CXCR4拮抗剂普乐沙福的合成工艺改进

摘要

Using ethylenediamine and diethyl malonate as starting materials, a new synthetic process of Plerixafor was developed. With Michael addition, cyclization, nucleophilic substitution by 1, 4-bis ( bromomethyl) benzene, and last redution using the I2-NaBH4 instead of expensive reductant reported in literatures, plerixafor was successful prepared. Comparing with reported method, this new synthetic route can significantly reduce the production cost, has less by-products, is simple and energy-efficient.%本文开发了普乐沙福的一种新合成工艺,以乙二胺、丙二酸二乙酯等常见试剂为起始原料,经Michael加成、成环、与1,4-二(卤代甲基)苯亲核取代,再利用I2-NaBH4还原体系替代文献报道的昂贵还原试剂制备普乐沙福.与原工艺相比,能显著降低生产成本、副产物少、后处理操作简便、节能环保.