首页> 外国专利> RACEMIC OR OPTICALLY ACTIVE ALPHA- (2,3,4-TRIMETHOXYPHENAETHYLAMINOMETHYL) -2-HYDROXYBENZYL ALCOHOL AND PHARMACEUTICALLY ACIDIC ACID SALTS THEREOF.

RACEMIC OR OPTICALLY ACTIVE ALPHA- (2,3,4-TRIMETHOXYPHENAETHYLAMINOMETHYL) -2-HYDROXYBENZYL ALCOHOL AND PHARMACEUTICALLY ACIDIC ACID SALTS THEREOF.

机译:种族或光学活性的α-(2,3,4-三羟苯乙酰胺基)-2-羟基苄基醇及其药学上的酸性盐。

摘要

Racemic or optically active alpha -(2,3,4-trimethoxyphenethylaminomethyl)-2-hydroxybenzylalcohol [I] may be prepared by condensing 2,3,4-trimethoxyphenethylamine with 2-benzyloxyphenylglyoxal or its hydrate, reducing the resultant alpha (2,3,4-tri-methoxyphenethylimino)-2-benzyloxyacetophenone to give alpha (2,3,4-trimethoxyphenethylaminomethyl)-2-benzyloxybenzylalcohol, if required, resolving the 2-benzyloxybenzylalcohol derivative into each of its optically active enantiomers, and subjecting the racemic modification or optically active enantiomer of said 2-benzyloxybenzylalcohol derivative to catalytic hydrogenation. The compound [I] and pharmaceutically acceptable acid addition salts thereof are useful as anti-diabetic agents. They may be also used in the treatment of thrombosis.
机译:外消旋或旋光的α-(2,3,4-三甲氧基苯乙基氨基甲基)-2-羟基苄醇[I]可通过将2,3,4-三甲氧基苯乙胺与2-苄氧基苯基乙二醛或其水合物缩合,还原生成的α(2,3 (4-三甲氧基苯乙基亚氨基)-2-苄氧基苯乙酮,如果需要的话,得到α(2,3,4-三甲氧基苯乙基氨基甲基)-2-苄氧基苄醇,将2-苄氧基苄醇衍生物拆分成每个旋光对映体,并进行外消旋修饰所述2-苄氧基苄醇衍生物的光学活性对映体或催化氢化的旋光对映体。化合物[Ⅰ]及其药学上可接受的酸加成盐可用作抗糖尿病药。它们也可以用于血栓形成的治疗。

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