利塞膦酸钠关键中间体3-乙酰基吡啶的合成

摘要

3-Acetylpyridine is a key intermediate for risedronate sodium.A highly improved and environmentally benign methodology with the advantages of simple materials, simple operation, high yield and suitable for scale-up, has been developed for the synthesis of 3-acetylpyridine from the metal-free Markovnikov-type hydration of 3-ethynylpyridine by using CF3SO3H/CF3CH2OH (n(CF3SO3H)(CF3CH2OH)=20%) as the catalyst under mild conditions.%3-乙酰基吡啶是合成利塞膦酸钠的关键中间体.室温下,以3-乙炔基吡啶在CF3SO3H/CF3CH2OH(n(CF3SO3H)(CF3CH2OH)=20%)催化体系中顺利进行马氏水合反应,反应收率较高,环境友好,该方法同时具有原料易得、反应条件温和、操作简便、适合工业化生产等优点.