Thieno[3,4-b][1,4]diazepine誘導体の合成

概要

論文の詳細を見る
The reaction of 5-substituted (a=CN, b=COOEt, c=COPh, d=CONH_2) 3,4-diamino-2-methylthiothiophenes (1a-b) with 1,3-dicarbonyl compounds (methyl acetoacetate, diethyl or dimethyl acetonedicarboxylate, diketene, ethyl benzoylacetate) gave the corresponding thieno [3,4-b] [1,4] diazepine derivatives (4,5,8,9,11-13). The condensation of 1 with ketenethioacetal derivatives (2-bis (methylthio) methylene-1,3-indandione, 3,3-bis (methylthio)-1-(p-substituted phenyl)-2-propen-1-one (a=p-H, b=p-Cl, c=p-Br)) afforded the corresponding diazepine derivatives, 11-substituted 2,4-bis (methylthio)-3H, 10H-indeno [1', 2' : 7,6] [1,4] diazepino [2,3-c] thiophen-5-ones (15a, b) and 2-cyano-6,8-bis (methylthio)-4-(p-substituted phenyl)-3H-thieno [3,4-b] [1,4] diazepines (19a-c) (a=p-H, b=p-Cl, c=p-Br), in good yields.
社団法人日本薬学会の論文
1980-07-25