)c1cccc2c1CSC2
O=C=NS(=O)(=O)c1cccc2c1CSC2
null
null
C=1(C(=CC=CC1)C)C
Functional Group Interconversion
OtherReaction
d6c69f89b87c5c421a628563544ee2b8b0164ec4561bcd29a2cbba0dce4075ac
5df9e857f75ada60baf9e936007533a18389016451154bd1ed26e91b5babd844
c1ccc2c(c1)CSC2
C-C-C-C-N=[C;H0;D2;+0:1]=[O;D1;H0:2].[NH2;D1;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]>>[O;D1;H0:2]=[C;H0;D2;+0:1]=[N;H0;D2;+0:3]-[#16:4](=[O;D1;H0:5])(=[O;D1;H0:6])-[c:7]
null
[]
null
null
5
MINUTE
A mixture of 5.5 g of 1,3-dihydrobenzo[c]thiophene-4-sulfonamide, 2.5 g of butyl isocyanate and 0.05 g of DABCO® in 50 ml of xylene was heated to 135° and 2.2 ml of liquid phosgene was added in small portions at approximately 135°. When the addition of phosgene was complete, heating was continued for 5 minutes before t...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Isocyanate
null
null
null
c1ccc2c(c1)CSC2
Other
C=1(C(=CC=CC1)C)C
null
0.083333
CCCCN=C=O.NS(=O)(=O)c1cccc2c1CSC2>C=1(C(=CC=CC1)C)C>O=C=NS(=O)(=O)c1cccc2c1CSC2
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-063544486b52402f879594b5f17cda45
COC(=O)Nc1nc(OC)cc(OC)n1.NS(=O)(=O)c1cccc2c1CS(=O)(=O)C2>>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2cccc3c2CSC3)n1
COC1=NC(=NC(=C1)OC)NC(OC)=O.C[Al](C)C.C1S(CC2=C1C=CC=C2S(=O)(=O)N)(=O)=O.Cl>>COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C1=CC=CC=2CSCC21
CO[C:11]([NH:10][c:9]1[n:8][c:5]([O:6][CH3:7])[cH:4][c:3]([O:2][CH3:1])[n:26]1)=[O:12].O=[S:24]1(=O)[CH2:23][c:22]2[c:17]([S:14]([NH2:13])(=[O:15])=[O:16])[cH:18][cH:19][cH:20][c:21]2[CH2:25]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([O:6][CH3:7])[n:8][c:9]([NH:10][C:11](=[O:12])[NH:13][S:14](=[O:15])(=[O:16])[c:17]2[cH:18][cH:1...
COC(=O)Nc1nc(OC)cc(OC)n1.NS(=O)(=O)c1cccc2c1CS(=O)(=O)C2
COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2cccc3c2CSC3)n1
null
null
C1(=CC=CC=C1)C.C(Cl)Cl
Acylation
OtherReaction
48c18f6ef5bb69256637d7ec4e1277e7b1fb85955944d5b1024807a279058c13
9cf7fb13481173a489ce6c8f5303d937443bb3154e5e0bf1c0e0faf659542570
O=C(Nc1ncccn1)NS(=O)(=O)c1cccc2c1CSC2
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[#7:3]-[c:4](:[#7;a:5]):[#7;a:6].O=[S;H0;D4;+0:7]1(=O)-[C:8]-[c:9](:[c:10]-[#16:11](-[NH2;D1;+0:12])(=[O;D1;H0:13])=[O;D1;H0:14]):[c:15]-[C:16]-1>>[#7;a:5]:[c:4](-[#7:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:12]-[#16:11](=[O;D1;H0:13])(=[O;D1;H0:14])-[c:10]:[c:9]1:[c:15]-[C:16]-[S;H0;D...
26.1
[{"value": 26.1, "product": "COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C1=CC=CC=2CSCC21", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 0.74 g of the sulfonamide prepared in Example 13 in 50 ml of methylene chloride was cooled to 10° to 15° under nitrogen, and 1.7 ml of a 2M solution of trimethylaluminum in toluene was added slowly. The suspension was allowed to warm to room temperature, 0.67 g of methyl N-(4,6-dimethoxypyrimidin-2-yl)c...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide.Carbamic ester.Ether.Sulfone
Sulfonamide.Urea.Monosulfide
c1ccc2c(c1)CSC2
c1ccc2c(c1)CSC2
c1cncnc1.c1ccc2c(c1)CSC2
HO-
C1(=CC=CC=C1)C.C(Cl)Cl
null
null
COC(=O)Nc1nc(OC)cc(OC)n1.NS(=O)(=O)c1cccc2c1CS(=O)(=O)C2>C1(=CC=CC=C1)C.C(Cl)Cl>COc1cc(OC)nc(NC(=O)NS(=O)(=O)c2cccc3c2CSC3)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-249b94811ba9490698afb75a6c5f7e0e
CN1Cc2cccc(S(=O)(=O)NC(C)(C)C)c2C1>>CN1Cc2cccc(S(N)(=O)=O)c2C1
CC(C)(C)NS(=O)(=O)C=1C=2CN(CC2C=CC1)C.B.Cl>>Cl.CN1CC=2C=CC=C(C2C1)S(=O)(=O)N
CC(C)(C)[NH:10][S:9]([c:8]1[cH:7][cH:6][cH:5][c:4]2[c:13]1[CH2:14][N:2]([CH3:1])[CH2:3]2)(=[O:11])=[O:12]>>[CH3:1][N:2]1[CH2:3][c:4]2[cH:5][cH:6][cH:7][c:8]([S:9]([NH2:10])(=[O:11])=[O:12])[c:13]2[CH2:14]1
CN1Cc2cccc(S(=O)(=O)NC(C)(C)C)c2C1
CN1Cc2cccc(S(N)(=O)=O)c2C1
null
null
CO
Deprotection
Tert-butyl deprotection of amine
f7e1da1b4c254f1e6d5afbf8cb56733a4fabd145b80e971e3b7e31007de9e7d6
278d0fb11b582c058ac903379d7fbe11ab8c395937a204965031cf0c344845a9
c1ccc2c(c1)CNC2
C-C(-C)(-C)-[NH;D2;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]>>[NH2;D1;+0:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[c:5]
null
[]
null
null
null
null
A suspension of 5.3 g of the compound prepared in Example 16 in 20 ml of methanol was cooled to 10° and 50 ml of concentrated hydrochloric acid was added dropwise at 10°-15° (gas evolution). The reaction mixture was allowed to warm to room temperature and then refluxed 3.75 hours. The reaction solution was cooled and c...
10.6084/m9.figshare.5104873.v1
null
Sulfonamide
Sulfonamide
null
null
c1ccc2c(c1)C[NH]C2
Other
CO
null
null
CN1Cc2cccc(S(=O)(=O)NC(C)(C)C)c2C1>CO>CN1Cc2cccc(S(N)(=O)=O)c2C1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-a50d1f052edd4cf8a047bd5fea03700d
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(C)nc(N)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1
NC1=NC(=CC(=N1)C)C.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>CC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([CH3:21])[cH:22][c:23]([CH3:24])[n:25]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:20]([CH3:21])...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(C)nc(N)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
null
null
To 37 g. of 2-amino-4,6-dimethylpyrimidine in 500 ml of anhydrous acetonitrile was added 67 g of 2-methoxycarbonylbenzenesulfonylisocyanate with stirring at ambient temperatures. The resulting mixture was thereafter stirred for sixteen hours and then filtered to remove the desired product which had precipitated as a wh...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(C)#N
null
null
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(C)nc(N)n1>C(C)#N>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-6ac58de6463b4514a146dc2fe7fd0150
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1ncccn1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1ncccn1
NC1=NC=CC=N1.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>N1=C(N=CC=C1)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][cH:20][cH:21][cH:22][n:23]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][cH:20][cH:21][cH:22][n:23]1
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1ncccn1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1ncccn1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
null
null
With stirring at ambient temperature, 1.0 g of 2-aminopyrimidine in 25 ml of anhydrous acetonitrile was added to 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate. After stirring that mixture for 24 hours, the resultant precipitate was filtered off to yield 2.2 of the desired compound which melted at 188°-192°. Its s...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(C)#N
null
null
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Nc1ncccn1>C(C)#N>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1ncccn1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-d7657689bdfa4d728e9fe502d770f8f4
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(C)nc(N)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1
NC1=NC(=CC(=N1)OC)C.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([CH3:21])[cH:22][c:23]([O:24][CH3:25])[n:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:20]([CH...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(C)nc(N)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
null
[]
null
null
16
HOUR
To a stirred suspension of 1.4 g of 2-amino-4-methoxy-6-methylpyrimidine in 30 ml of anhydrous methylene chloride was added at ambient temperature 2.4 of 2-methoxycarbonylbenzenesulfonylisocyanate. After stirring for 16 hours, the foregoing mixture was filtered to remove unreacted amine, and the filtrate evaporated at ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(Cl)Cl
null
16
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(C)nc(N)n1>C(Cl)Cl>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-29ddd2f7388744f782d178475a0763ad
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(OC)nc(N)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)cc(OC)n1
[OH-].[Na+].NC1=NC(=CC(=N1)OC)OC.C(Cl)Cl.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([O:21][CH3:22])[cH:23][c:24]([O:25][CH3:26])[n:27]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:2...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(OC)nc(N)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)cc(OC)n1
null
null
O
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6].[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[N;H0;D2;+0:11]=[C;H0;D2;+0:12]=[O;D1;H0:13]>>[O;D1;H0:7]=[#16:8](=[O;D1;H0:9])(-[c:10])-[NH;D2;+0:11]-[C;H0;D3;+0:12](=[O;D1;H0:13])-[NH;D2;+0:1]-[c:2](:[#7;a:3]:[c:4]):[#7;a:5]:[c:6]
43.1
[{"value": 43.1, "product": "COC1=NC(=NC(=C1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
16
HOUR
A mixture containing 1.6 g of 2-amino-4,6-dimethoxypyrimidine, 30 ml of anhydrous methylene chloride and 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate was stirred at ambient temperature and pressure for 16 hours. It was then filtered to remove unreacted amine and the filtrate evaporated at temperatures up to 40° ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
O
null
16
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1cc(OC)nc(N)n1>O>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)cc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-5c979161a8de4610822a99c0859d08c6
COc1nc(N)nc(OC)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl>>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)nc(OC)n1
NC1=NC(=NC(=N1)OC)OC.ClCCOC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OCCCl
[CH3:1][O:2][c:3]1[n:4][c:5]([NH2:6])[n:25][c:26]([O:27][CH3:28])[n:29]1.[C:7](=[O:8])=[N:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[C:19](=[O:20])[O:21][CH2:22][CH2:23][Cl:24]>>[CH3:1][O:2][c:3]1[n:4][c:5]([NH:6][C:7](=[O:8])[NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][c:...
COc1nc(N)nc(OC)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl
COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)nc(OC)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
null
[]
null
null
null
null
To 0.7 g of 2-amino-4,6-dimethoxy-1,3,5-triazine in 10 ml anhydrous methylene chloride solvent was added 1.45 g 2-(β-chloroethoxycarbonyl)benzenesulfonyl isocyanate. After stirring at ambient temperature for sixteen hours the solvent was removed under reduced pressure, the residue triturated with ether and the solid pr...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ncncn1.c1ccccc1
null
C(Cl)Cl
null
null
COc1nc(N)nc(OC)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl>C(Cl)Cl>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)nc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-7328358f9f674acfa9a4e50d2e72f16b
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl>>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)n1
NC1=NC(=NC(=N1)OC)C.ClCCOC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OCCCl
[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH2:9])[n:28]1.[C:10](=[O:11])=[N:12][S:13](=[O:14])(=[O:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[C:22](=[O:23])[O:24][CH2:25][CH2:26][Cl:27]>>[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][S:13](=[O:14])(=[O:15])[c:16]2[cH:17][cH:18][...
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl
COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[C;H0;D2;+0:9]=[N;H0;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14]>>[O;D1;H0:8]=[C;H0;D3;+0:9](-[NH;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
80.1
[{"value": 80.1, "product": "COC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OCCCl", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 0.7 g of 2-amino-4-methoxy-6-methyl-1,3,5-triazine in 10 ml anhydrous methylene chloride solvent was added 1.45 g 2-(β-chloroethoxycarbonyl)benzenesulfonyl isocyanate with stirring at ambient temperature. The mixture was thereafter stirred for sixteen hours. The solvent was evaporated under reduced pressure and the ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ncncn1.c1ccccc1
null
C(Cl)Cl
null
null
COc1nc(C)nc(N)n1.O=C=NS(=O)(=O)c1ccccc1C(=O)OCCCl>C(Cl)Cl>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OCCCl)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-379f1a67d29d44b48e396b3ea3fe3528
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1>>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)nc(OC)n1
NC1=NC(=NC(=N1)OC)OC.C(C)(C)OC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC(C)C
[C:7](=[O:8])=[N:9][S:10](=[O:11])(=[O:12])[c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]1[C:19](=[O:20])[O:21][CH:22]([CH3:23])[CH3:24].[CH3:1][O:2][c:3]1[n:4][c:5]([NH2:6])[n:25][c:26]([O:27][CH3:28])[n:29]1>>[CH3:1][O:2][c:3]1[n:4][c:5]([NH:6][C:7](=[O:8])[NH:9][S:10](=[O:11])(=[O:12])[c:13]2[cH:14][cH:15][cH:16][cH:17][...
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1
COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)nc(OC)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
26.2
[{"value": 26.2, "product": "COC1=NC(=NC(=N1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 0.7 g of 2-amino-4,6-dimethoxy-1,3,5-triazine suspended in 5.0 ml anhydrous methylene chloride was added 1.6 g of 2-isopropoxycarbonylbenzenesulfonyl isocyanate in 5.0 ml anhydrous methylene chloride. The resulting mixture was filtered to remove some unreacted 2-amino-4,6-dimethoxytriazine, the methylene chloride fi...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ncncn1.c1ccccc1
null
C(Cl)Cl
null
null
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1>C(Cl)Cl>COc1nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)nc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3e64374bceef4d3e98affc0f14b126ad
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1>>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)n1
NC1=NC(=NC(=N1)OC)C.C(C)(C)OC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC(C)C
[C:10](=[O:11])=[N:12][S:13](=[O:14])(=[O:15])[c:16]1[cH:17][cH:18][cH:19][cH:20][c:21]1[C:22](=[O:23])[O:24][CH:25]([CH3:26])[CH3:27].[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH2:9])[n:28]1>>[CH3:1][O:2][c:3]1[n:4][c:5]([CH3:6])[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][S:13](=[O:14])(=[O:15])[c:16]2[cH:17][cH:18...
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1
COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[C;H0;D2;+0:9]=[N;H0;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14]>>[O;D1;H0:8]=[C;H0;D3;+0:9](-[NH;D2;+0:10]-[#16:11](=[O;D1;H0:12])(=[O;D1;H0:13])-[c:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
51.1
[{"value": 51.1, "product": "COC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 26.8 g of 2-amino-4-methoxy-6-methyl-1,3,5-triazine in 300 ml anhydrous methylene chloride was added 67.0 g of 2-isopropoxycarbonylbenzenesulfonyl isocyanate in 100 ml anhydrous methylene chloride. The resultant suspension was stirred at ambient temperature for 72 hours, and filtered to yield 40.0 g of the desired p...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ncncn1.c1ccccc1
null
C(Cl)Cl
null
null
CC(C)OC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1>C(Cl)Cl>COc1nc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)OC(C)C)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-1a42b4a852c246918fc407ff080bfbe6
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)n1
NC1=NC(=NC(=N1)OC)OC.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)OC)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([O:21][CH3:22])[n:23][c:24]([O:25][CH3:26])[n:27]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:20...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
null
[]
null
null
16
HOUR
A mixture of 1.6 g of 2-amino-4,6-dimethoxy-1,3,5-triazine, 25 ml of anhydrous methylene chloride and 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate was stirred at ambient temperature for 16 hours. It was then filtered to remove unreacted amine and the filtrate evaporated at temperatures up to 40° under reduced pr...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1ncncn1
null
C(Cl)Cl
null
16
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(N)nc(OC)n1>C(Cl)Cl>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(OC)nc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-17f4e25cab9e495396ead1253b029761
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC)n1
NC1=NC(=NC(=N1)OC)C.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>COC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][c:20]([CH3:21])[n:22][c:23]([O:24][CH3:25])[n:26]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][c:20]([CH3...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC)n1
null
null
C(Cl)Cl
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[#7;a:7]:1
null
[]
null
null
null
null
To an anhydrous suspension of 1.4 g of 2-amino-4-methoxy-6-methyl-1,3,5-triazine in 25 ml of methylene chloride was added with stirring at ambient temperature and pressure 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate. The mixture was thereafter stirred for 16 hours and filtered. The filtrate was evaporated to dr...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1ncncn1
null
C(Cl)Cl
null
null
COC(=O)c1ccccc1S(=O)(=O)N=C=O.COc1nc(C)nc(N)n1>C(Cl)Cl>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-df9242c3024e438a932c728f85902814
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1nnc(N)nc1C>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nnc(C)c(C)n1
NC=1N=NC(=C(N1)C)C.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>CC=1N=C(N=NC1C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[n:19][n:20][c:21]([CH3:22])[c:23]([CH3:24])[n:25]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[n:19][n:20][c:21]([CH3...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1nnc(N)nc1C
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nnc(C)c(C)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1nccnn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[#7;a:4]:[c:5]:[c:6]:[#7;a:7]:1
70.8
[{"value": 70.8, "product": "CC=1N=C(N=NC1C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a stirred suspension of 1.2 g of 3-amino-5,6-dimethyl-1,2,4-triazine in 25 ml of anhydrous acetonitrile was added at ambient temperature 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate. After stirring for 24 hours at ambient temperature, the resultant precipitate was filtered off to yield 2.5 g of the desired co...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cnncn1
null
C(C)#N
null
24
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1nnc(N)nc1C>C(C)#N>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nnc(C)c(C)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-3896c410ab374976982939d1b785eef7
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(N)nc(C)n1>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1cc(C)nc(C)n1
NC1=NC(=NC(=C1)C)C.COC(=O)C1=C(C=CC=C1)S(=O)(=O)N=C=O>>CC1=NC(=CC(=N1)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC)C
[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16].[NH2:17][c:18]1[cH:19][c:20]([CH3:21])[n:22][c:23]([CH3:24])[n:25]1>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16])[NH:17][c:18]1[cH:19][c:20]([CH3:21]...
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(N)nc(C)n1
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1cc(C)nc(C)n1
null
null
C(C)#N
Acylation
Urea synthesis via isocyanate and primary amine
b2f9721fe12517bb4ddb059bee81df64632e89cc2635ea9f7de5f84d579af016
ad01beb75a98e2ae01d9fc14d1face2625004bf1eae4aa0352da70e1110fdd06
O=C(Nc1ccncn1)NS(=O)(=O)c1ccccc1
[NH2;D1;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1.[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[N;H0;D2;+0:12]=[C;H0;D2;+0:13]=[O;D1;H0:14]>>[O;D1;H0:8]=[#16:9](=[O;D1;H0:10])(-[c:11])-[NH;D2;+0:12]-[C;H0;D3;+0:13](=[O;D1;H0:14])-[NH;D2;+0:1]-[c:2]1:[#7;a:3]:[c:4]:[#7;a:5]:[c:6]:[c:7]:1
null
[]
null
null
null
null
To a suspension of 1.2 g of 4-amino-2,6-dimethylpyrimidine in 30 ml of dry acetonitrile with stirring was added 2.4 g of 2-methoxycarbonylbenzenesulfonylisocyanate. The mixture was stirred for two hours at ambient temperature, allowed to stand for sixteen hours and the desired product, which had precipitated, was remov...
10.6084/m9.figshare.5104873.v1
null
Primary amine
Sulfonamide.Urea
null
null
c1ccccc1.c1cncnc1
null
C(C)#N
null
null
COC(=O)c1ccccc1S(=O)(=O)N=C=O.Cc1cc(N)nc(C)n1>C(C)#N>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1cc(C)nc(C)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-78754e277bf64816b19f44ca82c06a8b
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1>>Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
CC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC.[OH-].[Na+]>>CC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)O
C[O:23][C:21]([c:20]1[c:15]([S:12]([NH:11][C:9]([NH:8][c:7]2[n:6][c:4]([CH3:5])[cH:3][c:2]([CH3:1])[n:24]2)=[O:10])(=[O:13])=[O:14])[cH:16][cH:17][cH:18][cH:19]1)=[O:22]>>[CH3:1][c:2]1[cH:3][c:4]([CH3:5])[n:6][c:7]([NH:8][C:9](=[O:10])[NH:11][S:12](=[O:13])(=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21](=[O:2...
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1
Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
null
null
O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
null
null
A mixture of 2.0 g of N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulfonamide and 11 ml. of 50% aqueous sodium hydroxide was warmed on a steam bath with shaking; 40 ml. of water was added and heating and shaking continued during the next half hour. The resulting solution was then filtered and ...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cncnc1.c1ccccc1
Other
O
null
null
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(C)n1>O>Cc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-b579e7d807ce471091ae61696148e0d8
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1>>COc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
COC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)OC.[OH-].[K+].Cl>>COC1=NC(=NC(=C1)C)NC(=O)NS(=O)(=O)C1=C(C=CC=C1)C(=O)O
C[O:24][C:22]([c:21]1[c:16]([S:13]([NH:12][C:10]([NH:9][c:8]2[n:7][c:5]([CH3:6])[cH:4][c:3]([O:2][CH3:1])[n:25]2)=[O:11])(=[O:14])=[O:15])[cH:17][cH:18][cH:19][cH:20]1)=[O:23]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([CH3:6])[n:7][c:8]([NH:9][C:10](=[O:11])[NH:12][S:13](=[O:14])(=[O:15])[c:16]2[cH:17][cH:18][cH:19][cH:20][c:21]2...
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1
COc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
null
null
O.C(C)O
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C(Nc1ncccn1)NS(=O)(=O)c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])-[c:4]>>[O;D1;H0:3]=[C:2](-[OH;D1;+0:1])-[c:4]
null
[]
null
null
24
HOUR
4.0 g of N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulfonamide was dissolved in a mixture of 20 ml of absolute ethanol, 2.5 ml of water and 2.5 g of potassium hydroxide. After stirring at 25° for 24 hours the mixture had become a semi-solid mass. Enough cold water was added to dissolve...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1cncnc1.c1ccccc1
Other
O.C(C)O
null
24
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)cc(OC)n1>O.C(C)O>COc1cc(C)nc(NC(=O)NS(=O)(=O)c2ccccc2C(=O)O)n1
ord_dataset-c34472859da14a81bfe0f74e60f15c43
ord-4436e129eaef4387a197daa3a9056f9a
CCOC(=O)C(C)Oc1nc(C)nc(N)n1.COC(=O)c1ccccc1S(=O)(=O)N=C=O>>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC(C)C(=O)O)n1
S(=O)(=O)(N=C=O)N=C=O.Cl.N(=C=O)S(=O)(=O)C1=C(C(=O)OC)C=CC=C1.NC1=NC(=NC(=N1)C)OC(C(=O)OCC)C.[OH-].[Na+].S(=O)(=O)(N=C=O)N=C=O>>C(=O)(O)C(C)OC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C(=O)OC)C=CC=C1
CC[O:29][C:27]([CH:25]([O:24][c:23]1[n:22][c:20]([CH3:21])[n:19][c:18]([NH2:17])[n:30]1)[CH3:26])=[O:28].[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[N:14]=[C:15]=[O:16]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][c:10]1[S:11](=[O:12])(=[O:13])[NH:14][C:15](=[O:16]...
CCOC(=O)C(C)Oc1nc(C)nc(N)n1.COC(=O)c1ccccc1S(=O)(=O)N=C=O
COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC(C)C(=O)O)n1
null
null
O.C(Cl)Cl
Acylation
OtherReaction
873ec03fe95613b89e1cc5a05f22b73e12ebaee68f679a7c1a383abbdb2c243b
5dcf854e8ae1ebe2ca3cab743b2d9636aaa3c8192f5216ab3e9c6da3c3a8eaed
O=C(Nc1ncncn1)NS(=O)(=O)c1ccccc1
C-C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4].[NH2;D1;+0:5]-[c:6]1:[#7;a:7]:[c:8]:[#7;a:9]:[c:10]:[#7;a:11]:1.[O;D1;H0:12]=[#16:13](=[O;D1;H0:14])(-[c:15])-[N;H0;D2;+0:16]=[C;H0;D2;+0:17]=[O;D1;H0:18]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1].[O;D1;H0:12]=[#16:13](=[O;D1;H0:14])(-[c:15])-[NH;D2;+0:16]-[C;H0;D3;+0:17](=[O;...
23.8
[{"value": 23.8, "product": "C(=O)(O)C(C)OC1=NC(=NC(=N1)C)NC(=O)NS(=O)(=O)C1=C(C(=O)OC)C=CC=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
Methyl 2-(isocyanatosulfonyl)benzoate (10.1 g) and 8.0 g of ethyl 2-[(4-amino-6-methyl-1,3,5-triazin-2-yl)oxy]propanoate were stirred in 80 ml of methylene chloride at ambient temperature for 18 hours. An additional 2 g of the sulfonylisocyanate was added and the reaction mixture was stirred for four more hours and the...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary amine
Sulfonamide.Carboxylic acid.Urea
null
null
c1ccccc1.c1ncncn1
Other
O.C(Cl)Cl
null
null
CCOC(=O)C(C)Oc1nc(C)nc(N)n1.COC(=O)c1ccccc1S(=O)(=O)N=C=O>O.C(Cl)Cl>COC(=O)c1ccccc1S(=O)(=O)NC(=O)Nc1nc(C)nc(OC(C)C(=O)O)n1