dataset_id
large_stringclasses
414 values
reaction_id
large_stringlengths
36
36
reaction_smiles
large_stringlengths
4
873
rxn_insight_reaction
large_stringlengths
19
1.07k
mapped_reaction_smiles
large_stringlengths
14
3.37k
reactant_smiles
large_stringlengths
1
581
product_smiles
large_stringlengths
1
433
reagent_smiles
large_stringclasses
634 values
catalyst_smiles
large_stringlengths
1
683
solvent_smiles
large_stringlengths
1
245
rxn_insight_class
large_stringclasses
11 values
rxn_insight_name
large_stringclasses
346 values
rxn_insight_tag
large_stringlengths
64
64
rxn_insight_tag2
large_stringlengths
64
64
rxn_insight_scaffold
large_stringlengths
5
288
rxn_insight_template
large_stringlengths
24
2.64k
yield_percent
float64
-0.8
90,205,160,000B
yield_measurements
large_stringlengths
2
864
temperature_value
float64
-230
30.1k
temperature_units
large_stringclasses
3 values
reaction_time_value
float64
0
4k
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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-018fd0e1351f4fd09b20fcddd97b4c7a
ord-18221401c57e4374b9d089c4d5b209c7
Brc1ccsc1.CC(=O)c1nc(C)oc1C>>Cc1nc(C(C)(O)c2ccsc2)c(C)o1
BrC1=CSC=C1.C(C)(=O)C=1N=C(OC1C)C>>CC=1OC(=C(N1)C(C)(O)C1=CSC=C1)C
Br[c:8]1[cH:9][cH:10][s:11][cH:12]1.[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])=[O:7])[c:13]([CH3:14])[o:15]1>>[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])([OH:7])[c:8]2[cH:9][cH:10][s:11][cH:12]2)[c:13]([CH3:14])[o:15]1
Brc1ccsc1.CC(=O)c1nc(C)oc1C
Cc1nc(C(C)(O)c2ccsc2)c(C)o1
null
null
null
C-C Coupling
Grignard_alcohol
ced8db25e742cc856055ca33877a37cbea1e62e1ac0cab97d987f0994afc50bc
b8801be51258f6ee39fb6aad45dd9677b1b9eed3d6e0018ffb065bca8e787abf
c1nc(Cc2ccsc2)co1
Br-[c;H0;D3;+0:1]1:[c:2]:[#16;a:3]:[c:4]:[c:5]:1.[C;D1;H3:6]-[c:7]1:[#8;a:8]:[c:9]:[#7;a:10]:[c:11]:1-[C;H0;D3;+0:12](-[C;D1;H3:13])=[O;H0;D1;+0:14]>>[C;D1;H3:6]-[c:7]1:[#8;a:8]:[c:9]:[#7;a:10]:[c:11]:1-[C;H0;D4;+0:12](-[C;D1;H3:13])(-[OH;D1;+0:14])-[c;H0;D3;+0:1]1:[c:2]:[#16;a:3]:[c:4]:[c:5]:1
null
[]
null
null
null
null
Starting with 3-bromothiophene and 4-acetyl-2,5-dimethyloxazole and following the general method of Example 4 the title compound was prepared. M.p. 83°-84° C. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
Tertiary alcohol
c1ccsc1
c1ccsc1
c1cocn1.c1ccsc1
Br-
null
null
null
Brc1ccsc1.CC(=O)c1nc(C)oc1C>>Cc1nc(C(C)(O)c2ccsc2)c(C)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-01df543a66bb4268b36a7edbe14246e3
CC(=O)c1cc(C)oc1C.Cc1cscn1>>Cc1cc(C(C)(O)c2scnc2C)c(C)o1
C(CCC)[Li].C(O)([O-])=O.[Na+].C[Si](C)(C)Cl.C(CCC)[Li].C(C)(=O)C1=C(OC(=C1)C)C.CC=1N=CSC1>>CC=1OC(=CC1C(C)(O)C1=C(N=CS1)C)C
[CH3:1][c:2]1[cH:3][c:4]([C:5]([CH3:6])=[O:7])[c:14]([CH3:15])[o:16]1.[cH:8]1[s:9][cH:10][n:11][c:12]1[CH3:13]>>[CH3:1][c:2]1[cH:3][c:4]([C:5]([CH3:6])([OH:7])[c:8]2[s:9][cH:10][n:11][c:12]2[CH3:13])[c:14]([CH3:15])[o:16]1
CC(=O)c1cc(C)oc1C.Cc1cscn1
Cc1cc(C(C)(O)c2scnc2C)c(C)o1
null
null
O1CCCC1
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1cc(Cc2cncs2)co1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[cH;D2;+0:6]:1.[C;D1;H3:7]-[c:8]1:[#8;a:9]:[c:10]:[c:11]:[c:12]:1-[C;H0;D3;+0:13](-[C;D1;H3:14])=[O;H0;D1;+0:15]>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c;H0;D3;+0:6]:1-[C;H0;D4;+0:13](-[C;D1;H3:14])(-[OH;D1;+0:15])-[c:12]1:[c:11]:[c:10]:[#8;a:9]:[c:8]:1-[C;D1;H3:7]
null
[]
-70
CELSIUS
1
HOUR
4-Methylthiazole (6.51 g) in dry tetrahydrofuran (50 ml) was stirred under an atmosphere of dry nitrogen and cooled to -70° C. and n-butyllithium (2.5M solution in hexane, 29 ml) was added dropwise. After 30 minutes trimethylsilylchloride (7.14 g) was added and the mixture was allowed to warm to room temperature. After...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1ccoc1.c1cscn1
null
O1CCCC1
-70
1
CC(=O)c1cc(C)oc1C.Cc1cscn1>O1CCCC1>Cc1cc(C(C)(O)c2scnc2C)c(C)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a210beaddfb84e2bacb0459a8fb6e751
CC(=O)c1ccco1.Cc1cscn1>>Cc1ncsc1C(C)(O)c1ccco1
CC=1N=CSC1.C(C)(=O)C=1OC=CC1>>O1C(=CC=C1)C(C)(O)C1=C(N=CS1)C
[C:7]([CH3:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13][o:14]1.[CH3:1][c:2]1[n:3][cH:4][s:5][cH:6]1>>[CH3:1][c:2]1[n:3][cH:4][s:5][c:6]1[C:7]([CH3:8])([OH:9])[c:10]1[cH:11][cH:12][cH:13][o:14]1
CC(=O)c1ccco1.Cc1cscn1
Cc1ncsc1C(C)(O)c1ccco1
null
null
null
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1coc(Cc2cncs2)c1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[#8;a:6]:[c:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11]:[#16;a:12]:[cH;D2;+0:13]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11]:[#16;a:12]:[c;H0;D3;+0:13]:1-[C;H0;D4;+0:2](-[C;D1;H3:1])(-[OH;D1;+0:3])-[c:4](:[c:5]):[#8;a:6]:[c:7]
null
[]
null
null
null
null
Starting with 4-methylthiazole and 2-acetylfuran and following the general method of Example 15 the title compound was prepared. M.p. 127°-128° C. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccoc1
null
null
null
null
CC(=O)c1ccco1.Cc1cscn1>>Cc1ncsc1C(C)(O)c1ccco1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c5c6c64398c34e29931916d91cb3bfd4
CC(=O)c1cccs1.Cc1cscn1>>Cc1ncsc1C(C)(O)c1cccs1
CC=1N=CSC1.C(C)(=O)C=1SC=CC1>>CC=1N=CSC1C(C)(O)C=1SC=CC1
[C:7]([CH3:8])(=[O:9])[c:10]1[cH:11][cH:12][cH:13][s:14]1.[CH3:1][c:2]1[n:3][cH:4][s:5][cH:6]1>>[CH3:1][c:2]1[n:3][cH:4][s:5][c:6]1[C:7]([CH3:8])([OH:9])[c:10]1[cH:11][cH:12][cH:13][s:14]1
CC(=O)c1cccs1.Cc1cscn1
Cc1ncsc1C(C)(O)c1cccs1
null
null
null
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1csc(Cc2cncs2)c1
[C;D1;H3:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:3])-[c:4](:[c:5]):[#16;a:6]:[c:7].[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11]:[#16;a:12]:[cH;D2;+0:13]:1>>[C;D1;H3:8]-[c:9]1:[#7;a:10]:[c:11]:[#16;a:12]:[c;H0;D3;+0:13]:1-[C;H0;D4;+0:2](-[C;D1;H3:1])(-[OH;D1;+0:3])-[c:4](:[c:5]):[#16;a:6]:[c:7]
null
[]
null
null
null
null
Starting with 4-methylthiazole and 2-acetylthiophene and following the general method of Example 15 the title compound was prepared. M.p. 146.5°-147.5° C. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccsc1
null
null
null
null
CC(=O)c1cccs1.Cc1cscn1>>Cc1ncsc1C(C)(O)c1cccs1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7674ce8e93ec4e02859f77b6a1662375
CC(=O)c1ccsc1.C[Si](C)(C)c1nccs1>>CC(O)(c1ccsc1)c1cncs1
C(O)([O-])=O.[Na+].C(C)(=O)C1=CSC=C1.C(CCC)[Li].C[Si](C=1SC=CN1)(C)C>>S1C=NC=C1C(C)(O)C1=CSC=C1
[CH3:1][C:2](=[O:3])[c:4]1[cH:5][cH:6][s:7][cH:8]1.C[Si](C)(C)[c:12]1[n:11][cH:10][cH:9][s:13]1>>[CH3:1][C:2]([OH:3])([c:4]1[cH:5][cH:6][s:7][cH:8]1)[c:9]1[cH:10][n:11][cH:12][s:13]1
CC(=O)c1ccsc1.C[Si](C)(C)c1nccs1
CC(O)(c1ccsc1)c1cncs1
null
null
C(C)OCC
C-C Coupling
OtherReaction
5a13a76517abc481d18e323a5c6c18a4e7b3154319796cea55453b7d5b071d2c
ba292e2f26094ec157e2ffb4e80ae84c33cd53ebd701e5703ae56960fea8e68f
c1cc(Cc2cncs2)cs1
C-[Si](-C)(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[cH;D2;+0:3]:[c:4]:[#7;a:5]:1.[C;D1;H3:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9]1:[c:10]:[c:11]:[#16;a:12]:[c:13]:1>>[C;D1;H3:6]-[C;H0;D4;+0:7](-[OH;D1;+0:8])(-[c:9]1:[c:10]:[c:11]:[#16;a:12]:[c:13]:1)-[c;H0;D3;+0:3]1:[#16;a:2]:[cH;D2;+0:1]:[#7;a:5]:[c:4]:1
null
[]
null
null
45
MINUTE
n-Butyllithium (2.5M solution in hexane, 5.6 ml) in diethylether (25 ml) was stirred at -70° C. under a nitrogen atmosphere and 2-trimethylsilylthiazole (2 g) in diethylether (25 ml) was added dropwise. After 30 minutes 3-acetylthiophene (1.93 g) in diethylether (25 ml) was added dropwise. After a further 45 minutes th...
10.6084/m9.figshare.5104873.v1
null
Ketone.Silyl protective group
Tertiary alcohol
c1cscn1
c1cscn1
c1ccsc1.c1cscn1
Other
C(C)OCC
null
0.75
CC(=O)c1ccsc1.C[Si](C)(C)c1nccs1>C(C)OCC>CC(O)(c1ccsc1)c1cncs1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f8ae87d4cdb04743b3be2fcbfdc05511
Cc1ncoc1C(C)(O)c1ccoc1>>C=C(c1ccoc1)c1ocnc1C
C(O)([O-])=O.[Na+].O1C=C(C=C1)C(C)(O)C1=C(N=CO1)C.Cl.C(C)OCC>>O1C=C(C=C1)C(=C)C1=C(N=CO1)C
O[C:2]([CH3:1])([c:3]1[cH:4][cH:5][o:6][cH:7]1)[c:8]1[o:9][cH:10][n:11][c:12]1[CH3:13]>>[CH2:1]=[C:2]([c:3]1[cH:4][cH:5][o:6][cH:7]1)[c:8]1[o:9][cH:10][n:11][c:12]1[CH3:13]
Cc1ncoc1C(C)(O)c1ccoc1
C=C(c1ccoc1)c1ocnc1C
null
null
C(Cl)(Cl)Cl
Functional Group Interconversion
OtherReaction
2308ca9261cc4508224f0a5bf7cda8624f4e05d90876372dcc82c257ed89c11a
eea2743fbea38c6dcccd1d257095859a33500c4f909c86118b5a2f77112ebdea
C=C(c1ccoc1)c1cnco1
O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1)-[c:8]1:[#8;a:9]:[c:10]:[#7;a:11]:[c:12]:1-[C;D1;H3:13]>>[C;D1;H3:13]-[c:12]1:[#7;a:11]:[c:10]:[#8;a:9]:[c:8]:1-[C;H0;D3;+0:1](=[CH2;D1;+0:2])-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1
null
[]
null
null
10
MINUTE
1-(3-Furyl)-1-(4-methyl-5-oxazolyl)ethanol (900 mg) in dry chloroform was treated with 1M anhydrous hydrogen chloride in diethylether (1.1 equivalents). After 10 minutes at room temperature, aqueous sodium hydrogen carbonate was added and the mixture was extracted with dichloromethane. The material thus obtained was pu...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Vinyl
null
null
c1ccoc1.c1cocn1
HO-
C(Cl)(Cl)Cl
null
0.166667
Cc1ncoc1C(C)(O)c1ccoc1>C(Cl)(Cl)Cl>C=C(c1ccoc1)c1ocnc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9563069ad89e455ea5d20776f1f48877
COC(C)(c1ccoc1)c1oc(C)nc1C>>C=C(c1ccoc1)c1oc(C)nc1C
CC=1OC(=C(N1)C)C(C)(OC)C1=COC=C1.Cl>>Cl.CC=1OC(=C(N1)C)C(=C)C1=COC=C1
CO[C:2]([CH3:1])([c:3]1[cH:4][cH:5][o:6][cH:7]1)[c:8]1[o:9][c:10]([CH3:11])[n:12][c:13]1[CH3:14]>>[CH2:1]=[C:2]([c:3]1[cH:4][cH:5][o:6][cH:7]1)[c:8]1[o:9][c:10]([CH3:11])[n:12][c:13]1[CH3:14]
COC(C)(c1ccoc1)c1oc(C)nc1C
C=C(c1ccoc1)c1oc(C)nc1C
null
null
C(C)OCC
Functional Group Interconversion
OtherReaction
ed5ebc279b9b9a90d76d9bfdf51247e16a646652657fa7c19d4e0abb0d5fb866
ad641e1d0d5bc929f413157ac3f03f6855b2543026034902e6df156b88622b6d
C=C(c1ccoc1)c1cnco1
C-O-[C;H0;D4;+0:1](-[CH3;D1;+0:2])(-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1)-[c:8]1:[#8;a:9]:[c:10]:[#7;a:11]:[c:12]:1-[C;D1;H3:13]>>[C;D1;H3:13]-[c:12]1:[#7;a:11]:[c:10]:[#8;a:9]:[c:8]:1-[C;H0;D3;+0:1](=[CH2;D1;+0:2])-[c:3]1:[c:4]:[c:5]:[#8;a:6]:[c:7]:1
null
[]
null
null
null
null
1-(2,4-Dimethyl-5-oxazolyl)-1-(3-furyl)-1-methoxyethane (790 mg) in dry diethylether was treated with 1M anhydrous hydrogen chloride in diethylether (1.2 equivalents). The title compound was obtained as a white solid which was filtered off, washed and dried. M.p. 128.5°-130° C. Conditions: See reaction.notes.procedure_...
10.6084/m9.figshare.5104873.v1
null
Ether
Vinyl
null
null
c1ccoc1.c1cocn1
HO-
C(C)OCC
null
null
COC(C)(c1ccoc1)c1oc(C)nc1C>C(C)OCC>C=C(c1ccoc1)c1oc(C)nc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3a2eac6693d1472983219b852d6d0ec0
CC(=O)c1ocnc1C.[Li][c]1ccco1>>Cc1ncoc1C(C)(O)c1ccco1
C(C)(=O)C1=C(N=CO1)C.[Li]C=1OC=CC1>>O1C(=CC=C1)C(C)(O)C1=C(N=CO1)C
[CH3:1][c:2]1[n:3][cH:4][o:5][c:6]1[C:7]([CH3:8])=[O:9].[Li][c:10]1[cH:11][cH:12][cH:13][o:14]1>>[CH3:1][c:2]1[n:3][cH:4][o:5][c:6]1[C:7]([CH3:8])([OH:9])[c:10]1[cH:11][cH:12][cH:13][o:14]1
CC(=O)c1ocnc1C.[Li][c]1ccco1
Cc1ncoc1C(C)(O)c1ccco1
null
null
C(C)OCC
C-C Coupling
OtherReaction
8ba84549b458a473bed1ce3f130210aec377300d749c212d5b3208f8322a4467
1ce2a90fc82c66bb25293f8dd2f68813821f177fdf0916a1c51bb26296b4d38b
c1coc(Cc2cnco2)c1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1-[C;H0;D3;+0:7](-[C;D1;H3:8])=[O;H0;D1;+0:9].[Li]-[c;H0;D3;+0:10]1:[#8;a:11]:[c:12]:[c:13]:[c:14]:1>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#8;a:5]:[c:6]:1-[C;H0;D4;+0:7](-[C;D1;H3:8])(-[OH;D1;+0:9])-[c;H0;D3;+0:10]1:[#8;a:11]:[c:12]:[c:13]:[c:14]:1
null
[]
null
null
8
HOUR
5-Acetyl-4-methyloxazole (4 g) in dry diethylether was added dropwise to a stirred solution of 2-lithiofuran (1 equivalent) in diethylether at -20° C. The mixture was allowed to warm to room temperature and was then left overnight. Work-up and flash chromatography then gave the title compound as a white solid, m.p. 73°...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aryl lithium
Tertiary alcohol
c1ccoc1
c1ccoc1
c1cocn1.c1ccoc1
Li
C(C)OCC
null
8
CC(=O)c1ocnc1C.[Li][c]1ccco1>C(C)OCC>Cc1ncoc1C(C)(O)c1ccco1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-64a5fb908811427eb165211883741e3d
CC(=O)c1sc(C)nc1C.[Li][c]1cccnc1>>Cc1nc(C)c(C(C)(O)c2cccnc2)s1
C(C)(=O)C1=C(N=C(S1)C)C.[Li]C=1C=NC=CC1.C(O)([O-])=O.[Na+]>>CC=1SC(=C(N1)C)C(C)(O)C=1C=NC=CC1
[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])=[O:9])[s:16]1.[Li][c:10]1[cH:11][cH:12][cH:13][n:14][cH:15]1>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])([OH:9])[c:10]2[cH:11][cH:12][cH:13][n:14][cH:15]2)[s:16]1
CC(=O)c1sc(C)nc1C.[Li][c]1cccnc1
Cc1nc(C)c(C(C)(O)c2cccnc2)s1
null
null
C(C)OCC
C-C Coupling
OtherReaction
8d05c101695e22ee37904717b9f3b8f3de2597fa76d2b14d2a001428eddaf89c
1ce2a90fc82c66bb25293f8dd2f68813821f177fdf0916a1c51bb26296b4d38b
c1cncc(Cc2cncs2)c1
[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1-[C;H0;D3;+0:7](-[C;D1;H3:8])=[O;H0;D1;+0:9].[Li]-[c;H0;D3;+0:10]1:[c:11]:[c:12]:[c:13]:[#7;a:14]:[c:15]:1>>[C;D1;H3:1]-[c:2]1:[#7;a:3]:[c:4]:[#16;a:5]:[c:6]:1-[C;H0;D4;+0:7](-[C;D1;H3:8])(-[OH;D1;+0:9])-[c;H0;D3;+0:10]1:[c:11]:[c:12]:[c:13]:[#7;a:14]:[c:15]:1
null
[]
null
null
3
HOUR
5-Acetyl-2,4-dimethylthiazole (2.5 g) in dry diethylether (10 ml) was added dropwise to a stirred solution of 3-lithiopyridine (from 3.5 g 3-bromopyridine) in diethylether at -70° C. After 3 hours the mixture was allowed to warm to room temperature. After a further 1 hour, aqueous sodium hydrogen carbonate was added an...
10.6084/m9.figshare.5104873.v1
null
Ketone.Aryl lithium
Tertiary alcohol
c1ccncc1
c1ccncc1
c1cscn1.c1ccncc1
Li
C(C)OCC
null
3
CC(=O)c1sc(C)nc1C.[Li][c]1cccnc1>C(C)OCC>Cc1nc(C)c(C(C)(O)c2cccnc2)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9af96c4c69f344379ebe313338e1ebf0
Brc1ccsc1.CC(=O)c1c(C)noc1C>>Cc1noc(C)c1C(C)(O)c1ccsc1
C(C)(=O)C=1C(=NOC1C)C.BrC1=CSC=C1>>CC1=NOC(=C1C(C)(O)C1=CSC=C1)C
Br[c:11]1[cH:12][cH:13][s:14][cH:15]1.[CH3:1][c:2]1[n:3][o:4][c:5]([CH3:6])[c:7]1[C:8]([CH3:9])=[O:10]>>[CH3:1][c:2]1[n:3][o:4][c:5]([CH3:6])[c:7]1[C:8]([CH3:9])([OH:10])[c:11]1[cH:12][cH:13][s:14][cH:15]1
Brc1ccsc1.CC(=O)c1c(C)noc1C
Cc1noc(C)c1C(C)(O)c1ccsc1
null
null
null
C-C Coupling
Grignard_alcohol
ced8db25e742cc856055ca33877a37cbea1e62e1ac0cab97d987f0994afc50bc
b8801be51258f6ee39fb6aad45dd9677b1b9eed3d6e0018ffb065bca8e787abf
c1cc(Cc2cnoc2)cs1
Br-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#16;a:4]:[c:5]:1.[C;D1;H3:6]-[c:7]1:[#7;a:8]:[#8;a:9]:[c:10](-[C;D1;H3:11]):[c:12]:1-[C;H0;D3;+0:13](-[C;D1;H3:14])=[O;H0;D1;+0:15]>>[C;D1;H3:6]-[c:7]1:[#7;a:8]:[#8;a:9]:[c:10](-[C;D1;H3:11]):[c:12]:1-[C;H0;D4;+0:13](-[C;D1;H3:14])(-[OH;D1;+0:15])-[c;H0;D3;+0:1]1:[c:2]:[c:3]:[#16;a:4]:[c...
null
[]
null
null
null
null
The title compound was prepared following the general method of Example 4 but starting with 4-acetyl-3,5-dimethylisoxazole and 3-bromothiophene. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
Tertiary alcohol
c1ccsc1
c1ccsc1
c1cnoc1.c1ccsc1
Br-
null
null
null
Brc1ccsc1.CC(=O)c1c(C)noc1C>>Cc1noc(C)c1C(C)(O)c1ccsc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-59fd6eb77b07405893186404a2c88e70
CI.Cc1nc(C)c(C(C)(O)c2ccoc2)o1>>COC(C)(c1ccoc1)c1oc(C)nc1C
C(O)([O-])=O.[Na+].O1C=C(C=C1)C(C)(O)C1=C(N=C(O1)C)C.[H-].[Na+].CI>>COC(C)(C1=COC=C1)C1=C(N=C(O1)C)C
I[CH3:1].[OH:2][C:3]([CH3:4])([c:5]1[cH:6][cH:7][o:8][cH:9]1)[c:10]1[o:11][c:12]([CH3:13])[n:14][c:15]1[CH3:16]>>[CH3:1][O:2][C:3]([CH3:4])([c:5]1[cH:6][cH:7][o:8][cH:9]1)[c:10]1[o:11][c:12]([CH3:13])[n:14][c:15]1[CH3:16]
CI.Cc1nc(C)c(C(C)(O)c2ccoc2)o1
COC(C)(c1ccoc1)c1oc(C)nc1C
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
cd10a9010f842ab825b304bd2965f17f9c39c4c64e5fc6cd91306ae51817de0d
9271b713ded6954f3329c61a211042ac37c82b3aff1b62cb455035e69339dd27
c1cc(Cc2cnco2)co1
I-[CH3;D1;+0:1].[#7;a:2]:[c:3]:[c:4](-[C:5](-[C;D1;H3:6])(-[OH;D1;+0:7])-[c:8]:[c:9]:[#8;a:10]):[#8;a:11]>>[#7;a:2]:[c:3]:[c:4](-[C:5](-[C;D1;H3:6])(-[O;H0;D2;+0:7]-[CH3;D1;+0:1])-[c:8]:[c:9]:[#8;a:10]):[#8;a:11]
null
[]
null
null
20
MINUTE
1-(3-Furyl)-1-(2,4-dimethyl-5-oxazolyl)ethanol (2g) in dry N,N-dimethylformamide (15 ml) was added to a stirred suspension of sodium hydride (80%, 300 mg) in dry N,N-dimethylformamide (10 ml) at 0° C. After 20 minutes, methyl iodide (1.5 g) was added dropwise. The mixture was allowed to warm to room temperature and aft...
10.6084/m9.figshare.5104873.v1
null
Tertiary alcohol
Ether
null
null
c1ccoc1.c1cocn1
HI
CN(C=O)C
null
0.333333
CI.Cc1nc(C)c(C(C)(O)c2ccoc2)o1>CN(C=O)C>COC(C)(c1ccoc1)c1oc(C)nc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b8d6ab59a04244b59a32293274773631
CC(=O)c1cccs1.Cc1ncsc1C>>Cc1nc(C(C)(O)c2cccs2)sc1C
C(C)(=O)C=1SC=CC1.C(CCC)[Li].CC=1N=CSC1C>>CC=1N=C(SC1C)C(C)(O)C=1SC=CC1
[C:5]([CH3:6])(=[O:7])[c:8]1[cH:9][cH:10][cH:11][s:12]1.[CH3:1][c:2]1[n:3][cH:4][s:13][c:14]1[CH3:15]>>[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])([OH:7])[c:8]2[cH:9][cH:10][cH:11][s:12]2)[s:13][c:14]1[CH3:15]
CC(=O)c1cccs1.Cc1ncsc1C
Cc1nc(C(C)(O)c2cccs2)sc1C
null
null
C(C)OCC
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1csc(Cc2nccs2)c1
[#16;a:1]1:[c:2]:[c:3]:[#7;a:4]:[cH;D2;+0:5]:1.[C;D1;H3:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9](:[c:10]):[#16;a:11]:[c:12]>>[C;D1;H3:6]-[C;H0;D4;+0:7](-[OH;D1;+0:8])(-[c:9](:[c:10]):[#16;a:11]:[c:12])-[c;H0;D3;+0:5]1:[#16;a:1]:[c:2]:[c:3]:[#7;a:4]:1
null
[]
null
null
30
MINUTE
n-Butyllithium (2.5M solution in hexanes, 9.7 ml) was added dropwise to a stirred solution of 4,5-dimethylthiazole (2.5 g) in dry diethyl ether (30 ml) at -70° C. under an atmosphere of dry nitrogen. After 30 minutes, 2-acetylthiophene (3.1 g) in diethyl ether (20 ml) was added dropwise. After a further 1 hour the mixt...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccsc1
null
C(C)OCC
null
0.5
CC(=O)c1cccs1.Cc1ncsc1C>C(C)OCC>Cc1nc(C(C)(O)c2cccs2)sc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-47117198c8d046e0b5bd18f8ec9abb21
Cc1cscn1.O=C(CCCCl)c1cccs1>>Cc1csc(C2(c3cccs3)CCCO2)n1
CC=1N=CSC1.ClCCCC(=O)C=1SC=CC1>>CC=1N=C(SC1)C1(OCCC1)C=1SC=CC1
[CH3:1][c:2]1[cH:3][s:4][cH:5][n:16]1.Cl[CH2:14][CH2:13][CH2:12][C:6]([c:7]1[cH:8][cH:9][cH:10][s:11]1)=[O:15]>>[CH3:1][c:2]1[cH:3][s:4][c:5]([C:6]2([c:7]3[cH:8][cH:9][cH:10][s:11]3)[CH2:12][CH2:13][CH2:14][O:15]2)[n:16]1
Cc1cscn1.O=C(CCCCl)c1cccs1
Cc1csc(C2(c3cccs3)CCCO2)n1
null
null
null
Heteroatom Alkylation and Arylation
OtherReaction
4ba89a1e75cd3cfd3160711124195e0db992f60c52150da9ca11cc10e8e21b21
98d62a2f88bda9a16db724874a7a21c7201c15ae486e75d3477ada88c887a7ad
c1csc(C2(c3nccs3)CCCO2)c1
Cl-[CH2;D2;+0:1]-[C:2]-[C:3]-[C;H0;D3;+0:4](=[O;H0;D1;+0:5])-[c:6](:[c:7]):[#16;a:8]:[c:9].[#16;a:10]1:[c:11]:[c:12]:[#7;a:13]:[cH;D2;+0:14]:1>>[c:9]:[#16;a:8]:[c:6](-[C;H0;D4;+0:4]1(-[c;H0;D3;+0:14]2:[#16;a:10]:[c:11]:[c:12]:[#7;a:13]:2)-[C:3]-[C:2]-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-1):[c:7]
null
[]
null
null
null
null
The title compound was prepared from 4-methylthiazole and 4-chloro-1-(2-thienyl)-1-butanone, using the general method of Example 36. M.p. 59°-60° C., 13C Nmr (CDCl3) 17.4, 26.2, 41.2, 69.3, 86.2, 113.9, 124.2, 124.7, 126.8, 148.9, 153.1 and 175.6 ppm. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Primary halide.Ketone
Ether
c1cscn1
c1cscn1.C1CCOC1
c1cscn1.c1ccsc1.C1CCOC1
HCl
null
null
null
Cc1cscn1.O=C(CCCCl)c1cccs1>>Cc1csc(C2(c3cccs3)CCCO2)n1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9c11173c9d7a4647bd65210ad622b55b
CC(=O)c1cc2ccccc2o1.Cc1csc([Si](C)(C)C)n1>>Cc1ncsc1C(C)(O)c1cc2ccccc2o1
C(C)(=O)C=1OC2=C(C1)C=CC=C2.C(CCC)[Li].CC=1N=C(SC1)[Si](C)(C)C>>O1C(=CC2=C1C=CC=C2)C(C)(O)C2=C(N=CS2)C
[C:7]([CH3:8])(=[O:9])[c:10]1[cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[o:18]1.C[Si](C)(C)[c:4]1[n:3][c:2]([CH3:1])[cH:6][s:5]1>>[CH3:1][c:2]1[n:3][cH:4][s:5][c:6]1[C:7]([CH3:8])([OH:9])[c:10]1[cH:11][c:12]2[cH:13][cH:14][cH:15][cH:16][c:17]2[o:18]1
CC(=O)c1cc2ccccc2o1.Cc1csc([Si](C)(C)C)n1
Cc1ncsc1C(C)(O)c1cc2ccccc2o1
null
null
C(C)OCC
C-C Coupling
OtherReaction
5a13a76517abc481d18e323a5c6c18a4e7b3154319796cea55453b7d5b071d2c
ba292e2f26094ec157e2ffb4e80ae84c33cd53ebd701e5703ae56960fea8e68f
c1ccc2oc(Cc3cncs3)cc2c1
C-[Si](-C)(-C)-[c;H0;D3;+0:1]1:[#16;a:2]:[cH;D2;+0:3]:[c:4](-[C;D1;H3:5]):[#7;a:6]:1.[C;D1;H3:7]-[C;H0;D3;+0:8](=[O;H0;D1;+0:9])-[c:10](:[c:11]):[#8;a:12]:[c:13]>>[C;D1;H3:5]-[c:4]1:[#7;a:6]:[cH;D2;+0:1]:[#16;a:2]:[c;H0;D3;+0:3]:1-[C;H0;D4;+0:8](-[C;D1;H3:7])(-[OH;D1;+0:9])-[c:10](:[c:11]):[#8;a:12]:[c:13]
null
[]
null
null
30
MINUTE
n-Butyllithium (2.5M solution in hexane, 1 equivalent) was added dropwise to a solution of 4-methyl-2-trimethylsilylthiazole (1 equivalent) in dry diethyl ether at -70° C. under an atmosphere of dry nitrogen. After 30 minutes, 2-acetylbenzofuran (1 equivalent) in diethyl ether was added. After 1 hour the mixture was al...
10.6084/m9.figshare.5104873.v1
null
Ketone.Silyl protective group
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccc2occc2c1
Other
C(C)OCC
null
0.5
CC(=O)c1cc2ccccc2o1.Cc1csc([Si](C)(C)C)n1>C(C)OCC>Cc1ncsc1C(C)(O)c1cc2ccccc2o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c6b8bc5eaf364257b6235f60aa86b148
CC(=O)c1ccco1.Cc1nn(C)c(C)c1Br>>Cc1nn(C)c(C)c1C(C)(O)c1ccco1
BrC=1C(=NN(C1C)C)C.C(C)(=O)C=1OC=CC1>>O1C(=CC=C1)C(C)(O)C=1C(=NN(C1C)C)C
[C:9]([CH3:10])(=[O:11])[c:12]1[cH:13][cH:14][cH:15][o:16]1.Br[c:8]1[c:2]([CH3:1])[n:3][n:4]([CH3:5])[c:6]1[CH3:7]>>[CH3:1][c:2]1[n:3][n:4]([CH3:5])[c:6]([CH3:7])[c:8]1[C:9]([CH3:10])([OH:11])[c:12]1[cH:13][cH:14][cH:15][o:16]1
CC(=O)c1ccco1.Cc1nn(C)c(C)c1Br
Cc1nn(C)c(C)c1C(C)(O)c1ccco1
null
null
null
C-C Coupling
Grignard_alcohol
867b05745a50e050669540e95bb7b56f7649cafafd59c323b0fc7ce5fb8c5702
b8801be51258f6ee39fb6aad45dd9677b1b9eed3d6e0018ffb065bca8e787abf
c1coc(Cc2cn[nH]c2)c1
Br-[c;H0;D3;+0:1]1:[c:2](-[C;D1;H3:3]):[#7;a:4]:[#7;a:5](-[C;D1;H3:6]):[c:7]:1-[C;D1;H3:8].[C;D1;H3:9]-[C;H0;D3;+0:10](=[O;H0;D1;+0:11])-[c:12](:[c:13]):[#8;a:14]:[c:15]>>[C;D1;H3:9]-[C;H0;D4;+0:10](-[OH;D1;+0:11])(-[c:12](:[c:13]):[#8;a:14]:[c:15])-[c;H0;D3;+0:1]1:[c:2](-[C;D1;H3:3]):[#7;a:4]:[#7;a:5](-[C;D1;H3:6]):[c...
null
[]
null
null
null
null
4-Bromo-1,3,5-trimethylpyrazole was converted into the corresponding 4-lithio compound which was then reacted in situ with 2-acetylfuran. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Aromatic halide.Ketone
Tertiary alcohol
c1cn[nH]c1
c1cn[nH]c1
c1cn[nH]c1.c1ccoc1
Br-
null
null
null
CC(=O)c1ccco1.Cc1nn(C)c(C)c1Br>>Cc1nn(C)c(C)c1C(C)(O)c1ccco1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9e8f852e5b4a473880332d65fd05ff5a
C[Si](C)(C)C(F)(F)F.Cc1nc(C)c(C(=O)c2ccoc2)o1>>Cc1nc(C)c(C(O)(c2ccoc2)C(F)(F)F)o1
Cl.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.O1C=C(C=C1)C(=O)C1=C(N=C(O1)C)C.FC(F)(F)[Si](C)(C)C.C(O)([O-])=O.[Na+]>>CC=1OC(=C(N1)C)C(C(F)(F)F)(O)C1=COC=C1
C[Si](C)(C)[C:14]([F:15])([F:16])[F:17].[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7](=[O:8])[c:9]2[cH:10][cH:11][o:12][cH:13]2)[o:18]1>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([OH:8])([c:9]2[cH:10][cH:11][o:12][cH:13]2)[C:14]([F:15])([F:16])[F:17])[o:18]1
C[Si](C)(C)C(F)(F)F.Cc1nc(C)c(C(=O)c2ccoc2)o1
Cc1nc(C)c(C(O)(c2ccoc2)C(F)(F)F)o1
null
null
O1CCCC1
C-C Coupling
OtherReaction
dfa995a1ded6b569a532c6523aafcfe2cc62e0013499fd31224672ecb3516b9f
2ce208121d6571fcaa14b1a3313dc208052e5b2c9201de548c57a6101c962912
c1cc(Cc2cnco2)co1
C-[Si](-C)(-C)-[C;H0;D4;+0:1](-[F;D1;H0:2])(-[F;D1;H0:3])-[F;D1;H0:4].[C;D1;H3:5]-[c:6]1:[#7;a:7]:[c:8]:[#8;a:9]:[c:10]:1-[C;H0;D3;+0:11](=[O;H0;D1;+0:12])-[c:13]1:[c:14]:[c:15]:[#8;a:16]:[c:17]:1>>[C;D1;H3:5]-[c:6]1:[#7;a:7]:[c:8]:[#8;a:9]:[c:10]:1-[C;H0;D4;+0:11](-[OH;D1;+0:12])(-[c:13]1:[c:14]:[c:15]:[#8;a:16]:[c:17...
null
[]
null
null
null
null
Tetrabutylammonium fluoride (250 mg) was added to a stirred solution of 2,4-dimethyl-5-oxazolyl 3-furyl ketone (1.7 g) and (trifluoromethyl) trimethylsilane (1.9 g) in dry tetrahydrofuran (30 ml) at -10° C. The mixture was allowed to warm to room temperature. After 45 minutes 6M hydrochloric acid (30 ml) was added. Aft...
10.6084/m9.figshare.5104873.v1
null
Trifluoro group.Ketone.Silyl protective group
Trifluoro group.Tertiary alcohol
null
null
c1cocn1.c1ccoc1
Other
O1CCCC1
null
null
C[Si](C)(C)C(F)(F)F.Cc1nc(C)c(C(=O)c2ccoc2)o1>O1CCCC1>Cc1nc(C)c(C(O)(c2ccoc2)C(F)(F)F)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a84f7dd10911495d860973d4009ad6f3
CC(=O)c1sc(C)nc1C.Cn1cccc1>>Cc1nc(C)c(C(C)(O)c2cccn2C)s1
C(C)(=O)C1=C(N=C(S1)C)C.CN(C)CCN(C)C.C(CCC)[Li].CN1C=CC=C1>>CC=1SC(=C(N1)C)C(C)(O)C=1N(C=CC1)C
[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])=[O:9])[s:16]1.[cH:10]1[cH:11][cH:12][cH:13][n:14]1[CH3:15]>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])([OH:9])[c:10]2[cH:11][cH:12][cH:13][n:14]2[CH3:15])[s:16]1
CC(=O)c1sc(C)nc1C.Cn1cccc1
Cc1nc(C)c(C(C)(O)c2cccn2C)s1
null
null
C(C)OCC
C-C Coupling
OtherReaction
74a7a57737bc3a3f8ff699a520b9acb98d9fd2843b33b3d885ba3bc512a8ff74
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1c[nH]c(Cc2cncs2)c1
[C;D1;H3:1]-[#7;a:2]1:[c:3]:[c:4]:[c:5]:[cH;D2;+0:6]:1.[C;D1;H3:7]-[c:8]1:[#7;a:9]:[c:10]:[#16;a:11]:[c:12]:1-[C;H0;D3;+0:13](-[C;D1;H3:14])=[O;H0;D1;+0:15]>>[C;D1;H3:1]-[#7;a:2]1:[c:3]:[c:4]:[c:5]:[c;H0;D3;+0:6]:1-[C;H0;D4;+0:13](-[C;D1;H3:14])(-[OH;D1;+0:15])-[c:12]1:[#16;a:11]:[c:10]:[#7;a:9]:[c:8]:1-[C;D1;H3:7]
null
[]
null
null
5
MINUTE
n-Butyllithium (2.5M solution in hexanes, 20 ml) in dry diethyl ether was cooled to -70° C. under dry nitrogen and TMEDA (5.8 g) was added. After 5 minutes, 1-methylpyrrole (5.4 g) in diethyl ether was added dropwise. After a further 15 minutes, 5-acetyl-2,4-dimethylthiazole (4.5 ml) was added dropwise. After 30 minute...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cc[nH]c1
c1ccc[nH]1
c1cscn1.c1ccc[nH]1
null
C(C)OCC
null
0.083333
CC(=O)c1sc(C)nc1C.Cn1cccc1>C(C)OCC>Cc1nc(C)c(C(C)(O)c2cccn2C)s1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5a5eb6ad04954fd4aa68e9d330119b48
CC(=O)c1ccsc1.Cc1ncsc1CCO>>Cc1nc(C(C)(O)c2ccsc2)sc1CCO
C(C)(=O)C1=CSC=C1.C(CCC)[Li].OCCC1=C(N=CS1)C>>OCCC1=C(N=C(S1)C(C)(O)C1=CSC=C1)C
[C:5]([CH3:6])(=[O:7])[c:8]1[cH:9][cH:10][s:11][cH:12]1.[CH3:1][c:2]1[n:3][cH:4][s:13][c:14]1[CH2:15][CH2:16][OH:17]>>[CH3:1][c:2]1[n:3][c:4]([C:5]([CH3:6])([OH:7])[c:8]2[cH:9][cH:10][s:11][cH:12]2)[s:13][c:14]1[CH2:15][CH2:16][OH:17]
CC(=O)c1ccsc1.Cc1ncsc1CCO
Cc1nc(C(C)(O)c2ccsc2)sc1CCO
null
null
O1CCCC1
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1csc(Cc2ccsc2)n1
[#16;a:1]1:[c:2]:[c:3]:[#7;a:4]:[cH;D2;+0:5]:1.[C;D1;H3:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9]1:[c:10]:[#16;a:11]:[c:12]:[c:13]:1>>[C;D1;H3:6]-[C;H0;D4;+0:7](-[OH;D1;+0:8])(-[c:9]1:[c:10]:[#16;a:11]:[c:12]:[c:13]:1)-[c;H0;D3;+0:5]1:[#16;a:1]:[c:2]:[c:3]:[#7;a:4]:1
null
[]
null
null
30
MINUTE
n-Butyllithium (2.5M solution in hexanes, 75 mmoles) was added to a stirred solution of 5-(2-hydroxyethyl)-4-methylthiazole (35 mmoles) in dry tetrahydrofuran (80 ml) at -70° C. under an atmosphere of dry nitrogen. After 30 minutes, 3-acetylthiophene (38 mmoles) in dry tetrahydrofuran (10 ml) was added dropwise. After ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccsc1
null
O1CCCC1
null
0.5
CC(=O)c1ccsc1.Cc1ncsc1CCO>O1CCCC1>Cc1nc(C(C)(O)c2ccsc2)sc1CCO
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-19e5e84795b74736b737dbe52b48c69c
CC(=O)c1oc(C)nc1C.[Li][c]1cocc1Br>>Cc1nc(C)c(C(C)(O)c2cocc2Br)o1
C(C)(=O)C1=C(N=C(O1)C)C.BrC=1C(=COC1)[Li]>>BrC=1C(=COC1)C(C)(O)C1=C(N=C(O1)C)C
[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])=[O:9])[o:16]1.[Li][c:10]1[cH:11][o:12][cH:13][c:14]1[Br:15]>>[CH3:1][c:2]1[n:3][c:4]([CH3:5])[c:6]([C:7]([CH3:8])([OH:9])[c:10]2[cH:11][o:12][cH:13][c:14]2[Br:15])[o:16]1
CC(=O)c1oc(C)nc1C.[Li][c]1cocc1Br
Cc1nc(C)c(C(C)(O)c2cocc2Br)o1
null
null
null
C-C Coupling
OtherReaction
8ba84549b458a473bed1ce3f130210aec377300d749c212d5b3208f8322a4467
1ce2a90fc82c66bb25293f8dd2f68813821f177fdf0916a1c51bb26296b4d38b
c1cc(Cc2cnco2)co1
[Br;D1;H0:1]-[c:2]1:[c:3]:[#8;a:4]:[c:5]:[c;H0;D3;+0:6]:1-[Li].[C;D1;H3:7]-[c:8]1:[#7;a:9]:[c:10]:[#8;a:11]:[c:12]:1-[C;H0;D3;+0:13](-[C;D1;H3:14])=[O;H0;D1;+0:15]>>[Br;D1;H0:1]-[c:2]1:[c:3]:[#8;a:4]:[c:5]:[c;H0;D3;+0:6]:1-[C;H0;D4;+0:13](-[C;D1;H3:14])(-[OH;D1;+0:15])-[c:12]1:[#8;a:11]:[c:10]:[#7;a:9]:[c:8]:1-[C;D1;H3...
null
[]
null
null
null
null
Following the general method of Example la but using 5-acetyl-2,4-dimethyloxazole and 4-bromo-3-lithiofuran (Liebigs Ann. Chem., 1986, 625-637), the title compound was prepared. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone.Aryl lithium
Tertiary alcohol
c1ccoc1
c1ccoc1
c1cocn1.c1ccoc1
Li
null
null
null
CC(=O)c1oc(C)nc1C.[Li][c]1cocc1Br>>Cc1nc(C)c(C(C)(O)c2cocc2Br)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c91163ae137242d2923ab319d4372fc6
CC(=O)c1ccsc1.COCc1scnc1C>>COCc1sc(C(C)(O)c2ccsc2)nc1C
C(C)(=O)C1=CSC=C1.COCC1=C(N=CS1)C>>COCC1=C(N=C(S1)C(C)(O)C1=CSC=C1)C
[C:7]([CH3:8])(=[O:9])[c:10]1[cH:11][cH:12][s:13][cH:14]1.[CH3:1][O:2][CH2:3][c:4]1[s:5][cH:6][n:15][c:16]1[CH3:17]>>[CH3:1][O:2][CH2:3][c:4]1[s:5][c:6]([C:7]([CH3:8])([OH:9])[c:10]2[cH:11][cH:12][s:13][cH:14]2)[n:15][c:16]1[CH3:17]
CC(=O)c1ccsc1.COCc1scnc1C
COCc1sc(C(C)(O)c2ccsc2)nc1C
null
null
null
C-C Coupling
OtherReaction
acd195ea3234757fa63ebadb8d31a476ea220e3bfd4b639c71b1e4fe8ddfd859
454f67ba8644982dc9f605915a0f36178771eadaffb50d3f1e0f17f2b6fdeb10
c1csc(Cc2ccsc2)n1
[#16;a:1]1:[c:2]:[c:3]:[#7;a:4]:[cH;D2;+0:5]:1.[C;D1;H3:6]-[C;H0;D3;+0:7](=[O;H0;D1;+0:8])-[c:9]1:[c:10]:[c:11]:[#16;a:12]:[c:13]:1>>[C;D1;H3:6]-[C;H0;D4;+0:7](-[OH;D1;+0:8])(-[c:9]1:[c:10]:[c:11]:[#16;a:12]:[c:13]:1)-[c;H0;D3;+0:5]1:[#16;a:1]:[c:2]:[c:3]:[#7;a:4]:1
null
[]
null
null
null
null
The title compound was prepared by following the general method of Example 36 but using 3-acetylthiophene and 5-methoxymethyl-4-methylthiazole. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Ketone
Tertiary alcohol
c1cscn1
c1cscn1
c1cscn1.c1ccsc1
null
null
null
null
CC(=O)c1ccsc1.COCc1scnc1C>>COCc1sc(C(C)(O)c2ccsc2)nc1C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d5df902db51f4973b3595b8e30064e32
C[Si](C)(C)N=[N+]=[N-].Cc1ncoc1C(C)(O)c1ccoc1>>Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1
O.O1C=C(C=C1)C(C)(O)C1=C(N=CO1)C.C[Si](C)(C)N=[N+]=[N-].B(F)(F)F>>N(=[N+]=[N-])C(C)(C1=C(N=CO1)C)C1=COC=C1
C[Si](C)(C)[N:9]=[N+:10]=[N-:11].O[C:7]([c:6]1[c:2]([CH3:1])[n:3][cH:4][o:5]1)([CH3:8])[c:12]1[cH:13][cH:14][o:15][cH:16]1>>[CH3:1][c:2]1[n:3][cH:4][o:5][c:6]1[C:7]([CH3:8])([N:9]=[N+:10]=[N-:11])[c:12]1[cH:13][cH:14][o:15][cH:16]1
C[Si](C)(C)N=[N+]=[N-].Cc1ncoc1C(C)(O)c1ccoc1
Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1
null
null
C1=CC=CC=C1
Heteroatom Alkylation and Arylation
OtherReaction
0509339f927cf4d56b29cc090967b960c097a7bdff4eba5e10a42acb1ecc7a22
af4082b86080041b9f6d702bf62e48a6b9d294ca1f4446f55ade86dd878f5885
c1cc(Cc2cnco2)co1
C-[Si](-C)(-C)-[N;H0;D2;+0:1]=[#7;+:2]=[N;-;D1;H0:3].O-[C;H0;D4;+0:4](-[C;D1;H3:5])(-[c:6]1:[c:7]:[c:8]:[#8;a:9]:[c:10]:1)-[c:11]1:[#8;a:12]:[c:13]:[#7;a:14]:[c:15]:1-[C;D1;H3:16]>>[C;D1;H3:16]-[c:15]1:[#7;a:14]:[c:13]:[#8;a:12]:[c:11]:1-[C;H0;D4;+0:4](-[C;D1;H3:5])(-[N;H0;D2;+0:1]=[#7;+:2]=[N;-;D1;H0:3])-[c:6]1:[c:7]:...
null
[]
null
null
8
HOUR
1-(3-Furyl)-1-(4-methyl-5-oxazolyl)ethanol (1 g) was suspended in benzene (4 ml). Trimethylsilylazide (822 μl) was added followed by boron trifluoride diethyletherate (770 μl). The mixture was stirred overnight at room temperature, then poured into water and extracted to give the title compound. Conditions: See reactio...
10.6084/m9.figshare.5104873.v1
null
Azide.Tertiary alcohol.Silyl protective group
Azide
null
null
c1cocn1.c1ccoc1
HO-
C1=CC=CC=C1
null
8
C[Si](C)(C)N=[N+]=[N-].Cc1ncoc1C(C)(O)c1ccoc1>C1=CC=CC=C1>Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-dab48b2bfda241a4b7f0f62acf90e643
Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1>>Cc1ncoc1C(C)(N)c1ccoc1
N(=[N+]=[N-])C(C)(C1=C(N=CO1)C)C1=COC=C1>>O1C=C(C=C1)C(C)(C1=C(N=CO1)C)N
[N-]=[N+]=[N:9][C:7]([c:6]1[c:2]([CH3:1])[n:3][cH:4][o:5]1)([CH3:8])[c:10]1[cH:11][cH:12][o:13][cH:14]1>>[CH3:1][c:2]1[n:3][cH:4][o:5][c:6]1[C:7]([CH3:8])([NH2:9])[c:10]1[cH:11][cH:12][o:13][cH:14]1
Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1
Cc1ncoc1C(C)(N)c1ccoc1
null
[Pd]
C(C)O
Reduction
Azide to amine reduction (Staudinger)
4c9e4990dae2bb965dec06bd45e318560989ee3681b61e443f7aa363b7cfa222
cd009d687d606bf351eac9390a176d16be38f2c8216a599b398641009c215027
c1cc(Cc2cnco2)co1
[#7;a:1]:[c:2]:[c:3](-[C:4](-[C;D1;H3:5])(-[N;H0;D2;+0:6]=[N+]=[N-])-[c:7]:[c:8]:[#8;a:9]):[#8;a:10]>>[#7;a:1]:[c:2]:[c:3](-[C:4](-[C;D1;H3:5])(-[NH2;D1;+0:6])-[c:7]:[c:8]:[#8;a:9]):[#8;a:10]
null
[]
null
null
null
null
The product from Example 65 in ethanol was hydrogenated in the presence of 10% palladium-on-charcoal to give the title compound. Conditions: See reaction.notes.procedure_details.
10.6084/m9.figshare.5104873.v1
null
Azide
Primary amine
null
null
c1cocn1.c1ccoc1
Other
[Pd].C(C)O
null
null
Cc1ncoc1C(C)(N=[N+]=[N-])c1ccoc1>[Pd].C(C)O>Cc1ncoc1C(C)(N)c1ccoc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8bbdc1d08b854285b965d5186398def4
COc1ccc(CCN)cc1.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>>COc1ccc(CCN=C=O)cc1
COC1=CC=C(C=C1)CCN.ClC(Cl)(OC(OC(Cl)(Cl)Cl)=O)Cl>>COC1=CC=C(C=C1)CCN=C=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][NH2:9])[cH:12][cH:13]1.ClC(Cl)(Cl)O[C:10](OC(Cl)(Cl)Cl)=[O:11]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][N:9]=[C:10]=[O:11])[cH:12][cH:13]1
COc1ccc(CCN)cc1.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl
COc1ccc(CCN=C=O)cc1
null
null
O1CCCC1
Miscellaneous
OtherReaction
38334b31448e1d8428e2cb6569eceaecc2305b2359c734a98433aa0746ff9140
a539b8d5e65abe163774733461d6850ba8234d38df1df3c2ccdeef5ce9de389b
c1ccccc1
Cl-C(-Cl)(-Cl)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-O-C(-Cl)(-Cl)-Cl.[C:3]-[C:4]-[NH2;D1;+0:5]>>[C:3]-[C:4]-[N;H0;D2;+0:5]=[C;H0;D2;+0:1]=[O;D1;H0:2]
0.1
[{"value": 0.1, "product": "COC1=CC=C(C=C1)CCN=C=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4.53 g (30 mol) of 4-methoxy-β-phenylethylamine are added dropwise to a solution of 2.96 g (10.0 mol) of triphosgene in 30 ml of dry tetrahydrofuran and the mixture is heated at the boiling point for 2 hours. The solution is cooled to room temperature and filtered and the filtrate is concentrated in vacuo. The colorles...
10.6084/m9.figshare.5104873.v1
null
Trichloro group.Trichloro group.Carbonic Ester.Primary amine
Isocyanate
null
null
c1ccccc1
HCl
O1CCCC1
null
null
COc1ccc(CCN)cc1.O=C(OC(Cl)(Cl)Cl)OC(Cl)(Cl)Cl>O1CCCC1>COc1ccc(CCN=C=O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ee33145d3712452584d543409e62c64a
C[Si](C)(C)OCCNCCO[Si](C)(C)C.O=S(=O)(Cl)c1ccccc1>>C[Si](C)(C)OCCN(CCO[Si](C)(C)C)S(=O)(=O)c1ccccc1
C[Si](C)(C)OCCNCCO[Si](C)(C)C.C(C)N(CC)CC.C1(=CC=CC=C1)S(=O)(=O)Cl>>C[Si](OCCN(S(=O)(=O)C1=CC=CC=C1)CCO[Si](C)(C)C)(C)C
[CH3:1][Si:2]([CH3:3])([CH3:4])[O:5][CH2:6][CH2:7][NH:8][CH2:9][CH2:10][O:11][Si:12]([CH3:13])([CH3:14])[CH3:15].Cl[S:16](=[O:17])(=[O:18])[c:19]1[cH:20][cH:21][cH:22][cH:23][cH:24]1>>[CH3:1][Si:2]([CH3:3])([CH3:4])[O:5][CH2:6][CH2:7][N:8]([CH2:9][CH2:10][O:11][Si:12]([CH3:13])([CH3:14])[CH3:15])[S:16](=[O:17])(=[O:18]...
C[Si](C)(C)OCCNCCO[Si](C)(C)C.O=S(=O)(Cl)c1ccccc1
C[Si](C)(C)OCCN(CCO[Si](C)(C)C)S(=O)(=O)c1ccccc1
null
null
C1=CC=CC=C1
Acylation
Sulfonamide synthesis (Schotten-Baumann) secondary amine
abeb6d9a0c70fe5baef0a8e555c2cd55ac2317f763ce7a0831775db7a04777d8
b7aca5a5d690b0846685a854bc946849e1041bfc3965161290b5ffb2821af09e
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6].[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]>>[C:7]-[C:8]-[N;H0;D3;+0:9](-[C:10]-[C:11])-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
88
[{"value": 88.0, "product": "C[Si](OCCN(S(=O)(=O)C1=CC=CC=C1)CCO[Si](C)(C)C)(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
To a mixture of 4.97 g of bis(2-trimethylsilyloxylethyl)amine, 3.03 g of triethylamine and 50 ml of benzene, 3.21 g of benzenesulfonyl chloride was added at 0° C. under stirring. After the addition, the mixture was taken out of the cooling bath and stirred further for 2 hours. The reaction mixture was filtered, mixture...
10.6084/m9.figshare.5104873.v1
null
Secondary amine.Sulfonyl halide
Tertiary amine
null
null
c1ccccc1
HCl
C1=CC=CC=C1
null
null
C[Si](C)(C)OCCNCCO[Si](C)(C)C.O=S(=O)(Cl)c1ccccc1>C1=CC=CC=C1>C[Si](C)(C)OCCN(CCO[Si](C)(C)C)S(=O)(=O)c1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-39d007a1ceb040768775ffb5002a1d9e
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
[Si](C)(C)(C(C)(C)C)OCCN(S(=O)(=O)C1=C(C=CC(=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)[Bi](C1=C(C=C(C=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)C1=C(C=C(C=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)S(N(CCO[Si](C)(C)C(...
CC(C)(C)[Si](C)(C)[O:19][CH2:18][CH2:17][N:16]([S:13]([c:12]1[cH:11][cH:10][c:9]([Bi:8]([c:7]2[cH:6][cH:5][c:4]([S:2](=[O:1])(=[O:3])[N:73]([CH2:74][CH2:75][O:76][Si](C)(C)C(C)(C)C)[CH2:77][CH2:78][O:79][Si](C)(C)C(C)(C)C)[cH:72][c:61]2[S:62](=[O:63])(=[O:64])[N:65]([CH2:66][CH2:67][O:68][Si](C)(C)C(C)(C)C)[CH2:69][CH2...
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
O=S(=O)(c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO)CCO)cc2S(=O)(=O)N(CCO)CCO)[c]2ccc(S(=O)(=O)N(CCO)CCO)cc2S(=O)(=O)N(CCO)CCO)c(S(=O)(=O)N(CCO)CCO)c1)N(CCO)CCO
null
null
ClCCl
Acylation
OtherReaction
359bed4e3c72098746a78db3da27cb1c0b97b319d671d22f5a85b7ad088942cb
599c6070da98d6760709ea4de50e837637a1694af54ce586f2fc58936c993de1
c1cc[c]([Bi]([c]2ccccc2)[c]2ccccc2)cc1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-[C:2]-[C:3].C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:4]-[C:5]-[C:6].C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:7]-[C:8]-[C:9].C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:10]-[C:11]-[C:12].C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:13]-[C:14]-[C:15].C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:16]-[C:17]-[C:18]...
79.5
[{"value": 79.5, "product": "OCCN(S(=O)(=O)C1=C(C=CC(=C1)S(N(CCO)CCO)(=O)=O)[Bi](C1=C(C=C(C=C1)S(N(CCO)CCO)(=O)=O)S(N(CCO)CCO)(=O)=O)C1=C(C=C(C=C1)S(N(CCO)CCO)(=O)=O)S(N(CCO)CCO)(=O)=O)CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
50
CELSIUS
null
null
13.59 g of the tris(2,4-bis(N,N-bis(2-t-butyldimethylsilyloxyethyl)sulfamoyl)phenyl)bismuthine preparation prepared in Example 5 was dissolved in a mixed solvent containing 13.6 ml of ethanol and 27 ml of dichloromethane, and 0.272 g of p-toluenesulfonic acid monohydrate was added thereto. The mixture was refluxed unde...
10.6084/m9.figshare.5104873.v1
null
Tosylate.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether prot...
Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol
c1ccccc1
null
c1ccccc1.c1ccccc1.c1ccccc1
TsOH.HO-
ClCCl
50
null
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3672ccce920d49079a5e6ae5ceeb8bc3
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
[Si](C)(C)(C(C)(C)C)OCCN(S(=O)(=O)C1=C(C=CC(=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)[Bi](C1=C(C=C(C=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)C1=C(C=C(C=C1)S(N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)(=O)=O)S(N(CCO[Si](C)(C)C(...
CC(C)(C)[Si](C)(C)[O:19][CH2:18][CH2:17][N:16]([S:13]([c:12]1[cH:11][cH:10][c:9]([Bi:8]([c:7]2[cH:6][cH:5][c:4]([S:2](=[O:1])(=[O:3])[N:73]([CH2:74][CH2:75][O:76][Si](C)(C)C(C)(C)C)[CH2:77]C[O:71][Si](C)(C)C(C)(C)C)[cH:72][c:61]2[S:62](=[O:63])(=[O:64])[N:65]([CH2:66][CH2:78][O:79][Si](C)(C)C(C)(C)C)[CH2:69][CH2:70][O:...
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
O=S(=O)(c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO)CCO)cc2S(=O)(=O)N(CCO)CCO)[c]2ccc(S(=O)(=O)N(CCO)CCO)cc2S(=O)(=O)N(CCO)CCO)c(S(=O)(=O)N(CCO)CCO)c1)N(CCO)CCO
null
null
O1CCCC1
Heteroatom Alkylation and Arylation
OtherReaction
27071b625f155943525e8e1dca0bcfaee51b4f12629eef0a240fd7b9410de62b
8da181d42bd002294543811ee0c10c300809942818f884161cd413d2680745af
c1cc[c]([Bi]([c]2ccccc2)[c]2ccccc2)cc1
C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:1]-C-[CH2;D2;+0:2]-[#7:3](-[#16:4])-[C:5]-[C:6]-[O;H0;D2;+0:7]-[Si](-C)(-C)-C(-C)(-C)-C.C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:8]-[CH2;D2;+0:9]-[C:10]-[#7:11](-[#16:12])-[CH2;D2;+0:13]-[CH2;D2;+0:14]-[O;H0;D2;+0:15]-[Si](-C)(-C)-C(-C)(-C)-C.C-C(-C)(-C)-[Si](-C)(-C)-[O;H0;D2;+0:16]-[C:...
94.7
[{"value": 94.7, "product": "OCCN(S(=O)(=O)C1=C(C=CC(=C1)S(N(CCO)CCO)(=O)=O)[Bi](C1=C(C=C(C=C1)S(N(CCO)CCO)(=O)=O)S(N(CCO)CCO)(=O)=O)C1=C(C=C(C=C1)S(N(CCO)CCO)(=O)=O)S(N(CCO)CCO)(=O)=O)CCO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
-30
CELSIUS
null
null
A solution of 1.38 g of the tris(2,4-bis(N,N-bis(2-t-butyldimethylsilyloxyethyl)sulfamoyl)phenyl)bismuthine preparation obtained in Example 5 in 15 ml of tetrahydrofuran was cooled to -30° C., and 5.88 ml of a 1 M/1 tetrahydrofuran solution of tetra-n-butylammonium fluoride was gradually added droprise under stirring. ...
10.6084/m9.figshare.5104873.v1
null
TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective group.TMS ether protective gr...
Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol.Primary alcohol
null
null
c1ccccc1.c1ccccc1.c1ccccc1
Other
O1CCCC1
-30
null
CC(C)(C)[Si](C)(C)OCCN(CCO[Si](C)(C)C(C)(C)C)S(=O)(=O)c1cc[c]([Bi]([c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)[c]2ccc(S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)cc2S(=O)(=O)N(CCO[Si](C)(C)C(C)(C)C)CCO[Si](C)(C)C(C)(C)C)c(S(=O)(=O)...
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-51c44092234a4bbebe6940b7ac132c46
CCNCC.CCOC(=O)CC(C)=O>>CCN(CC)C(=O)CC(C)=O
C(CC(=O)C)(=O)OCC.C(C)NCC>>C(C)N(C(CC(C)=O)=O)CC
[CH3:1][CH2:2][NH:3][CH2:4][CH3:5].CCO[C:6](=[O:7])[CH2:8][C:9]([CH3:10])=[O:11]>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[CH2:8][C:9]([CH3:10])=[O:11]
CCNCC.CCOC(=O)CC(C)=O
CCN(CC)C(=O)CC(C)=O
null
null
null
Acylation
Aminolysis of esters
d147787750807073759132276086de98566af6772417f9288b6300bf1de7801c
fa66342dd118fe5531ba6a998ac8fab92d2b0db4fd04688560eec7d04e9be0e4
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6].[C;D1;H3:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C;D1;H3:11]>>[C;D1;H3:5]-[C:4](=[O;D1;H0:6])-[C:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D3;+0:9](-[C:8]-[C;D1;H3:7])-[C:10]-[C;D1;H3:11]
65.7
[{"value": 65.7, "product": "C(C)N(C(CC(C)=O)=O)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
40 g (0.31 mol) of ethyl acetoacetate and 24 g (0.33 mol) of diethylamine were stirred in a Parr apparatus at 150° C. for 10'. The crude mixture was distilled at 115°-120° C./9 mmHg, to give 32 g of the title compound. Conditions: See reaction.notes.procedure_details. Workup: The crude mixture was distilled at 115°-120...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine
Tertiary amide
null
null
null
HO-
null
null
null
CCNCC.CCOC(=O)CC(C)=O>>CCN(CC)C(=O)CC(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-70526c16165b456992991e767fe845d3
CCN(CC)C(=O)CC(C)=O.N#[N+]c1ccccc1>>CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O
[Cl-].C1(=CC=CC=C1)[N+]#N.C(C)N(C(CC(C)=O)=O)CC.CC(=O)O[Na].O>>C(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[CH2:8][C:17]([CH3:18])=[O:19].[N:9]#[N+:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[C:8](=[N:9][NH:10][c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1)[C:17]([CH3:18])=[O:19]
CCN(CC)C(=O)CC(C)=O.N#[N+]c1ccccc1
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O
null
null
C(C)O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
c1ccccc1
[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[CH2;D2;+0:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9].[N;H0;D1;+0:10]#[N+;H0;D2:11]-[c:12](:[c:13]):[c:14]>>[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[C;H0;D3;+0:6](=[N;H0;D2;+0:10]-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
null
[]
10
CELSIUS
null
null
15.7 g (0.1 mol) of N,N-diethyl-3-oxobutyramide were mixed with 12 g (0.14 mol) of CH3COONa, 20 ml of water and 75 ml of ethanol. The solution obtained was cooled to 10° C. and 0.1 mol of freshly prepared solution of phenyldiazonium chloride [Organic Reactions, R. Adams Ed; Wiley, New York, 10, 32-33, (1951-1959)] were...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1
null
C(C)O
10
null
CCN(CC)C(=O)CC(C)=O.N#[N+]c1ccccc1>C(C)O>CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9d861ba9b54b4ef8a7a1d9b237766965
CCCNCCC.CCOC(=O)CC(C)=O>>CCCN(CCC)C(=O)CC(C)=O
C(CC(=O)C)(=O)OCC.C(CC)NCCC>>C(CC)N(C(CC(C)=O)=O)CCC
[CH3:1][CH2:2][CH2:3][NH:4][CH2:5][CH2:6][CH3:7].CCO[C:8](=[O:9])[CH2:10][C:11]([CH3:12])=[O:13]>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[C:8](=[O:9])[CH2:10][C:11]([CH3:12])=[O:13]
CCCNCCC.CCOC(=O)CC(C)=O
CCCN(CCC)C(=O)CC(C)=O
null
null
null
Acylation
Aminolysis of esters
d147787750807073759132276086de98566af6772417f9288b6300bf1de7801c
fa66342dd118fe5531ba6a998ac8fab92d2b0db4fd04688560eec7d04e9be0e4
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6].[C:7]-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]>>[C:7]-[C:8]-[N;H0;D3;+0:9](-[C:10]-[C:11])-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6]
0.6
[{"value": 0.6, "product": "C(CC)N(C(CC(C)=O)=O)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
43.4 g (43.3 mol) of ethyl acetoacetate and 33.7 g (43.3 mol) of dipropylamine were treated as described in preparation 1. The crude oil was distilled at 86°-89° C./ 0.8 mmHg, to give 44.3 g of the title compound. Conditions: See reaction.notes.procedure_details. Workup: as described in preparation 1; The crude oil was...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine
Tertiary amide
null
null
null
HO-
null
null
null
CCCNCCC.CCOC(=O)CC(C)=O>>CCCN(CCC)C(=O)CC(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-549c90cb2eaf4302a24586469500c664
CCCN(CCC)C(=O)CC(C)=O.N#[N+]c1ccccc1>>CCCN(CCC)C(=O)C(=NNc1ccccc1)C(C)=O
C(CC)N(C(CC(C)=O)=O)CCC.CC(=O)O[Na].O.[Cl-].C1(=CC=CC=C1)[N+]#N>>C(CC)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CCC
[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[C:8](=[O:9])[CH2:10][C:19]([CH3:20])=[O:21].[N:11]#[N+:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[C:8](=[O:9])[C:10](=[N:11][NH:12][c:13]1[cH:14][cH:15][cH:16][cH:17][cH:18]1)[C:19]([CH3:20])=[O:21]
CCCN(CCC)C(=O)CC(C)=O.N#[N+]c1ccccc1
CCCN(CCC)C(=O)C(=NNc1ccccc1)C(C)=O
null
null
C(C)O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
c1ccccc1
[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[CH2;D2;+0:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9].[N;H0;D1;+0:10]#[N+;H0;D2:11]-[c:12](:[c:13]):[c:14]>>[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[C;H0;D3;+0:6](=[N;H0;D2;+0:10]-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
14.5
[{"value": 14.5, "product": "C(CC)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
18.5 g (0.1 mol) of N,N-dipropyl-3-oxobutyramide, 12 g (0.146 mol) of CH3COONa, 20 ml of water, 75 ml of ethanol and a solution of 0.1 mol of phenyldiazonium chloride were treated as described in preparation 2. The precipitated solid was filtered and dried in vacuo yielding 4.2 g of the title compound. M.p.=79°-80° C. ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1
null
C(C)O
null
null
CCCN(CCC)C(=O)CC(C)=O.N#[N+]c1ccccc1>C(C)O>CCCN(CCC)C(=O)C(=NNc1ccccc1)C(C)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-78feaec48f454c398ecf0ddf11da5e02
CC(C)CO.CCOC(=O)CC(C)=O>>CC(=O)CC(=O)OCC(C)C
C(CC(=O)C)(=O)OCC.C(C(C)C)O.C1(=CC=C(C=C1)S(=O)(=O)O)C>>C(CC(=O)C)(=O)OCC(C)C
[OH:7][CH2:8][CH:9]([CH3:10])[CH3:11].CCO[C:5]([CH2:4][C:2]([CH3:1])=[O:3])=[O:6]>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[O:7][CH2:8][CH:9]([CH3:10])[CH3:11]
CC(C)CO.CCOC(=O)CC(C)=O
CC(=O)CC(=O)OCC(C)C
null
null
null
Acylation
Transesterification
c42e047d71ad2593a6d29093d1fe2ca16ccfd6db7b15eecf1eab340181aef83e
cb08be6428b0a3737df44d00995165c06a05fb7dec4fab744c09315c4f7771d4
null
C-C-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6].[C:7]-[C:8]-[OH;D1;+0:9]>>[C:7]-[C:8]-[O;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[C:3]-[C:4](-[C;D1;H3:5])=[O;D1;H0:6]
null
[]
null
null
null
null
30 ml of ethyl acetoacetate were dissolved in 350 ml of i-butyl alcohol and a catalytic amount of p-toluensulphonic acid (PTSA) was added. The solution was refluxed for 18 h. The reaction mixture was evaporated in vacuo and the residue was dissolved in ether. The resulted solution was treated with s.s. NaHCO3. The orga...
10.6084/m9.figshare.5104873.v1
null
Ester.Primary alcohol
Ester
null
null
null
HO-
null
null
null
CC(C)CO.CCOC(=O)CC(C)=O>>CC(=O)CC(=O)OCC(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eb91f88045c44fa2ba05b793165e13a8
CC(=O)CC(=O)OCC(C)C.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(=O)OCC(C)C
C(CC(=O)C)(=O)OCC(C)C.O.[Cl-].C1(=CC=CC=C1)[N+]#N>>C1(=CC=CC=C1)NN=C(C(=O)OCC(C)C)C(C)=O
[CH3:1][C:2](=[O:3])[CH2:4][C:13](=[O:14])[O:15][CH2:16][CH:17]([CH3:18])[CH3:19].[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13](=[O:14])[O:15][CH2:16][CH:17]([CH3:18])[CH3:19]
CC(=O)CC(=O)OCC(C)C.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(=O)OCC(C)C
null
null
C(C)O
Functional Group Addition
OtherReaction
ac990c1d08488fa2e65d155d0c3fe4275090c987d9bb341129ddd972268410d2
b6b5844d1b47f1f414d9a8547509e4caf3076e8d8ccfaed07a6c1e5bfa92686d
c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8].[N;H0;D1;+0:9]#[N+;H0;D2:10]-[c:11](:[c:12]):[c:13]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:5](=[N;H0;D2;+0:9]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[C:6](-[C;D1;H3:7])=[O;D1;H0:8]
88.1
[{"value": 88.1, "product": "C1(=CC=CC=C1)NN=C(C(=O)OCC(C)C)C(C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
15.8 g (0.1 mol) of i-butyl acetoacetate, 12 g (0.146 mol) of CH3 COONa, 20 ml of water, 75 ml of ethanol and a solution of 0.1 mol of phenyldiazonium chloride were treated as described in preparation 2. The precipitated solid was filtered an dried in vacuo yielding 23.1 g of the title compound. M.p.=45°-50° C. Conditi...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Hydrazone
null
null
c1ccccc1
null
C(C)O
null
null
CC(=O)CC(=O)OCC(C)C.N#[N+]c1ccccc1>C(C)O>CC(=O)C(=NNc1ccccc1)C(=O)OCC(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f260c158922847e2b6dce05f84aaf68d
CC1=CC(=O)OC(C)(C)O1.NCc1ccccc1>>CC(=O)CC(=O)NCc1ccccc1
CC1(OC(=CC(O1)=O)C)C.C(C1=CC=CC=C1)N>>C(C1=CC=CC=C1)NC(CC(C)=O)=O
CC1(C)O[C:5](=[O:6])[CH:4]=[C:2]([CH3:1])[O:3]1.[NH2:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[NH:7][CH2:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1
CC1=CC(=O)OC(C)(C)O1.NCc1ccccc1
CC(=O)CC(=O)NCc1ccccc1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
d3497dc1fa1b901da02291a01ed87bb0f2a9e66617453ae54be3d88b09104f0d
60464cf75aa3f9019baecc3c3022956a9a8a68b3326c8dcc2d0679ff3c32da26
c1ccccc1
C-C1(-C)-O-[C;H0;D3;+0:1](=[O;D1;H0:2])-[CH;D2;+0:3]=[C;H0;D3;+0:4](-[C;D1;H3:5])-[O;H0;D2;+0:6]-1.[NH2;D1;+0:7]-[C:8]-[c:9]>>[C;D1;H3:5]-[C;H0;D3;+0:4](=[O;H0;D1;+0:6])-[CH2;D2;+0:3]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[NH;D2;+0:7]-[C:8]-[c:9]
null
[]
null
null
null
null
9 ml (0.05 mol) of 2,2,6-trimethyl-4H-1,3-dioxin-4-one (diketene-acetone adduct) were added dropwise to a solution of 5.5 ml (0.05 mol) of benzylamine in 20 ml of toluene and the temperature was allowed to rise 70° C. The solution was refluxed for 2 h then the solvent was removed in vacuo. The crude product was tritura...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Primary amine
Ketone.Secondary amide
C1=COCOC1
null
c1ccccc1
HO-
C1(=CC=CC=C1)C
null
null
CC1=CC(=O)OC(C)(C)O1.NCc1ccccc1>C1(=CC=CC=C1)C>CC(=O)CC(=O)NCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-24aef19954464872a4172777d7b361e8
CC(=O)CC(=O)NCc1ccccc1.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1
[Cl-].C1(=CC=CC=C1)[N+]#N.C(C1=CC=CC=C1)NC(CC(C)=O)=O.[OH-].[Na+]>>C(C1=CC=CC=C1)NC(C(C(C)=O)=NNC1=CC=CC=C1)=O
[CH3:1][C:2](=[O:3])[CH2:4][C:13](=[O:14])[NH:15][CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1.[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13](=[O:14])[NH:15][CH2:16][c:17]1[cH:18][cH:19][cH:20][cH:21][cH:22]1
CC(=O)CC(=O)NCc1ccccc1.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1
null
null
O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
O=C(C=NNc1ccccc1)NCc1ccccc1
[C:1]-[#7:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[C:6](-[C;D1;H3:7])=[O;D1;H0:8].[N;H0;D1;+0:9]#[N+;H0;D2:10]-[c:11](:[c:12]):[c:13]>>[C:1]-[#7:2]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:5](=[N;H0;D2;+0:9]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[C:6](-[C;D1;H3:7])=[O;D1;H0:8]
null
[]
null
null
null
null
7.27 g (0.038) of N-benzyl-3-oxobutyramide were dissolved in a solution of 5.32 g (0.133 mol) of NaOH in 58 ml of water. To the ice-cooled stirred solution, 0.040 mol of phenyldiazonium chloride were added dropwise at such a rate as to keep the temperature at 0° C. The precipitated solid was filtered and recrystallised...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1.c1ccccc1
null
O
null
null
CC(=O)CC(=O)NCc1ccccc1.N#[N+]c1ccccc1>O>CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fc50405695d1443a80eda06a3dd99d45
C1CCNC1.C=C1CC(=O)O1>>CC(=O)CC(=O)N1CCCC1
C=C1CC(=O)O1.CC(=O)C.N1CCCC1>>O=C(CC(=O)N1CCCC1)C
[NH:7]1[CH2:8][CH2:9][CH2:10][CH2:11]1.[CH2:1]=[C:2]1[O:3][C:5](=[O:6])[CH2:4]1>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[N:7]1[CH2:8][CH2:9][CH2:10][CH2:11]1
C1CCNC1.C=C1CC(=O)O1
CC(=O)CC(=O)N1CCCC1
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
1993eb37d80a920c8fe458a795d74455bf51017aa874ab2592fe04454f920492
9efa0c835be0aa9453aa895a9d5c6a73c10e08e695158204e8f0348795b4fe67
C1CCNC1
[CH2;D1;+0:1]=[C;H0;D3;+0:2]1-[C:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[O;H0;D2;+0:6]-1.[C:7]1-[C:8]-[NH;D2;+0:9]-[C:10]-[C:11]-1>>[CH3;D1;+0:1]-[C;H0;D3;+0:2](=[O;H0;D1;+0:6])-[C:3]-[C;H0;D3;+0:4](=[O;D1;H0:5])-[N;H0;D3;+0:9]1-[C:8]-[C:7]-[C:11]-[C:10]-1
97.9
[{"value": 97.9, "product": "O=C(CC(=O)N1CCCC1)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
9 ml (0.05 mol) of diketene-acetone adduct and a solution of 4.2 ml (0.05 mol) of pyrrolidine in 20 ml of toluene were treated as described in preparation 7. The solvent was removed in vacuo and the residue was purified by chromatography on silica gel (EtOAc/MeOH 0%→1%) yielding 7.6 g of the title compound as a dark oi...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine.Vinyl
Ketone.Tertiary amide
C1CCNC1.C1COC1
C1CC[NH]C1
C1CC[NH]C1
null
C1(=CC=CC=C1)C
null
null
C1CCNC1.C=C1CC(=O)O1>C1(=CC=CC=C1)C>CC(=O)CC(=O)N1CCCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f388a24479e44c98bc290884466e1ad3
CC(=O)CC(=O)Nc1ccccc1.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1
C(CC(=O)C)(=O)NC1=CC=CC=C1.[OH-].[Na+].[Cl-].C1(=CC=CC=C1)[N+]#N>>C1(=CC=CC=C1)NC(C(C(C)=O)=NNC1=CC=CC=C1)=O
[CH3:1][C:2](=[O:3])[CH2:4][C:13](=[O:14])[NH:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1.[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13](=[O:14])[NH:15][c:16]1[cH:17][cH:18][cH:19][cH:20][cH:21]1
CC(=O)CC(=O)Nc1ccccc1.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1
null
null
O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
O=C(C=NNc1ccccc1)Nc1ccccc1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[C:5](=[O;D1;H0:6])-[#7:7]-[c:8].[N;H0;D1;+0:9]#[N+;H0;D2:10]-[c:11](:[c:12]):[c:13]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[C;H0;D3;+0:4](=[N;H0;D2;+0:9]-[NH;D2;+0:10]-[c:11](:[c:12]):[c:13])-[C:5](=[O;D1;H0:6])-[#7:7]-[c:8]
47.6
[{"value": 47.6, "product": "C1(=CC=CC=C1)NC(C(C(C)=O)=NNC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4.5 g (25.4 mmol) of acetoacetanilide, a solution of 3.46 g (89 mmol) of NaOH in 45 ml of water and 95 mmol of phenyldiazonium chloride were treated as described in preparation 8. The residue was crystallised from EtOH, yielding 3.4 g of the title compound. M.p.=96°-97° C. Conditions: See reaction.notes.procedure_detai...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1.c1ccccc1
null
O
null
null
CC(=O)CC(=O)Nc1ccccc1.N#[N+]c1ccccc1>O>CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-eb592b1203c74e969732293b7513ee02
C=C1CC(=O)O1.CNC>>CC(=O)CC(=O)N(C)C
C=C1CC(=O)O1.CC(=O)C.CNC>>CN(C(CC(C)=O)=O)C
[CH2:1]=[C:2]1[O:3][C:5](=[O:6])[CH2:4]1.[NH:7]([CH3:8])[CH3:9]>>[CH3:1][C:2](=[O:3])[CH2:4][C:5](=[O:6])[N:7]([CH3:8])[CH3:9]
C=C1CC(=O)O1.CNC
CC(=O)CC(=O)N(C)C
null
null
C1(=CC=CC=C1)C
Acylation
OtherReaction
064f44e0040954705f8be5256a3aced414ff315ce6eb541c993cd172d38561e4
9efa0c835be0aa9453aa895a9d5c6a73c10e08e695158204e8f0348795b4fe67
null
[C;D1;H3:1]-[NH;D2;+0:2]-[C;D1;H3:3].[CH2;D1;+0:4]=[C;H0;D3;+0:5]1-[C:6]-[C;H0;D3;+0:7](=[O;D1;H0:8])-[O;H0;D2;+0:9]-1>>[C;D1;H3:1]-[N;H0;D3;+0:2](-[C;D1;H3:3])-[C;H0;D3;+0:7](=[O;D1;H0:8])-[C:6]-[C;H0;D3;+0:5](-[CH3;D1;+0:4])=[O;H0;D1;+0:9]
null
[]
null
null
null
null
A solution of 9 ml (0.05 mmol) of diketene-acetone adduct in 20 ml of toluene was treated with gaseous dimethylamine at room temperature until the reaction was complete. The solvent was removed in vacuo and the residue was purified by chromatography on silica gel (EtOAc/MeOH 0%→10%) yielding 7.0 g of the title compound...
10.6084/m9.figshare.5104873.v1
null
Ester.Secondary amine.Vinyl
Ketone.Tertiary amide
C1COC1
null
null
null
C1(=CC=CC=C1)C
null
null
C=C1CC(=O)O1.CNC>C1(=CC=CC=C1)C>CC(=O)CC(=O)N(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b070703fd73b4d8680fe6f71c91c67d7
CC(=O)CC(=O)N(C)C.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(=O)N(C)C
CN(C(CC(C)=O)=O)C.[OH-].[Na+].[Cl-].C1(=CC=CC=C1)[N+]#N>>CN(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)C
[CH3:1][C:2](=[O:3])[CH2:4][C:13](=[O:14])[N:15]([CH3:16])[CH3:17].[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13](=[O:14])[N:15]([CH3:16])[CH3:17]
CC(=O)CC(=O)N(C)C.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(=O)N(C)C
null
null
O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
c1ccccc1
[C;D1;H3:1]-[#7:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[CH2;D2;+0:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9].[N;H0;D1;+0:10]#[N+;H0;D2:11]-[c:12](:[c:13]):[c:14]>>[C;D1;H3:1]-[#7:2](-[C;D1;H3:3])-[C:4](=[O;D1;H0:5])-[C;H0;D3;+0:6](=[N;H0;D2;+0:10]-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
42.9
[{"value": 42.9, "product": "CN(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
4.5 g (0.035 mol) of N,N-dimethyl-3-oxobutyramide, a solution of 4.9 g (0.122 mol) of NaOH in 45 ml of water and 0.037 mol of phenyldiazonium chloride were treated as described in preparation 8. The crude reaction mixture was purified by chromatography on silica gel (hexane/Et2O 0%→100%) obtaining 3.5 g of the title co...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1
null
O
null
null
CC(=O)CC(=O)N(C)C.N#[N+]c1ccccc1>O>CC(=O)C(=NNc1ccccc1)C(=O)N(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-fa496a7ce126439c8a04c703ffcedc08
CC(=O)CC(N)=O.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(N)=O
O=C(CC(=O)N)C.[OH-].[Na+].[Cl-].C1(=CC=CC=C1)[N+]#N>>C1(=CC=CC=C1)NN=C(C(=O)N)C(C)=O
[CH3:1][C:2](=[O:3])[CH2:4][C:13]([NH2:14])=[O:15].[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13]([NH2:14])=[O:15]
CC(=O)CC(N)=O.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(N)=O
null
null
O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
c1ccccc1
[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[CH2;D2;+0:4]-[C:5](-[N;D1;H2:6])=[O;D1;H0:7].[N;H0;D1;+0:8]#[N+;H0;D2:9]-[c:10](:[c:11]):[c:12]>>[C;D1;H3:1]-[C:2](=[O;D1;H0:3])-[C;H0;D3;+0:4](=[N;H0;D2;+0:8]-[NH;D2;+0:9]-[c:10](:[c:11]):[c:12])-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]
null
[]
null
null
null
null
5.0 g (0.049 mol) of 3-oxobutyramide, a solution of 6.9 g (0.171 mol) of NaOH in 75 ml of water and 0.051 mol of phenyldiazonium chloride were treated as described in preparation 8. The crude reaction mixture was purified by chromatography on silica gel(EtOAc) obtaining 3 g of the title compound which was used as such ...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1
null
O
null
null
CC(=O)CC(N)=O.N#[N+]c1ccccc1>O>CC(=O)C(=NNc1ccccc1)C(N)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ee71b009ed3f4c28bab5abd1c42abd9d
CC(=O)CC(=O)N(C(C)C)C(C)C.N#[N+]c1ccccc1>>CC(=O)C(=NNc1ccccc1)C(=O)N(C(C)C)C(C)C
C(C)(C)N(C(CC(C)=O)=O)C(C)C.[OH-].[Na+].[Cl-].C1(=CC=CC=C1)[N+]#N>>C(C)(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)C(C)C
[CH3:1][C:2](=[O:3])[CH2:4][C:13](=[O:14])[N:15]([CH:16]([CH3:17])[CH3:18])[CH:19]([CH3:20])[CH3:21].[N:5]#[N+:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][C:2](=[O:3])[C:4](=[N:5][NH:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1)[C:13](=[O:14])[N:15]([CH:16]([CH3:17])[CH3:18])[CH:19]([CH3:20])[CH3:21]
CC(=O)CC(=O)N(C(C)C)C(C)C.N#[N+]c1ccccc1
CC(=O)C(=NNc1ccccc1)C(=O)N(C(C)C)C(C)C
null
null
O
Functional Group Addition
OtherReaction
7ec843ece642d406b254050374a9acdeded6ee16c74f2d78979f305a41c35216
ea063a30965cc9c0238244fbd3133685f07e51f73fbeaf7c962038081c44c705
c1ccccc1
[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[CH2;D2;+0:6]-[C:7](-[C;D1;H3:8])=[O;D1;H0:9].[N;H0;D1;+0:10]#[N+;H0;D2:11]-[c:12](:[c:13]):[c:14]>>[C:1]-[#7:2](-[C:3])-[C:4](=[O;D1;H0:5])-[C;H0;D3;+0:6](=[N;H0;D2;+0:10]-[NH;D2;+0:11]-[c:12](:[c:13]):[c:14])-[C:7](-[C;D1;H3:8])=[O;D1;H0:9]
68.2
[{"value": 68.2, "product": "C(C)(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)C(C)C", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
7.0 g (0.038 mol) of N,N-diisopropyl-3-oxobutyramide, a solution of 5.3 g (0.133 mol) of NaOH in 58 ml of water and 0.04 mol of phenyldiazonium chloride were treated as described in preparation 8. The crude reaction mixture was purified by chromatography on silica gel (hexane/Et2O 95:5) obtaining 7.5 g of the title com...
10.6084/m9.figshare.5104873.v1
null
Ketone
Hydrazone
null
null
c1ccccc1
null
O
null
null
CC(=O)CC(=O)N(C(C)C)C(C)C.N#[N+]c1ccccc1>O>CC(=O)C(=NNc1ccccc1)C(=O)N(C(C)C)C(C)C
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-5378909b6f194efbaaaae9d5077f9d43
CCOC(=O)CC(=O)C(F)(F)F.N#[N+]c1ccccc1>>CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F
CCOC(=O)CC(=O)C(F)(F)F.CC(=O)O[Na].O.[Cl-].C1(=CC=CC=C1)[N+]#N>>C1(=CC=CC=C1)NN=C(C(=O)OCC)C(C(F)(F)F)=O
[CH3:1][CH2:2][O:3][C:4](=[O:5])[CH2:6][C:15](=[O:16])[C:17]([F:18])([F:19])[F:20].[N:7]#[N+:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[C:6](=[N:7][NH:8][c:9]1[cH:10][cH:11][cH:12][cH:13][cH:14]1)[C:15](=[O:16])[C:17]([F:18])([F:19])[F:20]
CCOC(=O)CC(=O)C(F)(F)F.N#[N+]c1ccccc1
CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F
null
null
C(C)O
Functional Group Addition
OtherReaction
ac990c1d08488fa2e65d155d0c3fe4275090c987d9bb341129ddd972268410d2
b6b5844d1b47f1f414d9a8547509e4caf3076e8d8ccfaed07a6c1e5bfa92686d
c1ccccc1
[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[CH2;D2;+0:5]-[C:6](=[O;D1;H0:7])-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11].[N;H0;D1;+0:12]#[N+;H0;D2:13]-[c:14](:[c:15]):[c:16]>>[C:1]-[#8:2]-[C:3](=[O;D1;H0:4])-[C;H0;D3;+0:5](=[N;H0;D2;+0:12]-[NH;D2;+0:13]-[c:14](:[c:15]):[c:16])-[C:6](=[O;D1;H0:7])-[C:8](-[F;D1;H0:9])(-[F;D1;H...
60
[{"value": 60.0, "product": "C1(=CC=CC=C1)NN=C(C(=O)OCC)C(C(F)(F)F)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
7.3 ml (0.05 mol) of ethyl 3-oxo-4,4,4-trifluoroacetoacetate, 6 g (0.073 mol) of CH3COONa, 20 ml of water, 37.5 ml of ethanol and a solution of 0.05 mol of phenyldiazonium chloride were treated as described in preparation 2. The crude product was purified by chromatography on silica gel (hexane/Et2O 0%→25%) obtaining 8...
10.6084/m9.figshare.5104873.v1
null
Ketone.Ester
Hydrazone
null
null
c1ccccc1
null
C(C)O
null
null
CCOC(=O)CC(=O)C(F)(F)F.N#[N+]c1ccccc1>C(C)O>CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-65c40f72159b46c38bd188c224445f20
C=COC(=O)Cl.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1.Cl
C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.CN(C)C1=CC=CC2=C1C(=CC=C2)N(C)C.C(=C)OC(=O)Cl>>Cl.COC=1C=C(C=CC1)[C@@]12CCNC[C@@H]2CCC(C1)=O
C=COC(=O)[Cl:20].CC[N:11]1[CH2:10][CH2:9][C@@:8]2([c:7]3[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:19]3)[C@H:13]([CH2:12]1)[CH2:14][CH2:15][C:16](=[O:17])[CH2:18]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([C@:8]23[CH2:9][CH2:10][NH:11][CH2:12][C@@H:13]2[CH2:14][CH2:15][C:16](=[O:17])[CH2:18]3)[cH:19]1.[ClH:20]
C=COC(=O)Cl.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1.Cl
null
null
ClCCCl
Miscellaneous
OtherReaction
3772a9f4b4332669564daf911df24c9f8519db39dd2cee234af6094fd48a7fbc
0cd324a7b0205d651c1ead3697762ad8fc9df01bb471480a7b4de674230fb053
O=C1CC[C@H]2CNCC[C@]2(c2ccccc2)C1
C-C-[N;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5].C=C-O-C(=O)-[Cl;H0;D1;+0:6]>>[C:5]-[C:4]-[NH;D2;+0:1]-[C:2]-[C:3].[ClH;D0;+0:6]
70.8
[{"value": 70.8, "product": "Cl.COC=1C=C(C=CC1)[C@@]12CCNC[C@@H]2CCC(C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
15
MINUTE
A solution of 1.2 g (4.2 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline and 1.8 g (12.6 mmol) of proton sponge in 34 ml of 1,2-dichloroethane was treated with 1.4 ml (16.8 mmol) of vinylchloroformate at 0° C. under nitrogen atmosphere. The reaction mixture was stirred ...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Ether.Tertiary amine.Vinyl
Secondary amine
C1CC[C@H]2C[NH]CC[C@@H]2C1
C1CC[C@H]2CNCC[C@H]2C1
c1ccccc1.C1CC[C@H]2CNCC[C@H]2C1
HO-
ClCCCl
null
0.25
C=COC(=O)Cl.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>ClCCCl>COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1.Cl
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d8b6f19e1cf843a08f290872c0b51286
BrCC1CC1.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1>>COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1
Cl.COC=1C=C(C=CC1)[C@@]12CCNC[C@@H]2CCC(C1)=O.C1(CC1)CBr.C([O-])([O-])=O.[K+].[K+].[I-].[K+]>>Cl.C1(CC1)CN1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O
Br[CH2:12][CH:13]1[CH2:14][CH2:15]1.[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([C@:8]23[CH2:9][CH2:10][NH:11][CH2:16][C@@H:17]2[CH2:18][CH2:19][C:20](=[O:21])[CH2:22]3)[cH:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([C@:8]23[CH2:9][CH2:10][N:11]([CH2:12][CH:13]4[CH2:14][CH2:15]4)[CH2:16][C@@H:17]2[CH2:18][CH2:19][C:...
BrCC1CC1.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1
COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
c6e833cca23f118c68a36bbb41859e9d07893cc24605eee90454f4e286f04398
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1CC[C@H]2CN(CC3CC3)CC[C@]2(c2ccccc2)C1
Br-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1.[C:5]-[C:6]-[NH;D2;+0:7]-[C:8]-[C:9]>>[C:5]-[C:6]-[N;H0;D3;+0:7](-[CH2;D2;+0:1]-[C:2]1-[C:3]-[C:4]-1)-[C:8]-[C:9]
26
[{"value": 26.0, "product": "Cl.C1(CC1)CN1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.88 g (3.08 mmol) of (±)-trans-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 0.44 g (3,23 mmol) of cyclopropylmethyl bromide, 0.64 g of potassium carbonate and a catalytical amount of potassium iodide in 15.4 ml of DMF were stirred at 60° C. for 2 h. The solvent was removed in v...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CC[C@H]2CNCC[C@H]2C1
C1CC[C@H]2C[NH]CC[C@H]2C1
c1ccccc1.C1CC1.C1CC[C@H]2C[NH]CC[C@H]2C1
HBr
CN(C)C=O
null
null
BrCC1CC1.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1>CN(C)C=O>COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9cef4a5077a74084b0f66091336f0c5e
CCCCBr.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1>>CCCCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
Cl.COC=1C=C(C=CC1)[C@@]12CCNC[C@@H]2CCC(C1)=O.C(CCC)Br.C([O-])([O-])=O.[K+].[K+].[I-].[K+]>>C(CCC)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O
Br[CH2:4][CH2:3][CH2:2][CH3:1].[NH:5]1[CH2:6][CH2:7][C@:8]2([c:9]3[cH:10][cH:11][cH:12][c:13]([O:14][CH3:15])[cH:16]3)[CH2:17][C:18](=[O:19])[CH2:20][CH2:21][C@H:22]2[CH2:23]1>>[CH3:1][CH2:2][CH2:3][CH2:4][N:5]1[CH2:6][CH2:7][C@:8]2([c:9]3[cH:10][cH:11][cH:12][c:13]([O:14][CH3:15])[cH:16]3)[CH2:17][C:18](=[O:19])[CH2:2...
CCCCBr.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1
CCCCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
null
null
CN(C)C=O
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
62ec5e6cc7d6988505f056dcfa4f57f44a5c16cd7a5130d4ceb03a3c06191c3a
523d37155b42c8dc851abeddadebb241cdd90bdf649ba750c35e13c8c752d7b0
O=C1CC[C@H]2CNCC[C@]2(c2ccccc2)C1
Br-[CH2;D2;+0:1]-[C:2]-[C:3].[C:4]-[C:5]-[NH;D2;+0:6]-[C:7]-[C:8]>>[C:4]-[C:5]-[N;H0;D3;+0:6](-[CH2;D2;+0:1]-[C:2]-[C:3])-[C:7]-[C:8]
24.9
[{"value": 24.9, "product": "C(CCC)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.71 g (2.55 mmol) of (±)-trans-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8, 8a-decahydroisoquinoline hydrochloride, 0.37 g (2.68 mmol) of butyl bromide, 0.53 g of potassium carbonate and a catalytical amount of potassium iodide in 15 ml of DMF were reacted as described in preparation 20, yielding 0.2 g of the title ...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Secondary amine
Tertiary amine
C1CC[C@H]2CNCC[C@@H]2C1
C1CC[C@H]2C[NH]CC[C@@H]2C1
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
HBr
CN(C)C=O
null
null
CCCCBr.COc1cccc([C@]23CCNC[C@@H]2CCC(=O)C3)c1>CN(C)C=O>CCCCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4eac917dd565431a9f46b59b364b582d
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.NO>>CCN1CC[C@]2(c3cccc(OC)c3)CC(=NO)CC[C@H]2C1
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.Cl.NO>>C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=NO
O=[C:16]1[CH2:15][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]3)[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:22][C@@H:21]2[CH2:20][CH2:19]1.[NH2:17][OH:18]>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]3)[CH2:15][C:16](=[N:17][OH:18])[CH2:19][CH2:20][C@H:2...
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.NO
CCN1CC[C@]2(c3cccc(OC)c3)CC(=NO)CC[C@H]2C1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
3fc1f10cfb677761aaa276368e7c40afd0a88b5ed184b5f398dacd07530a3fa9
1a0ef15294bdb221fb8888b5d4c7fcf00473b11e53da288791d32747daa48d23
N=C1CC[C@H]2CNCC[C@]2(c2ccccc2)C1
O=[C;H0;D3;+0:1](-[C:2]-[C:3])-[C:4]-[C:5].[NH2;D1;+0:6]-[O;D1;H1:7]>>[C:5]-[C:4]-[C;H0;D3;+0:1](=[N;H0;D2;+0:6]-[O;D1;H1:7])-[C:2]-[C:3]
96.6
[{"value": 96.6, "product": "C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=NO", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.5 g (1.54 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 0.456 g (6.56 mmol) of hydroxylamine hydrochloride and 0.64 g of KHCO3 in 10 ml of MeOH were refluxed for 45 min. The precipitate was filtered, the solvent was removed in vacuo and the residue ta...
10.6084/m9.figshare.5104873.v1
null
Ketone.Primary amine
Oxime
C1CC[C@H]2C[NH]CC[C@@H]2C1
C1CC[C@H]2C[NH]CC[C@@H]2C1
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
HO-
CO
null
null
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.NO>CO>CCN1CC[C@]2(c3cccc(OC)c3)CC(=NO)CC[C@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ceee2b4669514a49ad828e34aae4470f
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(C)=O>>CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C1(=CC=CC=C1)NN=C(C(=O)OCC)C(C)=O.CC(=O)O[Na]>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)OCC
O=[C:8]1[CH2:9][CH2:12][C@H:13]2[CH2:14][N:15]([CH2:16][CH3:17])[CH2:18][CH2:19][C@:20]2([c:21]2[cH:22][cH:23][cH:24][c:25]([O:26][CH3:27])[cH:28]2)[CH2:29]1.O=[C:10]([C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[N:7]Nc1ccccc1)[CH3:11]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[nH:7][c:8]2[c:9]([c:10]1[CH3:11])[CH2:12][C@@H:13...
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(C)=O
CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
3be4aad3c4d371a76ae664baccdc8bb6992e32dbd7ed2871d79c38fbfe0b2616
c182a26a1e4916f0df3a6716875f414b9379b6dc7bc3991b1a368fed15ba5da9
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C;H0;D3;+0:3](=[N;H0;D2;+0:4]-N-c1:c:c:c:c:c:1)-[C:5](=[O;D1;H0:6])-[#8:7]-[C:8].O=[C;H0;D3;+0:9]1-[C:10]-[C:11]-[C:12]-[C:13]-[CH2;D2;+0:14]-1>>[C:8]-[#8:7]-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:3]1:[nH;D2;+0:4]:[c;H0;D3;+0:9]2:[c;H0;D3;+0:14](:[c;H0;D3;+0:1]:1-[C;D1;H3:2])-[C:13]-[C:12]-[C:1...
61.3
[{"value": 61.3, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.8 g (2.47 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride and 0.87 g (93.7 mmol) of ethyl 2-phenylhydrazono-3-oxobutyrate [Organic Reactions, R. Adams Ed; Wiley, New York, 10, 32-33, (1951-1959)] were dissolved in a mixture of 3 mi of glacial acetic acid...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone.Ester
Ester
C1CC[C@H]2C[NH]CC[C@@H]2C1.c1ccccc1
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(C)=O>[Zn].C(C)(=O)O>CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3f82d7c91db94bdba2a3ad864f8f9a22
CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2>>CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(O)c1)C2
C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)OCC.B(Br)(Br)Br>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)OCC
C[O:26][c:25]1[cH:24][cH:23][cH:22][c:21]([C@@:20]23[C@H:13]([CH2:12][c:9]4[c:8]([nH:7][c:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[c:10]4[CH3:11])[CH2:28]2)[CH2:14][N:15]([CH2:16][CH3:17])[CH2:18][CH2:19]3)[cH:27]1>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[nH:7][c:8]2[c:9]([c:10]1[CH3:11])[CH2:12][C@@H:13]1[CH2:14][N:15]([CH...
CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(O)c1)C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
20.9
[{"value": 20.9, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.6 g (1.5 mmol) of (±)-trans-6-ethyl-2-ethoxycarbonyl-3-methyl-8a-(3-methoxyphenyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline were treated with 0.84 ml (9.0 mmol) of boron tribromide as described in example 2. The crude solid was purified by flash chromatography (AcOEt/MeOH/conc. NH4OH 80:20:2), yieldi...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccccc1
Other
null
null
null
CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2>>CCOC(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(O)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9a47955b82844c658fba77886c3a3881
CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(OC)c3)CCN(CC)C[C@H]1C2>>CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(O)c3)CCN(CC)C[C@H]1C2
Cl.C(CC)N(C(=O)N1C=C(C2=C1C[C@@]1(CCN(C[C@H]1C2)CC)C2=CC(=CC=C2)OC)C)CCC.B(Br)(Br)Br>>C(CC)N(C(=O)N1C=C(C2=C1C[C@@]1(CCN(C[C@H]1C2)CC)C2=CC(=CC=C2)O)C)CCC
C[O:23][c:22]1[cH:21][cH:20][cH:19][c:18]([C@:17]23[CH2:16][c:15]4[n:10]([C:8]([N:4]([CH2:3][CH2:2][CH3:1])[CH2:5][CH2:6][CH3:7])=[O:9])[cH:11][c:12]([CH3:13])[c:14]4[CH2:32][C@@H:31]2[CH2:30][N:27]([CH2:28][CH3:29])[CH2:26][CH2:25]3)[cH:24]1>>[CH3:1][CH2:2][CH2:3][N:4]([CH2:5][CH2:6][CH3:7])[C:8](=[O:9])[n:10]1[cH:11]...
CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(OC)c3)CCN(CC)C[C@H]1C2
CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(O)c3)CCN(CC)C[C@H]1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
0.56 g (1.15 mmol) of (±)-trans-dipropylaminocarbonyl-6-ethyl-3-methyl-8a-(3-methoxyphenyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline hydrochloride were treated with 0.65 ml (7 mmol) of boron tribromide as described in example 2. The residue was purified by flash chromatography (AcOEt/MeOH/conc. NH4OH 7...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1c[nH]c2c1C[C@@H]1CNCCC1C2
Other
null
null
null
CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(OC)c3)CCN(CC)C[C@H]1C2>>CCCN(CCC)C(=O)n1cc(C)c2c1C[C@]1(c3cccc(O)c3)CCN(CC)C[C@H]1C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-c4dcc751dbde49eaa01591fb6c337bfc
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1
Cl.C(C(C)C)OC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)OC)N1)C.B(Br)(Br)Br>>Cl.C(C(C)C)OC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)O)N1)C
C[O:12][c:11]1[cH:10][cH:9][cH:8][c:7]([C@@:6]23[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:30][C@H:29]2[CH2:28][c:27]2[c:15]([nH:16][c:17]([C:18](=[O:19])[O:20][CH2:21][CH:22]([CH3:23])[CH3:24])[c:25]2[CH3:26])[CH2:14]3)[cH:13]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([OH:12])[cH:13]3)[...
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1
CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
0.56 g of (±)-trans-2-(i-butoxycarbonyl)-6-ethyl-3-methyl-8a-(3-methoxyphenyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline hydrochloride were treated with 0.68 ml (7.26 mmol) of boron tribromide as described in example 2. The residue was purified by flash chromatography (AcOEt/MeOH/conc. NH4OH 75:25:2.5) ...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
Other
null
null
null
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)OCC(C)C)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a4e872fd5a6e4a58b4e93bf3d6bae84a
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(C)CC[C@@]1(c1cccc(OC)c1)C2
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CC.CC(=O)O[Na]>>C(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)C)C2=CC(=CC=C2)OC)N1)C)CC
O=[C:12]([C:8]([C:6]([N:3]([CH2:2][CH3:1])[CH2:4][CH3:5])=[O:7])=[N:9]Nc1ccccc1)[CH3:13].C[CH2:18][N:17]1[CH2:16][C@@H:15]2[CH2:14][CH2:11][C:10](=O)[CH2:30][C@@:21]2([c:22]2[cH:23][cH:24][cH:25][c:26]([O:27][CH3:28])[cH:29]2)[CH2:20][CH2:19]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]1[nH:9][c:10]2[c:11]([...
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(C)CC[C@@]1(c1cccc(OC)c1)C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
02f7ff219a45cc53342484f47524b7c84fa4304eb3eca6fa510465db3cfe5a17
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[CH2;D2;+0:1]-[#7:2](-[C:3])-[C:4]-[C:5]1-[C:6]-[CH2;D2;+0:7]-[C;H0;D3;+0:8](=O)-[C:9]-[C:10]-1.O=[C;H0;D3;+0:11](-[C;D1;H3:12])-[C;H0;D3;+0:13](=[N;H0;D2;+0:14]-N-c1:c:c:c:c:c:1)-[C:15](=[O;D1;H0:16])-[#7:17](-[C:18])-[C:19]>>[C:3]-[#7:2](-[CH3;D1;+0:1])-[C:4]-[C:5]1-[C:6]-[c;H0;D3;+0:7]2:[c;H0;D3;+0:8](:[nH;D2;+0:1...
14.7
[{"value": 14.7, "product": "C(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)C)C2=CC(=CC=C2)OC)N1)C)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
3 g (9.3 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 2.92 g (11.2 mmol) of N,N-diethyl-2-phenylhydrazono-3-oxobutyramide, 0.92 g (11.2 mmol) of CH3COONa, 2.8 g (42.8 mmol) of zinc dust and 9.3 ml of glacial acetic acid were treated as described in exa...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>[Zn].C(C)(=O)O>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(C)CC[C@@]1(c1cccc(OC)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-a50aa20c2f95459b844fc6848f1ecb10
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CCC(=O)C[C@H]2C1>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2
Cl.C(C)N1C[C@@H]2CC(CC[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CC.CC(=O)O[Na]>>C(C)N(C(=O)C1=C(C=2C[C@]3(CCN(C[C@@H]3CC2N1)C)C1=CC(=CC=C1)OC)C)CC
O=[C:12]([C:8]([C:6]([N:3]([CH2:2][CH3:1])[CH2:4][CH3:5])=[O:7])=[N:9]Nc1ccccc1)[CH3:13].C[CH2:27][N:26]1[CH2:25][CH2:24][C@:15]2([c:16]3[cH:17][cH:18][cH:19][c:20]([O:21][CH3:22])[cH:23]3)[CH2:14][CH2:11][C:10](=O)[CH2:30][C@H:29]2[CH2:28]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]1[nH:9][c:10]2[c:11]([c:...
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CCC(=O)C[C@H]2C1
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
a7c96afd46d67adcd8db93b524889f1b0e9b87cc8633c4df140052736ddcff04
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
c1ccc([C@]23CCNC[C@@H]2Cc2[nH]ccc2C3)cc1
C-[CH2;D2;+0:1]-[#7:2](-[C:3])-[C:4]-[C:5]1-[C:6]-[C:7]-[CH2;D2;+0:8]-[C;H0;D3;+0:9](=O)-[C:10]-1.O=[C;H0;D3;+0:11](-[C;D1;H3:12])-[C;H0;D3;+0:13](=[N;H0;D2;+0:14]-N-c1:c:c:c:c:c:1)-[C:15](=[O;D1;H0:16])-[#7:17](-[C:18])-[C:19]>>[C:3]-[#7:2](-[CH3;D1;+0:1])-[C:4]-[C:5]1-[C:6]-[C:7]-[c;H0;D3;+0:8]2:[c;H0;D3;+0:9](:[nH;D...
16.8
[{"value": 16.8, "product": "C(C)N(C(=O)C1=C(C=2C[C@]3(CCN(C[C@@H]3CC2N1)C)C1=CC(=CC=C1)OC)C)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.9 g (2.9 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-7-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride (J. Med. Chem., 35, 48, 1992), 0.9 g (3.5 mmol) of N,N-diethyl-2-phenylhydrazono-3-oxobutyramide, 0.28 g (3.5 mmol) of CH3COONa, 0.87 g (13.3 mmol) of zinc dust and 5 ml of glacial acetic acid were...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c([nH]1)C[C@H]1C[NH]CC[C@@H]1C2
c1ccccc1.c1cc2c([nH]1)C[C@H]1C[NH]CC[C@@H]1C2
HO-
[Zn].C(C)(=O)O
null
null
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.CCN1CC[C@]2(c3cccc(OC)c3)CCC(=O)C[C@H]2C1>[Zn].C(C)(=O)O>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9bb3a9b9e5d04bb5b051c031681b6c2c
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(O)c3)CCN(C)C[C@@H]1C2
C(C)N(C(=O)C1=C(C=2C[C@]3(CCN(C[C@@H]3CC2N1)C)C1=CC(=CC=C1)OC)C)CC.B(Br)(Br)Br>>C(C)N(C(=O)C1=C(C=2C[C@]3(CCN(C[C@@H]3CC2N1)C)C1=CC(=CC=C1)O)C)CC
C[O:21][c:20]1[cH:19][cH:18][cH:17][c:16]([C@@:15]23[CH2:14][c:11]4[c:10]([nH:9][c:8]([C:6]([N:3]([CH2:2][CH3:1])[CH2:4][CH3:5])=[O:7])[c:12]4[CH3:13])[CH2:29][C@H:28]2[CH2:27][N:25]([CH3:26])[CH2:24][CH2:23]3)[cH:22]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]1[nH:9][c:10]2[c:11]([c:12]1[CH3:13])[CH2:14][C...
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(O)c3)CCN(C)C[C@@H]1C2
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@]23CCNC[C@@H]2Cc2[nH]ccc2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
49.9
[{"value": 49.9, "product": "C(C)N(C(=O)C1=C(C=2C[C@]3(CCN(C[C@@H]3CC2N1)C)C1=CC(=CC=C1)O)C)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.29 g (0.71 mmol) of (±)-trans-2-diethylaminocarbonyl-3,7-dimethyl-4a-(3-methoxyphenyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[3,2-g]isoquinoline were treated with 0.4 ml (4.26 mmol) of boron tribromide as described in example 2. The residue was purified by flash chromatography (CH2Cl2 /MeOH/conc. NH4OH 80:12:0.8). Th...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c([nH]1)C[C@H]1C[NH]CC[C@@H]1C2
Other
null
null
null
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(OC)c3)CCN(C)C[C@@H]1C2>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@]1(c3cccc(O)c3)CCN(C)C[C@@H]1C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-4a987530b45942d59d9beddfbfacbbc6
CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C(C1=CC=CC=C1)NC(C(C(C)=O)=NNC1=CC=CC=C1)=O>>C(C1=CC=CC=C1)NC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)C)C2=CC(=CC=C2)OC)N1)C
O=[C:30]([C:19](=[N:18]Nc1ccccc1)[C:20](=[O:21])[NH:22][CH2:23][c:24]1[cH:25][cH:26][cH:27][cH:28][cH:29]1)[CH3:31].C[CH2:12][N:11]1[CH2:10][CH2:9][C@@:8]2([c:7]3[cH:6][cH:5][cH:4][c:3]([O:2][CH3:1])[cH:33]3)[C@H:14]([CH2:13]1)[CH2:15][CH2:16][C:17](=O)[CH2:32]2>>[CH3:1][O:2][c:3]1[cH:4][cH:5][cH:6][c:7]([C@@:8]23[CH2:...
CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
737b89c143e6b780fcc30370e3e4edb8ee05461cfbd75d6d7efab90d7bf53785
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
O=C(NCc1ccccc1)c1cc2c([nH]1)C[C@]1(c3ccccc3)CCNC[C@H]1C2
C-[CH2;D2;+0:1]-[#7:2](-[C:3])-[C:4]-[C:5]1-[C:6]-[CH2;D2;+0:7]-[C;H0;D3;+0:8](=O)-[C:9]-[C:10]-1.O=[C;H0;D3;+0:11](-[C;D1;H3:12])-[C;H0;D3;+0:13](=[N;H0;D2;+0:14]-N-c1:c:c:c:c:c:1)-[C:15](=[O;D1;H0:16])-[#7:17]-[C:18]>>[C:3]-[#7:2](-[CH3;D1;+0:1])-[C:4]-[C:5]1-[C:6]-[c;H0;D3;+0:7]2:[c;H0;D3;+0:8](:[nH;D2;+0:14]:[c;H0;...
null
[]
null
null
null
null
1 g (3.3 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 2.95 g (10 mmol) of N-benzyl-2-phenylhydrazono-3-oxobutyramide, 0.82 g (10 mmol) of CH3 COONa, 2.6 g (40 mmol) of zinc dust and 5 ml of glacial acetic acid were treated as described in example 1. Th...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c(n1)C[C@H]1CC[N]C[C@H]1C2
c1ccccc1.c1cc2c(n1)C[C@H]1CC[N]C[C@H]1C2.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CC(=O)C(=NNc1ccccc1)C(=O)NCc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>[Zn].C(C)(=O)O>COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2895d0d365944737af7826beeea98209
COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1>>Cc1c(C(=O)NCc2ccccc2)[nH]c2c1C[C@@H]1CN(C)CC[C@@]1(c1cccc(O)c1)C2
C(C1=CC=CC=C1)NC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)C)C2=CC(=CC=C2)OC)N1)C.B(Br)(Br)Br.Cl.CCOCC>>Cl.C(C1=CC=CC=C1)NC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)C)C2=CC(=CC=C2)O)N1)C
C[O:30][c:29]1[cH:28][cH:27][cH:26][c:25]([C@@:24]23[C@H:18]([CH2:17][c:16]4[c:2]([CH3:1])[c:3]([C:4](=[O:5])[NH:6][CH2:7][c:8]5[cH:9][cH:10][cH:11][cH:12][cH:13]5)[nH:14][c:15]4[CH2:32]2)[CH2:19][N:20]([CH3:21])[CH2:22][CH2:23]3)[cH:31]1>>[CH3:1][c:2]1[c:3]([C:4](=[O:5])[NH:6][CH2:7][c:8]2[cH:9][cH:10][cH:11][cH:12][c...
COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1
Cc1c(C(=O)NCc2ccccc2)[nH]c2c1C[C@@H]1CN(C)CC[C@@]1(c1cccc(O)c1)C2
null
null
CO
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(NCc1ccccc1)c1cc2c([nH]1)C[C@]1(c3ccccc3)CCNC[C@H]1C2
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
0.38 g of (±)-trans-2-benzylaminocarbonyl-3,6-dimethyl-8a-(3-methoxyphenyl)-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline were treated with 0.55 ml (5.7 mmol) of boron tribromide as described in example 2. The residue was dissolved in MeOH and the solution brought to acidic pH with HCl/Et2O. The solvent was...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccccc1
Other
CO
null
null
COc1cccc([C@@]23CCN(C)C[C@H]2Cc2c([nH]c(C(=O)NCc4ccccc4)c2C)C3)c1>CO>Cc1c(C(=O)NCc2ccccc2)[nH]c2c1C[C@@H]1CN(C)CC[C@@]1(c1cccc(O)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-840135d79ba844fc945788ee77b22f4f
CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C1(=CC=CC=C1)NC(C(C(C)=O)=NNC1=CC=CC=C1)=O>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)NC3=CC=CC=C3
O=[C:28]([C:18](=[N:17]Nc1ccccc1)[C:19](=[O:20])[NH:21][c:22]1[cH:23][cH:24][cH:25][cH:26][cH:27]1)[CH3:29].O=[C:16]1[CH2:15][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]3)[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:33][C@@H:32]2[CH2:31][CH2:30]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH...
CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
8bedcc1ec5488f2567cac7dc6b2d45e5a0271f1fd0d1fd73222e637ddd374a05
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
O=C(Nc1ccccc1)c1cc2c([nH]1)C[C@]1(c3ccccc3)CCNC[C@H]1C2
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C;H0;D3;+0:3](=[N;H0;D2;+0:4]-N-c1:c:c:c:c:c:1)-[C:5](=[O;D1;H0:6])-[#7:7]-[c:8].O=[C;H0;D3;+0:9]1-[C:10]-[C:11]-[C:12]-[C:13]-[CH2;D2;+0:14]-1>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:3](-[C:5](=[O;D1;H0:6])-[#7:7]-[c:8]):[nH;D2;+0:4]:[c;H0;D3;+0:9]2:[c;H0;D3;+0:14]:1-[C:13]-[C:12]-[C:1...
25.6
[{"value": 25.6, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)NC3=CC=CC=C3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.8 g (2.47 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 0.7 g (2.47 mmol) of N-phenyl-2-phenylhydrazono-3-oxobutyramide, 0.24 g (3 mmol) of CH3 COONa, 0.74 g (11.3 mmol) of zinc dust and 2.5 ml of glacial acetic acid were treated as described in examp...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CC(=O)C(=NNc1ccccc1)C(=O)Nc1ccccc1.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>[Zn].C(C)(=O)O>CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d7d0772f09424c2a8285b114d4b7d007
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)NC3=CC=CC=C3.B(Br)(Br)Br>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)NC3=CC=CC=C3
C[O:12][c:11]1[cH:10][cH:9][cH:8][c:7]([C@@:6]23[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:32][C@H:31]2[CH2:30][c:29]2[c:15]([nH:16][c:17]([C:18](=[O:19])[NH:20][c:21]4[cH:22][cH:23][cH:24][cH:25][cH:26]4)[c:27]2[CH3:28])[CH2:14]3)[cH:13]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([OH:12]...
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(Nc1ccccc1)c1cc2c([nH]1)C[C@]1(c3ccccc3)CCNC[C@H]1C2
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
22.1
[{"value": 22.1, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)NC3=CC=CC=C3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.28 g of (±)-trans-6-ethyl-8a-(3-methoxyphenyl)-3-methyl-2-phenylaminocarbonyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline were treated with 0.35 (1.9 mmol) of boron tribromide as described in example 2. The residue was purified by flash chromatography (EtOAc/MeOH/conc. NH4OH 80:20:2) yielding 0.06 g of ...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2.c1ccccc1
Other
null
null
null
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)Nc4ccccc4)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aadff68fc9964d3da32320a270554fa5
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC3CC3)CC[C@@]1(c1cccc(OC)c1)C2
Cl.C1(CC1)CN1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C(C)N(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)CC.CC(=O)O[Na]>>Cl.C1(CC1)CN1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)N(CC)CC
O=[C:12]([C:8]([C:6]([N:3]([CH2:2][CH3:1])[CH2:4][CH3:5])=[O:7])=[N:9]Nc1ccccc1)[CH3:13].O=[C:10]1[CH2:11][CH2:14][C@H:15]2[CH2:16][N:17]([CH2:18][CH:19]3[CH2:20][CH2:21]3)[CH2:22][CH2:23][C@:24]2([c:25]2[cH:26][cH:27][cH:28][c:29]([O:30][CH3:31])[cH:32]2)[CH2:33]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]...
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC3CC3)CC[C@@]1(c1cccc(OC)c1)C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
02f7ff219a45cc53342484f47524b7c84fa4304eb3eca6fa510465db3cfe5a17
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
c1ccc([C@@]23CCN(CC4CC4)C[C@H]2Cc2cc[nH]c2C3)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C;H0;D3;+0:3](=[N;H0;D2;+0:4]-N-c1:c:c:c:c:c:1)-[C:5](=[O;D1;H0:6])-[#7:7](-[C:8])-[C:9].O=[C;H0;D3;+0:10]1-[C:11]-[C:12]-[C:13]-[C:14]-[CH2;D2;+0:15]-1>>[C:8]-[#7:7](-[C:9])-[C:5](=[O;D1;H0:6])-[c;H0;D3;+0:3]1:[nH;D2;+0:4]:[c;H0;D3;+0:10]2:[c;H0;D3;+0:15](:[c;H0;D3;+0:1]:1-[C;D1;H3:2])-...
57.9
[{"value": 57.9, "product": "Cl.C1(CC1)CN1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)N(CC)CC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.28 g (0.80 mmol) of (±)-trans-2-cyclopropylmethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 0.56 g (2.14 mmol) of N,N-diethyl-2-phenylhydrazono-3-oxobutyramide, 0.131 g (1.6 mmol) of CH3COONa, 0.402 g (6.16 mmol) of zinc dust and 10 ml of glacial acetic acid were treated as...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.C1CC1.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CCN(CC)C(=O)C(=NNc1ccccc1)C(C)=O.COc1cccc([C@]23CCN(CC4CC4)C[C@@H]2CCC(=O)C3)c1>[Zn].C(C)(=O)O>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(CC3CC3)CC[C@@]1(c1cccc(OC)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-85e68abf33ca4928bc83045893ab7a1b
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1
Cl.CCOCC.C(C)(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)OC)N1)C)C(C)C.B(Br)(Br)Br>>Cl.C(C)(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)O)N1)C)C(C)C
C[O:12][c:11]1[cH:10][cH:9][cH:8][c:7]([C@@:6]23[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:32][C@H:31]2[CH2:30][c:29]2[c:15]([nH:16][c:17]([C:18](=[O:19])[N:20]([CH:21]([CH3:22])[CH3:23])[CH:24]([CH3:25])[CH3:26])[c:27]2[CH3:28])[CH2:14]3)[cH:13]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]...
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1
CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1
null
null
CO
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
1.0 g (2.2 mmol) of (±)-trans-2-diisopropylaminocarbonyl-6-ethyl-8a-(3-methoxyphenyl)-3-methyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g] isoquinoline were treated with 1.15 ml (12.0 mmol) of boron tribromide as described in example 2. The crude product was dissolved in MeOH and the solution brought to acidic pH wit...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
Other
CO
null
null
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1>CO>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C(C)C)C(C)C)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d4dc502d78a2417cbeb0d77e8113c760
CC(=O)C(=NNc1ccccc1)C(N)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(N)=O)c(C)c3C[C@@H]2C1
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C1(=CC=CC=C1)NN=C(C(=O)N)C(C)=O.CC(=O)O[Na].C(C)(=O)O>>NC(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)OC)N1)C
O=[C:22]([C:18](=[N:17]Nc1ccccc1)[C:19]([NH2:20])=[O:21])[CH3:23].O=[C:16]1[CH2:15][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]3)[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:27][C@@H:26]2[CH2:25][CH2:24]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([O:12][CH3:13])[cH:14]3)[...
CC(=O)C(=NNc1ccccc1)C(N)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(N)=O)c(C)c3C[C@@H]2C1
null
[Zn]
null
Miscellaneous
OtherReaction
8bedcc1ec5488f2567cac7dc6b2d45e5a0271f1fd0d1fd73222e637ddd374a05
c19b01bf1c2954a1ff8dd269aaeb96f6c0aebc2ca18c537766f4a468d99b4eb8
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
O=[C;H0;D3;+0:1](-[C;D1;H3:2])-[C;H0;D3;+0:3](=[N;H0;D2;+0:4]-N-c1:c:c:c:c:c:1)-[C:5](-[N;D1;H2:6])=[O;D1;H0:7].O=[C;H0;D3;+0:8]1-[C:9]-[C:10]-[C:11]-[C:12]-[CH2;D2;+0:13]-1>>[C;D1;H3:2]-[c;H0;D3;+0:1]1:[c;H0;D3;+0:3](-[C:5](-[N;D1;H2:6])=[O;D1;H0:7]):[nH;D2;+0:4]:[c;H0;D3;+0:8]2:[c;H0;D3;+0:13]:1-[C:12]-[C:11]-[C:10]-...
null
[]
null
null
null
null
3.24 g (10 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 6.16 g (30.0 mmol) of 2-phenylhydrazono-3-oxobutyramide, 2.46 g (7.0 mmol) of CH3COONa, 7.85 g (120.0 mmol) of zinc dust and 15 ml of glacial acetic acid were treated as described in example 1. Th...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone
null
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1
c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
HO-
[Zn]
null
null
CC(=O)C(=NNc1ccccc1)C(N)=O.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>[Zn]>CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(N)=O)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e47c72c20e604a20b47414090524ffc6
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F>>CCOC(=O)c1[nH]c2c(c1C(F)(F)F)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.C1(=CC=CC=C1)NN=C(C(=O)OCC)C(C(F)(F)F)=O.CC(=O)O[Na]>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C(F)(F)F)C(=O)OCC
O=[C:8]1[CH2:9][CH2:15][C@H:16]2[CH2:17][N:18]([CH2:19][CH3:20])[CH2:21][CH2:22][C@:23]2([c:24]2[cH:25][cH:26][cH:27][c:28]([O:29][CH3:30])[cH:31]2)[CH2:32]1.O=[C:10]([C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])=[N:7]Nc1ccccc1)[C:11]([F:12])([F:13])[F:14]>>[CH3:1][CH2:2][O:3][C:4](=[O:5])[c:6]1[nH:7][c:8]2[c:9]([c:10]1[C:11...
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F
CCOC(=O)c1[nH]c2c(c1C(F)(F)F)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
3be4aad3c4d371a76ae664baccdc8bb6992e32dbd7ed2871d79c38fbfe0b2616
c182a26a1e4916f0df3a6716875f414b9379b6dc7bc3991b1a368fed15ba5da9
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
O=[C;H0;D3;+0:1](-[C;H0;D3;+0:2](=[N;H0;D2;+0:3]-N-c1:c:c:c:c:c:1)-[C:4](=[O;D1;H0:5])-[#8:6]-[C:7])-[C:8](-[F;D1;H0:9])(-[F;D1;H0:10])-[F;D1;H0:11].O=[C;H0;D3;+0:12]1-[C:13]-[C:14]-[C:15]-[C:16]-[CH2;D2;+0:17]-1>>[C:7]-[#8:6]-[C:4](=[O;D1;H0:5])-[c;H0;D3;+0:2]1:[nH;D2;+0:3]:[c;H0;D3;+0:12]2:[c;H0;D3;+0:17](:[c;H0;D3;+...
66.6
[{"value": 66.6, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C(F)(F)F)C(=O)OCC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
3.24 g (10 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 8.65 g (30 mmol) of ethyl 2-phenylhydrazono-4,4,4-trifluoro-3-oxobutyrate, 2.46 g (30 mmol) of CH3COONa, 7.85 g (120 mmol) of zinc dust and 15 ml of glacial acetic acid were treated as described i...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone.Ester
Ester
C1CC[C@H]2C[NH]CC[C@@H]2C1.c1ccccc1
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccccc1
HO-
[Zn].C(C)(=O)O
null
null
CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1.CCOC(=O)C(=NNc1ccccc1)C(=O)C(F)(F)F>[Zn].C(C)(=O)O>CCOC(=O)c1[nH]c2c(c1C(F)(F)F)C[C@@H]1CN(CC)CC[C@@]1(c1cccc(OC)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-53e465a32b0c4c70bcd0b9d12d1a9382
CC(=O)C(=NNc1ccccc1)C(=O)N(C)C.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>>Cc1c[nH]c2c1CC1CNCCC1C2
Cl.C(C)N1C[C@@H]2CCC(C[C@]2(CC1)C1=CC(=CC=C1)OC)=O.CN(C(C(C(C)=O)=NNC1=CC=CC=C1)=O)C.CC(=O)O[Na]>>CC1=CNC=2CC3CCNCC3CC21
CN(C)C(=O)[C:3]([C:2](=O)[CH3:1])=[N:4]Nc1ccccc1.CC[N:10]1[CH2:9][C@@H:8]2[CH2:7][CH2:6][C:5](=O)[CH2:14][C@@:13]2(c2cccc(OC)c2)[CH2:12][CH2:11]1>>[CH3:1][c:2]1[cH:3][nH:4][c:5]2[c:6]1[CH2:7][CH:8]1[CH2:9][NH:10][CH2:11][CH2:12][CH:13]1[CH2:14]2
CC(=O)C(=NNc1ccccc1)C(=O)N(C)C.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1
Cc1c[nH]c2c1CC1CNCCC1C2
null
[Zn]
C(C)(=O)O
Miscellaneous
OtherReaction
17c398210d61b4b9a698f2ca3ce9b049a4f801567b1f4664f037ab8075bab0b9
344df68336dcd4690b45c2b4f31b820278a1bb019f647d1126a2f0747f1fba87
c1cc2c([nH]1)CC1CCNCC1C2
C-C-[N;H0;D3;+0:1]1-[C:2]-[C:3]-[C@;H0;D4;+0:4]2(-c3:c:c:c:c(-O-C):c:3)-[C:5]-[C;H0;D3;+0:6](=O)-[CH2;D2;+0:7]-[C:8]-[C@H;D3;+0:9]-2-[C:10]-1.C-N(-C)-C(=O)-[C;H0;D3;+0:11](=[N;H0;D2;+0:12]-N-c1:c:c:c:c:c:1)-[C;H0;D3;+0:13](=O)-[C;D1;H3:14]>>[C;D1;H3:14]-[c;H0;D3;+0:13]1:[cH;D2;+0:11]:[nH;D2;+0:12]:[c;H0;D3;+0:6]2:[c;H0...
84.8
[{"value": 84.8, "product": "CC1=CNC=2CC3CCNCC3CC21", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.0 g (3.1 mmol) of (±)-trans-2-ethyl-4a-(3-methoxyphenyl)-6-oxo-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline hydrochloride, 2.33 g (10 mmol) of N, N-dimethyl-2-phenylhydrazono-3-oxobutyramide, 0.82 g (1 0 mmol) of CH3COONa, 2.6 g (40 mmol) of zinc dust and 5 ml of glacial acetic acid were treated as described in exampl...
10.6084/m9.figshare.5104873.v1
null
Hydrazone.Ketone.Ketone.Ether.Tertiary amide.Tertiary amine
Secondary amine
c1ccccc1.C1CC[C@H]2C[NH]CC[C@@H]2C1.c1ccccc1
c1cc2c([nH]1)CC1CCNCC1C2
c1cc2c([nH]1)CC1CCNCC1C2
HO-
[Zn].C(C)(=O)O
null
null
CC(=O)C(=NNc1ccccc1)C(=O)N(C)C.CCN1CC[C@]2(c3cccc(OC)c3)CC(=O)CC[C@H]2C1>[Zn].C(C)(=O)O>Cc1c[nH]c2c1CC1CNCCC1C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3ae2e96f1f8c4014ac444d242c55c3da
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1
CN(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)OC)N1)C)C.B(Br)(Br)Br.Cl.CCOCC>>Cl.CN(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC)C2=CC(=CC=C2)O)N1)C)C
C[O:12][c:11]1[cH:10][cH:9][cH:8][c:7]([C@@:6]23[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:28][C@H:27]2[CH2:26][c:25]2[c:15]([nH:16][c:17]([C:18](=[O:19])[N:20]([CH3:21])[CH3:22])[c:23]2[CH3:24])[CH2:14]3)[cH:13]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([OH:12])[cH:13]3)[CH2:14][c:15]3[...
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1
CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1
null
null
CO
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
c1ccc([C@@]23CCNC[C@H]2Cc2cc[nH]c2C3)cc1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
null
[]
null
null
null
null
0.5 g (1.25 mmol) of (±)trans-2-dimethylaminocarbonyl-6-ethyl-8a-(3-methoxyphenyl)-3-methyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g] isoquinoline were treated with 0.725 ml (7.5 mmol) of boron tribromide as described in example 2. The etude product was dissolved in MeOH and the solution brought to acidic pH with H...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2
Other
CO
null
null
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1>CO>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N(C)C)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cd9b39ec611d404d9a8ea9bc73cb12d3
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CNCC[C@@]1(c1cccc(OC)c1)C2.O=Cc1ccco1>>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(Cc3ccco3)CC[C@@]1(c1cccc(OC)c1)C2
O1C(=CC=C1)C=O.C(#N)[BH3-].[Na+].Cl.C(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCNC[C@H]3C2)C2=CC(=CC=C2)OC)N1)C)CC.O1C(=CC=C1)C=O.C(#N)[BH3-].[Na+]>>Cl.C(C)N(C(=O)C1=C(C2=C(C[C@@]3(CCN(C[C@H]3C2)CC=2OC=CC2)C2=CC(=CC=C2)OC)N1)C)CC
[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]1[nH:9][c:10]2[c:11]([c:12]1[CH3:13])[CH2:14][C@@H:15]1[CH2:16][NH:17][CH2:24][CH2:25][C@@:26]1([c:27]1[cH:28][cH:29][cH:30][c:31]([O:32][CH3:33])[cH:34]1)[CH2:35]2.O=[CH:18][c:19]1[cH:20][cH:21][cH:22][o:23]1>>[CH3:1][CH2:2][N:3]([CH2:4][CH3:5])[C:6](=[O:7])[c:8]1[n...
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CNCC[C@@]1(c1cccc(OC)c1)C2.O=Cc1ccco1
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(Cc3ccco3)CC[C@@]1(c1cccc(OC)c1)C2
null
null
C(C)(=O)O.CO
Heteroatom Alkylation and Arylation
reductive amination
6051e74c13bd3699ee2da9cef24ae529ce1510384b28dcfec56f7d71af562bec
2d03f38884b1fbb0c0d6e6f2de31afb25102fec87f347c3a123e064c1bfef0ad
c1ccc([C@@]23CCN(Cc4ccco4)C[C@H]2Cc2cc[nH]c2C3)cc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[#8;a:4]:[c:5].[C:6]-[C:7]-[NH;D2;+0:8]-[C:9]-[C:10]>>[C:6]-[C:7]-[N;H0;D3;+0:8](-[CH2;D2;+0:1]-[c:2](:[c:3]):[#8;a:4]:[c:5])-[C:9]-[C:10]
null
[]
0
CELSIUS
15
HOUR
1.3 g (3.3 mmol) of (±)-trans-2-diethylaminocarbonyl-8a-(3-methoxyphenyl)-3-methyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline, 0.28 ml (4.95 mmol) of acetic acid, 0.33 ml (3.96 mmol) of 2-furaldehyde were dissolved in 50 ml of MeOH under nitrogen atmosphere. 0.415 g (6.6 mmol) of sodium cyanoborohydride ...
10.6084/m9.figshare.5104873.v1
null
Aldehyde.Secondary amine
Tertiary amine
c1cc2c([nH]1)C[C@@H]1CCNC[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2
c1cc2c([nH]1)C[C@@H]1CC[NH]C[C@H]1C2.c1ccoc1.c1ccccc1
Other
C(C)(=O)O.CO
0
15
CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CNCC[C@@]1(c1cccc(OC)c1)C2.O=Cc1ccco1>C(C)(=O)O.CO>CCN(CC)C(=O)c1[nH]c2c(c1C)C[C@@H]1CN(Cc3ccco3)CC[C@@]1(c1cccc(OC)c1)C2
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e576ebaa84304ffda5a1fb2e2ebe1efc
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1
C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)OC)NC(=C3C)C(=O)N3CCCC3.B(Br)(Br)Br>>C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)N3CCCC3
C[O:12][c:11]1[cH:10][cH:9][cH:8][c:7]([C@@:6]23[CH2:5][CH2:4][N:3]([CH2:2][CH3:1])[CH2:30][C@H:29]2[CH2:28][c:27]2[c:15]([nH:16][c:17]([C:18](=[O:19])[N:20]4[CH2:21][CH2:22][CH2:23][CH2:24]4)[c:25]2[CH3:26])[CH2:14]3)[cH:13]1>>[CH3:1][CH2:2][N:3]1[CH2:4][CH2:5][C@@:6]2([c:7]3[cH:8][cH:9][cH:10][c:11]([OH:12])[cH:13]3)...
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1
CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1
null
null
null
Deprotection
Cleavage of methoxy ethers to alcohols
c5320c7dfa4f544d4900efcae9b3262bf0d5286bcf39c86109232351f35b23d5
26a36596df80ec137b0e8087297418351c93c32819177f680675220622f215d4
O=C(c1cc2c([nH]1)C[C@]1(c3ccccc3)CCNC[C@H]1C2)N1CCCC1
C-[O;H0;D2;+0:1]-[c:2](:[c:3]):[c:4]>>[OH;D1;+0:1]-[c:2](:[c:3]):[c:4]
23.3
[{"value": 23.3, "product": "C(C)N1C[C@H]2CC3=C(C[C@@]2(CC1)C1=CC(=CC=C1)O)NC(=C3C)C(=O)N3CCCC3", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
0.63 g (1.37 mmol) of (±)-trans-6-ethyl-8a-(3-methoxyphenyl)-3-methyl-2-pyrrolidinocarbonyl-4,4a,5,6,7,8,8a,9-octahydro-1H-pyrrolo[2,3-g]isoquinoline were treated with 0.77 ml (8.22 mmol) of boron tribromide as described in example 2. The residue was purified by flash chromatography (EtOAc/MeOH/conc. NH4OH 80:20:0.5). ...
10.6084/m9.figshare.5104873.v1
null
Ether
Aromatic alcohol
null
null
c1ccccc1.c1cc2c(n1)C[C@@H]1CC[N]C[C@H]1C2.C1CC[NH]C1
Other
null
null
null
CCN1CC[C@@]2(c3cccc(OC)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1>>CCN1CC[C@@]2(c3cccc(O)c3)Cc3[nH]c(C(=O)N4CCCC4)c(C)c3C[C@@H]2C1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-10d566a7e6924599b73ffe5a8d4c02d6
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C.CI>>C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O
IC.C(C)(C)(C)OC(=O)N1C(CC[C@H]1CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)=O.[Li]N([Si](C)(C)C)[Si](C)(C)C>>C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C)=O
[CH2:2]1[CH2:3][C@@H:4]([CH2:5][O:6][Si:7]([c:8]2[cH:9][cH:10][cH:11][cH:12][cH:13]2)([c:14]2[cH:15][cH:16][cH:17][cH:18][cH:19]2)[C:20]([CH3:21])([CH3:22])[CH3:23])[N:24]([C:25](=[O:26])[O:27][C:28]([CH3:29])([CH3:30])[CH3:31])[C:32]1=[O:33].I[CH3:1]>>[CH3:1][C@@H:2]1[CH2:3][C@@H:4]([CH2:5][O:6][Si:7]([c:8]2[cH:9][cH:...
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C.CI
C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O
null
null
C1CCOC1
C-C Coupling
Methylation with MeI_secondary
a6c1ce0a3374e4ae08505cc3e98b837620321d13fa6cd312b247b9c30998e781
410ec9b1cc243569e4ff568c248f0b402403802e002b4018f576af3f6960507b
O=C1CC[C@@H](CO[SiH](c2ccccc2)c2ccccc2)N1
I-[CH3;D1;+0:1].[C;D1;H3:2]-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#8:6]-[C:7](=[O;D1;H0:8])-[#7:9]1-[C:10]-[C:11]-[CH2;D2;+0:12]-[C:13]-1=[O;D1;H0:14]>>[C;D1;H3:2]-[C:3](-[C;D1;H3:4])(-[C;D1;H3:5])-[#8:6]-[C:7](=[O;D1;H0:8])-[#7:9]1-[C:10]-[C:11]-[C@@H;D3;+0:12](-[CH3;D1;+0:1])-[C:13]-1=[O;D1;H0:14]
47.3
[{"value": 47.0, "product": "C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 47.3, "product": "C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired":...
null
null
1
HOUR
To a solution of (S)-1-t-butoxycarbonyl-5-t-butyldiphenylsiloxymethyl-pyrrolidine-2-one (15 g, 33 mmol) in THF (250 mL) at -78° C. a 1M solution of LiN(SiMe3)2 (35 mL, 35 mmol) was slowly added. After stirring for 1 hr, iodomethane (6.2 mL, 100 mmol) was added. The reaction mixture was allowed to stir for another 2 hr ...
10.6084/m9.figshare.5104873.v1
null
null
null
C1CC[NH]C1
C1CC[NH]C1
C1CC[NH]C1.c1ccccc1.c1ccccc1
HI
C1CCOC1
null
1
CC(C)(C)OC(=O)N1C(=O)CC[C@H]1CO[Si](c1ccccc1)(c1ccccc1)C(C)(C)C.CI>C1CCOC1>C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-6b339a53b1934e9da154c7d3ab813c29
C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O>>C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O
C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO[Si](C1=CC=CC=C1)(C1=CC=CC=C1)C(C)(C)C)C)=O.C(C)(=O)O.[F-].C(CCC)[N+](CCCC)(CCCC)CCCC.C(C)(=O)OCC>>C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO)C)=O
CC(C)(C)[Si](c1ccccc1)(c1ccccc1)[O:6][CH2:5][C@@H:4]1[CH2:3][C@@H:2]([CH3:1])[C:15](=[O:16])[N:7]1[C:8](=[O:9])[O:10][C:11]([CH3:12])([CH3:13])[CH3:14]>>[CH3:1][C@@H:2]1[CH2:3][C@@H:4]([CH2:5][OH:6])[N:7]([C:8](=[O:9])[O:10][C:11]([CH3:12])([CH3:13])[CH3:14])[C:15]1=[O:16]
C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O
C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O
null
null
C1CCOC1
Deprotection
Alcohol deprotection from silyl ethers
5607047bc82bb27c5a65769b01ea0774767f4428c871f65da0b6352111d7a6e9
5c02ee98cb6b210a313993bea9e102110eb73637a50746f5457590f98613069b
O=C1CCCN1
C-C(-C)(-C)-[Si](-[O;H0;D2;+0:1]-[C:2]-[C:3]-[#7:4])(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1>>[#7:4]-[C:3]-[C:2]-[OH;D1;+0:1]
null
[]
null
null
8
HOUR
To a solution of (3R,5S)-1-t-butoxycarbonyl-5-t-butyldiphenylsiloxymethyl-3-methyl-pyrrolidine-2-one (17.8 g, 38.1 mmol) and glacial acetic acid (2 eq) in dry THF (50 mL) at 0° C. was added a 1.0M solution of tetrabutylammonium fluoride in THF (150 mL, 150 mmol). The solution was allowed to warm room temperature and st...
10.6084/m9.figshare.5104873.v1
null
Silyl protective group
Primary alcohol
c1ccccc1.c1ccccc1
null
C1CC[NH]C1
Other
C1CCOC1
null
8
C[C@@H]1C[C@@H](CO[Si](c2ccccc2)(c2ccccc2)C(C)(C)C)N(C(=O)OC(C)(C)C)C1=O>C1CCOC1>C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-94c314721a7e472a8dbf1f4c15f24609
C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O.O>>C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O
I(=O)(=O)(=O)[O-].[Na+].C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1CO)C)=O.C(C)#N.C(Cl)(Cl)(Cl)Cl.O.ClCCl>>C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1C(=O)O)C)=O
[CH3:1][C@@H:2]1[CH2:3][C@@H:4]([CH2:5][OH:7])[N:8]([C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15])[C:16]1=[O:17].[OH2:6]>>[CH3:1][C@@H:2]1[CH2:3][C@@H:4]([C:5](=[O:6])[OH:7])[N:8]([C:9](=[O:10])[O:11][C:12]([CH3:13])([CH3:14])[CH3:15])[C:16]1=[O:17]
C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O.O
C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O
null
[Ru](Cl)(Cl)Cl
[Cl-].[Na+].O
Heteroatom Alkylation and Arylation
OtherReaction
345c33ef221a703d0195f5e2e95e13b23ff84fd249db06983973a14c521bda14
61cf901f3ab42f325ea04925d4645e2208b580d0b1f80879b3cd6caca2ef04e0
O=C1CCCN1
[C:1]-[C:2](-[CH2;D2;+0:3]-[O;D1;H1:4])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:13]=[O;D1;H0:14].[OH2;D0;+0:15]>>[C:1]-[C:2](-[C;H0;D3;+0:3](-[O;D1;H1:4])=[O;H0;D1;+0:15])-[#7:5](-[C:6](=[O;D1;H0:7])-[#8:8]-[C:9](-[C;D1;H3:10])(-[C;D1;H3:11])-[C;D1;H3:12])-[C:13]=[O;D1;H0...
54
[{"value": 54.0, "product": "C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1C(=O)O)C)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
2
HOUR
To a solution of (3R,5S)-1-t-butoxycarbonyl-5-hydroxymethyl-3-methylpyrrolidine-2-one in a solvent mixture of acetonitrile:carbon tetrachloride:water (2:2:3, 266 mL) was added sodium periodate (3 eq, 24.0 g) and ruthenium trichloride (2.2 mol %, 0.174 g). The solution was stirred 2 hr at room temperature and then dilut...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol
Carboxylic acid
null
null
C1CC[NH]C1
null
[Ru](Cl)(Cl)Cl.[Cl-].[Na+].O
null
2
C[C@@H]1C[C@@H](CO)N(C(=O)OC(C)(C)C)C1=O.O>[Ru](Cl)(Cl)Cl.[Cl-].[Na+].O>C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-739eba69493e45fba73186e7ab16d952
C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O.O>>C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O
C(C)(C)(C)OC(=O)N1C([C@@H](C[C@H]1C(=O)O)C)=O.O.[OH-].[Li+].O>>C(C)(C)(C)OC(=O)N[C@@H](C[C@H](C(=O)O)C)C(=O)O
[CH3:1][C@@H:2]1[CH2:3][C@@H:4]([C:13](=[O:14])[OH:15])[N:5]([C:6](=[O:7])[O:8][C:9]([CH3:10])([CH3:11])[CH3:12])[C:16]1=[O:17].[OH2:18]>>[CH3:1][C@H:2]([CH2:3][C@H:4]([NH:5][C:6](=[O:7])[O:8][C:9]([CH3:10])([CH3:11])[CH3:12])[C:13](=[O:14])[OH:15])[C:16](=[O:17])[OH:18]
C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O.O
C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O
null
null
C1CCOC1
Protection
OtherReaction
12ea568f5bbd96adab73aff3283996480961f612757e466255423c5645af0e6e
d205f1320160ea6fd9f0bda4863ee5979f7ad336699029216ee1832d3dc0743f
null
[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[#8:5]-[C:6](=[O;D1;H0:7])-[N;H0;D3;+0:8]1-[C:9](-[C:10](=[O;D1;H0:11])-[O;D1;H1:12])-[C:13]-[C:14](-[C;D1;H3:15])-[C;H0;D3;+0:16]-1=[O;D1;H0:17].[OH2;D0;+0:18]>>[C;D1;H3:1]-[C:2](-[C;D1;H3:3])(-[C;D1;H3:4])-[#8:5]-[C:6](=[O;D1;H0:7])-[NH;D2;+0:8]-[C:9](-[C:13]-[C:14](-[C;D...
99
[{"value": 99.0, "product": "C(C)(C)(C)OC(=O)N[C@@H](C[C@H](C(=O)O)C)C(=O)O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 98.8, "product": "C(C)(C)(C)OC(=O)N[C@@H](C[C@H](C(=O)O)C)C(=O)O", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
A solution of (3R,5S)-1-t-Butoxycarbonyl-5-carboxy-3-methylpyrrolidine-2-one (6.2 g, 25.5 mmol) in THF (50 mL) was treated with lithium hydroxide monohydrate (3 eq, 3.20 g) and water (5 mL). After stirring for 16 hr at room temperature the THF was removed in vacuo and water (20 mL) was added. The pH was adjusted to 3 b...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Substituted dicarboximide
Carbamic ester.Carboxylic acid
C1CC[NH]C1
null
null
null
C1CCOC1
null
null
C[C@@H]1C[C@@H](C(=O)O)N(C(=O)OC(C)(C)C)C1=O.O>C1CCOC1>C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-cc72150513eb4fa69899ef3b1e23e777
C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O>>C[C@H](C[C@H](N)C(=O)O)C(=O)O
C(C)(C)(C)OC(=O)N[C@@H](C[C@H](C(=O)O)C)C(=O)O>>C[C@H](C[C@H](N)C(=O)O)C(=O)O
CC(C)(C)OC(=O)[NH:5][C@@H:4]([CH2:3][C@@H:2]([CH3:1])[C:9](=[O:10])[OH:11])[C:6](=[O:7])[OH:8]>>[CH3:1][C@H:2]([CH2:3][C@H:4]([NH2:5])[C:6](=[O:7])[OH:8])[C:9](=[O:10])[OH:11]
C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O
C[C@H](C[C@H](N)C(=O)O)C(=O)O
null
null
FC(C(=O)O)(F)F.C(Cl)Cl
Reduction
Hydrogenolysis of amides/imides/carbamates
3c33dd2a2d355ee5ba0287367e209aa147a39aa00607f0c95fb2bf1ade45d014
c5b5dffe7dd8beebdc1baa8b5b05300a9f7079e65dcfd42ade6f8a77ff09537d
null
C-C(-C)(-C)-O-C(=O)-[NH;D2;+0:1]-[C:2](-[C:3])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]>>[C:3]-[C:2](-[NH2;D1;+0:1])-[C:4](=[O;D1;H0:5])-[O;D1;H1:6]
null
[]
null
null
48
HOUR
The Boc-protected diacid, (2S, 4R)-N-t-butoxycarbonyl- 4-methyl glutamic acid, was subjected to a mixture of trifluoroacetic acid:methylene chloride (40:60, 100 mL) for 3 hr at room temperature. The volatiles were removed in vacuo and the residue was azeotroped with toluene (50 mL). Water (150 mL) was added and the aqu...
10.6084/m9.figshare.5104873.v1
null
Carbamic ester.Ether.Boc
Primary amine
null
null
null
HO-
FC(C(=O)O)(F)F.C(Cl)Cl
null
48
C[C@H](C[C@H](NC(=O)OC(C)(C)C)C(=O)O)C(=O)O>FC(C(=O)O)(F)F.C(Cl)Cl>C[C@H](C[C@H](N)C(=O)O)C(=O)O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0c37bb1656a64973bff4ef3e79448c12
COC(=O)Cc1cccc2ccc(OC)cc12>>COc1ccc2cccc(CCO)c2c1
[H-].[H-].[Al+3].[Li+].[H-].[H-].[H-].COC1=CC=C2C=CC=C(C2=C1)CC(=O)OC.O>>COC1=CC=C2C=CC=C(C2=C1)CCO
CO[C:12]([CH2:11][c:10]1[cH:9][cH:8][cH:7][c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:15][c:14]21)=[O:13]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][OH:13])[c:14]2[cH:15]1
COC(=O)Cc1cccc2ccc(OC)cc12
COc1ccc2cccc(CCO)c2c1
null
null
CCOCC
Reduction
Reduction of ester to primary alcohol
21d61543c6ec8a8cebe1b3ef55ef3dd20acbf79a4f1c12a7fb51e32be7a3248a
1fbcd628a0426673c5d10aa49a977cd2d1ae02a8cdf57bbb10d94aa03a94e937
c1ccc2ccccc2c1
C-O-[C;H0;D3;+0:1](=[O;H0;D1;+0:2])-[C:3]-[c:4]>>[OH;D1;+0:2]-[CH2;D2;+0:1]-[C:3]-[c:4]
null
[]
null
null
null
null
3.34 g of lithium aluminum hydride are placed in a 250-cm3 flask, and ether is added gently with stirring. Using a dropping funnel, 5 g of methyl (7-methoxy-1-naphthyl)acetate previously dissolved in 50 cm3 of ether are added slowly. The reaction medium is left stirring for 30 minutes. It is poured very slowly into a m...
10.6084/m9.figshare.5104873.v1
null
Ester
Primary alcohol
null
null
c1ccc2ccccc2c1
Other
CCOCC
null
null
COC(=O)Cc1cccc2ccc(OC)cc12>CCOCC>COc1ccc2cccc(CCO)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-930d75a478a44c1f993455a3cf0bd573
COc1ccc2cccc(CCO)c2c1.CS(=O)(=O)Cl>>COc1ccc2cccc(CCOS(C)(=O)=O)c2c1
C(C)N(CC)CC.S(=O)(=O)(C)Cl.COC1=CC=C2C=CC=C(C2=C1)CCO>>S(C)(=O)(=O)OCCC1=CC=CC2=CC=C(C=C12)OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][OH:13])[c:18]2[cH:19]1.Cl[S:14]([CH3:15])(=[O:16])=[O:17]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][O:13][S:14]([CH3:15])(=[O:16])=[O:17])[c:18]2[cH:19]1
COc1ccc2cccc(CCO)c2c1.CS(=O)(=O)Cl
COc1ccc2cccc(CCOS(C)(=O)=O)c2c1
null
null
ClCCl
Acylation
Formation of Sulfonic Esters
2fa969eb2c954bb96793348a1b2335ec63fbd290dadec6e3e02295e1768e64cf
cb77b899e4adf980b1def97230ef2861660fd7f9602260ec64747d9afd3a795a
c1ccc2ccccc2c1
Cl-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4].[C:5]-[C:6]-[OH;D1;+0:7]>>[C:5]-[C:6]-[O;H0;D2;+0:7]-[S;H0;D4;+0:1](-[C;D1;H3:2])(=[O;D1;H0:3])=[O;D1;H0:4]
null
[]
-10
CELSIUS
null
null
In a 250-cm3 flask, 4 g of 2-(7-methoxy-1-naphthyl)ethanol are dissolved in 100 cm3 of dichloromethane, and 3.3 cm3 of triethylamine are added. The mixture is cooled in an ice bath at -10° C. and 2.75 g of mesyl chloride are then added dropwise and with stirring. The mixture is left stirring for 30 minutes. The aqueous...
10.6084/m9.figshare.5104873.v1
null
Primary alcohol.Sulfonyl halide
Mesylate
null
null
c1ccc2ccccc2c1
HCl
ClCCl
-10
null
COc1ccc2cccc(CCO)c2c1.CS(=O)(=O)Cl>ClCCl>COc1ccc2cccc(CCOS(C)(=O)=O)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-14978e6518ec43e492e5f892cd564bb7
CCc1ccccc1.O=C1CCC(=O)O1>>CCc1ccc(C(=O)CCC(=O)O)cc1
Cl.C(C)C1=CC=CC=C1.[Cl-].[Al+3].[Cl-].[Cl-].C1(CCC(=O)O1)=O>>O=C(CCC(=O)O)C1=CC=C(C=C1)CC
[CH3:1][CH2:2][c:3]1[cH:4][cH:5][cH:6][cH:14][cH:15]1.[C:7]1(=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[O:13]1>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([C:7](=[O:8])[CH2:9][CH2:10][C:11](=[O:12])[OH:13])[cH:14][cH:15]1
CCc1ccccc1.O=C1CCC(=O)O1
CCc1ccc(C(=O)CCC(=O)O)cc1
null
null
null
C-C Coupling
OtherReaction
95de0079bfd4d0e2b70eac1863ad8bac063c1a1557f674f5eb3c0cde67534555
4836357c99dfeeac9d5083fedc379181a858ae45ac77bd85eb46e7e1a9df36f0
c1ccccc1
[O;D1;H0:1]=[C:2]1-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[O;H0;D2;+0:7]-1.[c:8]:[c:9]:[cH;D2;+0:10]:[c:11]:[c:12]>>[O;D1;H0:1]=[C:2](-[OH;D1;+0:7])-[C:3]-[C:4]-[C;H0;D3;+0:5](=[O;D1;H0:6])-[c;H0;D3;+0:10](:[c:9]:[c:8]):[c:11]:[c:12]
null
[]
null
null
3
HOUR
5 cm3 of ethylbenzene and 2.6 g of aluminum chloride are mixed with magnetic stirring in a 50-cm3 flask. The solution is cooled in an ice bath and 1 g of succinic anhydride is then added. The reaction mixture is stirred for 1 h 30 min at a temperature of 0° C. and then for 3 h at room temperature. It is poured into ice...
10.6084/m9.figshare.5104873.v1
null
Anhydride
Carboxylic acid.Ketone
c1ccccc1.C1CCOC1
c1ccccc1
c1ccccc1
null
null
null
3
CCc1ccccc1.O=C1CCC(=O)O1>>CCc1ccc(C(=O)CCC(=O)O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ff41cf49840a4862bb629df3394008db
CCc1ccc(C(=O)CCC(=O)O)cc1>>CCc1ccc(CCCC(=O)O)cc1
C(C)[SiH](CC)CC.O=C(CCC(=O)O)C1=CC=C(C=C1)CC>>C(C)C1=CC=C(C=C1)CCCC(=O)O
O=[C:7]([c:6]1[cH:5][cH:4][c:3]([CH2:2][CH3:1])[cH:14][cH:13]1)[CH2:8][CH2:9][C:10](=[O:11])[OH:12]>>[CH3:1][CH2:2][c:3]1[cH:4][cH:5][c:6]([CH2:7][CH2:8][CH2:9][C:10](=[O:11])[OH:12])[cH:13][cH:14]1
CCc1ccc(C(=O)CCC(=O)O)cc1
CCc1ccc(CCCC(=O)O)cc1
null
null
FC(C(=O)O)(F)F
Reduction
OtherReaction
bdac4f77103f4da1c5b42ea95e05b0b7b31176b78204db5f4144ffca7b3d54d5
f9ba67182f94acd5fbe41487f8f71e26bccf898b8fc8091ef46f4363de5628d4
c1ccccc1
O=[C;H0;D3;+0:1](-[C:2]-[C:3]-[C:4](=[O;D1;H0:5])-[O;D1;H1:6])-[c:7](:[c:8]):[c:9]>>[O;D1;H0:5]=[C:4](-[O;D1;H1:6])-[C:3]-[C:2]-[CH2;D2;+0:1]-[c:7](:[c:8]):[c:9]
null
[]
null
null
86
HOUR
In a 100-cm3 flask, 2.5 g of 4-oxo-4-(4-ethylphenyl)butyric acid are dissolved with magnetic stirring in 19 cm3 of trifluoroacetic acid. 3.2 g of triethylsilane are added dropwise. The reaction mixture is stirred for 86 hours at room temperature. It is poured into ice. It is extracted with 3 volumes of ether. The organ...
10.6084/m9.figshare.5104873.v1
null
Ketone
null
null
null
c1ccccc1
Other
FC(C(=O)O)(F)F
null
86
CCc1ccc(C(=O)CCC(=O)O)cc1>FC(C(=O)O)(F)F>CCc1ccc(CCCC(=O)O)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ebf01e6b38bc42c089b9940d05b2423f
COc1ccc2cccc(CCCOS(C)(=O)=O)c2c1.[C-]#N>>COc1ccc2cccc(CCCC#N)c2c1
[C-]#N.[K+].S(C)(=O)(=O)OCCCC1=CC=CC2=CC=C(C=C12)OC>>COC1=CC=C2C=CC=C(C2=C1)CCCC#N
CS(=O)(=O)O[CH2:13][CH2:12][CH2:11][c:10]1[cH:9][cH:8][cH:7][c:6]2[cH:5][cH:4][c:3]([O:2][CH3:1])[cH:17][c:16]21.[C-:14]#[N:15]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][CH2:13][C:14]#[N:15])[c:16]2[cH:17]1
COc1ccc2cccc(CCCOS(C)(=O)=O)c2c1.[C-]#N
COc1ccc2cccc(CCCC#N)c2c1
null
null
CS(=O)C
C-C Coupling
OtherReaction
18f4bbb9c586d5002707644e5539611116bc9c01fc56c5a56ec0d1b0251f5f0b
89d1e6e004e8ba10561e22cfb8893e96c375691951aae8f42243dfb0e0a04eec
c1ccc2ccccc2c1
C-S(=O)(=O)-O-[CH2;D2;+0:1]-[C:2]-[C:3].[C-;H0;D1:4]#[N;D1;H0:5]>>[C:3]-[C:2]-[CH2;D2;+0:1]-[C;H0;D2;+0:4]#[N;D1;H0:5]
null
[]
null
null
null
null
In a 100-cm3 flask, the 3-(7-methoxy-1-naphthyl)propyl mesylate obtained in stage D is dissolved in DMSO. KCN is added and the mixture is brought to reflux for 2 h. It is allowed to cool. It is poured into a water/ice mixture. The resulting mixture is extracted with ether. The organic phase is washed with water, dried ...
10.6084/m9.figshare.5104873.v1
null
Mesylate
Nitrile
null
null
c1ccc2ccccc2c1
MsOH.HO-
CS(=O)C
null
null
COc1ccc2cccc(CCCOS(C)(=O)=O)c2c1.[C-]#N>CS(=O)C>COc1ccc2cccc(CCCC#N)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-23a827758ec74998ac781f9b6412b1c4
CC(=O)Cl.COc1ccc2cccc(CCCN)c2c1>>COc1ccc2cccc(CCCNC(C)=O)c2c1
Cl.C([O-])([O-])=O.[K+].[K+].Cl.COC1=CC=C2C=CC=C(C2=C1)CCCN.C(C)(=O)Cl>>COC1=CC=C2C=CC=C(C2=C1)CCCNC(C)=O
Cl[C:15]([CH3:16])=[O:17].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][CH2:13][NH2:14])[c:18]2[cH:19]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:9][c:10]([CH2:11][CH2:12][CH2:13][NH:14][C:15]([CH3:16])=[O:17])[c:18]2[cH:19]1
CC(=O)Cl.COc1ccc2cccc(CCCN)c2c1
COc1ccc2cccc(CCCNC(C)=O)c2c1
null
null
O
Acylation
Acylation of Nitrogen Nucleophiles by Acyl/Thioacyl/Carbamoyl Halides and Analogs_OS
38143a4d536201990008fd6f2c68e6571a341d1c367481869fbbbe36cb038937
0e6ae078978e324f714e184b4f72826d4e3bf2d9ab22d6e9f73740af687be16f
c1ccc2ccccc2c1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[C:4]-[C:5]-[NH2;D1;+0:6]>>[C:4]-[C:5]-[NH;D2;+0:6]-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3]
null
[]
null
null
2
HOUR
After 0.005 mol (equivalent to 1.26 g) of 3-(7-methoxy-1-naphthyl)propylamine hydrochloride has been dissolved in 20 cm3 of water, 0.015 mol of potassium carbonate is added. The amine precipitates. Thereafter, 50 cm3 of chloroform are added and 0.010 mol of acetyl chloride is added dropwise. The medium is left stirring...
10.6084/m9.figshare.5104873.v1
null
Acyl halide.Primary amine
Secondary amide
null
null
c1ccc2ccccc2c1
HCl
O
null
2
CC(=O)Cl.COc1ccc2cccc(CCCN)c2c1>O>COc1ccc2cccc(CCCNC(C)=O)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-97b454fff5d740a79020045a749f01a7
COc1ccc2cccc(CCCNC(C)=O)c2c1.O=C(Cl)c1ccccc1>>COc1ccc2cc(C(=O)c3ccccc3)cc(CCCNC(C)=O)c2c1
COC1=CC=C2C=CC=C(C2=C1)CCCNC(C)=O.C(C1=CC=CC=C1)(=O)Cl>>COC1=CC=C2C=C(C=C(C2=C1)CCCNC(C)=O)C(C1=CC=CC=C1)=O
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:17][c:18]([CH2:19][CH2:20][CH2:21][NH:22][C:23]([CH3:24])=[O:25])[c:26]2[cH:27]1.Cl[C:9](=[O:10])[c:11]1[cH:12][cH:13][cH:14][cH:15][cH:16]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][c:8]([C:9](=[O:10])[c:11]3[cH:12][cH:13][cH:14][cH:15][cH:16]3)[cH:17][c:18]([CH2:1...
COc1ccc2cccc(CCCNC(C)=O)c2c1.O=C(Cl)c1ccccc1
COc1ccc2cc(C(=O)c3ccccc3)cc(CCCNC(C)=O)c2c1
null
null
null
C-C Coupling
Friedel-Crafts acylation
12bfc1cb494a0014608d71eb38cabea029a6bf3a3526b0cc7babc0ad4f29f3e1
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
O=C(c1ccccc1)c1ccc2ccccc2c1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[c:6]:[c:7]:[cH;D2;+0:8]:[c:9]:[c:10]>>[O;D1;H0:2]=[C;H0;D3;+0:1](-[c:3](:[c:4]):[c:5])-[c;H0;D3;+0:8](:[c:7]:[c:6]):[c:9]:[c:10]
null
[]
null
null
null
null
By reacting N-[3-(7-methoxy-1-naphthyl)propyl]acetamide obtained in Example 1 with benzoyl chloride, the compound of the title is obtained. Conditions: See reaction.notes.procedure_details. Workup: the compound of the title is obtained
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1.c1ccccc1
HCl
null
null
null
COc1ccc2cccc(CCCNC(C)=O)c2c1.O=C(Cl)c1ccccc1>>COc1ccc2cc(C(=O)c3ccccc3)cc(CCCNC(C)=O)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-412e177c658c41ed889ff8abc67dfcca
CC(=O)Cl.COc1ccc2cccc(CCCNC(C)=O)c2c1>>COc1ccc2cc(C(C)=O)cc(CCCNC(C)=O)c2c1
COC1=CC=C2C=CC=C(C2=C1)CCCNC(C)=O.C(C)(=O)Cl>>COC1=CC=C2C=C(C=C(C2=C1)CCCNC(C)=O)C(C)=O
Cl[C:9]([CH3:10])=[O:11].[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][cH:8][cH:12][c:13]([CH2:14][CH2:15][CH2:16][NH:17][C:18]([CH3:19])=[O:20])[c:21]2[cH:22]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6]2[cH:7][c:8]([C:9]([CH3:10])=[O:11])[cH:12][c:13]([CH2:14][CH2:15][CH2:16][NH:17][C:18]([CH3:19])=[O:20])[c:21]2[cH:22]1
CC(=O)Cl.COc1ccc2cccc(CCCNC(C)=O)c2c1
COc1ccc2cc(C(C)=O)cc(CCCNC(C)=O)c2c1
null
null
null
C-C Coupling
Friedel-Crafts acylation
12bfc1cb494a0014608d71eb38cabea029a6bf3a3526b0cc7babc0ad4f29f3e1
fe2a4a0dfbb5b71b9a065e092364c64b22b4eb1ad4d6ba2a1e8edc9d31fce3e4
c1ccc2ccccc2c1
Cl-[C;H0;D3;+0:1](-[C;D1;H3:2])=[O;D1;H0:3].[c:4]:[c:5]:[cH;D2;+0:6]:[c:7]:[c:8]>>[C;D1;H3:2]-[C;H0;D3;+0:1](=[O;D1;H0:3])-[c;H0;D3;+0:6](:[c:5]:[c:4]):[c:7]:[c:8]
null
[]
null
null
null
null
By reacting N-[3-(7-methoxy-1-naphthyl)propyl]acetamide obtained in Example 1 with acetyl chloride, the compound of the title is obtained. Conditions: See reaction.notes.procedure_details. Workup: the compound of the title is obtained
10.6084/m9.figshare.5104873.v1
null
Acyl halide
Ketone
c1ccc2ccccc2c1
c1ccc2ccccc2c1
c1ccc2ccccc2c1
HCl
null
null
null
CC(=O)Cl.COc1ccc2cccc(CCCNC(C)=O)c2c1>>COc1ccc2cc(C(C)=O)cc(CCCNC(C)=O)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-f0a8b290beed4251bf550b18be2b89c0
Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)Cl.N=C(N)N>>Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)N=C(N)N
CC1=C(C(=O)Cl)C=C(C(=C1)C1C=CCC1)S(=O)(=O)C.NC(=N)N.[Cl-].NC(=[NH2+])N.[Na].CC1C(C(=O)OC)=CC(=C(C1=S(=O)=O)Br)C.C1=CCCC1>>NC(=NC(C1=C(C=C(C(=C1)S(=O)(=O)C)C1C=CCC1)C)=O)N
Cl[C:17]([c:16]1[c:2]([CH3:1])[cH:3][c:4]([CH:5]2[CH:6]=[CH:7][CH2:8][CH2:9]2)[c:10]([S:11]([CH3:12])(=[O:13])=[O:14])[cH:15]1)=[O:18].[NH:19]=[C:20]([NH2:21])[NH2:22]>>[CH3:1][c:2]1[cH:3][c:4]([CH:5]2[CH:6]=[CH:7][CH2:8][CH2:9]2)[c:10]([S:11]([CH3:12])(=[O:13])=[O:14])[cH:15][c:16]1[C:17](=[O:18])[N:19]=[C:20]([NH2:21...
Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)Cl.N=C(N)N
Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)N=C(N)N
null
null
COCCOC
Acylation
OtherReaction
179ae8baa325b2dace7c965a68a4b2b7e91bea49291f7cdbcd29e5947f465078
edbcca52d877d662e04f0d6de1a7107a8eca1d366ee6da0d92e37eb02a291876
C1=CC(c2ccccc2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[C:7](-[N;D1;H2:8])=[NH;D1;+0:9]>>[N;D1;H2:6]-[C:7](-[N;D1;H2:8])=[N;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
2
HOUR
A fresh guanidine solution prepared from 5.6 g of guanidinium chloride and 1.6 g of sodium in 40 ml of ethylene glycol dimethyl ether is added to a solution of 1.2 g of 2-methyl-4-(1-cyclopentene-3-yl)-5-methylsulfonylbenzoyl chloride [obtainable by reaction of methyl 2-methyl-4-bromo-5-methyl-sulfonyl-benzoate with cy...
10.6084/m9.figshare.5104873.v1
null
Acyl halide
null
null
null
c1ccccc1.C1=CCCC1
HCl
COCCOC
null
2
Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)Cl.N=C(N)N>COCCOC>Cc1cc(C2C=CCC2)c(S(C)(=O)=O)cc1C(=O)N=C(N)N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0c4cda8c04324a8b924c6c3506ced1f7
CS(=O)(=O)O>>CS(=O)(=O)[O-]
NC(=NC(C1=C(C=C(C(=C1)S(=O)(=O)C)C1C=CCC1)C)=O)N.CS(=O)(=O)O>>NC(=NC(C1=C(C=C(C(=C1)S(=O)(=O)C)C1C=CCC1)C)=O)N.CS(=O)(=O)[O-]
[CH3:1][S:2](=[O:3])(=[O:4])[OH:5]>>[CH3:1][S:2](=[O:3])(=[O:4])[O-:5]
CS(=O)(=O)O
CS(=O)(=O)[O-]
null
null
CC(=O)C
Oxidation
OtherReaction
8411f9fce1f185c5c08a89a741e7494817f2d5e55ac6ad2b663e4ffb9ef8fbab
82a3692de44364afcfd8cc4460435180e0752c31812bf6008d75e02664a32947
null
[C;D1;H3:1]-[#16:2](=[O;D1;H0:3])(=[O;D1;H0:4])-[OH;D1;+0:5]>>[C;D1;H3:1]-[#16:2](-[O-;H0;D1:5])(=[O;D1;H0:3])=[O;D1;H0:4]
null
[]
null
null
null
null
700 mg of N-diaminomethylene-2-methyl-4-(1-cyclopenten-3-yl)-5-methylsulfonylbenzamide [which can be prepared according to Example 1; m.p. 212°-214°] are dissolved in 20 ml of acetone, and 6.1 ml of methanesulfonic acid are added, while stirring. Filtration and lyophilization give N-diaminomethylene-2-methyl-4-(1-cyclo...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
null
null
CC(=O)C
null
null
CS(=O)(=O)O>CC(=O)C>CS(=O)(=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-90f641ecf797467592f5799ba146037c
CS(=O)(=O)c1cc(C(=O)Cl)ccc1C1C=CCC1.N=C(N)N>>CS(=O)(=O)c1cc(C(=O)N=C(N)N)ccc1C1C=CCC1
CS(=O)(=O)C=1C=C(C(=O)Cl)C=CC1C1C=CCC1.NC(=N)N>>NC(=NC(C1=CC(=C(C=C1)C1C=CCC1)S(=O)(=O)C)=O)N
Cl[C:8]([c:7]1[cH:6][c:5]([S:2]([CH3:1])(=[O:3])=[O:4])[c:16]([CH:17]2[CH:18]=[CH:19][CH2:20][CH2:21]2)[cH:15][cH:14]1)=[O:9].[NH:10]=[C:11]([NH2:12])[NH2:13]>>[CH3:1][S:2](=[O:3])(=[O:4])[c:5]1[cH:6][c:7]([C:8](=[O:9])[N:10]=[C:11]([NH2:12])[NH2:13])[cH:14][cH:15][c:16]1[CH:17]1[CH:18]=[CH:19][CH2:20][CH2:21]1
CS(=O)(=O)c1cc(C(=O)Cl)ccc1C1C=CCC1.N=C(N)N
CS(=O)(=O)c1cc(C(=O)N=C(N)N)ccc1C1C=CCC1
null
null
null
Acylation
OtherReaction
179ae8baa325b2dace7c965a68a4b2b7e91bea49291f7cdbcd29e5947f465078
edbcca52d877d662e04f0d6de1a7107a8eca1d366ee6da0d92e37eb02a291876
C1=CC(c2ccccc2)CC1
Cl-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5].[N;D1;H2:6]-[C:7](-[N;D1;H2:8])=[NH;D1;+0:9]>>[N;D1;H2:6]-[C:7](-[N;D1;H2:8])=[N;H0;D2;+0:9]-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3](:[c:4]):[c:5]
null
[]
null
null
null
null
Analogously to Example 1, by reaction of 2.2 g of 3-methylsulfonyl-4-(1-cyclopenten-3-yl)-benzoyl chloride with guanidine, customary working up gives N-diaminomethylene-3-methylsulfonyl-4-(1-cyclopenten-3-yl)benzamide, which can be recrystallized from acetonitrile/diethylether, m.p. 188°-190°. Conditions: See reaction....
10.6084/m9.figshare.5104873.v1
null
Acyl halide
null
null
null
c1ccccc1.C1=CCCC1
HCl
null
null
null
CS(=O)(=O)c1cc(C(=O)Cl)ccc1C1C=CCC1.N=C(N)N>>CS(=O)(=O)c1cc(C(=O)N=C(N)N)ccc1C1C=CCC1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-b9a7eb44685f468d8f6ff10d7448f0ce
C#Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O.N=C(N)N>>C=Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O
[H][H].NC(=NC(C1=C(C=C(C(=C1)S(=O)(=O)C)C#C)C)=O)N.CC1=C(C(=O)OC)C=C(C(=C1)Br)S(=O)(=O)C.CC1=C(C(=O)OC)C=C(C(=C1)C#C)S(=O)(=O)C.NC(=N)N>>NC(=NC(C1=C(C=C(C(=C1)S(=O)(=O)C)C=C)C)=O)N
NC(N)=N[C:8]([c:7]1[c:5]([CH3:6])[cH:4][c:3]([C:2]#[CH:1])[c:15]([S:16]([CH3:17])(=[O:18])=[O:19])[cH:14]1)=[O:9].[NH:10]=[C:11]([NH2:12])[NH2:13]>>[CH2:1]=[CH:2][c:3]1[cH:4][c:5]([CH3:6])[c:7]([C:8](=[O:9])[N:10]=[C:11]([NH2:12])[NH2:13])[cH:14][c:15]1[S:16]([CH3:17])(=[O:18])=[O:19]
C#Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O.N=C(N)N
C=Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O
null
[Pd].C(=O)([O-])[O-].[Ca+2]
CN(C)C=O
Acylation
OtherReaction
f724adc768b346031737a96e026428a011a44d8640356509ca79dfcc8ffff7d9
96baac3eb89613d5226811d099c12ee84b213a1838d7b0a18d41caca2f6cdb3f
c1ccccc1
N-C(-N)=N-[C;H0;D3;+0:1](=[O;D1;H0:2])-[c:3]1:[c:4]:[c:5]:[c:6](-[C;H0;D2;+0:7]#[CH;D1;+0:8]):[c:9]:[c:10]:1.[N;D1;H2:11]-[C:12](-[N;D1;H2:13])=[NH;D1;+0:14]>>[CH2;D1;+0:8]=[CH;D2;+0:7]-[c:6]1:[c:5]:[c:4]:[c:3](-[C;H0;D3;+0:1](=[O;D1;H0:2])-[N;H0;D2;+0:14]=[C:12](-[N;D1;H2:11])-[N;D1;H2:13]):[c:10]:[c:9]:1
null
[]
null
null
null
null
6.0 g of N-diaminomethylene-2-methyl-4-ethynyl-5-methylsulfonylbenzamide, m.p. 223°-226° [obtainable by reaction of methyl 2-methyl-4-bromo-5-methylsulfonyl-benzoate with Li acetylide to give methyl 2-methyl-4-ethynyl-5-methylsulfonyl-benzoate and subsequent reaction with guanidine] are dissolved in 300 ml of DMF and h...
10.6084/m9.figshare.5104873.v1
null
Primary amine.Primary amine.Alkyne
Vinyl
null
null
c1ccccc1
Other
[Pd].C(=O)([O-])[O-].[Ca+2].CN(C)C=O
null
null
C#Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O.N=C(N)N>[Pd].C(=O)([O-])[O-].[Ca+2].CN(C)C=O>C=Cc1cc(C)c(C(=O)N=C(N)N)cc1S(C)(=O)=O
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-aa0f7fe1f9b24e3d99fc0030bef32d89
COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>>COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1N
[N+](=O)([O-])C=1C=C(C=CC1OC)\C=C/C1=CC(=C(C(=C1)OC)OC)OC>>NC=1C=C(C=CC1OC)\C=C/C1=CC(=C(C(=C1)OC)OC)OC
O=[N+:23]([O-])[c:22]1[c:3]([O:2][CH3:1])[cH:4][cH:5][c:6](/[CH:7]=[CH:8]\[c:9]2[cH:10][c:11]([O:12][CH3:13])[c:14]([O:15][CH3:16])[c:17]([O:18][CH3:19])[cH:20]2)[cH:21]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[CH:8]\[c:9]2[cH:10][c:11]([O:12][CH3:13])[c:14]([O:15][CH3:16])[c:17]([O:18][CH3:19])[cH:20]2)[cH:21][c...
COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1N
null
[Zn]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=C\c1ccccc1)\c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
49.3
[{"value": 49.3, "product": "NC=1C=C(C=CC1OC)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.1, "product": "NC=1C=C(C=CC1OC)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
700 mg of (Z)-1-(3-nitro-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl) ethene were dissolved in 35 ml of acetic acid, and 7 g of zinc were added thereto and stirred for one hour. The reaction liquid was filtered, concentrated and purified by silica gel column chromatography (dichloromethane:hexane=2:1 by volume) to obtai...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Zn].C(C)(=O)O
null
1
COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>[Zn].C(C)(=O)O>COc1ccc(/C=C\c2cc(OC)c(OC)c(OC)c2)cc1N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7682e2cee87a4592adfa5b6aefdb5c2b
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.O=Cc1ccc(Cl)c([N+](=O)[O-])c1>>COc1cc(/C=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
[Cl-].[Na+].[N+](=O)([O-])C=1C=C(C=O)C=CC1Cl.[Br-].COC=1C=C(CP(C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)C=C(C1OC)OC.[H-].[Na+]>>[N+](=O)([O-])C=1C=C(C=CC1Cl)\C=C/C1=CC(=C(C(=C1)OC)OC)OC
c1ccc([PH](c2ccccc2)(c2ccccc2)[CH2:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[c:19]([O:20][CH3:21])[cH:18]2)cc1.O=[CH:7][c:8]1[cH:9][cH:10][c:11]([Cl:12])[c:13]([N+:14](=[O:15])[O-:16])[cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[CH:6]=[CH:7]\[c:8]2[cH:9][cH:10][c:11]([Cl:12])[c:13]([N+:14](=[O:15])[O-:16])[c...
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.O=Cc1ccc(Cl)c([N+](=O)[O-])c1
COc1cc(/C=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
null
null
C(C)(=O)O.C1=CC=CC=C1
C-C Coupling
OtherReaction
cb5f277ac55a0e763ef643becc05f1522019cc4161daceb249ed2d634b78153b
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
C(=C\c1ccccc1)\c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6](-[CH2;D2;+0:7]-[PH](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[c:8]>>[c:3]:[c:2](/[CH;D2;+0:1]=[CH;D2;+0:7]\[c:6](:[c:5]):[c:8]):[c:4]
50.9
[{"value": 50.9, "product": "[N+](=O)([O-])C=1C=C(C=CC1Cl)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.0 g of 3-nitro-4-chlorobenzaldehyde and 2.8 g of 3,4,5-trimethoxybenzyltriphenylphosphine bromide were dissolved in 50 ml of benzene, and a benzene solution containing 260 mg of sodium hydride dispersed therein was added thereto and reacted for 15 hours at room temperature. The reaction liquid was neutralized with ac...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1.c1ccccc1
HO-
C(C)(=O)O.C1=CC=CC=C1
null
null
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.O=Cc1ccc(Cl)c([N+](=O)[O-])c1>C(C)(=O)O.C1=CC=CC=C1>COc1cc(/C=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d94aaed8109c4f10b8798228c27f900e
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]>>COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
[Cl-].[Na+].[N+](=O)([O-])C=1C=C(C=O)C=CC1C.[Br-].COC=1C=C(CP(C2=CC=CC=C2)(C2=CC=CC=C2)C2=CC=CC=C2)C=C(C1OC)OC.[H-].[Na+]>>[N+](=O)([O-])C=1C=C(C=CC1C)\C=C/C1=CC(=C(C(=C1)OC)OC)OC
c1ccc([PH](c2ccccc2)(c2ccccc2)[CH2:6][c:5]2[cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[c:19]([O:20][CH3:21])[cH:18]2)cc1.O=[CH:7][c:8]1[cH:9][cH:10][c:11]([CH3:12])[c:13]([N+:14](=[O:15])[O-:16])[cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[CH:6]=[CH:7]\[c:8]2[cH:9][cH:10][c:11]([CH3:12])[c:13]([N+:14](=[O:15])[O-:16])...
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]
COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
null
null
C(C)(=O)O.C1=CC=CC=C1
C-C Coupling
OtherReaction
cb5f277ac55a0e763ef643becc05f1522019cc4161daceb249ed2d634b78153b
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
C(=C\c1ccccc1)\c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[c:5]:[c:6](-[CH2;D2;+0:7]-[PH](-c1:c:c:c:c:c:1)(-c1:c:c:c:c:c:1)-c1:c:c:c:c:c:1):[c:8]>>[c:3]:[c:2](/[CH;D2;+0:1]=[CH;D2;+0:7]\[c:6](:[c:5]):[c:8]):[c:4]
49.6
[{"value": 49.6, "product": "[N+](=O)([O-])C=1C=C(C=CC1C)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.0 g of 3-nitro-4-methylbenzaldehyde and 3.3 g of 3,4,5-trimethoxybenzyltriphenylphosphine bromide were dissolved in 50 ml of benzene, and a benzene solution containing 302 mg of sodium hydride dispersed therein was added thereto and reacted for 15 hours at room temperature. The reaction liquid was neutralized with ac...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccccc1.c1ccccc1
HO-
C(C)(=O)O.C1=CC=CC=C1
null
null
COc1cc(C[PH](c2ccccc2)(c2ccccc2)c2ccccc2)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]>C(C)(=O)O.C1=CC=CC=C1>COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-8e7d1432c9064f03900f1184067040ee
COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>>COc1cc(/C=C\c2ccc(C)c(N)c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=CC1C)\C=C/C1=CC(=C(C(=C1)OC)OC)OC>>NC=1C=C(C=CC1C)\C=C/C1=CC(=C(C(=C1)OC)OC)OC
O=[N+:14]([O-])[c:13]1[c:11]([CH3:12])[cH:10][cH:9][c:8](/[CH:7]=[CH:6]\[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:20]([O:21][CH3:22])[c:17]([O:18][CH3:19])[cH:16]2)[cH:15]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[CH:6]=[CH:7]\[c:8]2[cH:9][cH:10][c:11]([CH3:12])[c:13]([NH2:14])[cH:15]2)[cH:16][c:17]([O:18][CH3:19])[c:20]1[O:21][CH3:22...
COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
COc1cc(/C=C\c2ccc(C)c(N)c2)cc(OC)c1OC
null
[Zn]
C(C)(=O)O.ClCCl
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=C\c1ccccc1)\c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
49.1
[{"value": 46.5, "product": "NC=1C=C(C=CC1C)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.1, "product": "NC=1C=C(C=CC1C)\\C=C/C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
65 mg of (Z)-1-(3-nitro-4-methylphenyl)-2-(3,4,5-trimethoxyphenyl) ethene were dissolved in 4 ml of acetic acid and 4 ml of dichloromethane, and 300 mg of zinc were added thereto and stirred for one hour. The reaction liquid was filtered, concentrated and purified by silica gel column chromatography (dichloromethane:he...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Zn].C(C)(=O)O.ClCCl
null
1
COc1cc(/C=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>[Zn].C(C)(=O)O.ClCCl>COc1cc(/C=C\c2ccc(C)c(N)c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-404ecda70ed446ed84b005842ee3c774
COc1ccc(/C=C(\C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>>COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
[N+](=O)([O-])C=1C=C(C=CC1OC)\C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>[N+](=O)([O-])C=1C=C(C=CC1OC)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[C:8](\[C:9]#[N:10])[c:11]2[cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[c:19]([O:20][CH3:21])[cH:22]2)[cH:23][c:24]1[N+:25](=[O:26])[O-:27]>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[C:8](/[C:9]#[N:10])[c:11]2[cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[c:19]...
COc1ccc(/C=C(\C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
null
null
C(C)#N
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
C(=Cc1ccccc1)c1ccccc1
null
49.8
[{"value": 49.0, "product": "[N+](=O)([O-])C=1C=C(C=CC1OC)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 49.8, "product": "[N+](=O)([O-])C=1C=C(C=CC1OC)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
2.0 g of (Z)-3-(3-nitro-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile were dissolved in 500 ml of acetonitrile and exposed to visible light rays for 60 minutes. The reaction liquid was concentrated and crystallized from ethyl acetate to obtain 996 mg of the intended compound. The yield was 49%. Conditi...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1
null
C(C)#N
null
null
COc1ccc(/C=C(\C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>C(C)#N>COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ed51f9672c6c4e2fa5a22df5f59b9419
COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>>COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1N
[N+](=O)([O-])C=1C=C(C=CC1OC)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>NC=1C=C(C=CC1OC)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
O=[N+:25]([O-])[c:24]1[c:3]([O:2][CH3:1])[cH:4][cH:5][c:6](/[CH:7]=[C:8](/[C:9]#[N:10])[c:11]2[cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[c:19]([O:20][CH3:21])[cH:22]2)[cH:23]1>>[CH3:1][O:2][c:3]1[cH:4][cH:5][c:6](/[CH:7]=[C:8](/[C:9]#[N:10])[c:11]2[cH:12][c:13]([O:14][CH3:15])[c:16]([O:17][CH3:18])[c:19]([O:20...
COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]
COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1N
null
[Zn]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=Cc1ccccc1)c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
99.5
[{"value": 99.0, "product": "NC=1C=C(C=CC1OC)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 99.5, "product": "NC=1C=C(C=CC1OC)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
30
MINUTE
500 mg of (E)-3-(3-nitro-4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile were dissolved in 25 ml of acetic acid, and 5 g of zinc were added thereto and stirred for 30 minutes at room temperature. The reaction liquid was filtered and then concentrated. The concentrated liquid was purified by silica gel co...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Zn].C(C)(=O)O
null
0.5
COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1[N+](=O)[O-]>[Zn].C(C)(=O)O>COc1ccc(/C=C(/C#N)c2cc(OC)c(OC)c(OC)c2)cc1N
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0522bf4210474a18b5909e43c5604b2d
COc1cc(CC#N)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]>>COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=O)C=CC1C.COC=1C=C(C=C(C1OC)OC)CC#N.[OH-].[Na+]>>[N+](=O)([O-])C=1C=C(C=CC1C)\C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
[CH3:1][O:2][c:3]1[cH:4][c:5]([CH2:6][C:7]#[N:8])[cH:20][c:21]([O:22][CH3:23])[c:24]1[O:25][CH3:26].O=[CH:9][c:10]1[cH:11][cH:12][c:13]([CH3:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]/[c:10]2[cH:11][cH:12][c:13]([CH3:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)...
COc1cc(CC#N)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]
COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
null
[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC
ClCCl.O
C-C Coupling
OtherReaction
43d4e2f03e758941ee99f59641d5d56e6475fe935434d251d75d5cdebbe19869
cedc9d4b791e43eacf8e7ecfa6a98d1dc0438794e96e4f1c4bef436b78f82bd8
C(=C/c1ccccc1)\c1ccccc1
O=[CH;D2;+0:1]-[c:2](:[c:3]):[c:4].[N;D1;H0:5]#[C:6]-[CH2;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[N;D1;H0:5]#[C:6]/[C;H0;D3;+0:7](=[CH;D2;+0:1]\[c:2](:[c:3]):[c:4])-[c:8](:[c:9]):[c:10]
14.1
[{"value": 14.1, "product": "[N+](=O)([O-])C=1C=C(C=CC1C)\\C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 14.0, "product": "[N+](=O)([O-])C=1C=C(C=CC1C)\\C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
3
HOUR
5.0 g of 3-nitro-4-methylbenzaldehyde, 6.27 g of 3,4,5-trimethoxyphenylacetonitrile, 1.44 g of sodium hydroxide and 500 mg of trioctylmethylammonium chloride were dissolved in 25 ml of water and 500 ml of dichloromethane. The mixture was stirred vigorously for 3 hours at room temperature. The ice water was added to the...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
null
null
null
c1ccccc1.c1ccccc1
HO-
[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC.ClCCl.O
null
3
COc1cc(CC#N)cc(OC)c1OC.Cc1ccc(C=O)cc1[N+](=O)[O-]>[Cl-].C(CCCCCCC)[N+](C)(CCCCCCCC)CCCCCCCC.ClCCl.O>COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-57d4b77be99049839cad797e5f680f84
COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>>COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=CC1C)\C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>[N+](=O)([O-])C=1C=C(C=CC1C)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]/[c:10]2[cH:11][cH:12][c:13]([CH3:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)[cH:20][c:21]([O:22][CH3:23])[c:24]1[O:25][CH3:26]>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]\[c:10]2[cH:11][cH:12][c:13]([CH3:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)...
COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
null
null
CC(=O)C
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
C(=C\c1ccccc1)\c1ccccc1
null
7.2
[{"value": 7.2, "product": "[N+](=O)([O-])C=1C=C(C=CC1C)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.38 g of (Z)-3-(3-nitro-4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile was dissolved in 500 ml of acetone and the mixture was reacted in a photochemical apparatus (visible light) for 1 hour. The reaction mixture was concentrated and a quarter of it was purified on a silica gel plate to give 100 mg of th...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1
null
CC(=O)C
null
null
COc1cc(/C(C#N)=C/c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>CC(=O)C>COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-ed7ebba3c7234968814e60ccc77d8c58
COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>>COc1cc(/C(C#N)=C\c2ccc(C)c(N)c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=CC1C)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>NC=1C=C(C=CC1C)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
O=[N+:16]([O-])[c:15]1[c:13]([CH3:14])[cH:12][cH:11][c:10](/[CH:9]=[C:6](\[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[c:19]([O:20][CH3:21])[cH:18]2)[C:7]#[N:8])[cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]\[c:10]2[cH:11][cH:12][c:13]([CH3:14])[c:15]([NH2:16])[cH:17]2)[cH:18][c:19]([O:20][...
COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC
COc1cc(/C(C#N)=C\c2ccc(C)c(N)c2)cc(OC)c1OC
null
[Zn]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=C\c1ccccc1)\c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
78
[{"value": 78.0, "product": "NC=1C=C(C=CC1C)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
84 mg of (E)-3-(3-nitro-4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile was dissolved in 8 ml of acetic acid then zinc was added to the mixture. The mixture was stirred vigorously for 1 hour then filtered and concentrated. The residue was purified on a silica gel plate (dichloromethane) to give 60 mg of t...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Zn].C(C)(=O)O
null
1
COc1cc(/C(C#N)=C\c2ccc(C)c([N+](=O)[O-])c2)cc(OC)c1OC>[Zn].C(C)(=O)O>COc1cc(/C(C#N)=C\c2ccc(C)c(N)c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-0713a93170224a6cbc1dbbb08f705236
COc1cc(/C(C#N)=C/c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC>>COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=CC1Cl)\C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>[N+](=O)([O-])C=1C=C(C=CC1Cl)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]/[c:10]2[cH:11][cH:12][c:13]([Cl:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)[cH:20][c:21]([O:22][CH3:23])[c:24]1[O:25][CH3:26]>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]\[c:10]2[cH:11][cH:12][c:13]([Cl:14])[c:15]([N+:16](=[O:17])[O-:18])[cH:19]2)[c...
COc1cc(/C(C#N)=C/c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
null
null
CC(=O)C
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
C(=C\c1ccccc1)\c1ccccc1
null
26.7
[{"value": 26.7, "product": "[N+](=O)([O-])C=1C=C(C=CC1Cl)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
null
null
1.5 g of (Z)-3-(3-nitro-4-chlorophenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile was dissolved in 500 ml of acetone and the solution was reacted in a photochemical apparatus (visible light) for 1 hour. The reaction mixture was concentrated and a half of it was purified on a silica gel plate to give 400 mg of the i...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1
null
CC(=O)C
null
null
COc1cc(/C(C#N)=C/c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC>CC(=O)C>COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-7addc825e2ab4603a52563957c8959bb
COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC>>COc1cc(/C(C#N)=C\c2ccc(Cl)c(N)c2)cc(OC)c1OC
[N+](=O)([O-])C=1C=C(C=CC1Cl)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC>>NC=1C=C(C=CC1Cl)/C=C(/C#N)\C1=CC(=C(C(=C1)OC)OC)OC
O=[N+:16]([O-])[c:15]1[c:13]([Cl:14])[cH:12][cH:11][c:10](/[CH:9]=[C:6](\[c:5]2[cH:4][c:3]([O:2][CH3:1])[c:22]([O:23][CH3:24])[c:19]([O:20][CH3:21])[cH:18]2)[C:7]#[N:8])[cH:17]1>>[CH3:1][O:2][c:3]1[cH:4][c:5](/[C:6]([C:7]#[N:8])=[CH:9]\[c:10]2[cH:11][cH:12][c:13]([Cl:14])[c:15]([NH2:16])[cH:17]2)[cH:18][c:19]([O:20][CH...
COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC
COc1cc(/C(C#N)=C\c2ccc(Cl)c(N)c2)cc(OC)c1OC
null
[Zn]
C(C)(=O)O
Reduction
Reduction of nitro groups to amines
bbc242b150a51e69d3ad1caaa391f4422710431b398dcb880555f476706790be
7b0317532ea57a4fcedc1efc3e3c22eb5238d1c8330da53d4f9801fc2391f567
C(=C\c1ccccc1)\c1ccccc1
O=[N+;H0;D3:1](-[O-])-[c:2](:[c:3]):[c:4]>>[NH2;D1;+0:1]-[c:2](:[c:3]):[c:4]
33.6
[{"value": 33.0, "product": "NC=1C=C(C=CC1Cl)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "PERCENTYIELD", "is_desired": false}, {"value": 33.6, "product": "NC=1C=C(C=CC1Cl)/C=C(/C#N)\\C1=CC(=C(C(=C1)OC)OC)OC", "details": "CALCULATEDPERCENTYIELD", "is_desired": false}]
null
null
1
HOUR
(E)-3-(3-nitro-4-chlorophenyl)-2-(3,4,5-trimethoxyphenyl)-prop-2-ene-nitrile 330 mg was dissolved in 8 ml of acetic acid then zinc was added to the mixture. The mixture was stirred vigorously for one hour then filtered and concentrated. The residue was purified on a silica gel plate (dichloromethane) to give 102 mg of ...
10.6084/m9.figshare.5104873.v1
null
Nitro group
Primary amine
null
null
c1ccccc1.c1ccccc1
Other
[Zn].C(C)(=O)O
null
1
COc1cc(/C(C#N)=C\c2ccc(Cl)c([N+](=O)[O-])c2)cc(OC)c1OC>[Zn].C(C)(=O)O>COc1cc(/C(C#N)=C\c2ccc(Cl)c(N)c2)cc(OC)c1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e9dbcb3fceb74a8f85be0773e105b776
CCOc1ccc2[nH]c(=O)c(C(=O)OC)c(-c3ccc4c(c3)OCO4)c2c1.COc1ccccc1CCl>>CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC
ClC(=O)CC(=O)OC.NC1=C(C=C(C=C1)OCC)C(C1=CC2=C(C=C1)OCO2)=O.C(C)(C)(C)OC(=O)NC1=CC=C(C=C1)OCC.C(C)(C)(C)[Li].COC1=C(CCl)C=CC=C1.O1COC2=C1C=CC(=C2)C2=C(C(NC1=CC=C(C=C21)OCC)=O)C(=O)OC.NC1=C(C=C(C=C1)OCC)C(C1=CC2=C(C=C1)OCO2)=O.C1OC=2C=C(C=O)C=CC2O1>>O1COC2=C1C=CC(=C2)C2=C(C(N(C1=CC=C(C=C21)OCC)CC2=C(C=CC=C2)OC)=O)C(=O)OC
[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[c:10](-[c:11]1[cH:12][cH:13][c:14]3[c:15]([cH:16]1)[O:17][CH2:18][O:19]3)[c:20]([C:21](=[O:22])[O:23][CH3:24])[c:25](=[O:26])[nH:27]2.Cl[CH2:28][c:29]1[cH:30][cH:31][cH:32][cH:33][c:34]1[O:35][CH3:36]>>[CH3:1][CH2:2][O:3][c:4]1[cH:5][cH:6][c:7]2[c:8]([cH:9]1)[c:...
CCOc1ccc2[nH]c(=O)c(C(=O)OC)c(-c3ccc4c(c3)OCO4)c2c1.COc1ccccc1CCl
CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC
null
null
C([O-])([O-])=O.[K+].[K+].C1CCOC1.C[O-].[Na+].ClCCl.CN(C)C=O.C(C)N(C(C)C)C(C)C
Heteroatom Alkylation and Arylation
N-alkylation of secondary amines with alkyl halides
1472a48c3f9f0239b8165e6233084b0a0375c831b35ecd4cc0ba8f1bdeda2bcb
2e1e5fd9557b69cb528f6b2ffd179c67ef24ecb1a2c3994e1cdf0efe7ae19e9c
O=c1cc(-c2ccc3c(c2)OCO3)c2ccccc2n1Cc1ccccc1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](=[O;D1;H0:10]):[nH;D2;+0:11]:[c:12](:[c:13]):[c:14]>>[#8:5]-[C:6](=[O;D1;H0:7])-[c:8]:[c:9](=[O;D1;H0:10]):[n;H0;D3;+0:11](-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4]):[c:12](:[c:13]):[c:14]
null
[]
null
null
4
HOUR
A 50% solution of 0.4 g of 2-methoxybenzyl chloride ("A") in dichloromethane is added to a solution of 0.4 g of methyl 4-(1,3-benzodioxol-5-yl)-1, 2-dihydro-6-ethoxy-2-oxoquinoline-3-carboxylate (obtainable by reacting 1-amino-2-(3,4-methylenedioxybenzoyl)-4-ethoxybenzene and methyl chloroformylacetate in dichlorometha...
10.6084/m9.figshare.5104873.v1
null
Primary halide
null
c1cnc2ccccc2c1
c1ccc2ncccc2c1
c1ccc2c(c1)OCO2.c1ccc2ncccc2c1.c1ccccc1
HCl
C([O-])([O-])=O.[K+].[K+].C1CCOC1.C[O-].[Na+].ClCCl.CN(C)C=O.C(C)N(C(C)C)C(C)C
null
4
CCOc1ccc2[nH]c(=O)c(C(=O)OC)c(-c3ccc4c(c3)OCO4)c2c1.COc1ccccc1CCl>C([O-])([O-])=O.[K+].[K+].C1CCOC1.C[O-].[Na+].ClCCl.CN(C)C=O.C(C)N(C(C)C)C(C)C>CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-3aafaa9bc09e4d7e91b49eec25c1596b
CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC.CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC>>CCOc1ccc2nc(OCc3ccccc3OC)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c2c1
O1COC2=C1C=CC(=C2)C2=C(C(N(C1=CC=C(C=C21)OCC)CC2=C(C=CC=C2)OC)=O)C(=O)O.O1COC2=C1C=CC(=C2)C2=C(C(N(C1=CC=C(C=C21)OCC)CC2=C(C=CC=C2)OC)=O)C(=O)OC.[OH-].[K+]>>O1COC2=C1C=CC(=C2)C2=C(C(=NC1=CC=C(C=C21)OCC)OCC2=C(C=CC=C2)OC)C(=O)O
COc1ccccc1C[n:8]1[c:7]2[cH:6][cH:5][c:4]([O:3][CH2:2][CH3:1])[cH:35][c:34]2[c:24](-[c:25]2[cH:26][cH:27][c:28]3[c:29]([cH:30]2)[O:31][CH2:32][O:33]3)[c:20]([C:21](=[O:22])[OH:23])[c:9]1=[O:10].CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2[CH2:11][c:12]1[cH:13][cH:14][cH:15][cH:16][c:17]1[O:18][CH3:19]>>[CH3:1][CH2...
CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC.CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC
CCOc1ccc2nc(OCc3ccccc3OC)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c2c1
null
null
CO
Heteroatom Alkylation and Arylation
OtherReaction
cea3ffee7a800a1fbb53f73f4eeba415dfcf0713f519e40a4bf0949df30e9354
e6e00eccd20c93f6516a052b248fe94c4455c8eeab86eb83aaffcb64ebfad30a
c1ccc(COc2cc(-c3ccc4c(c3)OCO4)c3ccccc3n2)cc1
C-C-O-c1:c:c:c2:c(:c:1):c(-c1:c:c:c3:c(:c:1)-O-C-O-3):c(-C(=O)-O-C):c(=O):n:2-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].C-O-c1:c:c:c:c:c:1-C-[n;H0;D3;+0:5]1:[c:6](:[c:7]):[c:8]:[c:9]:[c:10](-[C:11](=[O;D1;H0:12])-[O;D1;H1:13]):[c;H0;D3;+0:14]:1=[O;H0;D1;+0:15]>>[O;D1;H0:12]=[C:11](-[O;D1;H1:13])-[c:10]1:[c:9]:[c:8]:[c:6](:[c:7...
null
[]
null
null
null
null
A solution of 0.5 g of methyl 4-(1,3-benzodioxol-5-yl)-1,2-dihydro-6-ethoxy-1-(2-methoxybenzyl)-2-oxoquinoline-3-carboxylate and 6 ml of 5N KOH in 10 ml of methanol is boiled under reflux for 2 hours. The usual working up results in 4-(1,3-benzodioxol-5-yl)-1,2-dihydro-6-ethoxy-1-(2-methoxybenzyl)-2-oxoquinoline-3-carb...
10.6084/m9.figshare.5104873.v1
null
Ester.Ether.Ether.Ether.Ether
Ether
c1ccccc1.c1ccc2ncccc2c1.c1ccc2c(c1)OCO2.c1ccc2ncccc2c1
c1ccc2ncccc2c1
c1ccc2ncccc2c1.c1ccccc1.c1ccc2c(c1)OCO2
HO-
CO
null
null
CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)O)c(=O)n2Cc1ccccc1OC.CCOc1ccc2c(c1)c(-c1ccc3c(c1)OCO3)c(C(=O)OC)c(=O)n2Cc1ccccc1OC>CO>CCOc1ccc2nc(OCc3ccccc3OC)c(C(=O)O)c(-c3ccc4c(c3)OCO4)c2c1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-9faac40bc60f4f9481fb3e21ace77f7b
Cc1cc(O)cc(=O)o1.ClCc1ccccc1>>Cc1cc(OCc2ccccc2)cc(=O)o1
C([O-])([O-])=O.[K+].[K+].C(C1=CC=CC=C1)Cl.OC1=CC(OC(=C1)C)=O.C1COCCOCCOCCOCCOCCO1>>C(C1=CC=CC=C1)OC1=CC(OC(=C1)C)=O
[CH3:1][c:2]1[cH:3][c:4]([OH:5])[cH:13][c:14](=[O:15])[o:16]1.Cl[CH2:6][c:7]1[cH:8][cH:9][cH:10][cH:11][cH:12]1>>[CH3:1][c:2]1[cH:3][c:4]([O:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[cH:13][c:14](=[O:15])[o:16]1
Cc1cc(O)cc(=O)o1.ClCc1ccccc1
Cc1cc(OCc2ccccc2)cc(=O)o1
null
null
CN(C=O)C
Heteroatom Alkylation and Arylation
Williamson Ether Synthesis
7e1040116e3a4cf0e8ec5cc7865388d9cd0efabce6d320a1c25a36e411018d8b
d5f4610d46ccc0478471c5bc0fb862644eaf764bbc5d93badb39d54f6ec8e0a5
O=c1cc(OCc2ccccc2)cco1
Cl-[CH2;D2;+0:1]-[c:2](:[c:3]):[c:4].[OH;D1;+0:5]-[c:6]1:[c:7]:[c:8]:[#8;a:9]:[c:10]:[c:11]:1>>[c:3]:[c:2](-[CH2;D2;+0:1]-[O;H0;D2;+0:5]-[c:6]1:[c:7]:[c:8]:[#8;a:9]:[c:10]:[c:11]:1):[c:4]
null
[]
null
null
4.5
HOUR
124.4 g (0.900 mol) potassium carbonate and 63 ml (0.547 mol) benzyl chloride were added in succession to a solution of 56.7 g (0.450 mol) 4-hydroxy-6-methyl-2H-pyran-2-one and 1.0 g (0.004 mol) 18-crown-6 in 900 ml anhydrous dimethyl-formamide. It was stirred vigorously for 4.5 hours at an internal temperature of 70°-...
10.6084/m9.figshare.5104873.v1
null
Primary halide.Aromatic alcohol
Ether
null
null
c1ccocc1.c1ccccc1
HCl
CN(C=O)C
null
4.5
Cc1cc(O)cc(=O)o1.ClCc1ccccc1>CN(C=O)C>Cc1cc(OCc2ccccc2)cc(=O)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-e1aa3216ef4c4a1fb552fae720596c8e
Cc1cc(OCc2ccccc2)cc(=O)o1.O=Cc1ccc(OCc2ccccc2)c(OCc2ccccc2)c1>>O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1
C(C)(C)NC(C)C.C(CCC)[Li].Cl.C(C1=CC=CC=C1)OC=1C=C(C=O)C=CC1OCC1=CC=CC=C1.C(C1=CC=CC=C1)OC1=CC(OC(=C1)C)=O.[Cl-].[NH4+]>>C(C1=CC=CC=C1)OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)OCC1=CC=CC=C1)OCC1=CC=CC=C1)=O
[O:1]=[c:2]1[cH:3][c:4]([O:5][CH2:6][c:7]2[cH:8][cH:9][cH:10][cH:11][cH:12]2)[cH:13][c:14]([CH3:15])[o:40]1.[CH:16](=[O:17])[c:18]1[cH:19][cH:20][c:21]([O:22][CH2:23][c:24]2[cH:25][cH:26][cH:27][cH:28][cH:29]2)[c:30]([O:31][CH2:32][c:33]2[cH:34][cH:35][cH:36][cH:37][cH:38]2)[cH:39]1>>[O:1]=[c:2]1[cH:3][c:4]([O:5][CH2:6...
Cc1cc(OCc2ccccc2)cc(=O)o1.O=Cc1ccc(OCc2ccccc2)c(OCc2ccccc2)c1
O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1
null
null
O1CCCC1
C-C Coupling
OtherReaction
995c7a5cbf37230035b00de18cd91aae550f6b3916b2678b4c13427cfa9d9370
a7cae52d902b2812376f5459a7a8b7ead54e8ef31fd78982d2e99bec532613ba
O=c1cc(OCc2ccccc2)cc(CCc2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1
[CH3;D1;+0:1]-[c:2](:[c:3]):[#8;a:4]:[c:5].[O;H0;D1;+0:6]=[CH;D2;+0:7]-[c:8](:[c:9]):[c:10]>>[OH;D1;+0:6]-[CH;D3;+0:7](-[CH2;D2;+0:1]-[c:2](:[c:3]):[#8;a:4]:[c:5])-[c:8](:[c:9]):[c:10]
68
[{"value": 68.0, "product": "C(C1=CC=CC=C1)OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)OCC1=CC=CC=C1)OCC1=CC=CC=C1)=O", "details": "PERCENTYIELD", "is_desired": false}, {"value": 67.3, "product": "C(C1=CC=CC=C1)OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)OCC1=CC=CC=C1)OCC1=CC=CC=C1)=O", "details": "CALCULATEDPERCENTYIELD", "is_desired": fal...
-78
CELSIUS
45
MINUTE
A solution of 10.1 g (14.0 ml, 100 mmol) diisopropylamine in 150 ml tetrahydrofuran was mixed under nitrogen at -78° C. with 41.0 ml (95 mmol) butyllithium (2.3M in n-hexane). It was allowed to reach 0° C. for a short time and immediately cooled again to -78° C. After a dropwise addition of a solution of 19.0 g (88 mmo...
10.6084/m9.figshare.5104873.v1
null
Aldehyde
Secondary alcohol
null
null
c1ccocc1.c1ccccc1.c1ccccc1.c1ccccc1.c1ccccc1
null
O1CCCC1
-78
0.75
Cc1cc(OCc2ccccc2)cc(=O)o1.O=Cc1ccc(OCc2ccccc2)c(OCc2ccccc2)c1>O1CCCC1>O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-65ca9c80774841d78cc6437f7406abeb
O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1>>O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1
C(C1=CC=CC=C1)OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)OCC1=CC=CC=C1)OCC1=CC=CC=C1)=O.[H][H]>>OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)O)O)=O
c1ccc(C[O:5][c:4]2[cH:3][c:2](=[O:1])[o:19][c:7]([CH2:8][CH:9]([OH:10])[c:11]3[cH:12][cH:13][c:14]([O:15]Cc4ccccc4)[c:16]([O:17]Cc4ccccc4)[cH:18]3)[cH:6]2)cc1>>[O:1]=[c:2]1[cH:3][c:4]([OH:5])[cH:6][c:7]([CH2:8][CH:9]([OH:10])[c:11]2[cH:12][cH:13][c:14]([OH:15])[c:16]([OH:17])[cH:18]2)[o:19]1
O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1
O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1
null
[Ni]
C(C)O
Deprotection
OtherReaction
329bfe228dff858bb5ec6a65da59966cadb6acb2bd1c2a9dde293efaaf235784
c285c154f8bc0deded5c4c3d0a24c6fc98572ede850256e8900bb913cdb4dd9a
O=c1cccc(CCc2ccccc2)o1
C(-[O;H0;D2;+0:1]-[c:2]1:[c:3]:[c:4]:[#8;a:5]:[c:6]:[c:7]:1)-c1:c:c:c:c:c:1.[c:8]:[c:9](-[O;H0;D2;+0:10]-C-c1:c:c:c:c:c:1):[c:11](-[O;H0;D2;+0:12]-C-c1:c:c:c:c:c:1):[c:13]>>[OH;D1;+0:10]-[c:9](:[c:8]):[c:11](-[OH;D1;+0:12]):[c:13].[OH;D1;+0:1]-[c:2]1:[c:3]:[c:4]:[#8;a:5]:[c:6]:[c:7]:1
70
[{"value": 70.0, "product": "OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)O)O)=O", "details": "PERCENTYIELD", "is_desired": false}]
null
null
null
null
35.6 g (66.6 mmol) 4-benzyloxy-6-[2-[3,4-dibenzyloxyphenyl)-2-hydroxy-ethyl)]-2H-pyran-2-one (VI) was hydrogenated for 6 hours at room temperature under a hydrogen pressure of 44 mbar in 1200 ml ethanol using 10 g W2 Raney nickel. After taking up 4.4 l hydrogen the catalyst was removed by suction filtration and it was ...
10.6084/m9.figshare.5104873.v1
null
Ether.Ether.Ether
Aromatic alcohol.Aromatic alcohol.Aromatic alcohol
c1ccccc1.c1ccccc1.c1ccccc1
null
c1ccocc1.c1ccccc1
Other
[Ni].C(C)O
null
null
O=c1cc(OCc2ccccc2)cc(CC(O)c2ccc(OCc3ccccc3)c(OCc3ccccc3)c2)o1>[Ni].C(C)O>O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-2778a9f71b614c56aa952dc1c3b7fac4
O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1>>O=c1cc(O)cc(C=Cc2ccc(O)c(O)c2)o1
C1(=CC=CC=C1)C.C(=O)OCC.CO.Cl.OC1=CC(OC(=C1)CC(O)C1=CC(=C(C=C1)O)O)=O.O1CCCC1>>OC=1C=C(C=CC1O)C=CC1=CC(=CC(O1)=O)O
O[CH:9]([CH2:8][c:7]1[cH:6][c:4]([OH:5])[cH:3][c:2](=[O:1])[o:18]1)[c:10]1[cH:11][cH:12][c:13]([OH:14])[c:15]([OH:16])[cH:17]1>>[O:1]=[c:2]1[cH:3][c:4]([OH:5])[cH:6][c:7]([CH:8]=[CH:9][c:10]2[cH:11][cH:12][c:13]([OH:14])[c:15]([OH:16])[cH:17]2)[o:18]1
O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1
O=c1cc(O)cc(C=Cc2ccc(O)c(O)c2)o1
null
null
C(=O)O
Functional Group Interconversion
OtherReaction
24323612d5486e9fd0704523d3a93bd4db9c6e3295677a91ceb1aea86b497d01
f8118e7f3e1d7109575c0c77239dee8da98ec71a2b23460bcda2084274bdf7e7
O=c1cccc(C=Cc2ccccc2)o1
O-[CH;D3;+0:1](-[CH2;D2;+0:2]-[c:3](:[c:4]):[#8;a:5]:[c:6])-[c:7](:[c:8]):[c:9]>>[c:8]:[c:7](-[CH;D2;+0:1]=[CH;D2;+0:2]-[c:3](:[c:4]):[#8;a:5]:[c:6]):[c:9]
null
[]
null
null
null
null
2 ml 3N HCl was added to a suspension of 8.0 g (30 mmol) 4-hydroxy-6-[2-(3,4-dihydroxyphenyl)-2-hydroxyethyl]-2H-pyran-2-one VII and 300 ml tetrahydrofuran. The resulting clear solution was heated for 2-3 hours under reflux until it was no longer possible to detect starting material. (TLC control, mobile solvent: tolue...
10.6084/m9.figshare.5104873.v1
null
Secondary alcohol
null
null
null
c1ccocc1.c1ccccc1
HO-
C(=O)O
null
null
O=c1cc(O)cc(CC(O)c2ccc(O)c(O)c2)o1>C(=O)O>O=c1cc(O)cc(C=Cc2ccc(O)c(O)c2)o1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-d1e6e90adf2744bfa6b435f6c7114ace
c1ccc([S+](c2ccccc2)c2ccccc2)cc1>>c1ccc([S+](c2ccccc2)c2ccccc2)cc1
ClCCl.ClCCl.[K+].FC(C(C(C(C(C(C(C(F)(F)F)(F)F)(F)F)(F)F)(F)F)(F)F)(F)F)(S(=O)(=O)[O-])F.[Cl-].C1(=CC=CC=C1)[S+](C1=CC=CC=C1)C1=CC=CC=C1>>FC(C(C(C(C(C(C(C(F)(F)F)(F)F)(F)F)(F)F)(F)F)(F)F)(F)F)(S(=O)(=O)[O-])F.C1(=CC=CC=C1)[S+](C1=CC=CC=C1)C1=CC=CC=C1
[cH:30]1[cH:31][cH:32][c:33]([S+:34]([c:35]2[cH:36][cH:37][cH:38][cH:39][cH:40]2)[c:41]2[cH:42][cH:43][cH:44][cH:45][cH:46]2)[cH:47][cH:48]1>>[cH:30]1[cH:31][cH:32][c:33]([S+:34]([c:35]2[cH:36][cH:37][cH:38][cH:39][cH:40]2)[c:41]2[cH:42][cH:43][cH:44][cH:45][cH:46]2)[cH:47][cH:48]1
c1ccc([S+](c2ccccc2)c2ccccc2)cc1
c1ccc([S+](c2ccccc2)c2ccccc2)cc1
null
null
O
Miscellaneous
OtherReaction
40ba59785861b8226ce5af6bdcbb9a37f0ff50a8c7ec7d4fc4c524cf906cc65c
56ebed4a8b3cebec83c37a71d68f0c87d1e404ab05a9ce792691e4e18a2379dd
c1ccc([S+](c2ccccc2)c2ccccc2)cc1
null
null
[]
null
null
30
MINUTE
To a suspension of perfluorooctanesulfonic acid potassium salt (24.64 g, 46.1 mmol) in water (150 ml) at room temperature under nitrogen was added dropwise triphenylsulfonium chloride (50% aqueous solution, 27.50 g) over 15 minutes. After stirring the suspension for 30 minutes, dichloromethane (75 ml) was added and the...
10.6084/m9.figshare.5104873.v1
null
null
null
null
null
c1ccccc1.c1ccccc1.c1ccccc1
null
O
null
0.5
c1ccc([S+](c2ccccc2)c2ccccc2)cc1>O>c1ccc([S+](c2ccccc2)c2ccccc2)cc1
ord_dataset-018fd0e1351f4fd09b20fcddd97b4c7a
ord-36355329f50b4fba91d75f1d3bd8c47f
O=S(=O)(Cl)c1ccc(C(F)(F)F)cc1>>O=S(=O)([O-])c1ccc(C(F)(F)F)cc1
[Cl-].C1(=CC=CC=C1)[S+](C1=CC=CC=C1)C1=CC=CC=C1.ClCCl.FC(C1=CC=C(C=C1)S(=O)(=O)Cl)(F)F.C([O-])([O-])=O.[Na+].[Na+]>>FC(C1=CC=C(C=C1)S(=O)(=O)[O-])(F)F.C1(=CC=CC=C1)[S+](C1=CC=CC=C1)C1=CC=CC=C1
Cl[S:2](=[O:1])(=[O:3])[c:5]1[cH:6][cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14]1>>[O:1]=[S:2](=[O:3])([O-:4])[c:5]1[cH:6][cH:7][c:8]([C:9]([F:10])([F:11])[F:12])[cH:13][cH:14]1
O=S(=O)(Cl)c1ccc(C(F)(F)F)cc1
O=S(=O)([O-])c1ccc(C(F)(F)F)cc1
null
null
O
Functional Group Interconversion
OtherReaction
6c113db978119dd30ec9ac70e3a1ccab457b8adfa2d854ef650cc9d0d938808f
5664dc87dc3eea7f40384c1c98932c2b6f77a01ae2083f96843fa9d662971745
c1ccccc1
Cl-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]>>[O;-;D1;H0:7]-[S;H0;D4;+0:1](=[O;D1;H0:2])(=[O;D1;H0:3])-[c:4](:[c:5]):[c:6]
null
[]
null
null
30
MINUTE
A suspension of 4-trifluoromethylbenzenesulfonyl chloride (20.53 g, 83.9 mmol) in water (150 ml) containing sodium carbonate (9.43 g, 88.10 mmol) was heated at reflux for 22 hours. After cooling to room temperature, triphenylsulfonium chloride (50% aqueous solution, 50.00 g) was added over 15 minutes. After stirring th...
10.6084/m9.figshare.5104873.v1
null
Sulfonyl halide
Sulfonic acid
null
null
c1ccccc1
null
O
null
0.5
O=S(=O)(Cl)c1ccc(C(F)(F)F)cc1>O>O=S(=O)([O-])c1ccc(C(F)(F)F)cc1