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    • 4. 发明授权
    • 3-Hydroxymethylbenzo[b]thiophene derivatives and process for their preparation
    • 3-羟甲基苯并[b]噻吩衍生物及其制备方法
    • US06774245B2
    • 2004-08-10
    • US10332079
    • 2003-01-02
    • Hiroshi SaitohTsuyoshi MizunoNaoki Tsuchiya
    • Hiroshi SaitohTsuyoshi MizunoNaoki Tsuchiya
    • C07D33356
    • C07D333/56
    • The present invention is a method of producing a 3-hydroxymethyl-benzo[b]thiophene derivative without the possible concomitant formation of isomers, which comprises selectively cyclizing a sulfoxide having X shown in the reaction scheme below: wherein R1 to R3 are, same or independently, a hydrogen atom, an alkyl group having 1 to 4 carbons, a trihalomethyl group, an alkoxy group having 1 to 4 carbons, an alkylthio group having 1 to 4 carbons, or a trihalomethoxy group; R4 is an acyl group; X is a halogen atom, a hydroxy group, an amino group, a mercapto group, an alkylthio group having 1 to 9 carbons, an acyloxy group having 1 to 9 carbons, an acylamino group having 1 to 9 carbons, or a trihalomethoxy group.
    • 本发明是一种不含可能伴随形成异构体的3-羟甲基 - 苯并[b]噻吩衍生物的制备方法,该方法包括选择性环化下述反应方案中所示的具有X的亚砜:其中R1至R3相同或相同 独立地为氢原子,碳原子数1〜4的烷基,三卤代甲基,碳原子数1〜4的烷氧基,碳原子数1〜4的烷硫基或三卤甲氧基。 R4是酰基; X是卤素原子,羟基,氨基,巯基,碳原子数1〜9的烷硫基,碳原子数1〜9的酰氧基,碳原子数1〜9的酰氨基或三卤代甲氧基。