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414 values
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large_stringlengths
36
36
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large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
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large_stringlengths
14
3.37k
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1
581
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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
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large_stringlengths
5
288
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large_stringlengths
24
2.64k
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float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
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large_stringclasses
3 values
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float64
0
4k
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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-01dbb772c5e249108f0b191ed17a2c0c
ord-a75e54f6a7504dcd907a03e3ff22457e
CC(=S)OCCl.Cn1ccnc1>>CC(=S)OC[n+]1ccn(C)c1.[Cl-]
CN1C=NC=C1.ClCOC(C)=S>>[Cl-].C(C)(=S)OC[N+]1=CN(C=C1)C
[CH3:1][C:2](=[S:3])[O:4][CH2:5][Cl:12].[n:6]1[cH:7][cH:8][n:9]([CH3:10])[cH:11]1>>[CH3:1][C:2](=[S:3])[O:4][CH2:5][n+:6]1[cH:7][cH:8][n:9]([CH3:10])[cH:11]1.[Cl-:12]
CC(=S)OCCl.Cn1ccnc1
CC(=S)OC[n+]1ccn(C)c1.[Cl-]
null
null
null
Functional Group Interconversion
OtherReaction
f75f0e838a29c549290e6181c709c5384561f85dfac9d38699be07b677e32d50
42c71821dc42e0c1902cec868cf7d0abd0a4511b0313126f4c5eb9aac58d5cad
c1c[nH+]c[nH]1
[C;D1;H3:1]-[#7;a:2]1:[c:3]:[n;H0;D2;+0:4]:[c:5]:[c:6]:1.[C;D1;H3:7]-[C:8](=[S;D1;H0:9])-[#8:10]-[CH2;D2;+0:11]-[Cl;H0;D1;+0:12]>>[C;D1;H3:1]-[#7;a:2]1:[c:3]:[n+;H0;D3:4](-[CH2;D2;+0:11]-[#8:10]-[C:8](-[C;D1;H3:7])=[S;D1;H0:9]):[c:5]:[c:6]:1.[Cl-;H0;D0:12]
null
[]
null
null
10
MINUTE
To 0.7 g (8.52 millimoles) of 1-methylimidazole was added slowly and with cooling, 1.5 g of (16.2 millimoles) chloromethylthioacetate. The solution solidified in 10 minutes and was left stoppered at room temperature overnight. Conditions: See reaction.notes.procedure_details. Workup: with cooling; was left; stoppered a...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether
c1c[nH]cn1
c1c[n+]cn1
c1c[n+]cn1
null
null
null
0.166667
CC(=S)OCCl.Cn1ccnc1>>CC(=S)OC[n+]1ccn(C)c1.[Cl-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a9feead895f943e08dea8241895071cb
FC(F)(F)C(F)(F)C(F)(F)I.O=C(CCl)CCl.c1nc[nH]n1>>FC(F)(F)C(F)(F)C(F)(F)C1(Cn2cncn2)CO1
N1N=CN=C1.C([O-])([O-])=O.[K+].[K+].ClCC(=O)CCl.[Cl-].[NH4+].C1(=CC=CC=C1)[Mg]Br.FC(C(F)(F)I)(C(F)(F)F)F>>FC(C(C1(OC1)CN1N=CN=C1)(F)F)(C(F)(F)F)F
I[C:8]([C:5]([C:2]([F:1])([F:3])[F:4])([F:6])[F:7])([F:9])[F:10].Cl[CH2:12][C:11]([CH2:18]Cl)=[O:19].[nH:13]1[cH:14][n:15][cH:16][n:17]1>>[F:1][C:2]([F:3])([F:4])[C:5]([F:6])([F:7])[C:8]([F:9])([F:10])[C:11]1([CH2:12][n:13]2[cH:14][n:15][cH:16][n:17]2)[CH2:18][O:19]1
FC(F)(F)C(F)(F)C(F)(F)I.O=C(CCl)CCl.c1nc[nH]n1
FC(F)(F)C(F)(F)C(F)(F)C1(Cn2cncn2)CO1
null
null
CN(C=O)C.[Cl-].[Na+].O.O.C(C)OCC
Heteroatom Alkylation and Arylation
OtherReaction
5987faaf33ecde06088464172ca0b8907c36c6835b86556126be864a0e21a050
9463313198c4cf1e31239253ca680f9356f76442f90ead176638713b939bb0f8
c1ncn(CC2CO2)n1
Cl-[CH2;D2;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[CH2;D2;+0:4]-Cl.I-[C;H0;D4;+0:5](-[F;D1;H0:6])(-[F;D1;H0:7])-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[C:11](-[F;D1;H0:12])(-[F;D1;H0:13])-[F;D1;H0:14].[#7;a:15]1:[c:16]:[nH;D2;+0:17]:[#7;a:18]:[c:19]:1>>[F;D1;H0:6]-[C;H0;D4;+0:5](-[F;D1;H0:7])(-[C:8](-[F;D1;H0:9])(-[F;D1;H0:...
2.1
[{"value": 2.1, "product": "FC(C(C1(OC1)CN1N=CN=C1)(F)F)(C(F)(F)F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of heptafluoropropyl iodide (14.58 g, 49.2 m.mole) in diethylether (65 ml) was stirred and cooled to -70°. A solution of phenylmagnesium bromide in diethylether (15.75 ml of a 3 molar solution; 47.25 m.mole) was then added dropwise at such a rate that the temperature of the reaction mixture did not exceed -6...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Tertiary halide.Primary halide.Primary halide.Ketone
Tertiary halide.Tertiary halide.Ether
c1nc[nH]n1
c1nc[nH]n1.C1CO1
c1nc[nH]n1.C1CO1
HCl.I-
CN(C=O)C.[Cl-].[Na+].O.O.C(C)OCC
null
0.25
FC(F)(F)C(F)(F)C(F)(F)I.O=C(CCl)CCl.c1nc[nH]n1>CN(C=O)C.[Cl-].[Na+].O.O.C(C)OCC>FC(F)(F)C(F)(F)C(F)(F)C1(Cn2cncn2)CO1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-654d2a1fc7d54165a1a2363bf543e3e1
CC(S(C)(=O)=O)S(=O)(=O)[O-].ClP(Cl)(Cl)(Cl)Cl>>CC(S(C)(=O)=O)S(=O)(=O)Cl
Cl.CS(=O)(=O)C(C)S(=O)(=O)[O-].[Na+].CS(=O)(=O)C(C)S(=O)(=O)[O-].[Na+].P(Cl)(Cl)(Cl)(Cl)Cl>>CS(=O)(=O)C(C)S(=O)(=O)Cl
[O-][S:7]([CH:2]([CH3:1])[S:3]([CH3:4])(=[O:5])=[O:6])(=[O:8])=[O:9].ClP(Cl)(Cl)(Cl)[Cl:10]>>[CH3:1][CH:2]([S:3]([CH3:4])(=[O:5])=[O:6])[S:7](=[O:8])(=[O:9])[Cl:10]
CC(S(C)(=O)=O)S(=O)(=O)[O-].ClP(Cl)(Cl)(Cl)Cl
CC(S(C)(=O)=O)S(=O)(=O)Cl
null
null
ClCCl
Functional Group Interconversion
OtherReaction
1d60417dbcce8291d459a7fb34824cf29ea6f69a30ac46aeb585ac8e7b69013e
4a93b4a9749514113cd3dffa44b64f21b1f88d26b8739299bcad711fe7a13a1b
null
Cl-P(-Cl)(-Cl)(-Cl)-[Cl;H0;D1;+0:1].[#16:2]-[C:3](-[C;D1;H3:4])-[S;H0;D4;+0:5](-[O-])(=[O;D1;H0:6])=[O;D1;H0:7]>>[#16:2]-[C:3](-[C;D1;H3:4])-[S;H0;D4;+0:5](-[Cl;H0;D1;+0:1])(=[O;D1;H0:6])=[O;D1;H0:7]
null
[]
null
null
20
MINUTE
A mixture of 5 g of sodium 1-(methylsulfonyl)ethanesulfonate (Formula II, X=R=CH3, Y=Na) and 5.34 g of phosphorus pentachloride was stirred under an inert atmosphere at room temperature. After about 20 minutes, the evolution of hydrogen chloride and the generation of heat were observed, and shortly thereafter the mixtu...
10.6084/m9.figshare.5104873.v1
null
Sulfonic acid
Sulfonyl halide
null
null
null
Other
ClCCl
null
0.333333
CC(S(C)(=O)=O)S(=O)(=O)[O-].ClP(Cl)(Cl)(Cl)Cl>ClCCl>CC(S(C)(=O)=O)S(=O)(=O)Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e42584a889aa47489b41adbbc5fd7a0b
CCN(CC)CC.CS(=O)(=O)Cl.OCCCl>>CS(=O)(=O)CS(=O)(=O)OCCCl
C(C)N(CC)CC.ClCCO.CS(=O)(=O)Cl>>CS(=O)(=O)CS(=O)(=O)OCCCl
CCN(CC)C[CH3:1].Cl[S:2](=[O:3])(=[O:4])[CH3:5].[OH:9][CH2:10][CH2:11][Cl:12]>>[CH3:1][S:2](=[O:3])(=[O:4])[CH2:5][S:6](=[O:7])(=[O:8])[O:9][CH2:10][CH2:11][Cl:12]
CCN(CC)CC.CS(=O)(=O)Cl.OCCCl
CS(=O)(=O)CS(=O)(=O)OCCCl
null
null
C(C)#N
Oxidation
OtherReaction
5ff5625b9b80dadb5cd70f9d61f0a4f01259c20af0e162e9aa149626cef6fb8d
d8adddb00d4da01ce543b4b6067a981164ee620a1cd22edfcbe14bd0de7deb95
null
C-C-N(-C-C)-C-[CH3;D1;+0:1].Cl-[S;H0;D4;+0:2](-[CH3;D1;+0:3])(=[O;D1;H0:4])=[O;D1;H0:5].[C:6]-[C:7]-[OH;D1;+0:8]>>[C:6]-[C:7]-[O;H0;D2;+0:8]-[#16:9](=[O;D1;H0:10])(=[O;D1;H0:11])-[CH2;D2;+0:3]-[S;H0;D4;+0:2](-[CH3;D1;+0:1])(=[O;D1;H0:4])=[O;D1;H0:5]
null
[]
null
null
1
HOUR
A solution of 133 g (1.32 mol.) of triethylamine in 400 ml of anhydrous acetonitrile was cooled to -30° to -40° C., and a solution of 100 g (0.88 mol.) of methanesulfonyl chloride in anhydrous acetonitrile (67 ml) was added dropwise at a rate that prevented the temperature from rising above -30° C. The mixture was stir...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Tertiary amine.Sulfonyl halide
Sulfone.Sulfonate
null
null
null
HCl
C(C)#N
null
1
CCN(CC)CC.CS(=O)(=O)Cl.OCCCl>C(C)#N>CS(=O)(=O)CS(=O)(=O)OCCCl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-79c238d7b16349c6ba9878c87b186e20
CC(=O)c1ccc(O)cc1.ClCCCBr>>CC(=O)c1ccc(OCCCCl)cc1
OC1=CC=C(C=C1)C(C)=O.BrCCCCl.[OH-].[K+]>>ClCCCOC1=CC=C(C=C1)C(C)=O
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([OH:8])[cH:13][cH:14]1.Br[CH2:9][CH2:10][CH2:11][Cl:12]>>[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]([O:8][CH2:9][CH2:10][CH2:11][Cl:12])[cH:13][cH:14]1
CC(=O)c1ccc(O)cc1.ClCCCBr
CC(=O)c1ccc(OCCCCl)cc1
null
null
CO
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
c1ccccc1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
68
[{"value": 68.0, "product": "ClCCCOC1=CC=C(C=C1)C(C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of p-hydroxyacetophenone (50.7 g, 0.37 mol) and 1-bromo-3-chloropropane (160 ml, 1.5 mol) in methanol (250 ml) was added portionwise potassium hydroxide (63 g, 1.12 mol). The mixture was stirred at reflux for 24 hours, cooled to room temperature, filtered through Celite and evaporated in vacuo. The residua...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1
HBr
CO
null
null
CC(=O)c1ccc(O)cc1.ClCCCBr>CO>CC(=O)c1ccc(OCCCCl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d942c39a6e844fd1a0e45833b16e0d3f
ClCCCOc1ccc(-c2cn3ccccc3n2)cc1>>CCCCN(CCCC)CCCOc1ccc(-c2cn3ccccc3n2)cc1
ClCCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2)C1>>C(CCC)N(CCCC)CCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2)C1
Cl[CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:1][cH:16][c:17](-[c:18]2[n:5][c:25]3[n:20]([cH:19]2)[cH:21][cH:22][cH:23][cH:24]3)[cH:27][cH:28]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][O:13][c:14]1[cH:15][cH:16][c:17](-[c:18]2[cH:19][n:20]3[cH:21][cH:22][cH:23][cH:24][c:25]3...
ClCCCOc1ccc(-c2cn3ccccc3n2)cc1
CCCCN(CCCC)CCCOc1ccc(-c2cn3ccccc3n2)cc1
null
null
C(CCC)NCCCC
Miscellaneous
OtherReaction
591490c6d5cf2519b6d716180b5ccc013cd7be0b0fd86285c9b63d9b0d4326b6
dd2fd64966e831a5c6f0bf6fdc3dbb91e77030e61e194c03e38ff8b04df63fff
c1ccc(-c2cn3ccccc3n2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4]-[c;H0;D3;+0:5]1:[c:6]:[c:7]:[c:8](-[c;H0;D3;+0:9]2:[c:10]:[#7;a:11](:[c:12]):[c;H0;D3;+0:13](:[c:14]:[c:15]):[n;H0;D2;+0:16]:2):[cH;D2;+0:17]:[cH;D2;+0:18]:1>>[C:19]-[C:20]-[N;H0;D3;+0:16](-[C:21]-[C:22]-[C:23]-[CH3;D1;+0:18])-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4]-[c;H0;D3;+0:5]1:[c:24]:[...
192
[{"value": 93.0, "product": "C(CCC)N(CCCC)CCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2)C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 192.0, "product": "C(CCC)N(CCCC)CCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A suspension of 2-(4-chloropropoxyphenyl)imidazo[1,2-a]-pyridine (5.2 g, 14 mmol) in dibutylamine (30 ml) was stirred at reflux for 5 hours. The excess dibutylamine was removed by distillation and the resulting oil was flash chromatographed (silica gel, 9:1 CH2Cl2 : acetone) to give the free base of the title compound ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether.Tertiary amine
c1ccccc1.c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
null
C(CCC)NCCCC
null
null
ClCCCOc1ccc(-c2cn3ccccc3n2)cc1>C(CCC)NCCCC>CCCCN(CCCC)CCCOc1ccc(-c2cn3ccccc3n2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9efe203deaa442a39739846cd4aff0b2
CCC(=O)c1ccc(O)cc1.CCCCNCCCC.Cc1cccnc1N.ClCCCBr>>CCCCN(CCCC)CCCOc1ccc(-c2nc3c(C)cccn3c2C)cc1
CC=1C(=NC=CC1)N.C(CCC)NCCCC.OC1=CC=C(C=C1)C(CC)=O.BrCCCCl.BrBr>>C(CCC)N(CCCC)CCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2C)C1C
O=[C:18]([c:17]1[cH:16][cH:15][c:14]([OH:13])[cH:30][cH:29]1)[CH2:27][CH3:28].[CH3:1][CH2:2][CH2:3][CH2:4][NH:5][CH2:6][CH2:7][CH2:8][CH3:9].[NH2:19][c:20]1[c:21]([CH3:22])[cH:23][cH:24][cH:25][n:26]1.Cl[CH2:10][CH2:11][CH2:12]Br>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]([CH2:6][CH2:7][CH2:8][CH3:9])[CH2:10][CH2:11][CH2:12][O...
CCC(=O)c1ccc(O)cc1.CCCCNCCCC.Cc1cccnc1N.ClCCCBr
CCCCN(CCCC)CCCOc1ccc(-c2nc3c(C)cccn3c2C)cc1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
45fdad3885031b4160ef11025b59908ff19264a75e5938f66dcbb58594528350
3277b3d365a6681ab73086f20be42bfaa9991749dff2a06105284a8ee9d8caef
c1ccc(-c2cn3ccccc3n2)cc1
Br-[CH2;D2;+0:1]-[C:2]-[CH2;D2;+0:3]-Cl.O=[C;H0;D3;+0:4](-[CH2;D2;+0:5]-[C;D1;H3:6])-[c;H0;D3;+0:7]1:[c:8]:[c:9]:[c:10](-[OH;D1;+0:11]):[c:12]:[c:13]:1.[C:14]-[C:15]-[NH;D2;+0:16]-[C:17]-[C:18].[NH2;D1;+0:19]-[c:20](:[c:21]):[n;H0;D2;+0:22]:[c:23]:[c:24]>>[C:14]-[C:15]-[N;H0;D3;+0:16](-[C:17]-[C:18])-[CH2;D2;+0:3]-[C:2...
62
[{"value": 62.0, "product": "C(CCC)N(CCCC)CCCOC1=CC=C(C=C1)C=1N=C2N(C=CC=C2C)C1C", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
p-Hydroxypropiophenone (50 g, 0.33 mmol) was reacted with 1-bromo-3-chloropropane and the resulting compound reacted with bromine as described in Example 1. The resulting compound was reacted with 3-methyl-2-aminopyridine (1.7 g, 16 mmol) and the product reacted with dibutylamine as described in Example 1 to produce 2....
10.6084/m9.figshare.5104873.v1
null
Primary halide.Primary halide.Ketone.Aromatic alcohol.Primary amine.Secondary amine
Ether.Tertiary amine
c1ccncc1
c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
HCl.Br-
null
null
null
CCC(=O)c1ccc(O)cc1.CCCCNCCCC.Cc1cccnc1N.ClCCCBr>>CCCCN(CCCC)CCCOc1ccc(-c2nc3c(C)cccn3c2C)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2f581a38daf94834b468162a35cf8171
Cc1cccn2cc(C(=O)c3ccc(OCCCCl)cc3)nc12>>CCCCN(CCCC)CCCOc1ccc(C(=O)c2cn3cccc(C)c3n2)cc1
ClCCCOC1=CC=C(C(=O)C=2N=C3N(C=CC=C3C)C2)C=C1>>C(CCC)N(CCCC)CCCOC1=CC=C(C(=O)C=2N=C3N(C=CC=C3C)C2)C=C1
Cl[CH2:10][CH2:11][CH2:12][O:13][c:14]1[cH:1][cH:16][c:17]([C:18](=[O:19])[c:20]2[cH:21][n:5]3[cH:6][cH:24][cH:25][c:26]([CH3:27])[c:28]3[n:29]2)[cH:30][cH:31]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][O:13][c:14]1[cH:15][cH:16][c:17]([C:18](=[O:19])[c:20]2[cH:21][n:22]3[...
Cc1cccn2cc(C(=O)c3ccc(OCCCCl)cc3)nc12
CCCCN(CCCC)CCCOc1ccc(C(=O)c2cn3cccc(C)c3n2)cc1
null
null
C(CCC)NCCCC
Miscellaneous
OtherReaction
591490c6d5cf2519b6d716180b5ccc013cd7be0b0fd86285c9b63d9b0d4326b6
dd2fd64966e831a5c6f0bf6fdc3dbb91e77030e61e194c03e38ff8b04df63fff
O=C(c1ccccc1)c1cn2ccccc2n1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4]-[c;H0;D3;+0:5]1:[c:6]:[c:7]:[c:8](-[C:9](=[O;D1;H0:10])-[c:11]2:[#7;a:12]:[c;H0;D3;+0:13]3:[c:14](-[C;D1;H3:15]):[c:16]:[cH;D2;+0:17]:[cH;D2;+0:18]:[n;H0;D3;+0:19]:3:[cH;D2;+0:20]:2):[cH;D2;+0:21]:[cH;D2;+0:22]:1>>[C:23]-[C:24]-[CH2;D2;+0:18]-[N;H0;D3;+0:19](-[C:25]-[C:26]-[C:27]-[CH...
197.7
[{"value": 100.0, "product": "C(CCC)N(CCCC)CCCOC1=CC=C(C(=O)C=2N=C3N(C=CC=C3C)C2)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 197.7, "product": "C(CCC)N(CCCC)CCCOC1=CC=C(C(=O)C=2N=C3N(C=CC=C3C)C2)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 2-(4-chloropropoxybenzoyl)-8-methylimidazo-[1,2-a]pyridine (2,4 g, 6.0 mmol) in dibutylamine (30 ml) was stirred at reflux for 8 hours. The excess dibutylamine was removed by distillation and the resulting oil was flash chromatographed (silica gel, acetone) to give the free base of the title compound (2.5 ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ether
Ether.Tertiary amine
c1ccccc1.c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
c1ccccc1.c1ccn2ccnc2c1
null
C(CCC)NCCCC
null
null
Cc1cccn2cc(C(=O)c3ccc(OCCCCl)cc3)nc12>C(CCC)NCCCC>CCCCN(CCCC)CCCOc1ccc(C(=O)c2cn3cccc(C)c3n2)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e27c01981aec452885615db0b8aa697e
Cc1ccnc(N)c1>>Cc1cn2ccccc2n1
C(CCC)NCCCC.CC1=CC(=NC=C1)N>>CC=1N=C2N(C=CC=C2)C1
[CH3:1][c:7]1[cH:6][cH:5][n:4][c:9]([NH2:10])[cH:8]1>>[CH3:1][c:2]1[cH:3][n:4]2[cH:5][cH:6][cH:7][cH:8][c:9]2[n:10]1
Cc1ccnc(N)c1
Cc1cn2ccccc2n1
null
null
null
Aromatic Heterocycle Formation
OtherReaction
6d486165009112780e608dff97176824bff10b35baa5286e796a3ea4a90aee71
0c2e6cfe0bdb8f8cd78303a7637b3ef339f807f5bc27c4a22ad516ce20b37476
c1ccn2ccnc2c1
[CH3;D1;+0:1]-[c;H0;D3;+0:2]1:[c:3]:[c:4]:[n;H0;D2;+0:5]:[c:6](-[NH2;D1;+0:7]):[c:8]:1>>[CH3;D1;+0:1]-[c:9]1:[c:10]:[n;H0;D3;+0:5]2:[c:4]:[c:3]:[cH;D2;+0:2]:[c:8]:[c:6]:2:[n;H0;D2;+0:7]:1
75
[{"value": 75.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
4-Methyl-2-aminopyridine (1.4 g, 12.5 mmol) was reacted with β-bromo-α-keto-(4-chloropropoxy)propiophenone as described in Example 8. The resulting product was reacted with dibutylamine as described in Example 8 to produce 2.9 g (75% yield) of the free base of the title compound which was converted to the HCl salt, mp ...
10.6084/m9.figshare.5104873.v1
null
Primary amine
null
c1ccncc1
c1ccn2ccnc2c1
c1ccn2ccnc2c1
Other
null
null
null
Cc1ccnc(N)c1>>Cc1cn2ccccc2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-79b7e20c21f04bd287a87a9adaed0cfb
CCCCN(CCCC)CCCCl.Cc1cccn2c(C(=O)c3ccc(O)cc3)cnc12>>CCCCN(CCCC)CCCOc1ccc(C(=O)c2cnc3c(C)cccn23)cc1
OC1=CC=C(C(=O)C2=CN=C3N2C=CC=C3C)C=C1.C(CCC)N(CCCC)CCCCl.[OH-].[K+]>>C(CCC)N(CCCC)CCCOC1=CC=C(C(=O)C2=CN=C3N2C=CC=C3C)C=C1
Cl[CH2:12][CH2:11][CH2:10][N:5]([CH2:4][CH2:3][CH2:2][CH3:1])[CH2:6][CH2:7][CH2:8][CH3:9].[OH:13][c:14]1[cH:15][cH:16][c:17]([C:18](=[O:19])[c:20]2[cH:21][n:22][c:23]3[c:24]([CH3:25])[cH:26][cH:27][cH:28][n:29]23)[cH:30][cH:31]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][O:...
CCCCN(CCCC)CCCCl.Cc1cccn2c(C(=O)c3ccc(O)cc3)cnc12
CCCCN(CCCC)CCCOc1ccc(C(=O)c2cnc3c(C)cccn23)cc1
null
null
CO
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=C(c1ccccc1)c1cnc2ccccn12
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[OH;D1;+0:4]-[c:5](:[c:6]):[c:7]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:4]-[c:5](:[c:6]):[c:7]
31
[{"value": 31.0, "product": null, "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 3-(4-hydroxybenzoyl)-8-methylimidazo[1,2-a]-pyridine (2.3 g, 9.6 mmol), dibutylaminopropyl chloride (6.8 g, 33 mmol) and potassium hydroxide (1.3 g, 23 mmol) in methanol (60 ml) was stirred at reflux for 96 hours. The mixture was concentrated and the resulting oil was flash chromatographed (silica gel, 2.5...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccccc1.c1ccn2ccnc2c1
HCl
CO
null
null
CCCCN(CCCC)CCCCl.Cc1cccn2c(C(=O)c3ccc(O)cc3)cnc12>CO>CCCCN(CCCC)CCCOc1ccc(C(=O)c2cnc3c(C)cccn23)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d9b4785edab5498986fa0d5639524ba5
CCCCCCCCN(C)C.CCl>>CCCCCCCC[N+](C)(C)C
CCl.C(CCCCCCC)N(C)C.C[O-].[Na+].CO.O=P12OP3(=O)OP(=O)(O1)OP(=O)(O2)O3.C(CCCCCCC)O>>C[O-].C(CCCCCCC)[N+](C)(C)C
[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][N:9]([CH3:11])[CH3:12].Cl[CH3:10]>>[CH3:1][CH2:2][CH2:3][CH2:4][CH2:5][CH2:6][CH2:7][CH2:8][N+:9]([CH3:10])([CH3:11])[CH3:12]
CCCCCCCCN(C)C.CCl
CCCCCCCC[N+](C)(C)C
null
[Cl-].C(CCCCCCC)[N+](C)(C)C
CO
Heteroatom Alkylation and Arylation
OtherReaction
4fb461fd1d845eeffcd721907fb84dda2a83d6f16d6187a0c591ac1d342a1cfa
7c33147a6170e63e1fbe1110c4ce069481be57a96b70c4a5a6d7e8253f321bd2
null
Cl-[CH3;D1;+0:1].[C:2]-[C:3]-[N;H0;D3;+0:4](-[C;D1;H3:5])-[C;D1;H3:6]>>[C:2]-[C:3]-[N+;H0;D4:4](-[C;D1;H3:5])(-[C;D1;H3:6])-[CH3;D1;+0:1]
null
[]
null
null
null
null
One mol of phosphoric anhydride was added to three mols of octyl alcohol over a period of one hour at 60°-70° C. while stirring. They were allowed to react which each other at 70° C. for three hours and a mixture of mono and dioctyl phosphate was obtained. Separately, 0.5 mol of octyl dimethylamine and 200 ml of methan...
10.6084/m9.figshare.5104873.v1
null
Tertiary amine
null
null
null
null
Other
[Cl-].C(CCCCCCC)[N+](C)(C)C.CO
null
null
CCCCCCCCN(C)C.CCl>[Cl-].C(CCCCCCC)[N+](C)(C)C.CO>CCCCCCCC[N+](C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2a2734eb88c143a38c09acebdd4195a1
CO.COc1ccc(C(O)C(Cl)=C(Cl)Cl)cc1>>COC(=O)/C(Cl)=C/c1ccc(OC)cc1
COC1=CC=C(C=C1)C(O)C(=C(Cl)Cl)Cl.S(O)(O)(=O)=O.CO.Cl>>COC(/C(=C/C1=CC=C(C=C1)OC)/Cl)=O
[CH3:1][OH:2].Cl[C:3](Cl)=[C:5]([Cl:6])[CH:7]([OH:4])[c:8]1[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15]1>>[CH3:1][O:2][C:3](=[O:4])/[C:5]([Cl:6])=[CH:7]/[c:8]1[cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14][cH:15]1
CO.COc1ccc(C(O)C(Cl)=C(Cl)Cl)cc1
COC(=O)/C(Cl)=C/c1ccc(OC)cc1
null
null
O
Acylation
OtherReaction
85a9acbb3963c3118be5d9eea104f46e6d1f681a056980835cd756054a03a5ad
05c3e2fd7be4c52576083ab6610a63b9a558e4326fe2c24a265da529743d42d3
c1ccccc1
Cl-[C;H0;D3;+0:1](-Cl)=[C;H0;D3;+0:2](-[Cl;D1;H0:3])-[CH;D3;+0:4](-[OH;D1;+0:5])-[c:6](:[c:7]):[c:8].[C;D1;H3:9]-[OH;D1;+0:10]>>[C;D1;H3:9]-[O;H0;D2;+0:10]-[C;H0;D3;+0:1](=[O;H0;D1;+0:5])/[C;H0;D3;+0:2](-[Cl;D1;H0:3])=[CH;D2;+0:4]/[c:6](:[c:7]):[c:8]
99
[{"value": 99.0, "product": "COC(/C(=C/C1=CC=C(C=C1)OC)/Cl)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
p-Methoxyphenyltrichlorovinyl carbinol (2.3 g, 8.6 millimoles) is added to a 40:60 (V/V) solution of sulfuric acid/methanol which is stirred under nitrogen at reflux (100° C.-106° C.) for 7 minutes. Rapid evolution of hydrogen chloride is noted and ceases after this period. The solution is cooled and poured into 40 ml ...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Alkenyl halide.Secondary alcohol.Methanol
Alkenyl halide.Ester
null
null
c1ccccc1
HCl
O
null
null
CO.COc1ccc(C(O)C(Cl)=C(Cl)Cl)cc1>O>COC(=O)/C(Cl)=C/c1ccc(OC)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0456d0b63d08430e9b2503ac98653c65
COC(=O)/C(Cl)=C/c1ccc(OC)cc1.OC(C(Cl)=C(Cl)Cl)c1ccc(Cl)cc1>>COC(=O)/C(Cl)=C/c1ccc(Cl)cc1
ClC1=CC=C(C=C1)C(O)C(=C(Cl)Cl)Cl.COC(/C(=C/C1=CC=C(C=C1)OC)/Cl)=O.Cl>>COC(/C(=C/C1=CC=C(C=C1)Cl)/Cl)=O
COc1cc[c:8](/[CH:7]=[C:5](/[C:3]([O:2][CH3:1])=[O:4])[Cl:6])cc1.OC(C(Cl)=C(Cl)Cl)c1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1>>[CH3:1][O:2][C:3](=[O:4])/[C:5]([Cl:6])=[CH:7]/[c:8]1[cH:9][cH:10][c:11]([Cl:12])[cH:13][cH:14]1
COC(=O)/C(Cl)=C/c1ccc(OC)cc1.OC(C(Cl)=C(Cl)Cl)c1ccc(Cl)cc1
COC(=O)/C(Cl)=C/c1ccc(Cl)cc1
null
null
null
Miscellaneous
OtherReaction
863cb6c491b8b6a6d8515759e2616072fce5116ba5532c5823ba4718c1a63042
b65bf6cd960929e38ef1569ca53784dd79edd5d3795bf9ad77bfbf40d36c41e0
c1ccccc1
C-O-c1:c:c:[c;H0;D3;+0:1](/[C:2]=[C:3](\[Cl;D1;H0:4])-[C:5](-[#8:6])=[O;D1;H0:7]):c:c:1.Cl-C(-Cl)=C(-Cl)-C(-O)-c1:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:1>>[#8:6]-[C:5](=[O;D1;H0:7])/[C:3](-[Cl;D1;H0:4])=[C:2]/[c;H0;D3;+0:1]1:[cH;D2;+0:8]:[c:9]:[c:10]:[c:11]:[cH;D2;+0:12]:1
93
[{"value": 93.0, "product": "COC(/C(=C/C1=CC=C(C=C1)Cl)/Cl)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
p-Chlorophenyltrichlorovinyl carbinol (6.0 g, 22.0 millimoles) is added to a refluxing solution of methanolic sulfuric acid (30 ml as noted in Example 4). Hydrogen chloride evolution is noted during the stirring procedure for 45 minutes. The mixture is cooled and has a workup as in Example 4, which affords z-methyl-2-c...
10.6084/m9.figshare.5104873.v1
null
Alkenyl halide.Alkenyl halide.Alkenyl halide.Ether.Secondary alcohol
null
c1ccccc1.c1ccccc1
c1ccccc1
c1ccccc1
HCl
null
null
null
COC(=O)/C(Cl)=C/c1ccc(OC)cc1.OC(C(Cl)=C(Cl)Cl)c1ccc(Cl)cc1>>COC(=O)/C(Cl)=C/c1ccc(Cl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4bb14ca94d854de98c85274ad779da40
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]>>O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
CN(C=O)C.S(=O)(Cl)Cl.[N+](=O)([O-])C1=C(C=CC=C1)CC(C(=O)O)=O>>OC(C(=O)O)CC1=C(C=CC=C1)[N+](=O)[O-]
[O:1]=[C:2]([OH:3])[C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[N+:13](=[O:14])[O-:15]>>[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[N+:13](=[O:14])[O-:15]
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]
O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
null
null
null
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6]-[c:7]>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4](-[OH;D1;+0:5])-[C:6]-[c:7]
95
[{"value": 95.0, "product": "OC(C(=O)O)CC1=C(C=CC=C1)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
To magnetically stirred N,N-dimethylformamide (23 ml., 297.3 mmol) cooled in ice was slowly added dropwise thionyl chloride (139 ml., ca. 1.91 mol). A solution of (+)-α-hydroxy-2-nitrobenzenepropanoic acid [11.60 g., 54.9 mmol, [α]D25 +49.94° (c 2.465, 95% EtOH)], obtained from the chiral reduction of 2-nitro -α-oxoben...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1
null
null
null
null
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]>>O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bbaa8fd2fc2a4f12ab8b5fe533c40c1c
Nc1ccccc1CC(Cl)C(=O)O>>O=C(O)[C@@H]1Cc2ccccc2N1
CC1NC(CCC1)C.ClC(C(=O)O)CC1=C(C=CC=C1)N.[OH-].[Na+].Cl>>N1[C@@H](CC2=CC=CC=C12)C(=O)O
Cl[CH:4]([C:2](=[O:1])[OH:3])[CH2:5][c:6]1[cH:7][cH:8][cH:9][cH:10][c:11]1[NH2:12]>>[O:1]=[C:2]([OH:3])[C@@H:4]1[CH2:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[NH:12]1
Nc1ccccc1CC(Cl)C(=O)O
O=C(O)[C@@H]1Cc2ccccc2N1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
OtherReaction
da993167d58388d7e927ece80102774e84bf539eaec6212c7b46fb267c1233b4
f727fed8b2cf723a92e5af137ab57c7229fb353af6a01a0b7b0aeb3a7b28a8b4
c1ccc2c(c1)CCN2
Cl-[CH;D3;+0:1](-[C:2]-[c:3]:[c:4](-[NH2;D1;+0:5]):[c:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]>>[O;D1;H0:8]=[C:7](-[O;D1;H1:9])-[C@@H;D3;+0:1]1-[C:2]-[c:3]:[c:4](:[c:6])-[NH;D2;+0:5]-1
74
[{"value": 74.0, "product": "N1[C@@H](CC2=CC=CC=C12)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
8
HOUR
(+)-α-Chloro-2-aminobenzenepropanoic acid 2,6-dimethylpiperidine salt (1.25 g., 4.00 mmol) was added to magnetically stirred N sodium hydroxide (4 ml.) under nitrogen. The solution was stirred under nitrogen overnight at room temperature. The pH was adjusted to a value between 2 and 3 (pH paper) with conc. hydrochloric...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Primary amine
Secondary amine
null
c1ccc2c(c1)CCN2
c1ccc2c(c1)CCN2
HCl
CN(C)C=O
null
8
Nc1ccccc1CC(Cl)C(=O)O>CN(C)C=O>O=C(O)[C@@H]1Cc2ccccc2N1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bb00c855c12145619bd8ea260945dc3b
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]>>O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
[N+](=O)([O-])C1=C(C=CC=C1)CC(C(=O)O)=O.N1[C@H](C(=O)O)CCC1.[BH4-].[Na+]>>OC(C(=O)O)CC1=C(C=CC=C1)[N+](=O)[O-]
[O:1]=[C:2]([OH:3])[C:4](=[O:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[N+:13](=[O:14])[O-:15]>>[O:1]=[C:2]([OH:3])[CH:4]([OH:5])[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[N+:13](=[O:14])[O-:15]
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]
O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
null
null
O1CCCC1
Reduction
Reduction of ketone to secondary alcohol
02790ac194d8bf7ccb13d6247c59412024d87f77d2c906ef7804f021f57d5070
1bd3cd74b454139c0a0068ac0135836499926b274bff569df163210c6c944a89
c1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[C:6]-[c:7]>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D3;+0:4](-[OH;D1;+0:5])-[C:6]-[c:7]
null
[]
null
null
6
DAY
L-(-)-proline (7.50 g., 65.1 mmol) and sodium borohydride (2.46 g., 65.1 mmol) were stirred in tetrahydrofuran under nitrogen for sixteen hours. Recrystallized o-nitrophenylpyruvic acid (14.17 g., 76.5 mmol) in tetrahydrofuran (50 ml.) was added dropwise, and the resulting solution was stirred at room temperature for s...
10.6084/m9.figshare.5104873.v1
null
Ketone
Secondary alcohol
null
null
c1ccccc1
null
O1CCCC1
null
144
O=C(O)C(=O)Cc1ccccc1[N+](=O)[O-]>O1CCCC1>O=C(O)C(O)Cc1ccccc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-4fa3d32004a64365b5c133d511bd3d13
O=C(O)C(O)Cc1ccccc1[N+](=O)[O-].O=S(Cl)Cl>>O=C(O)C(Cl)Cc1ccccc1[N+](=O)[O-]
S(=O)(Cl)Cl.C[N+](=CCl)C.[Cl-].CC1NC(CCC1)C.OC(C(=O)O)CC1=C(C=CC=C1)[N+](=O)[O-]>>CC1NC(CCC1)C.ClC(C(=O)O)CC1=C(C=CC=C1)[N+](=O)[O-]
O[CH:12]([C:10](=[O:9])[OH:11])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][c:20]1[N+:21](=[O:22])[O-:23].O=S(Cl)[Cl:13]>>[O:9]=[C:10]([OH:11])[CH:12]([Cl:13])[CH2:14][c:15]1[cH:16][cH:17][cH:18][cH:19][c:20]1[N+:21](=[O:22])[O-:23]
O=C(O)C(O)Cc1ccccc1[N+](=O)[O-].O=S(Cl)Cl
O=C(O)C(Cl)Cc1ccccc1[N+](=O)[O-]
null
null
CN(C=O)C.C(C)O.CCOCC.ClCCl
Functional Group Interconversion
Alcohol to chloride_SOCl2
ed0947fcf0a870fa4568d74e29e264525d0acf781c20c116470537e8cf1d911a
495868b18ac37eabad313a8861412e57f019fb3569a2b2e50afa3ee29413ec02
c1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[CH;D3;+0:2](-[C:3]-[c:4])-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]>>[Cl;H0;D1;+0:1]-[CH;D3;+0:2](-[C:3]-[c:4])-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]
null
[]
null
null
8
HOUR
To magnetically stirred N,N-dimethylformamide (3 mL) cooled in ice was added slowly dropwise thionyl chloride (4.5 ml., 61.7 mmol) and the resulting cold Vilsmeier reagent was diluted with dichloromethane (30 ml.). (-)-α-Hydroxy-2-nitrobenzenepropanoic acid [3.00 g., 14.2 mmol, [α]D25 -63.04° (c 0.955, 95% ethanol)] in...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
Secondary halide
null
null
c1ccccc1
HCl
CN(C=O)C.C(C)O.CCOCC.ClCCl
null
8
O=C(O)C(O)Cc1ccccc1[N+](=O)[O-].O=S(Cl)Cl>CN(C=O)C.C(C)O.CCOCC.ClCCl>O=C(O)C(Cl)Cc1ccccc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-9ef1ffbbe2ba4e948cd69ef247efc7ac
NS(=O)(=O)c1ccccc1I>>NS(=O)(=O)c1ccccc1
CC(C)(C)C(=O)OC=1C=CC(=CC1OC(=O)C(C)(C)C)C(CNC)O.Cl.IC1=C(C=CC=C1)S(=O)(=O)N.P(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1>>C1(=CC=CC=C1)S(=O)(=O)N
I[c:10]1[c:5]([S:2]([NH2:1])(=[O:3])=[O:4])[cH:6][cH:7][cH:8][cH:9]1>>[NH2:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][cH:7][cH:8][cH:9][cH:10]1
NS(=O)(=O)c1ccccc1I
NS(=O)(=O)c1ccccc1
null
Cl[Pd]Cl.[Cu]I
CN(C=O)C.C(C)N(CC)CC
Functional Group Interconversion
Aromatic dehalogenation
b66818d3926a4463fb8e1c3d4a89e94e47b4d46960d4bdb7bcfbeeec427cfd4e
56de34d4a44cb25d9380269ee5e138b0f24b40a3a0db22c5508049dc775a861f
c1ccccc1
I-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[#16:5]):[c:6]>>[#16:5]-[c:4](:[c:6]):[cH;D2;+0:1]:[c:2]:[c:3]
null
[]
null
null
null
null
To a solution of 28.3 g (0.1 mole) of 2-iodophenylsulfonamide in 350 ml of dimethylformamide and 100 ml of triethylamine are added 1.0 g of palladium dichloro-bis(triphenylphosphite) complex, PdCl2 [P(C6H5)3 ]2, and 0.5 g of copper(I) iodide (CuI). Gaseous propine is then introduced into this solution until the startin...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide
null
c1ccccc1
c1ccccc1
c1ccccc1
I-
Cl[Pd]Cl.[Cu]I.CN(C=O)C.C(C)N(CC)CC
null
null
NS(=O)(=O)c1ccccc1I>Cl[Pd]Cl.[Cu]I.CN(C=O)C.C(C)N(CC)CC>NS(=O)(=O)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-30de9da655d044c9895a8b402380e49a
F.FC(F)(F)C(Cl)(Cl)Oc1ccc(Cl)cc1>>FC(F)(F)C(F)(Cl)Oc1ccc(Cl)cc1
ClC(C(F)(F)F)(OC1=CC=C(C=C1)Cl)Cl.F.[Sb](Cl)(Cl)(Cl)(Cl)Cl>>ClC(C(F)(F)F)(OC1=CC=C(C=C1)Cl)F
[FH:6].Cl[C:5]([C:2]([F:1])([F:3])[F:4])([Cl:7])[O:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1>>[F:1][C:2]([F:3])([F:4])[C:5]([F:6])([Cl:7])[O:8][c:9]1[cH:10][cH:11][c:12]([Cl:13])[cH:14][cH:15]1
F.FC(F)(F)C(Cl)(Cl)Oc1ccc(Cl)cc1
FC(F)(F)C(F)(Cl)Oc1ccc(Cl)cc1
null
null
null
Miscellaneous
OtherReaction
6cbceb006a6c2bb4630a1bd9846208a4cd5d1f25fdbb5d103e5ad794516c8409
842a324f59ad0063075fe3cc48957e60bf881790a58fdb16332fd28d26a3c247
c1ccccc1
Cl-[C;H0;D4;+0:1](-[Cl;D1;H0:2])(-[#8:3]-[c:4])-[C:5](-[F;D1;H0:6])(-[F;D1;H0:7])-[F;D1;H0:8].[FH;D0;+0:9]>>[Cl;D1;H0:2]-[C;H0;D4;+0:1](-[F;H0;D1;+0:9])(-[#8:3]-[c:4])-[C:5](-[F;D1;H0:6])(-[F;D1;H0:7])-[F;D1;H0:8]
89.8
[{"value": 89.8, "product": "ClC(C(F)(F)F)(OC1=CC=C(C=C1)Cl)F", "details": "PERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
A 500 ml polytetrafluoroethylene reactor equipped with stirrer, thermometer and reflux condenser is charged with 55.9 g (0.2 mol) of 4-(1,1-dichloro-2,2,2-trifluoroethoxy)chlorobenzene in 100 ml of hydrogen fluoride. 3.0 g (0.01 mol; corresponding to 5 mol%) of antimony pentachloride are added at a temperature in the r...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Ether
Tertiary halide.Tertiary halide
null
null
c1ccccc1
HCl
null
null
0.333333
F.FC(F)(F)C(Cl)(Cl)Oc1ccc(Cl)cc1>>FC(F)(F)C(F)(Cl)Oc1ccc(Cl)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-53a85923a86c4172acc0fb7d8d5d8d30
F.FC(F)(F)CSC1C=CC=CC1(Cl)Cl>>FC(Sc1ccccc1Cl)C(F)(F)F
ClC1(C(C=CC=C1)SCC(F)(F)F)Cl.F.[Sb](Cl)(Cl)(Cl)(Cl)Cl>>ClC1=C(C=CC=C1)SC(C(F)(F)F)F
[FH:1].Cl[C:9]1([Cl:10])[CH:4]([S:3][CH2:2][C:11]([F:12])([F:13])[F:14])[CH:5]=[CH:6][CH:7]=[CH:8]1>>[F:1][CH:2]([S:3][c:4]1[cH:5][cH:6][cH:7][cH:8][c:9]1[Cl:10])[C:11]([F:12])([F:13])[F:14]
F.FC(F)(F)CSC1C=CC=CC1(Cl)Cl
FC(Sc1ccccc1Cl)C(F)(F)F
null
null
null
Miscellaneous
OtherReaction
8402e41d077c1491268f1c52e4ddce02c4e4bf14a63bd67ec224c8f5d2505e56
12c1c5c7dbba2ebea84dd1caaef720a655528dfbfbb69e7ad822d7d7004aede8
c1ccccc1
Cl-[C;H0;D4;+0:1]1(-[Cl;D1;H0:2])-[CH;D2;+0:3]=[CH;D2;+0:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-[CH;D3;+0:7]-1-[#16:8]-[CH2;D2;+0:9]-[C:10](-[F;D1;H0:11])(-[F;D1;H0:12])-[F;D1;H0:13].[FH;D0;+0:14]>>[Cl;D1;H0:2]-[c;H0;D3;+0:1]1:[cH;D2;+0:3]:[cH;D2;+0:4]:[cH;D2;+0:5]:[cH;D2;+0:6]:[c;H0;D3;+0:7]:1-[#16:8]-[CH;D3;+0:9](-[F;H0;D1;+0:...
null
[]
null
null
3
HOUR
A 500 ml polytetrafluoroethylene reactor equipped with stirrer, thermometer and reflux condenser is charged with 24.7 g (0.094 mol) of 1,1-dichloro-2,2,2-trifluoroethylthiobenzene which are subsequently condensed with 50 g of hydrogen fluoride. 4.2 g (0.014 mol; corresponding to 15 mol%) of antimony pentachloride are a...
10.6084/m9.figshare.5104873.v1
null
Tertiary halide.Tertiary halide.Monosulfide.Conjugated diene
Aromatic halide.Secondary halide.Monosulfide
C1=CCCC=C1
c1ccccc1
c1ccccc1
HCl
null
null
3
F.FC(F)(F)CSC1C=CC=CC1(Cl)Cl>>FC(Sc1ccccc1Cl)C(F)(F)F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-444e854447fe4b53ac481a298adcab6e
CC(=O)OC(C)=O.CC(=O)OC(C)=O.Cc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1>>CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1
C(C)(=O)OC(C)=O.FC(C(C(F)(F)F)(O)C1=CC=C(C=C1)C)(F)F.S(O)(O)(=O)=O.C(C)(=O)OC(C)=O>>C(C)(=O)OC(C1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)OC(C)=O)OC(C)=O
CC(=O)[O:6][C:16]([CH3:17])=[O:18].[CH3:1][C:2](=[O:3])[O:4][C:7]([CH3:8])=[O:9].[CH3:5][c:10]1[cH:11][cH:12][c:13]([C:14]([OH:15])([C:19]([F:20])([F:21])[F:22])[C:23]([F:24])([F:25])[F:26])[cH:27][cH:28]1>>[CH3:1][C:2](=[O:3])[O:4][CH:5]([O:6][C:7]([CH3:8])=[O:9])[c:10]1[cH:11][cH:12][c:13]([C:14]([O:15][C:16]([CH3:17...
CC(=O)OC(C)=O.CC(=O)OC(C)=O.Cc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1
CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1
null
[O-2].[O-2].[O-2].[Cr+6]
O
Acylation
OtherReaction
e7c92516b0703c73b4cb5fc5ac135249bfe4433a15f56fb3a6c1b91a8643705c
947488b7a4710cdb02433043d0982d6a7d3fbc564a4baa56670ebffc3bd3e1dd
c1ccccc1
C-C(=O)-[O;H0;D2;+0:1]-[C;H0;D3;+0:2](-[C;D1;H3:3])=[O;D1;H0:4].[C;D1;H3:5]-[C:6](=[O;D1;H0:7])-[O;H0;D2;+0:8]-[C;H0;D3;+0:9](-[C;D1;H3:10])=[O;D1;H0:11].[CH3;D1;+0:12]-[c:13](:[c:14]):[c:15].[F;D1;H0:16]-[C:17](-[F;D1;H0:18])(-[F;D1;H0:19])-[C:20](-[OH;D1;+0:21])(-[c:22])-[C:23](-[F;D1;H0:24])(-[F;D1;H0:25])-[F;D1;H0:...
null
[]
null
null
2
HOUR
To a solution of 156 g (0.60 mole) of 4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]toluene in 675 ml of acetic anhydride is added 135 ml of concentrated sulfuric acid at 0°. To the solution stirred at 0° is added a soluton of 168 g (1.68 mole) of chromium trioxide in 750 ml of acetic anhydride dropwise over a ...
10.6084/m9.figshare.5104873.v1
null
Anhydride.Anhydride.Tertiary alcohol
Ester.Ester.Ester
null
null
c1ccccc1
HO-
[O-2].[O-2].[O-2].[Cr+6].O
null
2
CC(=O)OC(C)=O.CC(=O)OC(C)=O.Cc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1>[O-2].[O-2].[O-2].[Cr+6].O>CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e7b09e39e6d0482c831f6c8380c5c8e2
CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1>>CC(=O)OC(c1ccc(C=O)cc1)(C(F)(F)F)C(F)(F)F
C(C)O.C(C)(=O)OC(C1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)OC(C)=O)OC(C)=O.S(O)(O)(=O)=O>>C(C)(=O)OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(C=O)C=C1
CC(=O)O[CH:10]([c:9]1[cH:8][cH:7][c:6]([C:5]([O:4][C:2]([CH3:1])=[O:3])([C:14]([F:15])([F:16])[F:17])[C:18]([F:19])([F:20])[F:21])[cH:13][cH:12]1)[O:11]C(C)=O>>[CH3:1][C:2](=[O:3])[O:4][C:5]([c:6]1[cH:7][cH:8][c:9]([CH:10]=[O:11])[cH:12][cH:13]1)([C:14]([F:15])([F:16])[F:17])[C:18]([F:19])([F:20])[F:21]
CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1
CC(=O)OC(c1ccc(C=O)cc1)(C(F)(F)F)C(F)(F)F
null
null
O
Miscellaneous
Acetal hydrolysis to aldehyde
99d6216d1e6a4ec3705c86679722b6c1ba2e1e83ea661cfbae8473cd3c1cd7da
5d4585057e84f16a9a41a81f9ae63243c1ba7e24e54ff5744f2d5edb4f856efa
c1ccccc1
C-C(=O)-O-[CH;D3;+0:1](-[O;H0;D2;+0:2]-C(-C)=O)-[c:3](:[c:4]):[c:5]>>[O;H0;D1;+0:2]=[CH;D2;+0:1]-[c:3](:[c:4]):[c:5]
89.1
[{"value": 89.1, "product": "C(C)(=O)OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(C=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 130 ml of ethanol are added 60 g (0.15 mole) of α,α-bis-acetyloxy-4-[1-(acetyloxy)-2,2,2-trifluoro-1-(trifluoromethyl)ethyl]toluene and 13.5 ml of concentrated sulfuric acid in 135 ml of water. The resulting solution is stirred and heated at reflux for thirty minutes. The solution is then cooled and extracted with 1...
10.6084/m9.figshare.5104873.v1
null
Ester.Ester
Aldehyde
null
null
c1ccccc1
HO-
O
null
null
CC(=O)OC(OC(C)=O)c1ccc(C(OC(C)=O)(C(F)(F)F)C(F)(F)F)cc1>O>CC(=O)OC(c1ccc(C=O)cc1)(C(F)(F)F)C(F)(F)F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d619ebd614624d4388075e24b6d34182
COC(=O)C(c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1)C(C)Br>>CC(=CC(=O)O)c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1
CCOCC.BrC(C(C(=O)OC)C1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)O)C.O1CCCC1>>CC(=CC(=O)O)C1=CC=C(C=C1)C(C(F)(F)F)(C(F)(F)F)O
C[O:6][C:4]([CH:3]([CH:2](Br)[CH3:1])[c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][cH:22]1)=[O:5]>>[CH3:1][C:2](=[CH:3][C:4](=[O:5])[OH:6])[c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][cH:22]1
COC(=O)C(c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1)C(C)Br
CC(=CC(=O)O)c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1
null
null
null
Miscellaneous
OtherReaction
2e5688f8c1aa40dce78bf69bd3bcf8baf2169534ff96670d7e6dadeca72a567f
062fc4dd58455c891e367b9166799a0526e52d510556dcf9aea549d31460a90c
c1ccccc1
Br-[CH;D3;+0:1](-[C;D1;H3:2])-[CH;D3;+0:3](-[C:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-C)-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[CH;D2;+0:3]-[C:4](=[O;D1;H0:5])-[OH;D1;+0:6])-[c;H0;D3;+0:7](:[c:8]:[c:9]):[c:10]:[c:11]
null
[]
null
null
null
null
To a solution of methyl 3-bromo-3-methyl-{4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}propanoate in tetrahydrofuran can be added an equivalent amount of 1,5-diazabicyclo[3.4.0]nonene-5. The resulting reaction mixture can be stirred at elevated temperature until thin layer chromatographic analysis of a ...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Ester
Carboxylic acid
c1ccccc1
c1ccccc1
c1ccccc1
HBr
null
null
null
COC(=O)C(c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1)C(C)Br>>CC(=CC(=O)O)c1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-faaf68394c7640afbc0442dba1d6486f
O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=[N+]([O-])O>>O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]
O.[N+](=O)(O)[O-].FC(C(C(F)(F)F)(O)C1=CC=C(C=C1)CCC(=O)O)(F)F.[N+](=O)(O)[O-]>>[N+](=O)([O-])C1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)O
[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([C:10]([OH:11])([C:12]([F:13])([F:14])[F:15])[C:16]([F:17])([F:18])[F:19])[cH:20][cH:21]1.O[N+:22](=[O:23])[O-:24]>>[O:1]=[C:2]([OH:3])[CH2:4][CH2:5][c:6]1[cH:7][cH:8][c:9]([C:10]([OH:11])([C:12]([F:13])([F:14])[F:15])[C:16]([F:17])([F:18])[F:19])[cH:20][c:21]1[N...
O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=[N+]([O-])O
O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]
null
null
S(O)(O)(=O)=O
Functional Group Addition
Aromatic nitration with HNO3
53848b8b2bb4e867226e49db2e60519b24be9379900e3ad7c56af54fe8fde7a5
ddce49825c02b8965f10c8d99e3c841d26e1f136da6037b417c09313e6d73097
c1ccccc1
O-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3].[C:4]-[c:5](:[c:6]):[cH;D2;+0:7]:[c:8]:[c:9]>>[C:4]-[c:5](:[c:6]):[c;H0;D3;+0:7](-[N+;H0;D3:1](-[O;-;D1;H0:2])=[O;D1;H0:3]):[c:8]:[c:9]
null
[]
null
null
18
HOUR
To a solution of 63.2 g (0.20 mole) of 4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoic acid in 160 ml of concentrated sulfuric acid is added 40 ml of fuming nitric acid (90%) dropwise with stirring at 0°-5°. Following the nitric acid addition the solution is allowed to warm to 20° with stirring o...
10.6084/m9.figshare.5104873.v1
null
Nitrate
Nitro group
c1ccccc1
c1ccccc1
c1ccccc1
HO-
S(O)(O)(=O)=O
null
18
O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=[N+]([O-])O>S(O)(O)(=O)=O>O=C(O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-325adc1ebbbf4db88aa4a692c9efebaa
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=S(=O)(O)Cl>>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl
ClS(=O)(=O)O.FC(C(C(F)(F)F)(O)C1=CC=C(C=C1)CCC(=O)OC)(F)F>>ClS(=O)(=O)C1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)OC
[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][cH:22]1.O[S:23](=[O:24])(=[O:25])[Cl:26]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[...
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=S(=O)(O)Cl
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl
null
null
null
Heteroatom Alkylation and Arylation
Aromatic sulfonyl chlorination
04bb0e110ac9bc3104a40572864ecdd042b39019cff0ea96d1a0ad7c9eb6ecf3
d32b60b8f9bfd187c6c9f1eef6a22a00f53525a7532b83aba763d5389c9e4280
c1ccccc1
O-[S;H0;D4;+0:1](-[Cl;D1;H0:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[c:6](:[c:7]):[cH;D2;+0:8]:[c:9]:[c:10]>>[C:5]-[c:6](:[c:7]):[c;H0;D3;+0:8](-[S;H0;D4;+0:1](-[Cl;D1;H0:2])(=[O;D1;H0:3])=[O;D1;H0:4]):[c:9]:[c:10]
null
[]
null
null
null
null
To excess chlorosulfonic acid cooled with an ice-acetone bath can be added methyl 4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoate with stirring. The solution should be stirred for several hours. Addition of the reaction mixture to ice and isolation of the product will give 2-chlorosulfonyl-4-[2,...
10.6084/m9.figshare.5104873.v1
null
null
Sulfonyl halide
c1ccccc1
c1ccccc1
c1ccccc1
HO-
null
null
null
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1.O=S(=O)(O)Cl>>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-74e636509a9640c291269b22cc9cdee6
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl>>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S
ClS(=O)(=O)C1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)OC>>SC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)OC
O=[S:23](=O)(Cl)[c:22]1[c:7]([CH2:6][CH2:5][C:3]([O:2][CH3:1])=[O:4])[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21]1>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][c:...
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S
null
[Zn]
C(C)(=O)O
Reduction
OtherReaction
67c58f2128339179ba957163c48f4a4ad5eac877ca5a6bdb7ff20914d4efc174
fdaccf528edde07917e32c5a4cba468523458b8901959f3cb21411d1f4e7837a
c1ccccc1
Cl-[S;H0;D4;+0:1](=O)(=O)-[c:2](:[c:3]):[c:4]>>[SH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
To excess chlorosulfonic acid cooled with an ice-acetone bath can be added methyl 4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoate with stirring. The solution should be stirred for several hours. Addition of the reaction mixture to ice and isolation of the product will give 2-chlorosulfonyl-4-[2,...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Aromatic thiol
null
null
c1ccccc1
Other
[Zn].C(C)(=O)O
null
null
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S(=O)(=O)Cl>[Zn].C(C)(=O)O>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2f5977fcdfc64a0bba0973c2c4fe06ab
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1SC>>CSc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
CSC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)OC.Cl>>CSC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)O
C[O:23][C:21]([CH2:20][CH2:19][c:18]1[c:3]([S:2][CH3:1])[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17]1)=[O:22]>>[CH3:1][S:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][c:18]1[CH2:19][CH2:20][C:21](=[O:22])[OH:2...
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1SC
CSc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
null
null
[OH-].[Na+]
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
null
null
To a solution of 3,4-dihydro-7-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]-2H-1-benzothiapyran-2-one in dimethylacetamide can be added a one molar excess of sodium hydroxide in methanol. The resulting solution should be heated, and a one molar excess of methyl iodide should be added with stirring. From the res...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1
Other
[OH-].[Na+]
null
null
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1SC>[OH-].[Na+]>CSc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e1c66fb4adac4f998bb29ae2b4de9a65
COc1cccc(Br)c1.O=C(C(F)(F)F)C(F)(F)F>>COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
BrC=1C=C(C=CC1)OC.BrCCBr.BrC=1C=C(C=CC1)OC.FC(C(=O)C(F)(F)F)(F)F.FC(C(=O)C(F)(F)F)(F)F.FC(C(=O)C(F)(F)F)(F)F.Cl.[Mg]>>COC1=CC(=CC=C1)C(C(F)(F)F)(C(F)(F)F)O
Br[c:7]1[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:18]1.[C:8](=[O:9])([C:10]([F:11])([F:12])[F:13])[C:14]([F:15])([F:16])[F:17]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([C:8]([OH:9])([C:10]([F:11])([F:12])[F:13])[C:14]([F:15])([F:16])[F:17])[cH:18]1
COc1cccc(Br)c1.O=C(C(F)(F)F)C(F)(F)F
COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
null
null
CCOCC.O.O1CCCC1
C-C Coupling
Grignard_alcohol
23831eb2f5100c758a065f977b2daac4728a2009a2a7f37e9b01c50283e9e583
b8801be51258f6ee39fb6aad45dd9677b1b9eed3d6e0018ffb065bca8e787abf
c1ccccc1
Br-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5].[F;D1;H0:6]-[C:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[C:12](-[F;D1;H0:13])(-[F;D1;H0:14])-[F;D1;H0:15]>>[F;D1;H0:6]-[C:7](-[F;D1;H0:8])(-[F;D1;H0:9])-[C;H0;D4;+0:10](-[OH;D1;+0:11])(-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4]:[c:5])-[C:12](-[F;D1;H0:13])(-[...
null
[]
null
null
18
HOUR
To a suspension of 13.5 g (0.55 g atoms) of sublimed magnesium chips in 25 ml of anhydrous tetrahydrofuran in a reaction flask fitted with a water-cooled condenser are added 10 g (0.05 mole) of 3-bromo-1-methoxybenzene and 0.5 ml of 1,2-dibromoethane. The resulting reaction mixture is stirred and heated gently until a ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
Tertiary alcohol
c1ccccc1
c1ccccc1
c1ccccc1
Br-
CCOCC.O.O1CCCC1
null
18
COc1cccc(Br)c1.O=C(C(F)(F)F)C(F)(F)F>CCOCC.O.O1CCCC1>COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5aad24de5b32448bacb79951b467fed3
COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1>>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O
COC1=CC(=CC=C1)C(C(F)(F)F)(C(F)(F)F)O.COC(Cl)Cl.Cl>>COC1=C(C=O)C=CC(=C1)C(C(F)(F)F)(O)C(F)(F)F
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][cH:18]1>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][c:18]1[CH:19]=[O:20]
COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O
null
[Ti](Cl)(Cl)(Cl)Cl
ClCCl.O
Miscellaneous
OtherReaction
c25c41cbe22c67cd8a516e3f8fc0980bea758f12933876480aae20d5765822e2
3cccf922e74135722ee21a46ad7578302a8603e1f71d6f2113cd42de4ba0cf73
c1ccccc1
[#8:1]-[c:2](:[c:3]):[cH;D2;+0:4]:[c:5]:[c:6]>>[#8:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[C:7]=[O;D1;H0:8]):[c:5]:[c:6]
48
[{"value": 48.0, "product": "COC1=C(C=O)C=CC(=C1)C(C(F)(F)F)(O)C(F)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
18
HOUR
To a solution of 31.6 g (0.12 mole) of 1-methoxy-3-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzene in 200 ml dichloromethane is added 38 g (0.2 mole) of titanium tetrachloride at 0°-5° with stirring under a nitrogen atmosphere. After the resulting solution is stirred for 15 minutes, 11.5 g (0.1 mole) of α,α...
10.6084/m9.figshare.5104873.v1
null
null
Aldehyde
c1ccccc1
c1ccccc1
c1ccccc1
Other
[Ti](Cl)(Cl)(Cl)Cl.ClCCl.O
null
18
COc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1>[Ti](Cl)(Cl)(Cl)Cl.ClCCl.O>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ec0779edb24c45fe9d209facc9386718
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O.O=C(O)CC(=O)O>>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O
COC1=C(C=O)C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O.C(CC(=O)O)(=O)O.N1CCCCC1>>COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)C=CC(=O)O
O=[CH:19][c:18]1[c:3]([O:2][CH3:1])[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17]1.O=C(O)[CH2:20][C:21](=[O:22])[OH:23]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][c:18]1[CH:19]=[CH:20][C:21](=[O:22...
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O.O=C(O)CC(=O)O
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O
null
null
N1=CC=CC=C1
C-C Coupling
OtherReaction
0c2382c2f7ea556671f2a3c58036f5e0661a08f7658c9ccbb421e2a9daac089b
a6032dd2ea62d1cf56f5cee7663c80211fe5b6aa714acc87461f75a8053630fd
c1ccccc1
O-C(=O)-[CH2;D2;+0:1]-[C:2](=[O;D1;H0:3])-[O;D1;H1:4].O=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[O;D1;H0:3]=[C:2](-[O;D1;H1:4])-[CH;D2;+0:1]=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]
61
[{"value": 61.0, "product": "COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)C=CC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 15 g (0.05 mole) 2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzaldehyde in 50 ml of pyridine are added 11 g (0.11 mole) of malonic acid and 1 g of piperidine. The solution is stirred and gradually heated to 80°. Heating and stirring are continued for 1 hour at 80°. The solution is...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Carboxylic acid
null
null
null
c1ccccc1
HO-
N1=CC=CC=C1
null
1
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=O.O=C(O)CC(=O)O>N1=CC=CC=C1>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5311bd096d1c45b1920e980fa0c4e746
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O>>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)C=CC(=O)O>>COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)O
[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][c:18]1[CH:19]=[CH:20][C:21](=[O:22])[OH:23]>>[CH3:1][O:2][c:3]1[cH:4][c:5]([C:6]([OH:7])([C:8]([F:9])([F:10])[F:11])[C:12]([F:13])([F:14])[F:15])[cH:16][cH:17][c:18]1[CH2:19][CH2:20][C:21](=[O:22])[OH:23]
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
null
null
C(C)O
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
c1ccccc1
[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH;D2;+0:4]=[CH;D2;+0:5]-[c:6](:[c:7]):[c:8]>>[O;D1;H0:1]=[C:2](-[O;D1;H1:3])-[CH2;D2;+0:4]-[CH2;D2;+0:5]-[c:6](:[c:7]):[c:8]
80.9
[{"value": 80.9, "product": "COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 100 ml of ethanol are added 8.8 g (0.025 mole) of 3-{2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}-2-propenoic acid to produce a solution which is added to a pressure bottle and flushed with nitrogen. To the solution is added 1 g of 10% palladium on carbon. The pressure bottle is placed in ...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
C(C)O
null
null
COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1C=CC(=O)O>C(C)O>COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0960a3e8f0f94a8c9c664b1b2f395258
CO.COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O>>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1OC
CO.COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)O.S(O)(O)(=O)=O>>COC1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)OC
[CH3:1][OH:2].O[C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][c:22]1[O:23][CH3:24]>>[CH3:1][O:2][C:3](=[O:4])[CH2:5][CH2:6][c:7]1[cH:8][cH:9][c:10]([C:11]([OH:12])([C:13]([F:14])([F:15])[F:16])[C:17]([F:18])([F:19])[F:20])[cH:21][c:2...
CO.COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O
COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1OC
null
null
C1(=CC=CC=C1)C
Protection
Esterification of Carboxylic Acids
9cecdbd189c6f9c3648521d17154d013842a5498de4e76e65efb1d842973340b
af0b8064f2e82ebe66c4c29d2391785ac1b993104265ccdc4d67ca79e36fa3c8
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4].[C;D1;H3:5]-[OH;D1;+0:6]>>[C:4]-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[O;H0;D2;+0:6]-[C;D1;H3:5]
null
[]
null
null
null
null
To a solution of 50 ml of methanol in 50 ml toluene are added 7.0 g (0.02 mole) of 2-methoxy-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzenepropanoic acid and 1 ml of concentrated sulfuric acid. The resulting solution is stirred, heated at reflux for 18 hours, then concentrated to 20 ml at reduced pressur...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Methanol
Ester
null
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
null
CO.COc1cc(C(O)(C(F)(F)F)C(F)(F)F)ccc1CCC(=O)O>C1(=CC=CC=C1)C>COC(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1OC
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6f660a7817ea40438cb69e468c18825b
CI.CN(C)C(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]>>COC(c1ccc(CCC(=O)N(C)C)c([N+](=O)[O-])c1)(C(F)(F)F)C(F)(F)F
CI.[H-].[Na+].[N+](=O)([O-])C1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)O)CCC(=O)N(C)C.C(C)O>>[N+](=O)([O-])C1=C(C=CC(=C1)C(C(F)(F)F)(C(F)(F)F)OC)CCC(=O)N(C)C
I[CH3:1].[OH:2][C:3]([c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][C:10](=[O:11])[N:12]([CH3:13])[CH3:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]1)([C:20]([F:21])([F:22])[F:23])[C:24]([F:25])([F:26])[F:27]>>[CH3:1][O:2][C:3]([c:4]1[cH:5][cH:6][c:7]([CH2:8][CH2:9][C:10](=[O:11])[N:12]([CH3:13])[CH3:14])[c:15]([N+:16](=[O:17])[O...
CI.CN(C)C(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]
COC(c1ccc(CCC(=O)N(C)C)c([N+](=O)[O-])c1)(C(F)(F)F)C(F)(F)F
null
null
CN(C=O)C.O
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
cd10a9010f842ab825b304bd2965f17f9c39c4c64e5fc6cd91306ae51817de0d
9271b713ded6954f3329c61a211042ac37c82b3aff1b62cb455035e69339dd27
c1ccccc1
I-[CH3;D1;+0:1].[F;D1;H0:2]-[C:3](-[F;D1;H0:4])(-[F;D1;H0:5])-[C:6](-[OH;D1;+0:7])(-[c:8])-[C:9](-[F;D1;H0:10])(-[F;D1;H0:11])-[F;D1;H0:12]>>[CH3;D1;+0:1]-[O;H0;D2;+0:7]-[C:6](-[c:8])(-[C:3](-[F;D1;H0:2])(-[F;D1;H0:4])-[F;D1;H0:5])-[C:9](-[F;D1;H0:10])(-[F;D1;H0:11])-[F;D1;H0:12]
null
[]
null
null
null
null
To a suspension of 2.15 (0.085 mole) of sodium hydride in 200 ml dimethylformamide is added 29.1 g (0.075 mole) of 3-{2-nitro-4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl}-N,N-dimethylpropanamide in in 50 ml dimethylformamide at such a rate that excessive foaming is avoided. To the resulting suspension,...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
c1ccccc1
HI
CN(C=O)C.O
null
null
CI.CN(C)C(=O)CCc1ccc(C(O)(C(F)(F)F)C(F)(F)F)cc1[N+](=O)[O-]>CN(C=O)C.O>COC(c1ccc(CCC(=O)N(C)C)c([N+](=O)[O-])c1)(C(F)(F)F)C(F)(F)F
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-23f42f8623e741769a45a5605a83b535
O=C(O)Cc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1>>OCCc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
FC(C(C(F)(F)F)(O)C=1C=C(C=CC1)CC(=O)O)(F)F.Cl.[H][H]>>FC(C(C(F)(F)F)(O)C=1C=C(C=CC1)CCO)(F)F
O=[C:2]([OH:1])[CH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([C:9]([OH:10])([C:11]([F:12])([F:13])[F:14])[C:15]([F:16])([F:17])[F:18])[cH:19]1>>[OH:1][CH2:2][CH2:3][c:4]1[cH:5][cH:6][cH:7][c:8]([C:9]([OH:10])([C:11]([F:12])([F:13])[F:14])[C:15]([F:16])([F:17])[F:18])[cH:19]1
O=C(O)Cc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
OCCc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
null
null
O1CCCC1
Reduction
Reduction of carboxylic acid to primary alcohol
0db83a5ebe1e318b78b55461cf7eb8f7c004eef0f9e3b6666d3df4c96b5f665e
93b4621647b04d2ad2f2825215b1567f171ba61fe10d136b5db6ea0470aa4932
c1ccccc1
O=[C;H0;D3;+0:1](-[O;D1;H1:2])-[C:3]-[c:4]>>[O;D1;H1:2]-[CH2;D2;+0:1]-[C:3]-[c:4]
38.9
[{"value": 38.9, "product": "FC(C(C(F)(F)F)(O)C=1C=C(C=CC1)CCO)(F)F", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To one liter of 1M borane-tetrahydrofuran complex was added a solution of 100 g (0.33 mole) of 3-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]benzeneactic acid in 200 ml of tetrahydrofuran. The solution is refluxed for 16 hours under nitrogen. The solution is then refluxed with 400 ml of 6N hydrochloric acid unt...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Primary alcohol
null
null
c1ccccc1
Other
O1CCCC1
null
null
O=C(O)Cc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1>O1CCCC1>OCCc1cccc(C(O)(C(F)(F)F)C(F)(F)F)c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a92e3cb04a4c44e3b5b26d5940e91aac
N.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2>>Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]
N.[N+](=O)([O-])C=1C=C(C2=C(CCO2)C1)[N+](=O)[O-].N>>NC1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])CCO
[NH3:1].[c:2]12[c:3]([cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16])[CH2:4][CH2:5][O:6]2>>[NH2:1][c:2]1[c:3]([CH2:4][CH2:5][OH:6])[cH:7][c:8]([N+:9](=[O:10])[O-:11])[cH:12][c:13]1[N+:14](=[O:15])[O-:16]
N.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2
Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]
null
null
C(=O)N
Heteroatom Alkylation and Arylation
OtherReaction
24a8aa98ea4b138beed710c2dd2b7e94d3484ed8bd12c7cd785386be788cc67a
10642a6ebaaa1448d06340590fc3ea6841ffa4c71e268d51eace72898564c2ca
c1ccccc1
[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4]1:[c:5](:[c:6])-[C:7]-[C:8]-[O;H0;D2;+0:9]-1.[NH3;D0;+0:10]>>[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[NH2;D1;+0:10]):[c:5](-[C:7]-[C:8]-[OH;D1;+0:9]):[c:6]
null
[]
110
CELSIUS
null
null
0.17 Mole (35.7 g) of 2,3-dihydro-5,7-dinitrobenzofuran, prepared according to Chatelus Ann. Chim. [12], 4,505-547 (1949), is suspended in 350 ml of 20% strength ammonia solution and 220 ml of formamide. After 8 hours' heating at 110° C., a further 100 ml of 20% strength ammonia solution are added. Heating is maintaine...
10.6084/m9.figshare.5104873.v1
null
Ether
Primary alcohol.Primary amine
c1ccc2c(c1)CCO2
c1ccccc1
c1ccccc1
null
C(=O)N
110
null
N.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2>C(=O)N>Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-e4c770bdf0d9415a9eb6b135abc8f215
NCCO.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2>>O=[N+]([O-])c1cc(CCO)c(NCCO)c([N+](=O)[O-])c1
[N+](=O)([O-])C=1C=C(C2=C(CCO2)C1)[N+](=O)[O-].NCCO>>OCCNC1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])CCO
[NH2:11][CH2:12][CH2:13][OH:14].[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]2[c:10]([c:15]([N+:16](=[O:17])[O-:18])[cH:19]1)[O:9][CH2:8][CH2:7]2>>[O:1]=[N+:2]([O-:3])[c:4]1[cH:5][c:6]([CH2:7][CH2:8][OH:9])[c:10]([NH:11][CH2:12][CH2:13][OH:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]1
NCCO.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2
O=[N+]([O-])c1cc(CCO)c(NCCO)c([N+](=O)[O-])c1
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
b24e0ea252c670da45f2c12df08b1960f84bcf6fa77abfb845213ed2c4543985
d7adf528712633f83e6bae148cdd27bcd1da32e03c86fb5a52b2cfb0297b6748
c1ccccc1
[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4]1:[c:5](:[c:6])-[C:7]-[C:8]-[O;H0;D2;+0:9]-1.[C:10]-[C:11]-[NH2;D1;+0:12]>>[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[NH;D2;+0:12]-[C:11]-[C:10]):[c:5](-[C:7]-[C:8]-[OH;D1;+0:9]):[c:6]
null
[]
null
null
null
null
0.29 Mole (60.9 g) of 2,3-dihydro-5,7-dinitrobenzofuran is added in small portions at room temperature to 122 ml of 2-aminoethanol. After the addition is complete, the reaction medium is brought for 15 minutes to 95° C. 500 ml of water are added; after the mixture is cooled, the expected product is drained, and this, a...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Primary alcohol.Secondary amine
c1ccc2c(c1)CCO2
c1ccccc1
c1ccccc1
null
O
null
null
NCCO.O=[N+]([O-])c1cc2c(c([N+](=O)[O-])c1)OCC2>O>O=[N+]([O-])c1cc(CCO)c(NCCO)c([N+](=O)[O-])c1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5155b74041e040c5848aa97537ebe3cb
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.N>>CC(O)Cc1cc([N+](=O)[O-])cc([N+](=O)[O-])c1N
[N+](=O)([O-])C=1C=C(C2=C(CC(O2)C)C1)[N+](=O)[O-].N.COCCO>>NC1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])CC(C)O
[CH3:1][CH:2]1[O:3][c:16]2[c:5]([cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][c:12]2[N+:13](=[O:14])[O-:15])[CH2:4]1.[NH3:17]>>[CH3:1][CH:2]([OH:3])[CH2:4][c:5]1[cH:6][c:7]([N+:8](=[O:9])[O-:10])[cH:11][c:12]([N+:13](=[O:14])[O-:15])[c:16]1[NH2:17]
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.N
CC(O)Cc1cc([N+](=O)[O-])cc([N+](=O)[O-])c1N
null
null
O
Heteroatom Alkylation and Arylation
OtherReaction
b9645d4be24e8bef17d95fe9ef844ab65d6e908840b53a61f48178de893a44e4
2cc1049c9dc921d9b8eaebe5bfda8bea348225850bbf2fd843a9e1f05f422894
c1ccccc1
[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4]1:[c:5](:[c:6])-[C:7]-[C:8](-[C;D1;H3:9])-[O;H0;D2;+0:10]-1.[NH3;D0;+0:11]>>[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[NH2;D1;+0:11]):[c:5](-[C:7]-[C:8](-[C;D1;H3:9])-[OH;D1;+0:10]):[c:6]
null
[]
70
CELSIUS
null
null
0.39 Mole (88 g) of 2,3-dihydro-5,7-dinitro-2-methylbenzofuran, prepared according to J.A.C.S. 80, p. 4711-4714 (1958), is suspended in 1.1 l of 20% strength ammonia solution and 600 ml of Methyl Cellosolve. After 18 hours' heating at 70° C., the reaction mixture is cooled. The precipitate formed is drained and, after ...
10.6084/m9.figshare.5104873.v1
null
Ether
Secondary alcohol.Primary amine
c1ccc2c(c1)CCO2
c1ccccc1
c1ccccc1
null
O
70
null
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.N>O>CC(O)Cc1cc([N+](=O)[O-])cc([N+](=O)[O-])c1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-52be2b750bf64c28aee0f8bfed4840c7
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.CN>>CNc1c(CC(C)O)cc([N+](=O)[O-])cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C=C(C2=C(CC(O2)C)C1)[N+](=O)[O-].CN>>CNC1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])CC(C)O
[c:3]12[c:4]([cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[N+:16](=[O:17])[O-:18])[CH2:5][CH:6]([CH3:7])[O:8]2.[CH3:1][NH2:2]>>[CH3:1][NH:2][c:3]1[c:4]([CH2:5][CH:6]([CH3:7])[OH:8])[cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[N+:16](=[O:17])[O-:18]
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.CN
CNc1c(CC(C)O)cc([N+](=O)[O-])cc1[N+](=O)[O-]
null
null
C(C)O
Heteroatom Alkylation and Arylation
OtherReaction
0fe390b9bc848b8b0bb983a36ab8baa599ce53655fa07f9b7bc8f136ff5b6b07
04c78336d85647f6dca3040f384f77009d1b541aac7f8ccf33aa9798091ceab8
c1ccccc1
[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4]1:[c:5](:[c:6])-[C:7]-[C:8](-[C;D1;H3:9])-[O;H0;D2;+0:10]-1.[C;D1;H3:11]-[NH2;D1;+0:12]>>[#7;+:1]-[c:2](:[c:3]):[c;H0;D3;+0:4](-[NH;D2;+0:12]-[C;D1;H3:11]):[c:5](-[C:7]-[C:8](-[C;D1;H3:9])-[OH;D1;+0:10]):[c:6]
null
[]
null
null
10
HOUR
0.056 Mole (12.5 g) of 2,3-dihydro-5,7-dinitro-2-methyl-benzofuran is suspended in 100 ml of a 33% strength solution of methylamine in ethanol. After 10 hours' stirring at room temperature in a sealed Erlenmeyer, the reaction mixture is brought for 30 minutes to the refluxing temperature of the alcohol. After the mixtu...
10.6084/m9.figshare.5104873.v1
null
Ether.Primary amine
Secondary alcohol.Secondary amine
c1ccc2c(c1)CCO2
c1ccccc1
c1ccccc1
null
C(C)O
null
10
CC1Cc2cc([N+](=O)[O-])cc([N+](=O)[O-])c2O1.CN>C(C)O>CNc1c(CC(C)O)cc([N+](=O)[O-])cc1[N+](=O)[O-]
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-0f00b2a48ac44f1f81b28c45b15724f2
Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]>>Nc1cc([N+](=O)[O-])cc(CCO)c1N
NC1=C(C=C(C=C1[N+](=O)[O-])[N+](=O)[O-])CCO.O.O.O.O.O.O.O.O.O.[S-2].[Na+].[Na+].[S]>>NC1=C(C=C(C=C1N)[N+](=O)[O-])CCO
O=[N+:1]([O-])[c:2]1[cH:3][c:4]([N+:5](=[O:6])[O-:7])[cH:8][c:9]([CH2:10][CH2:11][OH:12])[c:13]1[NH2:14]>>[NH2:1][c:2]1[cH:3][c:4]([N+:5](=[O:6])[O-:7])[cH:8][c:9]([CH2:10][CH2:11][OH:12])[c:13]1[NH2:14]
Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]
Nc1cc([N+](=O)[O-])cc(CCO)c1N
null
null
C(C)(C)O.O
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]
null
[]
null
null
null
null
To a suspension of 0.119 mole (27 g) of 2-(2-amino-3,5-dinitrophenyl)ethanol obtained in Example 1 in 67.5 ml of isopropanol to which an equal volume of water has been added, a solutionof 38.4 g of sodium sulphide nonahydrate and 5.4 g of sulphur in 10 ml of water is added dropwise at 60°-65° C. Heating is maintained f...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1
Other
C(C)(C)O.O
null
null
Nc1c(CCO)cc([N+](=O)[O-])cc1[N+](=O)[O-]>C(C)(C)O.O>Nc1cc([N+](=O)[O-])cc(CCO)c1N
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-12421d0797394bc59f5eb474f7a37fd6
ClCCCCl.[Li][P](c1ccccc1)c1ccccc1>>ClCCCP(c1ccccc1)c1ccccc1
P(C1=CC=CC=C1)C1=CC=CC=C1.[Li]P(C1=CC=CC=C1)C1=CC=CC=C1.ClCCCCl.C(CCC)[Li]>>P(C1=CC=CC=C1)(C1=CC=CC=C1)CCCCl
Cl[CH2:4][CH2:3][CH2:2][Cl:1].[Li][P:5]([c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1>>[Cl:1][CH2:2][CH2:3][CH2:4][P:5]([c:6]1[cH:7][cH:8][cH:9][cH:10][cH:11]1)[c:12]1[cH:13][cH:14][cH:15][cH:16][cH:17]1
ClCCCCl.[Li][P](c1ccccc1)c1ccccc1
ClCCCP(c1ccccc1)c1ccccc1
null
null
O.O1CCCC1.C(C)OCC
Miscellaneous
OtherReaction
0cee6f48ecb82f0bf47fd5d9d42e2dd8fcb51b36e7641d6549e2ebcac266a3bf
60e0209a3e01281b77ea7e07e181a846736713b5a4a90ae8d47a0480f9ce79e5
c1ccc(Pc2ccccc2)cc1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3].[Li]-[P;H0;D3;+0:4](-[c:5](:[c:6]):[c:7])-[c:8](:[c:9]):[c:10]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[P;H0;D3;+0:4](-[c:5](:[c:6]):[c:7])-[c:8](:[c:9]):[c:10]
null
[]
0
CELSIUS
1
HOUR
To a 500 mL round bottom flask there was added 400 mL of dry tetrahydrofuran followed by 0.081 mole of HPPh2. The mixture was cooled to 0° C. and 0.081 mole of n-butyl lithium was slowly added to generate LiPPh2 ; this was slowly warmed to room temperature and stirred for about one hour. The solution was transferred to...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
null
null
c1ccccc1.c1ccccc1
Li
O.O1CCCC1.C(C)OCC
0
1
ClCCCCl.[Li][P](c1ccccc1)c1ccccc1>O.O1CCCC1.C(C)OCC>ClCCCP(c1ccccc1)c1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5aa13ac42e5f4ec7a4920f45b70632bb
COC(=O)[C@H](C)N.Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)O>>COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C
CN1CCOCC1.CN1CCOCC1.C(C)(C)(C)OC(=O)N[C@@H](CC1=C(C=C(C=C1C)O)C)C(=O)O.Cl.COC([C@@H](N)C)=O>>CC(C)(OC(=O)NC(CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)OC)C
[CH3:1][O:2][C:3](=[O:4])[C@H:5]([CH3:6])[NH2:7].O[C:8](=[O:9])[C@H:10]([CH2:11][c:12]1[c:13]([CH3:14])[cH:15][c:16]([OH:17])[cH:18][c:19]1[CH3:20])[NH:21][C:22](=[O:23])[O:24][C:25]([CH3:26])([CH3:27])[CH3:28]>>[CH3:1][O:2][C:3](=[O:4])[C@@H:5]([CH3:6])[NH:7][C:8](=[O:9])[CH:10]([CH2:11][c:12]1[c:13]([CH3:14])[cH:15][...
COC(=O)[C@H](C)N.Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)O
COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C
null
null
C(Cl)Cl
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
c1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C@@H;D3;+0:3](-[#7:4]-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8](-[C;D1;H3:9])(-[C;D1;H3:10])-[C;D1;H3:11])-[C:12]-[c:13].[C;D1;H3:14]-[#8:15]-[C:16](=[O;D1;H0:17])-[C:18](-[C;D1;H3:19])-[NH2;D1;+0:20]>>[C;D1;H3:14]-[#8:15]-[C:16](=[O;D1;H0:17])-[C:18](-[C;D1;H3:19])-[NH;D2;+0:20]-[C;H0;D3;+0:1](=...
98.9
[{"value": 98.9, "product": "CC(C)(OC(=O)NC(CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)OC)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-30
CELSIUS
16
HOUR
Racemic t-butoxycarbonyl 2,6-dimethyltyrosine (3.9 g, 10 mmoles) was dissolved in 30 ml of CH2Cl2 by adding 1.12 ml (10 mmoles) of NMM. After bringing this mixture to reflux it was cooled to -30° C. and 1.32 ml (10 mmoles) of IBCF were added to this stirred solution. The temperature was allowed to rise to -15° C. and t...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1
HO-
C(Cl)Cl
-30
16
COC(=O)[C@H](C)N.Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)O>C(Cl)Cl>COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-49bfa957cdb54d11874d4d10e9a37feb
COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C>>Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O
CC(C)(OC(=O)NC(CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)OC)C>>CC(C)(OC(=O)N[C@@H](CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)O)C
C[O:27][C:25]([C@H:23]([NH:22][C:20]([CH:11]([CH2:10][c:9]1[c:2]([CH3:1])[cH:3][c:4]([OH:5])[cH:6][c:7]1[CH3:8])[NH:12][C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19])=[O:21])[CH3:24])=[O:26]>>[CH3:1][c:2]1[cH:3][c:4]([OH:5])[cH:6][c:7]([CH3:8])[c:9]1[CH2:10][C@H:11]([NH:12][C:13](=[O:14])[O:15][C:16]([CH3:17])...
COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C
Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O
null
null
C(Cl)(Cl)Cl
Deprotection
Ester saponification (methyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
c1ccccc1
C-[O;H0;D2;+0:1]-[C:2](-[C:3])=[O;D1;H0:4]>>[C:3]-[C:2](=[O;D1;H0:4])-[OH;D1;+0:1]
null
[]
null
null
null
null
The title compound was prepared by the methods of Example 9 using diastereomer F of the title compound of Example 6. [α]D -21.7 (CHCl3) Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
c1ccccc1
Other
C(Cl)(Cl)Cl
null
null
COC(=O)[C@@H](C)NC(=O)C(Cc1c(C)cc(O)cc1C)NC(=O)OC(C)(C)C>C(Cl)(Cl)Cl>Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-7d46ffa09cc44e9392e4d49e8eb54422
Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O.NCCCc1ccccc1>>Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
C1(=CC=CC=C1)CCCN.C(Cl)Cl.CC(C)(OC(=O)N[C@@H](CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)O)C.CN1CCOCC1>>CC(C)(OC(=O)N[C@@H](CC1=C(C=C(C=C1C)O)C)C(=O)N[C@H](C)C(=O)NCCCC1=CC=CC=C1)C
O[C:25]([C@H:23]([NH:22][C:20]([C@H:11]([CH2:10][c:9]1[c:2]([CH3:1])[cH:3][c:4]([OH:5])[cH:6][c:7]1[CH3:8])[NH:12][C:13](=[O:14])[O:15][C:16]([CH3:17])([CH3:18])[CH3:19])=[O:21])[CH3:24])=[O:26].[NH2:27][CH2:28][CH2:29][CH2:30][c:31]1[cH:32][cH:33][cH:34][cH:35][cH:36]1>>[CH3:1][c:2]1[cH:3][c:4]([OH:5])[cH:6][c:7]([CH3...
Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O.NCCCc1ccccc1
Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
null
null
CCOC(=O)C
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(CCc1ccccc1)NCC(=O)NCCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6]=[O;D1;H0:7].[C:8]-[C:9]-[NH2;D1;+0:10]>>[C:8]-[C:9]-[NH;D2;+0:10]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6]=[O;D1;H0:7]
null
[]
-45
CELSIUS
8
HOUR
A CH2Cl2 solution (100 ml) of the title compound from Example 9, (16.6 g, 43.6 mmole) was charged with 4.4 g (43.6 mmoles) of NMM and cooled to -45° C. To this solution was added 5.7 g (43.6 mmole) of IBCF and the mixture warmed to 10° C. The solution was then cooled to -25° C. before adding 7.4 g (54.5 mmole) of 3-phe...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1ccccc1.c1ccccc1
HO-
CCOC(=O)C
-45
8
Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)O.NCCCc1ccccc1>CCOC(=O)C>Cc1cc(O)cc(C)c1C[C@H](NC(=O)OC(C)(C)C)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1397e52558304bc794ebf0497ed5c6b3
Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)O>>Cc1cc(O)ccc1C[C@H](N)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
Cl.CC1=C(C[C@H](N)C(=O)N[C@H](C)C(=O)O)C(=CC(=C1)O)C>>Cl.CC1=C(C[C@H](N)C(=O)N[C@H](C)C(=O)NCCCC2=CC=CC=C2)C=CC(=C1)O
O[C:17]([C@H:15]([NH:14][C:12]([C@H:10]([CH2:9][c:8]1[c:2]([CH3:1])[cH:3][c:4]([OH:5])[cH:6][c:7]1[CH3:20])[NH2:11])=[O:13])[CH3:16])=[O:18]>>[CH3:1][c:2]1[cH:3][c:4]([OH:5])[cH:6][cH:7][c:8]1[CH2:9][C@H:10]([NH2:11])[C:12](=[O:13])[NH:14][C@H:15]([CH3:16])[C:17](=[O:18])[NH:19][CH2:20][CH2:21][CH2:22][c:23]1[cH:24][cH...
Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)O
Cc1cc(O)ccc1C[C@H](N)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
null
null
CO
Aromatic Heterocycle Formation
OtherReaction
a8edcf7f55c2099e919c769dad8b38e5b55b77735d1757e3d7663e8e9f428c78
4b0f179f25479ea547f672763d671b032388c9c64c1dbabd2800d76835b4a424
O=C(CCc1ccccc1)NCC(=O)NCCCc1ccccc1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6]=[O;D1;H0:7].[C:8]-[c:9](:[c:10]):[c;H0;D3;+0:11](-[CH3;D1;+0:12]):[c:13]:[c:14]>>[C:15]-[C:16]-[CH2;D2;+0:12]-[#7:17]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3](-[C;D1;H3:4])-[#7:5]-[C:6]=[O;D1;H0:7].[C:8]-[c:9](:[c:10]):[cH;D2;+0:11]:[c:13]:[c:14]
null
[]
null
null
null
null
The title compound was prepared by the method of Example 4 from diastereomer F of the title compound of Example 11, Route B. [α]D -23.8 (MeOH) Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Secondary amide
c1ccccc1
c1ccccc1.c1ccccc1
c1ccccc1.c1ccccc1
null
CO
null
null
Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](C)C(=O)O>CO>Cc1cc(O)ccc1C[C@H](N)C(=O)N[C@H](C)C(=O)NCCCc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-adb591f5d8e14cf994f271977a5de703
C=CCN1C(=O)c2ccccc2C1=O.Cc1cccc(C)c1Br>>Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O
BrC1=C(C=CC=C1C)C.C(C=C)N1C(C=2C(C1=O)=CC=CC2)=O.C(C)(=O)[O-].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>CC1=C(C(=CC=C1)C)C=CCN1C(C2=CC=CC=C2C1=O)=O
[CH2:9]=[CH:10][CH2:11][N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22].Br[c:8]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][c:6]1[CH3:7]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH:9]=[CH:10][CH2:11][N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22]
C=CCN1C(=O)c2ccccc2C1=O.Cc1cccc(C)c1Br
Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O
null
null
CCOCC.O.C(C)N(CC)CC
C-C Coupling
OtherReaction
2d4a44695e29e4a9ab430c3b66736ad86dd99247e7216f16f3ca137abca78747
df8442c9f2045421fb18548edb9c6acaeb9710f63e741d9f72e0000ca35c948a
O=C1c2ccccc2C(=O)N1CC=Cc1ccccc1
Br-[c;H0;D3;+0:1](:[c:2](-[C;D1;H3:3]):[c:4]):[c:5](-[C;D1;H3:6]):[c:7].[C:8]-[C:9]=[CH2;D1;+0:10]>>[C:8]-[C:9]=[CH;D2;+0:10]-[c;H0;D3;+0:1](:[c:2](-[C;D1;H3:3]):[c:4]):[c:5](-[C;D1;H3:6]):[c:7]
null
[]
100
CELSIUS
null
null
A mixture 9.3 g (50 mmole) of 2-bromo-m-xylene, 15.0 g (80 mmole) of N-allylphthalimide, 0.56 (2.5 mmole) of paladium acetate and 1.44 (5.5 mmole) of triphenylphosphine were dissolved in 111 ml of triethylamine. The solution was placed in a sealed container and heated at 100° C. for 24 hours. The reaction was then dilu...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Allyl
null
c1ccccc1
c1ccccc1
c1ccccc1.c1ccc2c(c1)C[NH]C2
HBr
CCOCC.O.C(C)N(CC)CC
100
null
C=CCN1C(=O)c2ccccc2C1=O.Cc1cccc(C)c1Br>CCOCC.O.C(C)N(CC)CC>Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3ee8fe3c20534d3ebb7f9a94b9cce103
Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O>>Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O
CC1=C(C(=CC=C1)C)C=CCN1C(C2=CC=CC=C2C1=O)=O.CO>>CC1=C(C(=CC=C1)C)CCCN1C(C2=CC=CC=C2C1=O)=O
[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH:9]=[CH:10][CH2:11][N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH2:9][CH2:10][CH2:11][N:12]1[C:13](=[O:14])[c:15]2[cH:16][cH:17][cH:18][cH:19][c:20]2[C:21]1=[O:22]
Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O
Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O
null
[Pd]
C1CCOC1
Reduction
Hydrogenation (double to single)
0bc3968b35f0839c230afb4215314da278abd4e1f10e42ec3012c5512de49ea5
312e9350dcad67590617294c0eb017edf0b9fbfe6133c06a3f393b871a889092
O=C1c2ccccc2C(=O)N1CCCc1ccccc1
[O;D1;H0:1]=[C:2]-[#7:3](-[C:4]-[CH;D2;+0:5]=[CH;D2;+0:6]-[c:7](:[c:8]):[c:9])-[C:10]=[O;D1;H0:11]>>[O;D1;H0:1]=[C:2]-[#7:3](-[C:4]-[CH2;D2;+0:5]-[CH2;D2;+0:6]-[c:7](:[c:8]):[c:9])-[C:10]=[O;D1;H0:11]
null
[]
null
null
24
HOUR
The title compound of Example 32 (10 g, 34 mmole) dissolved in 120 ml of THF and 100 ml of MeOH was reduced in a standard Parr hydrogenation apparatus using 1 g of 5% Pd/C as catalyst. The reaction was run at room temperature under a pressure of 5 psi for 24 hours. The residue after removing all solvent under reduced p...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccc2c(c1)C[NH]C2
null
[Pd].C1CCOC1
null
24
Cc1cccc(C)c1C=CCN1C(=O)c2ccccc2C1=O>[Pd].C1CCOC1>Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-59ee8f90580b491d9685262ca4315869
Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O>>Cc1cccc(C)c1CCCN
CC1=C(C(=CC=C1)C)CCCN1C(C2=CC=CC=C2C1=O)=O.C(C)O.NN>>CC1=C(C(=CC=C1)C)CCCN
O=C1c2ccccc2C(=O)[N:12]1[CH2:11][CH2:10][CH2:9][c:8]1[c:2]([CH3:1])[cH:3][cH:4][cH:5][c:6]1[CH3:7]>>[CH3:1][c:2]1[cH:3][cH:4][cH:5][c:6]([CH3:7])[c:8]1[CH2:9][CH2:10][CH2:11][NH2:12]
Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O
Cc1cccc(C)c1CCCN
null
null
null
Reduction
Phthalimide deprotection
d9f63cee80ef758bd939ff2a10772447b3092f1576180488281833a98eb1691a
dbfe4201a9328005dfaec4c3f363ddbb4ef3c9b825f648735dc97b2b57396333
c1ccccc1
O=C1-[N;H0;D3;+0:1](-[C:2]-[C:3])-C(=O)-c2:c:c:c:c:c:2-1>>[C:3]-[C:2]-[NH2;D1;+0:1]
59
[{"value": 59.0, "product": "CC1=C(C(=CC=C1)C)CCCN", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
A 10 g (34.4 mmole) sample of the title compound of Example 33 was refluxed for 2 hours in 150 ml of ethanol containing 1.2 g (36.7 mmole) of 97% hydrazine. After concentrating the solution, the white crystalline residue was mixed with 100 ml of 10% NaOH and 100 ml of ether. The aqueous phase was separated and extracte...
10.6084/m9.figshare.5104873.v1
null
Substituted dicarboximide
Primary amine
c1ccc2c(c1)C[NH]C2
null
c1ccccc1
HO-
null
null
null
Cc1cccc(C)c1CCCN1C(=O)c2ccccc2C1=O>>Cc1cccc(C)c1CCCN
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-561ce089a1d34a40a3b38cb98f549b86
O=Cc1ccccc1>>O=Cc1ccccc1
C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O>>C(C1=CC=CC=C1)=O.C(C=CC1=CC=CC=C1)=O
[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[O:11]=[CH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1
O=Cc1ccccc1
O=Cc1ccccc1
null
null
null
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccccc1
null
null
[]
null
null
null
null
FIG. 2 is the GC-IR spectrum for the bottoms in the distillation pot. The peak indicated by reference numeral 20 is the peak for benzaldehyde. The peak indicated by reference numeral 21 is the peak for the cinnamaldehyde. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1
null
null
null
null
O=Cc1ccccc1>>O=Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-29e2e1d3d5724c9c82294db3f2de9b86
Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](NC(=O)/C(=N\OC3CCNC3=O)c3csc(NC(c4ccccc4)(c4ccccc4)c4ccccc4)n3)[C@H]2SC1
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O.N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O.ON1N=NC2=C1C=CC=C2.C1(CCCCC1)N=C=NC1CCCCC1>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)C2=...
[CH3:1][n:2]1[n:3][n:4][n:5][c:6]1[S:7][CH2:8][C:9]1=[C:10]([C:11](=[O:12])[O:13][CH:14]([c:15]2[cH:16][cH:17][cH:18][cH:19][cH:20]2)[c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)[N:27]2[C:28](=[O:29])[C@@H:30]([NH2:31])[C@H:68]2[S:69][CH2:70]1.O[C:32](=[O:33])/[C:34](=[N:35]\[O:36][CH:37]1[CH2:38][CH2:39][NH:40][C:41]1=...
Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](NC(=O)/C(=N\OC3CCNC3=O)c3csc(NC(c4ccccc4)(c4ccccc4)c4ccccc4)n3)[C@H]2SC1
null
null
O1CCCC1
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(OC(c1ccccc1)c1ccccc1)C1=C(CSc2nnn[nH]2)CS[C@@H]2[C@H](NC(=O)/C(=N\OC3CCNC3=O)c3csc(NC(c4ccccc4)(c4ccccc4)c4ccccc4)n3)C(=O)N12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6](:[#7;a:7]):[c:8]:[#16;a:9].[#16:10]-[C:11]1-[#7:12](-[C:13](-[C:14](-[#8:15])=[O;D1;H0:16])=[C:17])-[C:18](=[O;D1;H0:19])-[C:20]-1-[NH2;D1;+0:21]>>[#16:10]-[C:11]1-[#7:12](-[C:13](-[C:14](-[#8:15])=[O;D1;H0:16])=[C:17])-[C:18](=[O;D1;H0:19])-[C:20]-1-[NH;D2;+0:...
59
[{"value": 59.0, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O)=N/OC1C(NCC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
3.25 g of (Z)-2-(2-tritylaminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetic acid are dissolved in 200 ml of tetrahydrofuran, and 3.14 g of benzhydryl 7β-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylate, 1.03 g of 1-hydroxybenzotriazole and 1.57 g of dicyclohexylcarbodiimide are added thereto...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
c1nnn[nH]1.c1ccccc1.c1ccccc1.C1CCNC1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1.C1=CN2CC[C@H]2SC1
HO-
O1CCCC1
null
2
Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>O1CCCC1>Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](NC(=O)/C(=N\OC3CCNC3=O)c3csc(NC(c4ccccc4)(c4ccccc4)c4ccccc4)n3)[C@H]2SC1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c50403bc6f784521a924357c892f597a
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O.N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O.C1(=C(C(=C(C(=C1F)F)F)N)F)N.Cl.Cl.C/C(=N\[Si](C)(C)C)/O[Si](C)(C)C.C(C(=O)Cl)(=O)Cl>>NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O)=N/OC1C(NCC1)=O
[NH2:16][C@@H:17]1[C:18](=[O:19])[N:20]2[C:21]([C:22](=[O:23])[O-:24])=[C:25]([CH2:26][n+:27]3[cH:28][cH:29][cH:30][cH:31][cH:32]3)[CH2:33][S:34][C@H:35]12.O[C:14](/[C:5]([c:4]1[n:3][c:2]([NH:1]C(c2ccccc2)(c2ccccc2)c2ccccc2)[s:37][cH:36]1)=[N:6]\[O:7][CH:8]1[CH2:9][CH2:10][NH:11][C:12]1=[O:13])=[O:15]>>[NH2:1][c:2]1[n:...
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
null
null
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
Acylation
OtherReaction
781d8b3e409913340b6b1c61f41541a2f6dd66b9360c098a962238abbba4c82c
f20b37f950c024a98c8d203fe176865f0c41c478cf7e4a7e1363e3b299d98172
O=C(N[C@@H]1C(=O)N2C=C(C[n+]3ccccc3)CS[C@H]12)/C(=N\OC1CCNC1=O)c1cscn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6]1:[#7;a:7]:[c:8](-[NH;D2;+0:9]-C(-c2:c:c:c:c:c:2)(-c2:c:c:c:c:c:2)-c2:c:c:c:c:c:2):[#16;a:10]:[c:11]:1.[#16:12]-[C:13]1-[#7:14](-[C:15](=[O;D1;H0:16])-[C:17]-1-[NH2;D1;+0:18])-[C:19](-[C:20](-[O;-;D1;H0:21])=[O;D1;H0:22])=[C:23]>>[#16:12]-[C:13]1-[#7:14](-[C:15]...
null
[]
null
null
15
MINUTE
0.57 g of oxalyl chloride is added at -5° to 0° C. to 15 ml of chloroform containing 0.35 g of dimethylformamide, and the mixture is stirred at the same temperature for 15 minutes. A mixture of 1.54 g of (Z)-2-(2-tritylaminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetic acid, 0.3 g of triethylamine and 15 ml of ch...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Secondary amine
Secondary amide.Primary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
c1cscn1.C1CCNC1.C1=CN2CC[C@H]2SC1.C1=CC=[NH+]C=C1
HO-
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
null
0.25
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bf05a855f14647528c0f0fc05e736fca
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O.C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O.C/C(=N\[Si](C)(C)C)/O[Si](C)(C)C.C1(=C(C(=C(C(=C1F)F)F)N)F)N.Cl.Cl.C(C(=O)Cl)(=O)Cl>>NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O)=N/OC1C(NCC1)=O
[NH2:16][C@@H:17]1[C:18](=[O:19])[N:20]2[C:21]([C:22](=[O:23])[O-:24])=[C:25]([CH2:26][n+:27]3[cH:28][cH:29][cH:30][cH:31][cH:32]3)[CH2:33][S:34][C@H:35]12.O[C:14](/[C:5]([c:4]1[n:3][c:2]([NH:1]C(c2ccccc2)(c2ccccc2)c2ccccc2)[s:37][cH:36]1)=[N:6]\[O:7][CH:8]1[CH2:9][CH2:10][NH:11][C:12]1=[O:13])=[O:15]>>[NH2:1][c:2]1[n:...
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
null
null
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
Acylation
OtherReaction
781d8b3e409913340b6b1c61f41541a2f6dd66b9360c098a962238abbba4c82c
f20b37f950c024a98c8d203fe176865f0c41c478cf7e4a7e1363e3b299d98172
O=C(N[C@@H]1C(=O)N2C=C(C[n+]3ccccc3)CS[C@H]12)/C(=N\OC1CCNC1=O)c1cscn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6]1:[#7;a:7]:[c:8](-[NH;D2;+0:9]-C(-c2:c:c:c:c:c:2)(-c2:c:c:c:c:c:2)-c2:c:c:c:c:c:2):[#16;a:10]:[c:11]:1.[#16:12]-[C:13]1-[#7:14](-[C:15](=[O;D1;H0:16])-[C:17]-1-[NH2;D1;+0:18])-[C:19](-[C:20](-[O;-;D1;H0:21])=[O;D1;H0:22])=[C:23]>>[#16:12]-[C:13]1-[#7:14](-[C:15]...
null
[]
null
null
15
MINUTE
1.56 g of oxalyl chloride are added at -5° to 0° C. to 39 ml of chloroform containing 0.99 ml of dimethylformamide, and the mixture is stirred at the same temperature for 15 minutes. A solution of 4.23 g of (Z)-2-(2-tritylaminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetic acid (d-isomer) and 0.84 g of triethylami...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Secondary amine
Secondary amide.Primary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
c1cscn1.C1CCNC1.C1=CN2CC[C@H]2SC1.C1=CC=[NH+]C=C1
HO-
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
null
0.25
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-956934eb3d094e4c9e92a29f8cc49c84
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O.C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O.C/C(=N\[Si](C)(C)C)/O[Si](C)(C)C.C1(=C(C(=C(C(=C1F)F)F)N)F)N.Cl.Cl.C(C(=O)Cl)(=O)Cl>>NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)C[N+]2=CC=CC=C2)C(=O)[O-])C1=O)=N/OC1C(NCC1)=O
[NH2:16][C@@H:17]1[C:18](=[O:19])[N:20]2[C:21]([C:22](=[O:23])[O-:24])=[C:25]([CH2:26][n+:27]3[cH:28][cH:29][cH:30][cH:31][cH:32]3)[CH2:33][S:34][C@H:35]12.O[C:14](/[C:5]([c:4]1[n:3][c:2]([NH:1]C(c2ccccc2)(c2ccccc2)c2ccccc2)[s:37][cH:36]1)=[N:6]\[O:7][CH:8]1[CH2:9][CH2:10][NH:11][C:12]1=[O:13])=[O:15]>>[NH2:1][c:2]1[n:...
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
null
null
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
Acylation
OtherReaction
781d8b3e409913340b6b1c61f41541a2f6dd66b9360c098a962238abbba4c82c
f20b37f950c024a98c8d203fe176865f0c41c478cf7e4a7e1363e3b299d98172
O=C(N[C@@H]1C(=O)N2C=C(C[n+]3ccccc3)CS[C@H]12)/C(=N\OC1CCNC1=O)c1cscn1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6]1:[#7;a:7]:[c:8](-[NH;D2;+0:9]-C(-c2:c:c:c:c:c:2)(-c2:c:c:c:c:c:2)-c2:c:c:c:c:c:2):[#16;a:10]:[c:11]:1.[#16:12]-[C:13]1-[#7:14](-[C:15](=[O;D1;H0:16])-[C:17]-1-[NH2;D1;+0:18])-[C:19](-[C:20](-[O;-;D1;H0:21])=[O;D1;H0:22])=[C:23]>>[#16:12]-[C:13]1-[#7:14](-[C:15]...
null
[]
null
null
15
MINUTE
1.81 g of oxalyl chloride are added at -5° to 0° C. to 45 ml of chloroform containing 1.15 ml of dimethylformamide, and the mixture is stirred at the same temperature for 15 minutes. A solution of 4.90 g of (Z)-2-(2-tritylaminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetic acid (l-isomer) and 0.97 g of triethylami...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine.Secondary amine
Secondary amide.Primary amine
c1ccccc1.c1ccccc1.c1ccccc1
null
c1cscn1.C1CCNC1.C1=CN2CC[C@H]2SC1.C1=CC=[NH+]C=C1
HO-
CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC
null
0.25
N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccccc3)CS[C@H]12.O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>CN(C=O)C.C(Cl)(Cl)Cl.O.C(C)N(CC)CC>Nc1nc(/C(=N/OC2CCNC2=O)C(=O)N[C@@H]2C(=O)N3C(C(=O)[O-])=C(C[n+]4ccccc4)CS[C@H]23)cs1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dcdecb3ff4504c268e9963b236d8ca55
CN1CCC(O/N=C(\C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O.Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1>>CN1CCC(O/N=C(\C(=O)N[C@@H]2C(=O)N3C(C(=O)OC(c4ccccc4)c4ccccc4)=C(CSc4nnnn4C)CS[C@H]23)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(N(CC1)C)=O.N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O.ON1N=NC2=C1C=CC=C2.C1(CCCCC1)N=C=NC1CCCCC1>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)...
O[C:9](/[C:8](=[N:7]\[O:6][CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[C:70]1=[O:71])[c:45]1[cH:46][s:47][c:48]([NH:49][C:50]([c:51]2[cH:52][cH:53][cH:54][cH:55][cH:56]2)([c:57]2[cH:58][cH:59][cH:60][cH:61][cH:62]2)[c:63]2[cH:64][cH:65][cH:66][cH:67][cH:68]2)[n:69]1)=[O:10].[NH2:11][C@@H:12]1[C:13](=[O:14])[N:15]2[C:16]([C:17](...
CN1CCC(O/N=C(\C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O.Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1
CN1CCC(O/N=C(\C(=O)N[C@@H]2C(=O)N3C(C(=O)OC(c4ccccc4)c4ccccc4)=C(CSc4nnnn4C)CS[C@H]23)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O
null
null
O1CCCC1
Acylation
Carboxylic acid with primary amine to amide
37494d655fc476b499cf056f6435518833ae87795aab58744c3c61cc6e2d35e8
1acc31e468ee9ff2d6601bea2d2eb10c464508bb7150073479303b3753dd92b4
O=C(OC(c1ccccc1)c1ccccc1)C1=C(CSc2nnn[nH]2)CS[C@@H]2[C@H](NC(=O)/C(=N\OC3CCNC3=O)c3csc(NC(c4ccccc4)(c4ccccc4)c4ccccc4)n3)C(=O)N12
O-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\[#8:5])-[c:6](:[#7;a:7]):[c:8]:[#16;a:9].[#16:10]-[C:11]1-[#7:12](-[C:13](=[O;D1;H0:14])-[C:15]-1-[NH2;D1;+0:16])-[C:17](-[C:18](-[#8:19])=[O;D1;H0:20])=[C:21]>>[#16:10]-[C:11]1-[#7:12](-[C:13](=[O;D1;H0:14])-[C:15]-1-[NH;D2;+0:16]-[C;H0;D3;+0:1](=[O;D1;H0:2])/[C:3](=[#7:4]\...
55.6
[{"value": 55.6, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)N[C@H]1[C@@H]2N(C(=C(CS2)CSC2=NN=NN2C)C(=O)OC(C2=CC=CC=C2)C2=CC=CC=C2)C1=O)=N/OC1C(N(CC1)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
1.5 g of (Z)-2-(2-tritylaminothiazol-4yl)-2-[(1-methyl-2-pyrrolidon-3-yl)oxyimino]acetic acid are dissolved in 50 ml of tetrahydrofuran, and 1.4 g of benzhydryl 7β-amino-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-3-cephem-4-carboxylate, 0.6 g of 1-hydroxybenzotriazole and 0.92 g of dicyclohexylcarbodiimide are added the...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Primary amine
Secondary amide
null
null
C1CC[NH]C1.c1ccccc1.c1ccccc1.c1nnn[nH]1.C1=CN2CC[C@H]2SC1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1
HO-
O1CCCC1
null
2
CN1CCC(O/N=C(\C(=O)O)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O.Cn1nnnc1SCC1=C(C(=O)OC(c2ccccc2)c2ccccc2)N2C(=O)[C@@H](N)[C@H]2SC1>O1CCCC1>CN1CCC(O/N=C(\C(=O)N[C@@H]2C(=O)N3C(C(=O)OC(c4ccccc4)c4ccccc4)=C(CSc4nnnn4C)CS[C@H]23)c2csc(NC(c3ccccc3)(c3ccccc3)c3ccccc3)n2)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a830c0378624496eadb696b60415d2c3
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.O=C1NCCC1Br>>CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
O.C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/O.BrC1C(NCC1)=O>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/OC1C(NCC1)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])/[C:6](=[N:7]\[OH:8])[c:15]1[cH:16][s:17][c:18]([NH:19][C:20]([c:21]2[cH:22][cH:23][cH:24][cH:25][cH:26]2)([c:27]2[cH:28][cH:29][cH:30][cH:31][cH:32]2)[c:33]2[cH:34][cH:35][cH:36][cH:37][cH:38]2)[n:39]1.Br[CH:9]1[CH2:10][CH2:11][NH:12][C:13]1=[O:14]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])/[C:6...
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.O=C1NCCC1Br
CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
317eedb09d1c792890d47d514a35926bbc4daa99bfe57136559b667b95b04fd5
17b9e5d9dc3dddebe82873b428e215e82f0ae8a4833be65593459a08ce2dbc71
O=C1NCCC1ON=Cc1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-1=[O;D1;H0:6].[#16;a:7]:[c:8]:[c:9](/[C:10](=[#7:11]/[OH;D1;+0:12])-[C:13](-[#8:14])=[O;D1;H0:15]):[#7;a:16]>>[#16;a:7]:[c:8]:[c:9](/[C:10](=[#7:11]/[O;H0;D2;+0:12]-[CH;D3;+0:1]1-[C:2]-[C:3]-[#7:4]-[C:5]-1=[O;D1;H0:6])-[C:13](-[#8:14])=[O;D1;H0:15]):[#7;a:16]
85.7
[{"value": 85.7, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/OC1C(NCC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
20
MINUTE
15.8 g of ethyl (Z)-2-(2-tritylaminothiazol-4-yl)-2-hydroxyiminoacetate are dissolved in 70 ml of dimethylsulfoxide, and 5.8 g of anhydrous potassium carbonate are added thereto. The mixture is stirred at room temperature for 20 minutes. 6.6 g of 3-bromo-2-pyrrolidone are added to said mixture, and the mixture is stirr...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Oxime
null
C1CCNC1
C1CCNC1
C1CCNC1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1
HBr
CS(=O)C
null
0.333333
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.O=C1NCCC1Br>CS(=O)C>CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-af5206e6c1674815b192c0f7deab3abf
CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>>O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/OC1C(NCC1)=O.[OH-].[Na+]>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O
CC[O:3][C:2](=[O:1])/[C:4](=[N:5]\[O:6][CH:7]1[CH2:8][CH2:9][NH:10][C:11]1=[O:12])[c:13]1[cH:14][s:15][c:16]([NH:17][C:18]([c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)([c:25]2[cH:26][cH:27][cH:28][cH:29][cH:30]2)[c:31]2[cH:32][cH:33][cH:34][cH:35][cH:36]2)[n:37]1>>[O:1]=[C:2]([OH:3])/[C:4](=[N:5]\[O:6][CH:7]1[CH2:8][CH...
CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
null
null
CO
Deprotection
Ester saponification (alkyl deprotection)
d872e08ad5c85a4add6cd04e6e987e73fead5f79b3f30ba61a81ba5029b29894
38ae1ee78433b9acfb0390501446149c80f88f23ac2d84c60b3369bdab75cec9
O=C1NCCC1ON=Cc1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
C-C-[O;H0;D2;+0:1]-[C:2](=[O;D1;H0:3])\[C:4]=[#7:5]>>[#7:5]=[C:4]\[C:2](=[O;D1;H0:3])-[OH;D1;+0:1]
75.1
[{"value": 75.1, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)O)=N/OC1C(NCC1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
16.0 g of ethyl (Z)-2-(2-tritylaminothiazol-4-yl)-2-[(2-pyrrolidon-3-yl)oxyimino]acetate are added to a mixture of 160 ml of methanol and 30 ml of an aqueous 2N sodium hydroxide solution, and the mixture is refluxed for 30 minutes under heating. After cooling, crystalline precipitates are collected by filtration and wa...
10.6084/m9.figshare.5104873.v1
null
Ester
Carboxylic acid
null
null
C1CCNC1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1
Other
CO
null
null
CCOC(=O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1>CO>O=C(O)/C(=N\OC1CCNC1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c1ad53f92a1a465b9cea596d9c8433a5
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CN1CCC(Br)C1=O>>CCOC(=O)/C(=N\OC1CCN(C)C1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
O.C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/O.CN1C(C(CC1)Br)=O>>C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/OC1C(N(CC1)C)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])/[C:6](=[N:7]\[OH:8])[c:16]1[cH:17][s:18][c:19]([NH:20][C:21]([c:22]2[cH:23][cH:24][cH:25][cH:26][cH:27]2)([c:28]2[cH:29][cH:30][cH:31][cH:32][cH:33]2)[c:34]2[cH:35][cH:36][cH:37][cH:38][cH:39]2)[n:40]1.Br[CH:9]1[CH2:10][CH2:11][N:12]([CH3:13])[C:14]1=[O:15]>>[CH3:1][CH2:2][O:3][C:4](=[O...
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CN1CCC(Br)C1=O
CCOC(=O)/C(=N\OC1CCN(C)C1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
null
null
CS(=O)C
Heteroatom Alkylation and Arylation
OtherReaction
f54144ece452cc9ef90c8d4f40dc02acdd537713d549f4c07da5ccec39a0bd23
17b9e5d9dc3dddebe82873b428e215e82f0ae8a4833be65593459a08ce2dbc71
O=C1NCCC1ON=Cc1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
Br-[CH;D3;+0:1]1-[C:2]-[C:3]-[#7:4](-[C;D1;H3:5])-[C:6]-1=[O;D1;H0:7].[#16;a:8]:[c:9]:[c:10](/[C:11](=[#7:12]/[OH;D1;+0:13])-[C:14](-[#8:15])=[O;D1;H0:16]):[#7;a:17]>>[#16;a:8]:[c:9]:[c:10](/[C:11](=[#7:12]/[O;H0;D2;+0:13]-[CH;D3;+0:1]1-[C:2]-[C:3]-[#7:4](-[C;D1;H3:5])-[C:6]-1=[O;D1;H0:7])-[C:14](-[#8:15])=[O;D1;H0:16]...
64.2
[{"value": 64.2, "product": "C(C1=CC=CC=C1)(C1=CC=CC=C1)(C1=CC=CC=C1)NC=1SC=C(N1)/C(/C(=O)OCC)=N/OC1C(N(CC1)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
10
MINUTE
2.7 g of ethyl (Z)-2-(2-tritylaminothiazol-4-yl)-2-hydroxyiminoacetate are dissolved in 12 ml of dimethylsulfoxide, and 1.0 g of anhydrous potassium carbonate is added thereto under nitrogen gas atmosphere. The mixture is stirred at room temperature for 10 minutes. 1.2 g of 1-methyl-3-bromo-2-pyrrolidone are added to t...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Oxime
null
C1CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1cscn1.c1ccccc1.c1ccccc1.c1ccccc1
HBr
CS(=O)C
null
0.166667
CCOC(=O)/C(=N\O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1.CN1CCC(Br)C1=O>CS(=O)C>CCOC(=O)/C(=N\OC1CCN(C)C1=O)c1csc(NC(c2ccccc2)(c2ccccc2)c2ccccc2)n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3facba9af3ca4dc89a1396be78296749
O=C(O)[C@@H](O)[C@H](O)C(=O)O>>O=C(O)C[C@H](O)C(=O)O
[C@H]([C@@H](C(=O)O)O)(C(=O)O)O>>C([C@@H](O)CC(=O)O)(=O)O
O[C@H:4]([C:2](=[O:1])[OH:3])[C@H:5]([OH:6])[C:7](=[O:8])[OH:9]>>[O:1]=[C:2]([OH:3])[CH2:4][C@H:5]([OH:6])[C:7](=[O:8])[OH:9]
O=C(O)[C@@H](O)[C@H](O)C(=O)O
O=C(O)C[C@H](O)C(=O)O
null
null
CO
Reduction
OtherReaction
3c5af32aa639db2ebe4d9851942e9468e1838e06ae5b2c1669bca1d5e0922c33
46f8a11b80b06e754a5a34198d843342612a5e7ede950bda52ce3a500cedba0b
null
O-[C@H;D3;+0:1](-[C:2](=[O;D1;H0:3])-[O;D1;H1:4])-[C:5](-[O;D1;H1:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]>>[O;D1;H0:3]=[C:2](-[O;D1;H1:4])-[CH2;D2;+0:1]-[C:5](-[O;D1;H1:6])-[C:7](=[O;D1;H0:8])-[O;D1;H1:9]
null
[]
null
null
null
null
One of the intermediates, (S)-1-methyl-3-pyrrolidinol, was synthetized with retention of optical purity as shown in Chart IX starting with (S)-malic acid. The (S)-1-methyl-3-pyrrolidinol was shown to be dextrorotatory. As an alternative method of obtaining the resolved isomers of 1-methyl-3-pyrrolidinol, the racemic mi...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
null
null
null
Other
CO
null
null
O=C(O)[C@@H](O)[C@H](O)C(=O)O>CO>O=C(O)C[C@H](O)C(=O)O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b0c0fc9ef6e847a68cadcb68fa16fa36
CN1CCC(O)C1.NC(=O)c1ccccc1O>>CN1CCC(Oc2ccccc2C(N)=O)C1
[NH2-].[Na+].CN1CC(CC1)O.C[O-].[Na+].C(C=1C(O)=CC=CC1)(=O)N.C=1(C(=CC=CC1)S(=O)(=O)Cl)C>>CN1CC(CC1)OC1=C(C(=O)N)C=CC=C1
O[CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:16]1.[OH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][c:12]1[C:13]([NH2:14])=[O:15]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[cH:8][cH:9][cH:10][cH:11][c:12]2[C:13]([NH2:14])=[O:15])[CH2:16]1
CN1CCC(O)C1.NC(=O)c1ccccc1O
CN1CCC(Oc2ccccc2C(N)=O)C1
null
null
CN(C=O)C.C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
44b469410ea73be701b0efff512ad33f9e3763acd25fb255ddd7939c9cf1269d
776ba735002e33225fbc578943016110c2c43efefd97bfeea4ec3cc2e2e1532f
c1ccc(OC2CCNC2)cc1
O-[CH;D3;+0:1]1-[C:2]-[#7:3](-[C;D1;H3:4])-[C:5]-[C:6]-1.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11](-[OH;D1;+0:12]):[c:13]>>[C;D1;H3:4]-[#7:3]1-[C:2]-[CH;D3;+0:1](-[O;H0;D2;+0:12]-[c:11](:[c:13]):[c:10]-[C:8](-[N;D1;H2:7])=[O;D1;H0:9])-[C:6]-[C:5]-1
null
[]
70
CELSIUS
2.5
HOUR
To 85.6 g (2.2 moles) of sodium amide in 1.5 liter of dry toluene was added 202 g (2 moles) of 1-methyl-3-pyrrolidinol so as not to exceed a temperature of 50° C. The mixture was then heated to 70° C. for 4.5 hours. The mixture was cooled and 381 g (2 moles) of o-toluenesulfonylchloride was added at a rapid drop while ...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Aromatic alcohol
Ether
C1CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1
HO-
CN(C=O)C.C1(=CC=CC=C1)C
70
2.5
CN1CCC(O)C1.NC(=O)c1ccccc1O>CN(C=O)C.C1(=CC=CC=C1)C>CN1CCC(Oc2ccccc2C(N)=O)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8bc1bf72c6db4804aa9927d96d2d0b1c
CN1CCC(O)C1.O=C(O)c1cccnc1Cl>>CN1CCC(Oc2ncccc2C(=O)[O-])C1
C(C)(=O)[O-].[Na+].CN1CC(CC1)O.[H-].[Na+].ClC1=C(C(=O)O)C=CC=N1>>CN1CC(CC1)OC1=NC=CC=C1C(=O)[O-].[Na+]
[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([OH:6])[CH2:16]1.Cl[c:7]1[n:8][cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[OH:15]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[n:8][cH:9][cH:10][cH:11][c:12]2[C:13](=[O:14])[O-:15])[CH2:16]1
CN1CCC(O)C1.O=C(O)c1cccnc1Cl
CN1CCC(Oc2ncccc2C(=O)[O-])C1
null
null
CS(=O)C
Functional Group Interconversion
OtherReaction
573c3c8886c76f2095afc82b06ef70e7d8fe65f8893d97368a94b4e921cf8529
7f2e55d61afc782af1f96328fe8bb733d85eb8b217d202347fa855aaaeb12032
c1ccc(OC2CCNC2)nc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]):[c:8].[#7:9]-[C:10]-[C:11](-[OH;D1;+0:12])-[C:13]>>[#7:9]-[C:10]-[C:11](-[O;H0;D2;+0:12]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5](-[O-;H0;D1:7])=[O;D1;H0:6]):[c:8])-[C:13]
null
[]
null
null
10
MINUTE
To a stirred suspension of 6.4 g (0.13 mole) of 50% sodium hydride (mineral oil) in 50 ml of dimethylsulfoxide was added dropwise 6.4 g (0.063 mole) of 1-methyl-3-pyrrolidinol. During addition, the temperature rose from 25° C. to 31° C. After 10 minutes, a solution of 10 g (0.063 mole) of 2-chloronicotinic acid in 50 m...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Secondary alcohol
Ether
c1ccncc1
c1ccncc1
C1CC[NH]C1.c1ccncc1
HCl
CS(=O)C
null
0.166667
CN1CCC(O)C1.O=C(O)c1cccnc1Cl>CS(=O)C>CN1CCC(Oc2ncccc2C(=O)[O-])C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cb8859507f564718bbce4716cd124083
CN1CCC(Br)C1.NC(=O)c1cc(Cl)ccc1O.NC(=O)c1ccccc1O>>CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.O
BrC1CN(CC1)C.ClC1=CC=C(C(C(=O)N)=C1)O.[H-].[Na+].C(C=1C(O)=CC=CC1)(=O)N>>O.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C
Br[CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:17]1.[OH:6][c:7]1[cH:8][cH:9][c:10]([Cl:11])[cH:12][c:13]1[C:14]([NH2:15])=[O:16].[cH:18]1[cH:25][c:24]([OH:23])[c:30]([C:31]([NH2:32])=[O:33])[cH:29][cH:27]1>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[cH:8][cH:9][c:10]([Cl:11])[cH:12][c:13]2[C:14]([NH2:15])=[O:16])[CH2:17]...
CN1CCC(Br)C1.NC(=O)c1cc(Cl)ccc1O.NC(=O)c1ccccc1O
CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.O
null
null
CN(C=O)C.O
Aromatic Heterocycle Formation
OtherReaction
01b90862cba7fba60c84a18798f089b5127049a78a40950ed9f28fdd21c81fe5
74e0a2077a887e150582bccf28106f84aebd7243b3a5a6678934f2544b9ecf2f
c1ccc(OC2CCNC2)cc1.c1ccc(OC2CCNC2)cc1
Br-[CH;D3;+0:1]1-[C:2]-[#7:3](-[C;D1;H3:4])-[C:5]-[C:6]-1.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[c:10]1:[c:11]:[cH;D2;+0:12]:[cH;D2;+0:13]:[cH;D2;+0:14]:[c:15]:1-[OH;D1;+0:16].[N;D1;H2:17]-[C:18](=[O;D1;H0:19])-[c:20]:[c:21](-[OH;D1;+0:22]):[c:23]>>[C;D1;H3:4]-[#7:3]1-[C:2]-[CH;D3;+0:1](-[O;H0;D2;+0:22]-[c:21](:[c:23]):[c:20...
34.1
[{"value": 23.0, "product": "O.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C", "details": "PERCENTYIELD", "is_desired": false}, {"value": 34.1, "product": "O.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C.ClC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a cooled suspension of 2.4 g (0.41 mole) sodium hydride in 50 ml of dimethylformamide was added dropwise 17 g (0.1 mole) of 5-chlorosalicylamide dissolved in 50 ml of dimethylformamide at a rate such that the temperature did not exceed 20° C. After addition of the salicylamide was complete, 16.7 g (0.1 mole) of 3-br...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Aromatic alcohol.Aromatic alcohol
Aromatic halide.Ether.Ether.Tertiary amine
C1CC[NH]C1.c1ccccc1
C1CC[NH]C1.C1CC[NH]C1.c1ccccc1
C1CC[NH]C1.c1ccccc1.C1CC[NH]C1.c1ccccc1
Br-
CN(C=O)C.O
null
null
CN1CCC(Br)C1.NC(=O)c1cc(Cl)ccc1O.NC(=O)c1ccccc1O>CN(C=O)C.O>CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.CN1CCC(Oc2ccc(Cl)cc2C(N)=O)C1.O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-5bf0c62c0ba34c788309186cc279405a
CN1CCC(O)C1.NC(=O)c1ccc2ccccc2c1O>>CN1CCC(Oc2c(C(N)=O)ccc3ccccc23)C1
CS(=O)(=O)Cl.CN1CC(CC1)O.C(C)N(CC)CC.[Na].OC1=C(C=CC2=CC=CC=C12)C(=O)N>>CN1CC(CC1)OC1=C(C=CC2=CC=CC=C12)C(=O)N
O[CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:20]1.[OH:6][c:7]1[c:8]([C:9]([NH2:10])=[O:11])[cH:12][cH:13][c:14]2[cH:15][cH:16][cH:17][cH:18][c:19]12>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[c:8]([C:9]([NH2:10])=[O:11])[cH:12][cH:13][c:14]3[cH:15][cH:16][cH:17][cH:18][c:19]23)[CH2:20]1
CN1CCC(O)C1.NC(=O)c1ccc2ccccc2c1O
CN1CCC(Oc2c(C(N)=O)ccc3ccccc23)C1
null
null
C1=CC=CC=C1.O
Heteroatom Alkylation and Arylation
Mitsunobu aryl ether
44b469410ea73be701b0efff512ad33f9e3763acd25fb255ddd7939c9cf1269d
776ba735002e33225fbc578943016110c2c43efefd97bfeea4ec3cc2e2e1532f
c1ccc2c(OC3CCNC3)cccc2c1
O-[CH;D3;+0:1]1-[C:2]-[#7:3](-[C;D1;H3:4])-[C:5]-[C:6]-1.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11](-[OH;D1;+0:12]):[c:13]>>[C;D1;H3:4]-[#7:3]1-[C:2]-[CH;D3;+0:1](-[O;H0;D2;+0:12]-[c:11](:[c:13]):[c:10]-[C:8](-[N;D1;H2:7])=[O;D1;H0:9])-[C:6]-[C:5]-1
null
[]
75
CELSIUS
15
MINUTE
In another vessel, 79 g (0.69 mole) of methanesulfonylchloride was added dropwise to a solution of 69.7 g (0.69 mole) of 1-methyl-3-pyrrolidinol and 77 g (0.76 mole) of triethylamine in 500 ml of dry benzene while cooling with an ice bath. The mixture was stirred 15 minutes and filtered. The filter cake was washed with...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol.Aromatic alcohol
Ether
C1CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1ccc2ccccc2c1
HO-
C1=CC=CC=C1.O
75
0.25
CN1CCC(O)C1.NC(=O)c1ccc2ccccc2c1O>C1=CC=CC=C1.O>CN1CCC(Oc2c(C(N)=O)ccc3ccccc23)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d8c0cc498d57496e9455a867931d8c90
CN1CCC(S)C1.O=C(O)c1cccnc1Cl>>CN1CCC(Sc2ncccc2C(=O)O)C1
ClC1=C(C(=O)O)C=CC=N1.CN1CC(CC1)S.[H-].[Na+]>>CN1CC(CC1)SC1=NC=CC=C1C(=O)O
[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([SH:6])[CH2:16]1.Cl[c:7]1[n:8][cH:9][cH:10][cH:11][c:12]1[C:13](=[O:14])[OH:15]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([S:6][c:7]2[n:8][cH:9][cH:10][cH:11][c:12]2[C:13](=[O:14])[OH:15])[CH2:16]1
CN1CCC(S)C1.O=C(O)c1cccnc1Cl
CN1CCC(Sc2ncccc2C(=O)O)C1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Ullmann-Goldberg Substitution thiol
83e1471f87e837809a4e2fb3e1de305c0d7a6603480e04a86024c7cd55ed85fb
b7fe376f7aad2517725eef26ab981e4baa6c31c5f38fdf89e7c52a4a2c6cc1d2
c1ccc(SC2CCNC2)nc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]):[c:8].[#7:9]-[C:10]-[C:11](-[SH;D1;+0:12])-[C:13]>>[#7:9]-[C:10]-[C:11](-[S;H0;D2;+0:12]-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[O;D1;H1:7]):[c:8])-[C:13]
null
[]
60
CELSIUS
8
HOUR
To a stirred suspension of 80 g (2 mole) of 60% sodium hydride (in mineral oil) in 800 ml of dry dimethylformamide, all heated to 60° C. and using nitrogen gas flow was added dropwise, a solution of 157.0 g (1 mole) of 2-chloronicotinic acid and 117 g (1 mole) of 1-methyl-3-pyrrolidinethiol in 300 ml of dimethylformami...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Aliphatic thiol
Monosulfide
c1ccncc1
c1ccncc1
C1CC[NH]C1.c1ccncc1
HCl
CN(C=O)C
60
8
CN1CCC(S)C1.O=C(O)c1cccnc1Cl>CN(C=O)C>CN1CCC(Sc2ncccc2C(=O)O)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a745416737d6407f8a23a934d3424d3d
O=C(O)c1cccnc1Cl.OC1CN(C2CCCCC2)C1>>O=C([O-])c1cccnc1OC1CN(C2CCCCC2)C1
C1(CCCCC1)N1CC(C1)O.ClC1=C(C(=O)O)C=CC=N1.[H-].[Na+]>>C1(CCCCC1)N1CC(C1)OC1=NC=CC=C1C(=O)[O-].[Na+]
Cl[c:9]1[c:4]([C:2](=[O:1])[OH:3])[cH:5][cH:6][cH:7][n:8]1.[OH:10][CH:11]1[CH2:12][N:13]([CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19]2)[CH2:20]1>>[O:1]=[C:2]([O-:3])[c:4]1[cH:5][cH:6][cH:7][n:8][c:9]1[O:10][CH:11]1[CH2:12][N:13]([CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18][CH2:19]2)[CH2:20]1
O=C(O)c1cccnc1Cl.OC1CN(C2CCCCC2)C1
O=C([O-])c1cccnc1OC1CN(C2CCCCC2)C1
null
null
CN(C=O)C
Functional Group Interconversion
OtherReaction
573c3c8886c76f2095afc82b06ef70e7d8fe65f8893d97368a94b4e921cf8529
7f2e55d61afc782af1f96328fe8bb733d85eb8b217d202347fa855aaaeb12032
c1ccc(OC2CN(C3CCCCC3)C2)nc1
Cl-[c;H0;D3;+0:1](:[#7;a:2]:[c:3]):[c:4](-[C:5](=[O;D1;H0:6])-[OH;D1;+0:7]):[c:8].[OH;D1;+0:9]-[C:10]1-[C:11]-[#7:12]-[C:13]-1>>[O-;H0;D1:7]-[C:5](=[O;D1;H0:6])-[c:4](:[c:8]):[c;H0;D3;+0:1](-[O;H0;D2;+0:9]-[C:10]1-[C:11]-[#7:12]-[C:13]-1):[#7;a:2]:[c:3]
86
[{"value": 86.0, "product": "C1(CCCCC1)N1CC(C1)OC1=NC=CC=C1C(=O)[O-].[Na+]", "details": "PERCENTYIELD", "is_desired": false}, {"value": 85.8, "product": "C1(CCCCC1)N1CC(C1)OC1=NC=CC=C1C(=O)[O-].[Na+]", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
2
HOUR
A solution of 105 g (0.68 mole) of 1-cyclohexyl-3-azetidinol and 106 g (0.68 mole) of 2-chloronicotinic acid in 400 ml of dry dimethylformamide was added at a rapid drop to 52 g (1.35 mole) of 60% sodium hydride/mineral oil suspended in 400 ml of dry dimethylformamide at 60° C. Mild exothermic reaction was noted. After...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Secondary alcohol
Ether
c1ccncc1
c1ccncc1
c1ccncc1.C1C[NH]C1.C1CCCCC1
HCl
CN(C=O)C
60
2
O=C(O)c1cccnc1Cl.OC1CN(C2CCCCC2)C1>CN(C=O)C>O=C([O-])c1cccnc1OC1CN(C2CCCCC2)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b3282ab649924efeb49346007aa7bf75
Clc1ccc2ccccc2n1.O=C=O>>O=C(O)c1cc2ccccc2nc1Cl
C(C)(C)NC(C)C.C(CCC)[Li].CCCCCC.ClC1=NC2=CC=CC=C2C=C1.C(=O)=O>>ClC1=NC2=CC=CC=C2C=C1C(=O)O
[cH:4]1[cH:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[n:12][c:13]1[Cl:14].[O:1]=[C:2]=[O:3]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]2[cH:7][cH:8][cH:9][cH:10][c:11]2[n:12][c:13]1[Cl:14]
Clc1ccc2ccccc2n1.O=C=O
O=C(O)c1cc2ccccc2nc1Cl
null
null
O1CCCC1
Acylation
OtherReaction
78ee4f870a2bb40b1759c2e4cd484e204c5b2b946629ed40af42c92cfb454773
f2fa2063dd26da08ea200eb6cbb3037b91013a82352a2b60120e98f9e54cbd88
c1ccc2ncccc2c1
[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:[cH;D2;+0:7]:1.[O;D1;H0:8]=[C;H0;D2;+0:9]=[O;H0;D1;+0:10]>>[Cl;D1;H0:1]-[c:2]1:[#7;a:3]:[c:4]:[c:5]:[c:6]:[c;H0;D3;+0:7]:1-[C;H0;D3;+0:9](=[O;D1;H0:8])-[OH;D1;+0:10]
62
[{"value": 62.0, "product": "ClC1=NC2=CC=CC=C2C=C1C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
-65
CELSIUS
null
null
To a solution of 21.3 ml (0.15 mole) of diisopropyl amine in 300 ml of dry tetrahydrofuran under a continuous nitrogen blanket, at -70° C., was added 61.6 ml of 2.7M n-butyllithium in hexane (0.165 mole) while maintaining the temperature at -60° to -70° C. Subsequent to this addition, the temperature was maintained at ...
10.6084/m9.figshare.5104873.v1
null
Carbon dioxide
Carboxylic acid
c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1
null
O1CCCC1
-65
null
Clc1ccc2ccccc2n1.O=C=O>O1CCCC1>O=C(O)c1cc2ccccc2nc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bbe4662ee3c84951be6a4e98c39cf4dd
Clc1cncc(Cl)c1.O=C=O>>O=C(O)c1c(Cl)cncc1Cl
C(=O)=O.C(C)(C)NC(C)C.C(CCC)[Li].ClC=1C=NC=C(C1)Cl>>ClC=1C=NC=C(C1C(=O)O)Cl
[cH:4]1[c:5]([Cl:6])[cH:7][n:8][cH:9][c:10]1[Cl:11].[O:1]=[C:2]=[O:3]>>[O:1]=[C:2]([OH:3])[c:4]1[c:5]([Cl:6])[cH:7][n:8][cH:9][c:10]1[Cl:11]
Clc1cncc(Cl)c1.O=C=O
O=C(O)c1c(Cl)cncc1Cl
null
null
CCCCCC.O1CCCC1
Acylation
OtherReaction
aa033d9bf3794a09c2037c20bc6de9e9f91edade53ff65b01042aec8736af92c
f2fa2063dd26da08ea200eb6cbb3037b91013a82352a2b60120e98f9e54cbd88
c1ccncc1
[Cl;D1;H0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[c:6](-[Cl;D1;H0:7]):[cH;D2;+0:8]:1.[O;D1;H0:9]=[C;H0;D2;+0:10]=[O;H0;D1;+0:11]>>[Cl;D1;H0:1]-[c:2]1:[c:3]:[#7;a:4]:[c:5]:[c:6](-[Cl;D1;H0:7]):[c;H0;D3;+0:8]:1-[C;H0;D3;+0:10](=[O;D1;H0:9])-[OH;D1;+0:11]
null
[]
-70
CELSIUS
0.5
HOUR
To a solution of 4.96 ml (0.036 mole) of diisopropylamine in 200 ml of tetrahydrofuran at -65° C. under a nitrogen blanket was added dropwise 14.9 ml of 2.5M n-butyllithium in hexane while maintaining the above temperature. Twenty minutes subsequent to that addition, a solution 5.0 g (0.034 mole) of 3,5-dichloropyridin...
10.6084/m9.figshare.5104873.v1
null
Carbon dioxide
Carboxylic acid
c1ccncc1
c1ccncc1
c1ccncc1
null
CCCCCC.O1CCCC1
-70
0.5
Clc1cncc(Cl)c1.O=C=O>CCCCCC.O1CCCC1>O=C(O)c1c(Cl)cncc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d01d6df666e947e8b991d4358df01960
COC(=O)c1ccc2cnccc2c1O.N>>NC(=O)c1ccc2cnccc2c1O
N.COC(=O)C=1C(=C2C=CN=CC2=CC1)O.N>>OC1=C2C=CN=CC2=CC=C1C(=O)N
CO[C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][n:9][cH:10][cH:11][c:12]2[c:13]1[OH:14].[NH3:1]>>[NH2:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][n:9][cH:10][cH:11][c:12]2[c:13]1[OH:14]
COC(=O)c1ccc2cnccc2c1O.N
NC(=O)c1ccc2cnccc2c1O
null
null
null
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
c1ccc2cnccc2c1
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
null
null
5-Hydroxy-6-isoquinolinecarboxylic acid methyl ester as reported by Dyke, S. F. et al., in Tetrahedron 1973, 29(6), 857-62, is reacted with excess ammonia in a steel bomb for 12-18 hr. The excess ammonia is allowed to evaporate and the residue is crystallized from a suitable solvent mix such as ethyl acetate-toluene to...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1ccc2cnccc2c1
HO-
null
null
null
COC(=O)c1ccc2cnccc2c1O.N>>NC(=O)c1ccc2cnccc2c1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a902a7150ecd47d6a1975e8b2de5b2ae
Cc1ccc2ccc(C(=O)O)c(O)c2n1>>COC(=O)c1ccc2ccc(C)nc2c1O
OC=1C(=CC=C2C=CC(=NC12)C)C(=O)O.B(F)(F)F.C([O-])(O)=O.[Na+]>>COC(=O)C1=CC=C2C=CC(=NC2=C1O)C
[OH:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][c:11]([CH3:12])[n:13][c:14]2[c:15]1[OH:16]>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[cH:6][cH:7][c:8]2[cH:9][cH:10][c:11]([CH3:12])[n:13][c:14]2[c:15]1[OH:16]
Cc1ccc2ccc(C(=O)O)c(O)c2n1
COC(=O)c1ccc2ccc(C)nc2c1O
null
null
null
Miscellaneous
Protection of carboxylic acid
56520e0abb4535dce9a663824ca803b71c2c0dd72dfd246317d953596a987bd2
2ccc7a30191c2c171b49e8a0217bee87430687dd0f567141eca025a75b7e3136
c1ccc2ncccc2c1
[O;D1;H0:1]=[C:2](-[OH;D1;+0:3])-[c:4]>>[C;D1;H3:5]-[O;H0;D2;+0:3]-[C:2](=[O;D1;H0:1])-[c:4]
null
[]
null
null
null
null
8-Hydroxy-2-methyl-7-quinolinecarboxylic acid (as reported by Meek, W. H. et al., in J. Chem. Eng. Data 1969, 14(3), 388-91) is reacted with methanolic boron trifluoride solution for several hours. The resulting mixture is added to an aqueous solution of sodium bicarbonate to give finally a basic solution. The solution...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccc2ncccc2c1
Other
null
null
null
Cc1ccc2ccc(C(=O)O)c(O)c2n1>>COC(=O)c1ccc2ccc(C)nc2c1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-abab3f08dfb7407e8adcdfc18a9a3ffd
COC(=O)c1ccc2ccc(C)nc2c1O.N>>Cc1ccc2ccc(C(N)=O)c(O)c2n1
N.COC(=O)C1=CC=C2C=CC(=NC2=C1O)C.N>>OC=1C(=CC=C2C=CC(=NC12)C)C(=O)N
CO[C:9]([c:8]1[cH:7][cH:6][c:5]2[cH:4][cH:3][c:2]([CH3:1])[n:15][c:14]2[c:12]1[OH:13])=[O:11].[NH3:10]>>[CH3:1][c:2]1[cH:3][cH:4][c:5]2[cH:6][cH:7][c:8]([C:9]([NH2:10])=[O:11])[c:12]([OH:13])[c:14]2[n:15]1
COC(=O)c1ccc2ccc(C)nc2c1O.N
Cc1ccc2ccc(C(N)=O)c(O)c2n1
null
null
null
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[c:6]:[#7;a:7].[NH3;D0;+0:8]>>[#7;a:7]:[c:6]:[c:5]:[c:3](-[C;H0;D3;+0:1](-[NH2;D1;+0:8])=[O;D1;H0:2]):[c:4]
null
[]
null
null
null
null
8-Hydroxy-2-methyl-7-quinolinecarboxylic acid methyl ester is reacted with excess ammonia in a steel bomb for 12-18 hr. The excess ammonia is allowed to evaporate and the residue is crystallized from a suitable solvent to give the title compound. Conditions: See reaction.notes.procedure_details. Workup: to evaporate; t...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1ccc2ncccc2c1
HO-
null
null
null
COC(=O)c1ccc2ccc(C)nc2c1O.N>>Cc1ccc2ccc(C(N)=O)c(O)c2n1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c857701e44354b45bafe59192161b725
O=C(O)c1c(O)ccc2ncccc12>>COC(=O)c1c(O)ccc2ncccc12
OC1=C(C=2C=CC=NC2C=C1)C(=O)O.B(F)(F)F.C([O-])(O)=O.[Na+]>>COC(=O)C=1C=2C=CC=NC2C=CC1O
[OH:2][C:3](=[O:4])[c:5]1[c:6]([OH:7])[cH:8][cH:9][c:10]2[n:11][cH:12][cH:13][cH:14][c:15]12>>[CH3:1][O:2][C:3](=[O:4])[c:5]1[c:6]([OH:7])[cH:8][cH:9][c:10]2[n:11][cH:12][cH:13][cH:14][c:15]12
O=C(O)c1c(O)ccc2ncccc12
COC(=O)c1c(O)ccc2ncccc12
null
null
null
Miscellaneous
Protection of carboxylic acid
56520e0abb4535dce9a663824ca803b71c2c0dd72dfd246317d953596a987bd2
2ccc7a30191c2c171b49e8a0217bee87430687dd0f567141eca025a75b7e3136
c1ccc2ncccc2c1
[O;D1;H0:1]=[C:2](-[OH;D1;+0:3])-[c:4]>>[C;D1;H3:5]-[O;H0;D2;+0:3]-[C:2](=[O;D1;H0:1])-[c:4]
null
[]
null
null
null
null
6-Hydroxy-5-quinolinecarboxylic acid [as reported by Da Re, P. et al. in Ann. Chem. (Rome) 1970, 60(3), 215-24 (C.A. 73, 25338m)] is reacted with methanolic boron trifluoride solution for several hours. The resulting mixture is added to an aqueous solution of sodium bicarbonate to give finally a basic solution. The sol...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid
Ester
null
null
c1ccc2ncccc2c1
Other
null
null
null
O=C(O)c1c(O)ccc2ncccc12>>COC(=O)c1c(O)ccc2ncccc12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8364f102cacd4f039922a83884184b50
COC(=O)c1c(O)ccc2ncccc12.N>>NC(=O)c1c(O)ccc2ncccc12
N.COC(=O)C=1C=2C=CC=NC2C=CC1O.N>>OC1=C(C=2C=CC=NC2C=C1)C(=O)N
CO[C:2](=[O:3])[c:4]1[c:5]([OH:6])[cH:7][cH:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]12.[NH3:1]>>[NH2:1][C:2](=[O:3])[c:4]1[c:5]([OH:6])[cH:7][cH:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]12
COC(=O)c1c(O)ccc2ncccc12.N
NC(=O)c1c(O)ccc2ncccc12
null
null
null
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[c:6]:[#7;a:7].[NH3;D0;+0:8]>>[#7;a:7]:[c:6]:[c:5]:[c:3](-[C;H0;D3;+0:1](-[NH2;D1;+0:8])=[O;D1;H0:2]):[c:4]
null
[]
null
null
null
null
6-Hydroxy-5-quinolinecarboxylic acid methyl ester is reacted with excess ammonia in a steel bomb for 12-18 hr. The excess ammonia is allowed to evaporate and the residue is crystallized from a suitable solvent to give the title compound. Conditions: See reaction.notes.procedure_details. Workup: to evaporate; the residu...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1ccc2ncccc2c1
HO-
null
null
null
COC(=O)c1c(O)ccc2ncccc12.N>>NC(=O)c1c(O)ccc2ncccc12
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-a272ef90d6fd48a2baa2dfdab2953f6f
COC(=O)c1ccc2cccnc2c1O.N>>NC(=O)c1ccc2cccnc2c1O
N.COC(=O)C1=CC=C2C=CC=NC2=C1O.N>>OC=1C(=CC=C2C=CC=NC12)C(=O)N
CO[C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][n:11][c:12]2[c:13]1[OH:14].[NH3:1]>>[NH2:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][c:7]2[cH:8][cH:9][cH:10][n:11][c:12]2[c:13]1[OH:14]
COC(=O)c1ccc2cccnc2c1O.N
NC(=O)c1ccc2cccnc2c1O
null
null
null
Acylation
OtherReaction
d5b10d4f469e7a196a3b04a6a9e159a7d90514b6df5b50c1197d4b1b774c04e1
adc0ef6f6c1340dd2dbab737c85bf17fc842769181c5db1a2b4f82b391b28f9f
c1ccc2ncccc2c1
C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]:[c:6]:[#7;a:7].[NH3;D0;+0:8]>>[#7;a:7]:[c:6]:[c:5]:[c:3](-[C;H0;D3;+0:1](-[NH2;D1;+0:8])=[O;D1;H0:2]):[c:4]
null
[]
null
null
null
null
8-Hydroxy-7-quinolinecarboxylic acid methyl ester [as reported by Eckstein, Z. et al. in Pol. J. Chem. 1979, 53(11), 2373-7 (C.A. 92, 215243s)] is reacted with excess ammonia in a steel bomb for 12-18 hr. The excess ammonia is allowed to evaporate and the residue is crystallized from a suitable solvent to give the titl...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary amide
null
null
c1ccc2ncccc2c1
HO-
null
null
null
COC(=O)c1ccc2cccnc2c1O.N>>NC(=O)c1ccc2cccnc2c1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b804369893e54bd59770ee9a23839cc6
CN.O=C(O)C[C@H](O)C(=O)O>>CN1C(=O)C[C@H](O)C1=O
C([C@@H](O)CC(=O)O)(=O)O.CN>>O[C@@H]1C(N(C(C1)=O)C)=O
[CH3:1][NH2:2].O[C:3](=[O:4])[CH2:5][C@H:6]([OH:7])[C:8](O)=[O:9]>>[CH3:1][N:2]1[C:3](=[O:4])[CH2:5][C@H:6]([OH:7])[C:8]1=[O:9]
CN.O=C(O)C[C@H](O)C(=O)O
CN1C(=O)C[C@H](O)C1=O
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
c87adbc4872314c499da8105023ac82c15f4a7000eff749dc6651a62a17f08b1
b7eb222f11e89f2ccff57aab9a5106ae4173f0ba94ac518e1a9f3b22a378531d
O=C1CCC(=O)N1
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[O;D1;H1:5])-[C;H0;D3;+0:6](-O)=[O;D1;H0:7].[C;D1;H3:8]-[NH2;D1;+0:9]>>[C;D1;H3:8]-[N;H0;D3;+0:9]1-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[O;D1;H1:5])-[C;H0;D3;+0:6]-1=[O;D1;H0:7]
null
[]
null
null
null
null
To a stirred solution of 134 g (1 mole) of (S)-malic acid in 700 ml of toluene was added 97 ml of 40% aqueous methylamine. The temperature slowly rose to 50° C. After 0.5 hr the stirred mixture was heated to reflux and the water was collected in a Dean-Stark trap for 48 hours. A total of 93 ml of water was collected. T...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Carboxylic acid.Primary amine
Substituted dicarboximide
null
C1CC[NH]C1
C1CC[NH]C1
HO-
C1(=CC=CC=C1)C
null
null
CN.O=C(O)C[C@H](O)C(=O)O>C1(=CC=CC=C1)C>CN1C(=O)C[C@H](O)C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-1c2ca15851eb4519b4b2de95c0278d64
O=C(O)c1cc(Br)cnc1O.O=S(Cl)Cl>>O=C(O)c1cc(Br)cnc1Cl
BrC=1C=NC(=C(C(=O)O)C1)O.S(=O)(Cl)Cl>>BrC=1C=C(C(=NC1)Cl)C(=O)O
O[c:10]1[c:4]([C:2](=[O:1])[OH:3])[cH:5][c:6]([Br:7])[cH:8][n:9]1.O=S(Cl)[Cl:11]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([Br:7])[cH:8][n:9][c:10]1[Cl:11]
O=C(O)c1cc(Br)cnc1O.O=S(Cl)Cl
O=C(O)c1cc(Br)cnc1Cl
null
null
CN(C=O)C
Functional Group Interconversion
Alcohol to chloride_SOCl2
ab85b19a1f19bdb0596b983dc6471067aedf5e7b894e737e6d16cd077bd81b42
e71580a8ffadb7b2717ecd7d68c1d3c0ca161ba5e6a787a49dad5a1359adc993
c1ccncc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[c;H0;D3;+0:2](:[#7;a:3]:[c:4]):[c:5](-[C:6](=[O;D1;H0:7])-[O;D1;H1:8]):[c:9]>>[Cl;H0;D1;+0:1]-[c;H0;D3;+0:2](:[#7;a:3]:[c:4]):[c:5](-[C:6](=[O;D1;H0:7])-[O;D1;H1:8]):[c:9]
null
[]
null
null
null
null
To 15 g (0.069 mole) of 5-bromo-2-hydroxy nicotinic acid was added 75 ml of thionyl chloride and 3 ml of dimethylformamide. The mixture was heated to reflux for 30 minutes. After cooling, the excess thionyl chloride was removed by rotary evaporation and the residue poured into water (1 liter) with vigorous agitation. T...
10.6084/m9.figshare.5104873.v1
null
Aromatic alcohol
Aromatic halide
c1ccncc1
c1ccncc1
c1ccncc1
HCl
CN(C=O)C
null
null
O=C(O)c1cc(Br)cnc1O.O=S(Cl)Cl>CN(C=O)C>O=C(O)c1cc(Br)cnc1Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-f3db1044f1d24b8cbe93aa3f0f632b1b
BrBr.O=C(O)c1cccnc1O>>O=C(O)c1cc(Br)cnc1O
Br[O-].[Na+].BrBr.[OH-].[Na+].Cl.OC1=C(C(=O)O)C=CC=N1.[OH-].[Na+].Br[O-].[Na+]>>BrC=1C=C(C(=NC1)O)C(=O)O
Br[Br:7].[O:1]=[C:2]([OH:3])[c:4]1[cH:5][cH:6][cH:8][n:9][c:10]1[OH:11]>>[O:1]=[C:2]([OH:3])[c:4]1[cH:5][c:6]([Br:7])[cH:8][n:9][c:10]1[OH:11]
BrBr.O=C(O)c1cccnc1O
O=C(O)c1cc(Br)cnc1O
null
null
O
Functional Group Interconversion
Bromination
66a492ff31bfcbb52d9a760416ba269a4cf5a439a6c2ca9c2c3a3ed0a750b974
3c4065ab4a8681675e06a527dcad54d701c7bfdcac9f73f87773b05034108934
c1ccncc1
Br-[Br;H0;D1;+0:1].[O;D1;H0:2]=[C:3](-[O;D1;H1:4])-[c:5]1:[c:6]:[#7;a:7]:[c:8]:[cH;D2;+0:9]:[c:10]:1>>[Br;H0;D1;+0:1]-[c;H0;D3;+0:9]1:[c:10]:[c:5](-[C:3](=[O;D1;H0:2])-[O;D1;H1:4]):[c:6]:[#7;a:7]:[c:8]:1
63.5
[{"value": 63.5, "product": "BrC=1C=C(C(=NC1)O)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
24
HOUR
To a solution of 10 g (0.07 mole) of 2-hydroxy-nicotinic acid in 16.8 g of 50% sodium hydroxide (0.21 mole) diluted with 25 ml of water was added 200 ml of sodium hypobromite solution prepared by adding 13.6 g (0.17 mole) of bromine to a solution of 20.16 g of 50% sodium hydroxide (0.25 mole) in 125 ml of water at 0° C...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1ccncc1
c1ccncc1
c1ccncc1
HBr
O
null
24
BrBr.O=C(O)c1cccnc1O>O>O=C(O)c1cc(Br)cnc1O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ade44fe67a2945baad793a7536771fc1
CN1CCC(CS(=O)(=O)[O-])C1.NC(=O)c1cc([N+](=O)[O-])ccc1Cl>>CN1CCC(Oc2ccc([N+](=O)[O-])cc2C(N)=O)C1
CN1CC(CC1)CS(=O)(=O)[O-].S(C)(=O)(=O)[O-].ClC1=C(C(=O)N)C=C(C=C1)[N+](=O)[O-].CN1CC(CC1)CS(=O)(=O)[O-].[H-].[Na+].[H-].[Na+]>>CN1CC(CC1)OC1=C(C(=O)N)C=C(C=C1)[N+](=O)[O-]
O=S(=O)(C[CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:19]1)[O-:6].Cl[c:7]1[cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]1[C:16]([NH2:17])=[O:18]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[cH:8][cH:9][c:10]([N+:11](=[O:12])[O-:13])[cH:14][c:15]2[C:16]([NH2:17])=[O:18])[CH2:19]1
CN1CCC(CS(=O)(=O)[O-])C1.NC(=O)c1cc([N+](=O)[O-])ccc1Cl
CN1CCC(Oc2ccc([N+](=O)[O-])cc2C(N)=O)C1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
439d911140614b99d4b0270213d2dd4bbc4a10d8d14603e62682d5b8fe95f5ea
c6d4374ac8a696f9ab980fdeb90e66ca3eeaeaef655a92a405538f38cf46f692
c1ccc(OC2CCNC2)cc1
Cl-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]):[c:8].O=S(=O)(-[O-;H0;D1:9])-C-[CH;D3;+0:10]1-[C:11]-[#7:12](-[C;D1;H3:13])-[C:14]-[C:15]-1>>[C;D1;H3:13]-[#7:12]1-[C:11]-[CH;D3;+0:10](-[O;H0;D2;+0:9]-[c;H0;D3;+0:1](:[c:2]:[c:3]):[c:4](-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]):[c:8])-[C:15]-[C:14]-1
12
[{"value": 12.0, "product": "CN1CC(CC1)OC1=C(C(=O)N)C=C(C=C1)[N+](=O)[O-]", "details": "PERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a cooled suspension of sodium hydride (2.42 g of 60% content 0.06 mole) in 50 ml of dimethylformamide under nitrogen was added dropwise a solution of 10 g (0.055 mole) of 2-chloro-5-nitrobenzamide in 20 ml dimethylformamide. The suspension was stirred at room temperature for 1 hr and heated to 60° C. at which time 9...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Sulfonic acid
Ether
C1CC[NH]C1.c1ccccc1
C1CC[NH]C1.c1ccccc1
C1CC[NH]C1.c1ccccc1
HCl
CN(C=O)C
null
1
CN1CCC(CS(=O)(=O)[O-])C1.NC(=O)c1cc([N+](=O)[O-])ccc1Cl>CN(C=O)C>CN1CCC(Oc2ccc([N+](=O)[O-])cc2C(N)=O)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-997cc09958b640a1bde80518045ba4ee
CN1CCC(OS(C)(=O)=O)C1.NC(=O)c1cc(F)ccc1O>>CN1CCC(Oc2ccc(F)cc2C(N)=O)C1
[H-].[Na+].FC=1C=CC(=C(C(=O)N)C1)O.CS(=O)(=O)OC1CN(CC1)C>>FC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C
CS(=O)(=O)O[CH:5]1[CH2:4][CH2:3][N:2]([CH3:1])[CH2:17]1.[OH:6][c:7]1[cH:8][cH:9][c:10]([F:11])[cH:12][c:13]1[C:14]([NH2:15])=[O:16]>>[CH3:1][N:2]1[CH2:3][CH2:4][CH:5]([O:6][c:7]2[cH:8][cH:9][c:10]([F:11])[cH:12][c:13]2[C:14]([NH2:15])=[O:16])[CH2:17]1
CN1CCC(OS(C)(=O)=O)C1.NC(=O)c1cc(F)ccc1O
CN1CCC(Oc2ccc(F)cc2C(N)=O)C1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
OtherReaction
4cd4e2ef4402daea1a0b7965dafdb4b00359862c567c9e06b889c2e49b6abe2e
b300ae9ac00448343b04f8595ac10c40ddc175401f75ad1a9cb423839305bb59
c1ccc(OC2CCNC2)cc1
C-S(=O)(=O)-O-[CH;D3;+0:1]1-[C:2]-[#7:3](-[C;D1;H3:4])-[C:5]-[C:6]-1.[N;D1;H2:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11](-[OH;D1;+0:12]):[c:13]>>[C;D1;H3:4]-[#7:3]1-[C:2]-[CH;D3;+0:1](-[O;H0;D2;+0:12]-[c:11](:[c:13]):[c:10]-[C:8](-[N;D1;H2:7])=[O;D1;H0:9])-[C:6]-[C:5]-1
42
[{"value": 42.0, "product": "FC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
60
CELSIUS
null
null
To a suspension of 0.44 g (60% in oil, 0.011 mole) of sodium hydride in 10 ml of dimethylformamide was added 1.55 g (0.01 mole) of 5-fluoro-2-hydroxybenzamide in 10 ml of dimethylformamide under nitrogen atmosphere at room temperature. The reaction mixture was heated to 60° C. and 1.80 g (0.01 mole) of 1-methyl-3-pyrro...
10.6084/m9.figshare.5104873.v1
null
Mesylate.Aromatic alcohol
Ether
C1CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1
MsOH.HO-
CN(C=O)C
60
null
CN1CCC(OS(C)(=O)=O)C1.NC(=O)c1cc(F)ccc1O>CN(C=O)C>CN1CCC(Oc2ccc(F)cc2C(N)=O)C1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-435668a26a354206868b7fe31bf80b92
CN1CCC(Oc2ccccc2C(N)=O)C1.Cl>>CN1CC(CCCl)Oc2ccccc2C1=O
Cl.[OH-].[Na+].CN1CC(CC1)OC1=C(C(=O)N)C=CC=C1>>ClCCC1OC2=C(C(N(C1)C)=O)C=CC=C2
N[C:15]([c:14]1[c:9]([O:8][CH:4]2[CH2:3][N:2]([CH3:1])[CH2:6][CH2:5]2)[cH:10][cH:11][cH:12][cH:13]1)=[O:16].[ClH:7]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16]
CN1CCC(Oc2ccccc2C(N)=O)C1.Cl
CN1CC(CCCl)Oc2ccccc2C1=O
null
null
O
Acylation
OtherReaction
cb864e5df478d892e502caba9af2a6ef1f73e19f716eb33c67df2d58a7f12def
92f5a12174e525b54b2c2f8873e5699366007dab21a88f20092a23357fd3b663
O=C1NCCOc2ccccc21
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-1.[ClH;D0;+0:12]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-[Cl;H0;D1;+0:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
To 54 g (1.35 mole) of sodium hydroxide in 800 ml of water was added 148 g (0.67 mole) of 2-[(1-methyl-3-pyrrolidinyl)oxy]benzamide and the mixture brought to reflux for 18 hr. The pH was adjusted to 7 with hydrochloric acid and the solution filtered and concentrated. The residue was boiled with 400 ml of isopropanol a...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
O
null
null
CN1CCC(Oc2ccccc2C(N)=O)C1.Cl>O>CN1CC(CCCl)Oc2ccccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-cff393a1d9df4371b88ee0b282584eb9
O=C(O)c1ccccc1OC1CCN(Cc2ccccc2)C1.O=S(Cl)Cl>>O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1
C(C1=CC=CC=C1)N1CC(CC1)OC1=C(C(=O)O)C=CC=C1.S(=O)(Cl)Cl.C(C)N(CC)CC>>C(C1=CC=CC=C1)N1CC(OC2=C(C1=O)C=CC=C2)CCCl
O[C:2](=[O:1])[c:3]1[cH:4][cH:5][cH:6][cH:7][c:8]1[O:9][CH:10]1[CH2:11][CH2:12][N:15]([CH2:16][c:17]2[cH:18][cH:19][cH:20][cH:21][cH:22]2)[CH2:14]1.O=S(Cl)[Cl:13]>>[O:1]=[C:2]1[c:3]2[cH:4][cH:5][cH:6][cH:7][c:8]2[O:9][CH:10]([CH2:11][CH2:12][Cl:13])[CH2:14][N:15]1[CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1
O=C(O)c1ccccc1OC1CCN(Cc2ccccc2)C1.O=S(Cl)Cl
O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1
null
null
null
Acylation
OtherReaction
04ab18d7b86ac41d547f1a7cc24bd254cd42e07805bd192d850a732fbf8e3594
480e1213f0b6ae6e64eb6b56f0bbf3a6616fa40d8d7548a0768841fd453e5729
O=C1c2ccccc2OCCN1Cc1ccccc1
Cl-S(=O)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[c:7]-[C:8]-[N;H0;D3;+0:9]1-[C:10]-[C:11]-[C:12]-[CH2;D2;+0:13]-1>>[Cl;H0;D1;+0:1]-[CH2;D2;+0:13]-[C:12]-[C:11]-[C:10]-[N;H0;D3;+0:9](-[C:8]-[c:7])-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
15
MINUTE
To 85.7 g (0.29 mole) of 2-[(1-benzyl-3-pyrrolidinyl)oxy]-benzoic acid was added 150 ml of thionyl chloride. The solution stood for 15 min and was then refluxed 30 min. and concentrated in vacuo. The residue was twice treated with 250 ml of chloroform and concentrated in vacuo. The residue was dissolved in 500 ml of ch...
10.6084/m9.figshare.5104873.v1
null
Carboxylic acid.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2.c1ccccc1
HCl
null
null
0.25
O=C(O)c1ccccc1OC1CCN(Cc2ccccc2)C1.O=S(Cl)Cl>>O=C1c2ccccc2OC(CCCl)CN1Cc1ccccc1
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c645a85016454f99b612218797b734fd
CN1CCC(Oc2ncccc2C(=O)[O-])C1.ClC(Cl)(Cl)Cl>>CN1CC(CCCl)Oc2ncccc2C1=O
Cl.CN1CC(CC1)OC1=NC=CC=C1C(=O)[O-].[Na+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl>>Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2
[O-][C:15]([c:14]1[c:9]([O:8][CH:4]2[CH2:3][N:2]([CH3:1])[CH2:6][CH2:5]2)[n:10][cH:11][cH:12][cH:13]1)=[O:16].ClC(Cl)(Cl)[Cl:7]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16]
CN1CCC(Oc2ncccc2C(=O)[O-])C1.ClC(Cl)(Cl)Cl
CN1CC(CCCl)Oc2ncccc2C1=O
null
null
C(Cl)(Cl)Cl.C(C)O
Acylation
OtherReaction
34de71827526778a78cc572135af6e5ce66bf4e9ffb544c5773eef67e62f48d3
5929549c823e536f9598bef60fbc0516c2bebaf6b6c4ab82e5ffc04c678caaab
O=C1NCCOc2ncccc21
Cl-C(-Cl)(-Cl)-[Cl;H0;D1;+0:1].[C;D1;H3:2]-[N;H0;D3;+0:3]1-[C:4]-[C:5](-[#8:6]-[c:7](:[#7;a:8]:[c:9]):[c:10](-[C;H0;D3;+0:11](-[O-])=[O;D1;H0:12]):[c:13])-[C:14]-[CH2;D2;+0:15]-1>>[C;D1;H3:2]-[N;H0;D3;+0:3]1-[C:4]-[C:5](-[C:14]-[CH2;D2;+0:15]-[Cl;H0;D1;+0:1])-[#8:6]-[c:7](:[#7;a:8]:[c:9]):[c:10](:[c:13])-[C;H0;D3;+0:11...
null
[]
null
null
null
null
Hydrogen chloride gas was bubbled into a suspension of 150 g (0.61 mole) of sodium 2-[(1-methyl-3-pyrrolidinyl)oxy]-3-pyridinecarboxylate in 1 liter of chloroform until a pH of 6 was reached. To the stirred mixture was added 350 g (1.34 mole) of triphenylphosphine and 350 g (2.3 mole) of carbon tetrachloride and the re...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Trichloro group.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
Other
C(Cl)(Cl)Cl.C(C)O
null
null
CN1CCC(Oc2ncccc2C(=O)[O-])C1.ClC(Cl)(Cl)Cl>C(Cl)(Cl)Cl.C(C)O>CN1CC(CCCl)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-c053b5e3777d41259742c324f8181dc6
CN1CCC(Oc2cc(Cl)ccc2C(N)=O)C1.Cl>>CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O
S(=O)(Cl)Cl.Cl.[OH-].[Na+].ClC1=CC(=C(C(=O)N)C=C1)OC1CN(CC1)C>>ClC1=CC2=C(C(N(CC(O2)CCCl)C)=O)C=C1
N[C:16]([c:15]1[c:9]([O:8][CH:4]2[CH2:3][N:2]([CH3:1])[CH2:6][CH2:5]2)[cH:10][c:11]([Cl:12])[cH:13][cH:14]1)=[O:17].[ClH:7]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]([Cl:12])[cH:13][cH:14][c:15]2[C:16]1=[O:17]
CN1CCC(Oc2cc(Cl)ccc2C(N)=O)C1.Cl
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O
null
null
O.C(C)(=O)OCC
Acylation
OtherReaction
cb864e5df478d892e502caba9af2a6ef1f73e19f716eb33c67df2d58a7f12def
92f5a12174e525b54b2c2f8873e5699366007dab21a88f20092a23357fd3b663
O=C1NCCOc2ccccc21
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-1.[ClH;D0;+0:12]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-[Cl;H0;D1;+0:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
59
[{"value": 59.0, "product": "ClC1=CC2=C(C(N(CC(O2)CCCl)C)=O)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 58.9, "product": "ClC1=CC2=C(C(N(CC(O2)CCCl)C)=O)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 10.4 g (0.26 mole) of sodium hydroxide in 150 ml of water was added 32 g (0.13 mole) of 4-chloro-2-[(1-methyl-3-pyrrolidinyl)oxy]benzamide and the mixture was heated at reflux for 24 hr. The reaction mixture was adjusted to pH 6 with concentrated hydrochloric acid and filtered and the filtrate concentr...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
O.C(C)(=O)OCC
null
null
CN1CCC(Oc2cc(Cl)ccc2C(N)=O)C1.Cl>O.C(C)(=O)OCC>CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-df7988810032401cab96c5b96767b633
CN1CCC(Oc2ccc(Br)cc2C(N)=O)C1.Cl>>CN1CC(CCCl)Oc2ccc(Br)cc2C1=O
S(=O)(Cl)Cl.[OH-].[Na+].BrC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C.C(C)N(CC)CC.Cl>>BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=O)C1
N[C:16]([c:15]1[c:9]([O:8][CH:4]2[CH2:3][N:2]([CH3:1])[CH2:6][CH2:5]2)[cH:10][cH:11][c:12]([Br:13])[cH:14]1)=[O:17].[ClH:7]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][c:15]2[C:16]1=[O:17]
CN1CCC(Oc2ccc(Br)cc2C(N)=O)C1.Cl
CN1CC(CCCl)Oc2ccc(Br)cc2C1=O
null
null
O
Acylation
OtherReaction
cb864e5df478d892e502caba9af2a6ef1f73e19f716eb33c67df2d58a7f12def
92f5a12174e525b54b2c2f8873e5699366007dab21a88f20092a23357fd3b663
O=C1NCCOc2ccccc21
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-1.[ClH;D0;+0:12]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-[Cl;H0;D1;+0:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
60.2
[{"value": 60.0, "product": "BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=O)C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 60.2, "product": "BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=O)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
15
CELSIUS
1
HOUR
To a solution of 9.6 g (0.24 mole) of sodium hydroxide in 200 ml of water was added 37 g (0.12 mole) of 5-bromo-2-[(1-methyl-3-pyrrolidinyl)oxy]-benzamide and the mixture was heated at reflux for 18 hr. The pH of the mixture was adjusted to 6.7 with concentrated hydrochloric acid solution. The solution was concentrated...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
O
15
1
CN1CCC(Oc2ccc(Br)cc2C(N)=O)C1.Cl>O>CN1CC(CCCl)Oc2ccc(Br)cc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2aa2b529cc9e41ec87acb8746e1f89c9
COc1ccc(OC2CCN(C)C2)c(C(N)=O)c1.Cl>>COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2
[OH-].[Na+].COC=1C=CC(=C(C(=O)N)C1)OC1CN(CC1)C.C(C)N(CC)CC.Cl.S(=O)(Cl)Cl.Cl.[OH-].[Na+]>>ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)OC
N[C:9]([c:7]1[c:6]([O:18][CH:14]2[CH2:13][N:11]([CH3:12])[CH2:16][CH2:15]2)[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8]1)=[O:10].[ClH:17]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9](=[O:10])[N:11]([CH3:12])[CH2:13][CH:14]([CH2:15][CH2:16][Cl:17])[O:18]2
COc1ccc(OC2CCN(C)C2)c(C(N)=O)c1.Cl
COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2
null
null
O
Acylation
OtherReaction
cb864e5df478d892e502caba9af2a6ef1f73e19f716eb33c67df2d58a7f12def
92f5a12174e525b54b2c2f8873e5699366007dab21a88f20092a23357fd3b663
O=C1NCCOc2ccccc21
N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[C;D1;H3:6]-[N;H0;D3;+0:7]1-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-1.[ClH;D0;+0:12]>>[C;D1;H3:6]-[N;H0;D3;+0:7](-[C:8]-[C:9]-[C:10]-[CH2;D2;+0:11]-[Cl;H0;D1;+0:12])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
23.2
[{"value": 23.0, "product": "ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 23.2, "product": "ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 19.2 g (0.48 mole) of sodium hydroxide in 500 ml of water was added 60 g (0.24 mole) of 5-methoxy-2-[(1-methyl-3-pyrrolidinyl)oxy]-benzamide and the mixture was heated at reflux for 24 hr. The reaction mixture was cooled and the pH adjusted to 6.8 with concentrated hydrochloric acid. The mixture was co...
10.6084/m9.figshare.5104873.v1
null
Primary amide.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
O
null
1
COc1ccc(OC2CCN(C)C2)c(C(N)=O)c1.Cl>O>COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8b003d3c47b34351abfb5f38c61627e5
CN1CC(CCCl)Oc2ccccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ccccc2C1=S
P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+].ClCCC1OC2=C(C(N(C1)C)=O)C=CC=C2>>ClCCC1OC2=C(C(N(C1)C)=S)C=CC=C2
O=[C:15]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:16])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[S:16]
CN1CC(CCCl)Oc2ccccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ccccc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
null
[]
null
null
null
null
A mixture of 18.5 g (0.0834 mole) of phosphorus pentasulfide and 18.5 g potassium sulfide was ground together and added to a solution of 100 g (0.417 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepin-5(4H)-one in dry toluene, the mixture refluxed 24 hr. and filtered. The filtrate was concentrated and par...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2ccccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-6e0e6792bd184b57bc64b7b90119b242
CN1CC(CCCl)Oc2ncccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ncccc2C1=S
Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClCCC1OC2=C(C(N(C1)C)=S)C=CC=N2
O=[C:15]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:16])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[S:16]
CN1CC(CCCl)Oc2ncccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ncccc2C1=S
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
816a6edebc5f63ded7e13b08c00c5ed3d008d78e0a633be008bee89d24cf2686
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ncccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7](:[#7;a:8]:[c:9])-[#8:10].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:11])(-S-2)-S-3>>[#8:10]-[c:7](:[#7;a:8]:[c:9]):[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:11])-[#7:2](-[C;D1;H3:3])-[C:4]
null
[]
null
null
null
null
To a solution of 59 g (0.25 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]oxazepin-5(4H)one hydrochloride in 1500 ml of chloroform was added 41.5 g (0.19 mole) of phosphorus pentasulfide and the mixture was heated to reflux for 18 hr. The mixture was filtered and the filtrate was extracted with dilut...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1cnc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
Other
C(Cl)(Cl)Cl
null
null
CN1CC(CCCl)Oc2ncccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C(Cl)(Cl)Cl>CN1CC(CCCl)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-b8c658f123854d16ae3bbcb4846c2600
CN1CC(CCCl)Oc2cc3ccccc3cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2cc3ccccc3cc2C1=S
ClCCC1OC2=C(C(N(C1)C)=O)C=C1C=CC=CC1=C2.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+]>>ClCCC1OC2=C(C(N(C1)C)=S)C=C1C=CC=CC1=C2
O=[C:19]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[cH:17][c:18]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:20])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[cH:17][c:18]2[C:19]1=[S:20]
CN1CC(CCCl)Oc2cc3ccccc3cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2cc3ccccc3cc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
1eb83fcd5217da399ee5559afc76959b0a672b869d20760af7ca5ba8a49566a7
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2cc3ccccc3cc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
null
[]
null
null
null
null
To a solution of 16.6 g (0.06 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylnaphth[2,3-f][1,4]oxazepin-5(4H)-one in 150 ml of dry toluene was added a mixture of 8.6 g (0.045 mole) of phosphorus pentasulfide and 8.6 g of potassium sulfide which had been ground together. The reaction mixture was stirred and heated at re...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2cc3c(cc2c1)C[NH]CCO3.S1P2SP3SP1SP(S2)S3
c1ccc2cc3c(cc2c1)C[NH]CCO3
c1ccc2cc3c(cc2c1)C[NH]CCO3
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2cc3ccccc3cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2cc3ccccc3cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-88fc48739333487995ac8ade2e3f01a2
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S
ClC1=CC2=C(C(N(CC(O2)CCCl)C)=O)C=C1.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+]>>ClC1=CC2=C(C(N(CC(O2)CCCl)C)=S)C=C1
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]([Cl:12])[cH:13][cH:14][c:15]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:17])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]([Cl:12])[cH:13][cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
73.2
[{"value": 55.0, "product": "ClC1=CC2=C(C(N(CC(O2)CCCl)C)=S)C=C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 73.2, "product": "ClC1=CC2=C(C(N(CC(O2)CCCl)C)=S)C=C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 43 g (0.16 mole) of 8-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepin-5(4H)-one in 400 ml of dry toluene was added a mixture of 23 g (0.12 mole) of phosphorus pentasulfide and 23 g of potassium sulfide which had been ground together. The reaction mixture was stirred and heated at reflux ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2cc(Cl)ccc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2cc(Cl)ccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-bf2c4a25c1be4e5398f1ee32fffc150d
CN1CC(CCCl)Oc2ccc(Br)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ccc(Br)cc2C1=S
BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=O)C1.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+]>>BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][c:15]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:17])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([Br:13])[cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCCl)Oc2ccc(Br)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ccc(Br)cc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
72.6
[{"value": 72.0, "product": "BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 72.6, "product": "BrC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 11.0 g (0.035 mole) of 7-bromo-2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepin-5(4H)-one in 150 ml of dry toluene was added a mixture of 13.4 g (0.07 mole) of phosphorus pentasulfide and 13.4 g of potassium sulfide which had been ground together. The reaction mixture was heated at reflux for 5 ...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2ccc(Br)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccc(Br)cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-dbc1d0fc06cc4d08ac04f8d8f4685b9b
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S
P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+].ClCCC1OC2=C(C(N(C1)C)=O)C=CC1=CC=CC=C12>>ClCCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12
O=[C:19]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[c:10]1[cH:11][cH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][c:18]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:20])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[c:10]([cH:11][cH:12][c:13]3[cH:14][cH:15][cH:16][cH:17][c:18]23)[C:19]1=[S:20]
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
4f9bdc2466921bc2076c80e5ea2471371d474d3969b50466e61ceafbbbe1642d
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2c1ccc1ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
84.1
[{"value": 84.0, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12", "details": "PERCENTYIELD", "is_desired": false}, {"value": 84.1, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=CC1=CC=CC=C12", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A mixture of 9.55 g of phosphorus pentasulfide and 9.5 g of potassium sulfide were ground together and added to a solution of 20.2 g (0.07 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylnaphth[2,1-f][1,4]oxazepin-5(4H)-one in 200 ml of dry toluene. The mixture was stirred and heated at reflux for 7 hr. The hot reaction...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c3c(ccc2c1)C[NH]CCO3.S1P2SP3SP1SP(S2)S3
c1ccc2c3c(ccc2c1)C[NH]CCO3
c1ccc2c3c(ccc2c1)C[NH]CCO3
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2c(ccc3ccccc23)C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-8c189722a6464305b05c5f2ecbd00eea
CN1CC(CCCl)Oc2ccc(Cl)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2ccc(Cl)cc2C1=S
ClC=1C=CC2=C(C(N(CC(O2)CCCl)C)=O)C1.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+]>>ClC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:17])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][c:12]([Cl:13])[cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCCl)Oc2ccc(Cl)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2ccc(Cl)cc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
86.1
[{"value": 68.0, "product": "ClC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.1, "product": "ClC=1C=CC2=C(C(N(CC(O2)CCCl)C)=S)C1", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 20 g (0.07 mole) of 7-chloro-2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-benzoxazepin-5(4H)-one in 200 ml of toluene was added a mixture of 9.55 g (0.05 mole) of phosphorus pentasulfide and 9.5 g of potassium sulfide which had been ground together. The reaction mixture was filtered and the filtrate conc...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2ccc(Cl)cc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccc(Cl)cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-ffbaf1c2ea5949e094d1b0c62e55de55
COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>COc1ccc2c(c1)C(=S)N(C)CC(CCCl)O2
ClCCC1OC2=C(C(N(C1)C)=O)C=C(C=C2)OC.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3.[S-2].[K+].[K+]>>ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)OC
O=[C:9]1[c:7]2[c:6]([cH:5][cH:4][c:3]([O:2][CH3:1])[cH:8]2)[O:18][CH:14]([CH2:15][CH2:16][Cl:17])[CH2:13][N:11]1[CH3:12].S=P12SP3(=S)SP(=S)(S1)SP(=[S:10])(S2)S3>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[c:7]([cH:8]1)[C:9](=[S:10])[N:11]([CH3:12])[CH2:13][CH:14]([CH2:15][CH2:16][Cl:17])[O:18]2
COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
COc1ccc2c(c1)C(=S)N(C)CC(CCCl)O2
null
null
C(Cl)(Cl)Cl
Heteroatom Alkylation and Arylation
OtherReaction
43ac2affde81267970c96bfb182f28e85d876733ab6e6103821469d8ecc8ebf9
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2ccccc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[c:6]):[c:7]-[#8:8].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:9])(-S-2)-S-3>>[#8:8]-[c:7]:[c:5](:[c:6])-[C;H0;D3;+0:1](=[S;H0;D1;+0:9])-[#7:2](-[C;D1;H3:3])-[C:4]
86.3
[{"value": 65.0, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.3, "product": "ClCCC1OC2=C(C(N(C1)C)=S)C=C(C=C2)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a solution of 10.3 g (0.04 mole) of 2-(2-chloroethyl)-2,3-dihydro-7-methoxy-4-methyl-1,4-benzoxazepin-5(4H)-one in 200 ml of chloroform was added a mixture of 5.7 g (0.03 mole) of phosphorus pentasulfide and 5.7 g of potassium sulfide which had been ground together. The reaction mixture was stirred and heated at ref...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2c(c1)C[NH]CCO2.S1P2SP3SP1SP(S2)S3
c1ccc2c(c1)C[NH]CCO2
c1ccc2c(c1)C[NH]CCO2
Other
C(Cl)(Cl)Cl
null
null
COc1ccc2c(c1)C(=O)N(C)CC(CCCl)O2.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C(Cl)(Cl)Cl>COc1ccc2c(c1)C(=S)N(C)CC(CCCl)O2
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-3255470380604e3ea543506a53fd60a0
CN1CCC(Sc2ncccc2C(=O)O)C1.ClC(Cl)Cl>>CN1CC(CCCl)Sc2ncccc2C1=O
CN1CC(CC1)SC1=NC=CC=C1C(=O)O.C(Cl)(Cl)Cl.C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1>>ClCCC1SC2=C(C(N(C1)C)=O)C=CC=N2
O[C:15]([c:14]1[c:9]([S:8][CH:4]2[CH2:3][N:2]([CH3:1])[CH2:6][CH2:5]2)[n:10][cH:11][cH:12][cH:13]1)=[O:16].ClC(Cl)[Cl:7]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[S:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[O:16]
CN1CCC(Sc2ncccc2C(=O)O)C1.ClC(Cl)Cl
CN1CC(CCCl)Sc2ncccc2C1=O
null
null
C(Cl)(Cl)(Cl)Cl
Acylation
OtherReaction
b95719b87574728c235c5497a52281e1c88156104d975f0a6e21c1cff9b129f8
b49eb23b5b6ae322cfab26d1040968fb1a3018654a4d628d6b2e1582e31b01dc
O=C1NCCSc2ncccc21
Cl-C(-Cl)-[Cl;H0;D1;+0:1].O-[C;H0;D3;+0:2](=[O;D1;H0:3])-[c:4](:[c:5]):[c:6](-[#16:7]-[C:8]1-[C:9]-[N;H0;D3;+0:10](-[C;D1;H3:11])-[CH2;D2;+0:12]-[C:13]-1):[#7;a:14]:[c:15]>>[C;D1;H3:11]-[N;H0;D3;+0:10]1-[C:9]-[C:8](-[C:13]-[CH2;D2;+0:12]-[Cl;H0;D1;+0:1])-[#16:7]-[c:6](:[#7;a:14]:[c:15]):[c:4](:[c:5])-[C;H0;D3;+0:2]-1=[...
null
[]
null
null
null
null
A mixture of 80.75 g (0.34 mole) of 2-[(1-methyl-3-pyrrolidinyl)thio]-3-pyridinecarboxylic acid, 500 ml of chloroform, 200 g of carbon tetrachloride and 178 g (0.68 mole) of triphenylphosphine was stirred at reflux for 2.5 hr. The resulting solution was extracted with one 500 ml and three 125 ml portions of 1N hydrochl...
10.6084/m9.figshare.5104873.v1
null
Secondary halide.Secondary halide.Secondary halide.Carboxylic acid.Tertiary amine
Primary halide.Tertiary amide
C1CC[NH]C1
c1cnc2c(c1)C[NH]CCS2
c1cnc2c(c1)C[NH]CCS2
HCl
C(Cl)(Cl)(Cl)Cl
null
null
CN1CCC(Sc2ncccc2C(=O)O)C1.ClC(Cl)Cl>C(Cl)(Cl)(Cl)Cl>CN1CC(CCCl)Sc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2835159553ab4fcdb331894bd71cc090
CN1CC(CCCl)Sc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>>CN1CC(CCCl)Sc2ncccc2C1=S
ClCCC1SC2=C(C(N(C1)C)=O)C=CC=N2.COC1=CC=C(C=C1)P1(SP(S1)(C1=CC=C(C=C1)OC)=S)=S>>ClCCC1SC2=C(C(N(C1)C)=S)C=CC=N2
O=[C:15]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[S:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]21.COc1ccc(P2(=S)SP(c3ccc(OC)cc3)(=[S:16])S2)cc1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[S:8][c:9]2[n:10][cH:11][cH:12][cH:13][c:14]2[C:15]1=[S:16]
CN1CC(CCCl)Sc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1
CN1CC(CCCl)Sc2ncccc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
a9e26ac969be1f2f1da5297fa4500a483fb9a743fb354b404df74b4cf1e3597f
6bfe9cf75b76e7dc07d0e23f56b0121cbe043c2e701d72c5be7acc1ccd1adcd8
S=C1NCCSc2ncccc21
C-O-c1:c:c:c(-P2(=S)-S-P(=[S;H0;D1;+0:1])(-c3:c:c:c(-O-C):c:c:3)-S-2):c:c:1.O=[C;H0;D3;+0:2](-[#7:3](-[C;D1;H3:4])-[C:5])-[c:6](:[c:7]):[c:8](:[#7;a:9]:[c:10])-[#16:11]>>[#16:11]-[c:8](:[#7;a:9]:[c:10]):[c:6](:[c:7])-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[#7:3](-[C;D1;H3:4])-[C:5]
null
[]
null
null
null
null
A mixture of 4.3 g (0.017 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]thiazepin-5(4H)-one, 100 ml of toluene and 4.8 g (0.012 mole) of 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane-2,4-disulfide was refluxed for 3 hr and then extracted twice with dilute sodium hydroxide. The organic layer wa...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Monosulfide.Monosulfide
Thioamide
c1cnc2c(c1)C[NH]CCS2.c1ccccc1.P1SPS1.c1ccccc1
c1cnc2c(c1)C[NH]CCS2
c1cnc2c(c1)C[NH]CCS2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Sc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>C1(=CC=CC=C1)C>CN1CC(CCCl)Sc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-2f0a54101bda4c5984ec97659afe8d34
CN1CC(CCCl)Oc2ccncc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>>CN1CC(CCCl)Oc2ccncc2C1=S.Cl
ClCCC1OC2=C(C(N(C1)C)=O)C=NC=C2.COC1=CC=C(C=C1)P2(=S)SP(=S)(S2)C3=CC=C(C=C3)OC>>Cl.ClCCC1OC2=C(C(N(C1)C)=S)C=NC=C2
O=[C:15]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][n:12][cH:13][c:14]21.COc1ccc(P2(=S)SP(c3ccc(OC)cc3)(=[S:16])S2)cc1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][cH:11][n:12][cH:13][c:14]2[C:15]1=[S:16].[ClH:17]
CN1CC(CCCl)Oc2ccncc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1
CN1CC(CCCl)Oc2ccncc2C1=S.Cl
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
04ec00afe311ae1bac323818e55a61a601447b5418e04284e19e06cf3a0fa74b
6bfe9cf75b76e7dc07d0e23f56b0121cbe043c2e701d72c5be7acc1ccd1adcd8
S=C1NCCOc2ccncc21
C-O-c1:c:c:c(-P2(=S)-S-P(=[S;H0;D1;+0:1])(-c3:c:c:c(-O-C):c:c:3)-S-2):c:c:1.O=[C;H0;D3;+0:2](-[#7:3](-[C;D1;H3:4])-[C:5])-[c:6](:[c:7]:[#7;a:8]:[c:9]):[c:10]-[#8:11]>>[#8:11]-[c:10]:[c:6](:[c:7]:[#7;a:8]:[c:9])-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[#7:3](-[C;D1;H3:4])-[C:5]
null
[]
null
null
null
null
2-(2-Chloroethyl)-2,3-dihydro-4-methylpyrido[3,4-f][1,4]oxazepin-5(4H)-one, 15 g (0.06 mole), was dissolved in 200 ml of dry toluene and 15 g (0.037 mole) of [2,4-bis (4-methoxyphenyl)-1,3,2,4-dithiaphosphetane-2,4-disulfide was added. The mixture was refluxed for 2.5 hr and the toluene solution decanted. The residue w...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Monosulfide.Monosulfide
Thioamide
c1cc2c(cn1)C[NH]CCO2.c1ccccc1.P1SPS1.c1ccccc1
c1cc2c(cn1)C[NH]CCO2
c1cc2c(cn1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2ccncc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ccncc2C1=S.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-11860a3dcb584788ab48608c74e8cc2e
CN1CC(CCCl)Oc2ncccc2C1=O.Cl>>CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O
Cl.ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.S(=O)(=O)(Cl)Cl>>ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O
[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][cH:12][cH:14][c:15]2[C:16]1=[O:17].[ClH:13]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][c:12]([Cl:13])[cH:14][c:15]2[C:16]1=[O:17]
CN1CC(CCCl)Oc2ncccc2C1=O.Cl
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O
null
null
CN(C=O)C
Functional Group Addition
Chlorination
ad372abf1019cea33b6a7dcea0ff6c8338a6fd5f614d94a79ff142e83977e890
0a2f22058f27970cef4a98a778644dbe9c44e91f66c74cd24db321993177608a
O=C1NCCOc2ncccc21
[#7:1]-[C:2](=[O;D1;H0:3])-[c:4]1:[c:5]:[cH;D2;+0:6]:[c:7]:[#7;a:8]:[c:9]:1-[#8:10].[ClH;D0;+0:11]>>[#7:1]-[C:2](=[O;D1;H0:3])-[c:4]1:[c:5]:[c;H0;D3;+0:6](-[Cl;H0;D1;+0:11]):[c:7]:[#7;a:8]:[c:9]:1-[#8:10]
6.4
[{"value": 6.4, "product": "ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A sample of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f][1,4]-oxazepin-5-(4H)-one hydrochloride (10 g, 136 mole) was dissolved in dimethylformamide (150 ml) and heated to reflux. Sulfuryl chloride (20 g, 0.148 mole) was then added dropwise over a period of 40-50 minutes. The reaction was allowed to stir at reflu...
10.6084/m9.figshare.5104873.v1
null
null
Aromatic halide
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
null
CN(C=O)C
null
null
CN1CC(CCCl)Oc2ncccc2C1=O.Cl>CN(C=O)C>CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-d509aa5423c6487cbbe6785e60b235b3
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>>CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S
ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=O.COC1=CC=C(C=C1)P1(SP(S1)(C1=CC=C(C=C1)OC)=S)=S>>ClC1=CC=2C(N(CC(OC2N=C1)CCCl)C)=S
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][c:12]([Cl:13])[cH:14][c:15]21.COc1ccc(P2(=S)SP(c3ccc(OC)cc3)(=[S:17])S2)cc1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[n:10][cH:11][c:12]([Cl:13])[cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
0a918a3e4aff4213dc84ed5746fe3e4f2528e6cf920242bc5ada6cfd1a73c2d5
6bfe9cf75b76e7dc07d0e23f56b0121cbe043c2e701d72c5be7acc1ccd1adcd8
S=C1NCCOc2ncccc21
C-O-c1:c:c:c(-P2(=S)-S-P(=[S;H0;D1;+0:1])(-c3:c:c:c(-O-C):c:c:3)-S-2):c:c:1.O=[C;H0;D3;+0:2](-[#7:3](-[C;D1;H3:4])-[C:5])-[c:6](:[c:7]):[c:8](:[#7;a:9]:[c:10])-[#8:11]>>[#8:11]-[c:8](:[#7;a:9]:[c:10]):[c:6](:[c:7])-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[#7:3](-[C;D1;H3:4])-[C:5]
null
[]
null
null
2
HOUR
7-Chloro-2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido [3,2-f][1,4]oxazepin-5(4H)-one, 6.0 g (0.022 mole) was suspended in 200 ml of toluene. To this suspension was added 2,4-bis(4-methoxyphenyl)-1,3-dithia-2,4-diphosphetane-2,4-dilsulfide. The mixture was heated to reflux with vigorous stirring for 2 hours. Because the...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Monosulfide.Monosulfide
Thioamide
c1cnc2c(c1)C[NH]CCO2.c1ccccc1.P1SPS1.c1ccccc1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
2
CN1CC(CCCl)Oc2ncc(Cl)cc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2ncc(Cl)cc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-29596a0f7ab14275afad8e96b1c3628f
CN1CC(CCCl)Oc2ncccc2C1=O.O=C1NC(=O)c2ccccc21>>CN1CC(CCN2C(=O)c3ccccc3C2=O)Oc2ncccc2C1=O
ClCCC1OC2=C(C(N(C1)C)=O)C=CC=N2.C1(C=2C(C(N1)=O)=CC=CC2)=O.[K]>>O=C1N(C(C2=CC=CC=C12)=O)CCC1OC2=C(C(N(C1)C)=O)C=CC=N2
Cl[CH2:6][CH2:5][CH:4]1[CH2:3][N:2]([CH3:1])[C:25](=[O:26])[c:24]2[c:19]([n:20][cH:21][cH:22][cH:23]2)[O:18]1.[NH:7]1[C:8](=[O:9])[c:10]2[cH:11][cH:12][cH:13][cH:14][c:15]2[C:16]1=[O:17]>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][N:7]2[C:8](=[O:9])[c:10]3[cH:11][cH:12][cH:13][cH:14][c:15]3[C:16]2=[O:17])[O:18][c:19]2[n...
CN1CC(CCCl)Oc2ncccc2C1=O.O=C1NC(=O)c2ccccc21
CN1CC(CCN2C(=O)c3ccccc3C2=O)Oc2ncccc2C1=O
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
2022cc53c1563230994721760c16c873bbdd2982bbfbeeef5b40885f32de1173
ed5b40ca5c14bda1cdc43d7e7526ae39e9e787b52b58ca2afd56239c19d62539
O=C1NCC(CCN2C(=O)c3ccccc3C2=O)Oc2ncccc21
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[#8:4].[O;D1;H0:5]=[C:6]1-[NH;D2;+0:7]-[C:8](=[O;D1;H0:9])-[c:10]:[c:11]-1>>[#8:4]-[C:3]-[C:2]-[CH2;D2;+0:1]-[N;H0;D3;+0:7]1-[C:6](=[O;D1;H0:5])-[c:11]:[c:10]-[C:8]-1=[O;D1;H0:9]
37
[{"value": 36.0, "product": "O=C1N(C(C2=CC=CC=C12)=O)CCC1OC2=C(C(N(C1)C)=O)C=CC=N2", "details": "PERCENTYIELD", "is_desired": false}, {"value": 37.0, "product": "O=C1N(C(C2=CC=CC=C12)=O)CCC1OC2=C(C(N(C1)C)=O)C=CC=N2", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
100
CELSIUS
5
HOUR
To a solution of 4.92 g (0.02 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methylpyrido[3,2-f]-1,4-oxazepin-5-(4H)one in 35 ml of dimethylformamide was added 7.55 g (0.041 mole) of potassium phthalimide. The mixture was stirred for 5 hr at 100° C. and left standing at room temperature overnight. Dimethylformamide was remov...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Unsubstituted dicarboximide
Substituted dicarboximide
c1ccc2c(c1)CNC2
c1ccc2c(c1)C[NH]C2
c1ccc2c(c1)C[NH]C2.c1cnc2c(c1)C[NH]CCO2
HCl
CN(C=O)C
100
5
CN1CC(CCCl)Oc2ncccc2C1=O.O=C1NC(=O)c2ccccc21>CN(C=O)C>CN1CC(CCN2C(=O)c3ccccc3C2=O)Oc2ncccc2C1=O
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-83c82ca7cc2843bba7adbd8cf14ed2fd
CN1CC(CCC#N)Oc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>>CN1CC(CCC#N)Oc2ncccc2C1=S
COC1=CC=C(C=C1)P1(SP(S1)(C1=CC=C(C=C1)OC)=S)=S.CN1CC(OC2=C(C1=O)C=CC=N2)CCC#N.COC1=CC=C(C=C1)P1(SP(S1)(C1=CC=C(C=C1)OC)=S)=S>>CN1CC(OC2=C(C1=S)C=CC=N2)CCC#N
O=[C:16]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][C:7]#[N:8])[O:9][c:10]2[n:11][cH:12][cH:13][cH:14][c:15]21.COc1ccc(P2(=S)SP(c3ccc(OC)cc3)(=[S:17])S2)cc1>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][C:7]#[N:8])[O:9][c:10]2[n:11][cH:12][cH:13][cH:14][c:15]2[C:16]1=[S:17]
CN1CC(CCC#N)Oc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1
CN1CC(CCC#N)Oc2ncccc2C1=S
null
null
C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
0a918a3e4aff4213dc84ed5746fe3e4f2528e6cf920242bc5ada6cfd1a73c2d5
6bfe9cf75b76e7dc07d0e23f56b0121cbe043c2e701d72c5be7acc1ccd1adcd8
S=C1NCCOc2ncccc21
C-O-c1:c:c:c(-P2(=S)-S-P(=[S;H0;D1;+0:1])(-c3:c:c:c(-O-C):c:c:3)-S-2):c:c:1.O=[C;H0;D3;+0:2](-[#7:3](-[C;D1;H3:4])-[C:5])-[c:6](:[c:7]):[c:8](:[#7;a:9]:[c:10])-[#8:11]>>[#8:11]-[c:8](:[#7;a:9]:[c:10]):[c:6](:[c:7])-[C;H0;D3;+0:2](=[S;H0;D1;+0:1])-[#7:3](-[C;D1;H3:4])-[C:5]
24.9
[{"value": 13.8, "product": "CN1CC(OC2=C(C1=S)C=CC=N2)CCC#N", "details": "PERCENTYIELD", "is_desired": false}, {"value": 24.9, "product": "CN1CC(OC2=C(C1=S)C=CC=N2)CCC#N", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
To a solution of 11.0 g (0.04 mole) of 2,3,4,5-tetrahydro-4-methyl-5-oxopyrido[3,2-f][1,4]-oxazepine-2-propanenitrile in 175 ml toluene was added 10.5 g (0.026 mole) of 2,4-bis(4-methoxyphenyl)-1,3-dithia-2,4-diphosphetane-2,4-disulfide. The reaction mixture was heated to reflux for 2 hr with vigorous mechanical stirri...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Tertiary amide.Monosulfide.Monosulfide
Thioamide
c1cnc2c(c1)C[NH]CCO2.c1ccccc1.P1SPS1.c1ccccc1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
Other
C1(=CC=CC=C1)C
null
1
CN1CC(CCC#N)Oc2ncccc2C1=O.COc1ccc(P2(=S)SP(=S)(c3ccc(OC)cc3)S2)cc1>C1(=CC=CC=C1)C>CN1CC(CCC#N)Oc2ncccc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-697c078422cb40a2878f7893b80f69c2
CN1CCC(C)(O)C1.O=C(O)c1cccnc1Cl>>CN1CC(C)(CCCl)Oc2ncccc2C1=O.Cl
[H-].[Na+].O1CCCC1.CN(C=O)C.ClC1=C(C(=O)O)C=CC=N1.CN1CC(CC1)(O)C>>Cl.ClCCC1(OC2=C(C(N(C1)C)=O)C=CC=N2)C
[CH3:1][N:2]1[CH2:3][C:4]([CH3:5])([OH:9])[CH2:6][CH2:7]1.O[C:16]([c:15]1[c:10]([Cl:8])[n:11][cH:12][cH:13][cH:14]1)=[O:17]>>[CH3:1][N:2]1[CH2:3][C:4]([CH3:5])([CH2:6][CH2:7][Cl:8])[O:9][c:10]2[n:11][cH:12][cH:13][cH:14][c:15]2[C:16]1=[O:17].[ClH:18]
CN1CCC(C)(O)C1.O=C(O)c1cccnc1Cl
CN1CC(C)(CCCl)Oc2ncccc2C1=O.Cl
null
null
null
Acylation
OtherReaction
438615aaa7c67c86d9535b47b3b7b90895cfd938eb5b9a43590840d2835a2eaa
0eb6298bc44bc2b383aa42afc4dbdd5fb5155671f80555f7d307ebee31e1f5c0
O=C1NCCOc2ncccc21
O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c;H0;D3;+0:5](-[Cl;H0;D1;+0:6]):[#7;a:7]:[c:8].[C;D1;H3:9]-[N;H0;D3;+0:10]1-[C:11]-[C:12](-[C;D1;H3:13])(-[OH;D1;+0:14])-[C:15]-[CH2;D2;+0:16]-1>>[C;D1;H3:9]-[N;H0;D3;+0:10]1-[C:11]-[C:12](-[C;D1;H3:13])(-[C:15]-[CH2;D2;+0:16]-[Cl;H0;D1;+0:6])-[O;H0;D2;+0:14]-[c;H0;D3;+0:5]...
10
[{"value": 10.0, "product": "Cl.ClCCC1(OC2=C(C(N(C1)C)=O)C=CC=N2)C", "details": "PERCENTYIELD", "is_desired": false}]
77
CELSIUS
8
HOUR
To a suspension of 60 g (60% in oil, 1.5 mole) of sodium hydride in 400 ml of tetrahydrofuran heated to reflux was added a solution of 110 g (0.70 mole) of 2-chloronicotinic acid and 80 (0.70 mole) of 1,3-dimethyl-3-pyrrolidinol so as to maintain good reflux. Heating at reflux was continued overnight. The mass spectra ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Tertiary alcohol.Tertiary amine
Primary halide.Ether.Tertiary amide
C1CC[NH]C1.c1ccncc1
c1cnc2c(c1)C[NH]CCO2
c1cnc2c(c1)C[NH]CCO2
null
null
77
8
CN1CCC(C)(O)C1.O=C(O)c1cccnc1Cl>>CN1CC(C)(CCCl)Oc2ncccc2C1=O.Cl
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-969df2bb37174a8b86b8541a3ae806a4
CN1CC(CCCl)Oc2cc3ccccc3nc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>CN1CC(CCCl)Oc2cc3ccccc3nc2C1=S
ClCCC1OC=2C(=NC=3C=CC=CC3C2)C(N(C1)C)=O.P12(=S)SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>>ClCCC1OC=2C(=NC=3C=CC=CC3C2)C(N(C1)C)=S
O=[C:19]1[N:2]([CH3:1])[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[n:17][c:18]21.S=P12SP3(=S)SP(=S)(S1)SP(=[S:20])(S2)S3>>[CH3:1][N:2]1[CH2:3][CH:4]([CH2:5][CH2:6][Cl:7])[O:8][c:9]2[cH:10][c:11]3[cH:12][cH:13][cH:14][cH:15][c:16]3[n:17][c:18]2[C:19]1=[S:20]
CN1CC(CCCl)Oc2cc3ccccc3nc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3
CN1CC(CCCl)Oc2cc3ccccc3nc2C1=S
null
null
C(C)#N.C1(=CC=CC=C1)C
Heteroatom Alkylation and Arylation
OtherReaction
e784457bf758d431573169c722031f6d35830e2503345896e0e42caba7d885fd
92373f703706fcd3b2fa077124e423e859506b3bebedf9bbb6de44eb68d5c891
S=C1NCCOc2cc3ccccc3nc21
O=[C;H0;D3;+0:1](-[#7:2](-[C;D1;H3:3])-[C:4])-[c:5](:[#7;a:6]:[c:7]):[c:8]-[#8:9].S=P12-S-P3(=S)-S-P(=S)(-S-1)-S-P(=[S;H0;D1;+0:10])(-S-2)-S-3>>[#8:9]-[c:8]:[c:5](:[#7;a:6]:[c:7])-[C;H0;D3;+0:1](=[S;H0;D1;+0:10])-[#7:2](-[C;D1;H3:3])-[C:4]
86.9
[{"value": 52.0, "product": "ClCCC1OC=2C(=NC=3C=CC=CC3C2)C(N(C1)C)=S", "details": "PERCENTYIELD", "is_desired": false}, {"value": 86.9, "product": "ClCCC1OC=2C(=NC=3C=CC=CC3C2)C(N(C1)C)=S", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To 3.0 g (0.01 mole) of 2-(2-chloroethyl)-2,3-dihydro-4-methyl-1,4-oxazepino[6,7-b]-quinolin-5(4H)-one in 30 ml of acetonitrile was added 1.3 g (0.006 mole) of phosphorus pentasulfide. The mixture was stirred vigorously at reflux for 2 hr. After cooling, the reaction mixture was diluted with 60 ml of toluene and filter...
10.6084/m9.figshare.5104873.v1
null
Tertiary amide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide.Monosulfide
Thioamide
c1ccc2nc3c(cc2c1)OCC[NH]C3.S1P2SP3SP1SP(S2)S3
c1ccc2nc3c(cc2c1)OCC[NH]C3
c1ccc2nc3c(cc2c1)OCC[NH]C3
Other
C(C)#N.C1(=CC=CC=C1)C
null
null
CN1CC(CCCl)Oc2cc3ccccc3nc2C1=O.S=P12SP3(=S)SP(=S)(S1)SP(=S)(S2)S3>C(C)#N.C1(=CC=CC=C1)C>CN1CC(CCCl)Oc2cc3ccccc3nc2C1=S
ord_dataset-01dbb772c5e249108f0b191ed17a2c0c
ord-93749aa381254392b61d61749772cb78
CN1CCC(O)C1.O=C(O)c1c(Cl)cncc1Cl.c1ccc(P(c2ccccc2)c2ccccc2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1>>CN1Cc2c(Cl)cncc2OC(CCCl)C1.O=P(c1ccccc1)(c1ccccc1)c1ccccc1
C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl.[H-].[Na+].C1(=CC=CC=C1)P(C1=CC=CC=C1)C1=CC=CC=C1.C(Cl)(Cl)(Cl)Cl.CN1CC(CC1)O.ClC=1C=NC=C(C1C(=O)O)Cl>>ClC1=CN=CC2=C1CN(CC(O2)CCCl)C.C1(=CC=CC=C1)P(C1=CC=CC=C1)(C1=CC=CC=C1)=O
[CH3:1][N:2]1[CH2:3][CH2:13][CH:12]([OH:11])[CH2:16]1.O[C:14]([c:4]1[c:5]([Cl:6])[cH:7][n:8][cH:9][c:10]1[Cl:15])=[O:17].c1ccc(P(c2ccccc2)[c:25]2[cH:26][cH:27][cH:28][cH:29][cH:30]2)cc1.c1ccc([P:18]([c:19]2[cH:20][cH:21][cH:22][cH:23][cH:24]2)[c:31]2[cH:32][cH:33][cH:34][cH:35][cH:36]2)cc1>>[CH3:1][N:2]1[CH2:3][c:4]2[c...
CN1CCC(O)C1.O=C(O)c1c(Cl)cncc1Cl.c1ccc(P(c2ccccc2)c2ccccc2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1
CN1Cc2c(Cl)cncc2OC(CCCl)C1.O=P(c1ccccc1)(c1ccccc1)c1ccccc1
null
null
CN(C=O)C.C(C)N(CC)CC
Heteroatom Alkylation and Arylation
OtherReaction
aa75494d3c8cc5852672fc746a29df809e506396b90c8c63cd244985800cc08f
d89c6255ff7e0a1f92df0e88d8a75c65b37e0288b3d5758af16f3a275b2ebcab
O=P(c1ccccc1)(c1ccccc1)c1ccccc1.c1cc2c(cn1)OCCNC2
O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[c;H0;D3;+0:3]1:[c:4](-[Cl;D1;H0:5]):[c:6]:[#7;a:7]:[c:8]:[c;H0;D3;+0:9]:1-[Cl;H0;D1;+0:10].[C;D1;H3:11]-[#7:12]1-[C:13]-[C:14](-[OH;D1;+0:15])-[CH2;D2;+0:16]-[CH2;D2;+0:17]-1.[c:18]:[c:19](-[P;H0;D3;+0:20](-[c:21](:[c:22]):[c:23])-c1:c:c:c:c:c:1):[c:24].[c:25]:[c:26]:[c;H0;D3;+0:27](-...
null
[]
60
CELSIUS
1
HOUR
To a suspension of 2.1 g (60% in oil, 0.052 mole) of sodium hydride in 125 ml of dimethylformamide heated to 60° C. under a nitrogen gas blanket was added a solution of 2.65 g (0.026 mole) of N-methyl-3-pyrrolidinol and 5.0 g (0.026 mole) of 3,5-dichloropyridine-4-carboxylic acid in 40 ml of dimethylformamide dropwise ...
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Carboxylic acid.Secondary alcohol
Primary halide.Ether
C1CC[NH]C1.c1ccncc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
c1cc2c(cn1)OCC[NH]C2.c1ccccc1
c1cc2c(cn1)OCC[NH]C2.c1ccccc1.c1ccccc1.c1ccccc1
HO-
CN(C=O)C.C(C)N(CC)CC
60
1
CN1CCC(O)C1.O=C(O)c1c(Cl)cncc1Cl.c1ccc(P(c2ccccc2)c2ccccc2)cc1.c1ccc(P(c2ccccc2)c2ccccc2)cc1>CN(C=O)C.C(C)N(CC)CC>CN1Cc2c(Cl)cncc2OC(CCCl)C1.O=P(c1ccccc1)(c1ccccc1)c1ccccc1