p-Toluenesulfonic acid monohydrate → Methyl 2-fluoro-4-[(2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonyl]benzoate

HRID 1881622ノート

反応式

HRID 1881622 の反応式
[C:1]([C:5]1[CH:10]=[CH:9][C:8]([C:11]2[S:12][CH:13]=[C:14]([C:17]([CH3:19])=O)[C:15]=2[OH:16])=[CH:7][CH:6]=1)([CH3:4])([CH3:3])[CH3:2].[F:20][C:21]1[CH:30]=[C:29]([C:31]([NH:33][NH2:34])=[O:32])[CH:28]=[CH:27][C:22]=1[C:23]([O:25][CH3:26])=[O:24].O.S(C1C=CC(C)=CC=1)(O)(=O)=O>>[F:20][C:21]1[CH:30]=[C:29]([C:31]([NH:33][N:34]=[C:17]([C:14]2[C:15]([OH:16])=[C:11]([C:8]3[CH:9]=[CH:10][C:5]([C:1]([CH3:4])([CH3:3])[CH3:2])=[CH:6][CH:7]=3)[S:12][CH:13]=2)[CH3:19])=[O:32])[CH:28]=[CH:27][C:22]=1[C:23]([O:25][CH3:26])=[O:24]

参加物

4

反応物 3

HCID 521998p-Toluenesulfonic acid monohydrateHCID 442072892-(4-t-Butylphenyl)-3-hydroxy-4-methylcarbonylthiopheneHCID 67050257Methyl 2-fluoro-4-hydrazinocarbonylbenzoate

生成物 1

HCID 72360131Methyl 2-fluoro-4-[(2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonyl]benzoate収率 94.2%

実験手順

From 2-(4-t-butylphenyl)-3-hydroxy-4-methylcarbonylthiophene (59.0 mg, 0.215 mmol), methyl 2-fluoro-4-hydrazinocarbonylbenzoate (45.6 mg, 0.215 mmol) and tosylic acid monohydrate (12.3 mg, 0.0645 mmol), 94.9 mg of the desired product was obtained in the same manner as in Synthetic Example 65 as a pale yellow solid (yield 94%).

出典と根拠

ORDレコード
ord-73924b88e8534e8c82a888316c1ffe64
出典データセット
uspto-grants-2012_11
特許番号
US08318796B2

反応ノート

読み込み中…