上海医药工业研究院近年来化学药物合成工艺研究进展

Progress on Studies of Synthetic Process of Chemical Drugs in SIPI

上海医药工业研究院最近10年,在化学药物合成工艺的研究方面取得了一定成绩,其中3个项目获国家科技进步二等奖,3个项目获上海市科技进步一等奖。本文主要依据我院近十年来已公开发表的论文,分3部分进行总结和讨论:1.保留原路线的工艺改进,涉及下列药物的合成方法 :奥氮平、比阿培南、群多普利、阿戈美拉汀、吉非替尼、米诺膦酸、替罗非班、缬沙坦、阿福特罗、瑞他莫林、尼洛替尼、阿瑞匹坦、马西替坦、右哌甲酯、麻黄碱和依折麦布;2.重新设计合成路线,包括非那嗪奈、替比夫定、决奈达隆、沃替西汀、雷美替胺、西格列汀、达泊西汀、SIPI-4884、泊马度胺、罗氟司特、卡利拉嗪、吡喹酮等12个药物的合成;3.有机反应方法学研究。

The following three parts on the synthetic process of chemical drugs were reviewed according to the publications by scientists from Shanghai Institute of Pharmaceutical Industry （SIPI） during the recent ten years： 1. The process improvements based on the original synthesis; 2. Design the new synthetic route; 3. Study on the methodlogy of the organic reactions. In part one, 16 drugs including olanzapine, biapenem, trandolapril, agomelatine, gefitinib, minodronic acid, tirofiban, valsartan, arformoterol, retapamulin, nilotinib, aprepitant, macitentan, dexmethylphenidate, ephedrine and ezetimibe were involved. In part two, the new synthesis about 12 drugs such as fenazinel, telbivudine, dronedarone, vortioxetine, ramelteon, sitagliptin, dapoxetine, SIPI-4884, pomalidomide, roflumilast, cariprazine and praziquantel were discussed.