硼替佐米的合成  

Synthesis of bortezomib

作　　者：丛艳伟 栾春芳 陈宏[2] 张琪 白炘劼 

机构地区：[1]昆明贵研药业有限公司,昆明650106 [2]昆明贵金属研究所,昆明650106

出　　处：《中国新药杂志》2014年第6期698-700,共3页Chinese Journal of New Drugs

摘　　要：目的:合成抗肿瘤新药硼替佐米。方法:以N-(2-吡嗪基羰基)-L-苯丙氨酸同(1R)-(S)-频哪醇-1-三氟乙酸铵-3-甲基丁烷硼酸盐作为起始原料,经缩合、脱保护基、水解等反应制成硼替佐米。结果与结论:该方法通过制备一种关键的含氟中间体,使得产品合成过程中后面的几步反应基本在水相中完成,减少了有机溶剂的用量,同时产品较分散、易收集,适用于产业化生产。Objective ： To synthesize bortezomib. Methods： N-（Pyrazine-2-ylcarbonyl） -L-phenylamine and （ 1R ） - （S） -pinanediol-1 -ammoniumtriflouroacetate-3-methylbutane-1 -boronate were used as starting materials to synthesize bortezomib by condensation, deprotection, and hydrolysis. Result and Conclusion： A key intermediate with element F in its chemical structure is prepared in this method, which makes the subsequent several steps can be conducted in water, thus the usage amount of organic solvent is reduced. In addition, the product has low vis- cosity and is easy to collect, so the new method can be applied in industrialized production.

关 键 词：抗肿瘤药 硼替佐米 合成 

分 类 号：R914.5[医药卫生—药物化学]