Regioselective preparation of substituted N-(1H-pyrazolylmethyl) amide compound, comprises reacting hydrazinomethyl carboxylic acid amide derivative with diacetylene derivative

摘要

Regioselective preparation of substituted N-(1H-pyrazolylmethyl) amide compound (I), comprises reacting hydrazinomethyl carboxylic acid amide derivative (II) with diacetylene derivative (III). Regioselective preparation of substituted N-(1H-pyrazolylmethyl) amide compound of formula (I), comprises reacting hydrazinomethyl carboxylic acid amide derivative of formula (R 3>-C(=O)-NH-CH 2-NH-NH 2) (II) with diacetylene derivative of formula (R 1>-CC-CC-R 2>) (III). R 1>, R 2>6-10C aryl (optionally substituted by halo), 1-4C alkyl (both optionally mono- or polysubstituted by 1-4C alkyl, 1-4C alkylsulfonyl, 1-4C alkoxy, 1-4C acyl, OH, trimethylsilyl, NO 2, CN, carbonyl, carboxyl or 1-5C carboxyalkyl), 3-8C cycloalkyl, preferably cyclopropyl or cyclobutyl, alkyl-aryl with 1-4C alkyl and 6-10C aryl, trialkylsilyl with 1-4C alkyl or H (preferred); and R 3>6-10C aryl (optionally substituted by halo), 1-20C alkyl (both optionally mono- or polysubstituted by 1-4C alkyl, 1-4C alkylsulfonyl, 1-4C alkoxy, 1-4C acyl, OH, trimethylsilyl, NO 2, CN, carbonyl, carboxyl or 1-5C carboxyalkyl), 3-8C cycloalkyl, alkyl-aryl with 1-4C alkyl and 6-10C aryl or H. [Image].