帕博西尼母核中间体的合成工艺优化  

Improved Synthesis of Palbociclib Intermediate

作　　者：雷雪 姜晓晔 LEI Xue;JIANG Xiao-ye(City College,Wuhan University of Science and Technology,Wuhan 430083,China)

机构地区：[1]武汉科技大学城市学院,湖北武汉430083

出　　处：《精细化工中间体》2020年第5期24-26,76,共4页Fine Chemical Intermediates

基　　金：武汉科技大学城市学院院级一般科学研究项目(2020CYYBKY001)。

摘　　要：以2,4-二氯-5-溴嘧啶作为起始原料,经过取代反应、 Heck反应、关环反应3步合成得到帕博西尼母核中间体2-氯-8-环戊基-5-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮,产品纯度达99.50%。优化条件下总收率63.38%。工艺原料便宜易得、操作简单、条件温和,收率和纯度较为理想,适合工业化生产。The key intermediate of palbociclib, 2-chloro-8-cyclopentyl-5-methylpyrido[2, 3-d]pyrimidin-7(8 H)-one was obtained through a three-step process including substitution reaction, Heck reaction and cyclization reaction using 5-bromo-2,4-dichloropyrimidine as the starting material with a purity of 99.50%. Under optimized conditions,the total yield is 63.38%. This improved process is cost-reducing, simple operation, mild condition, ideal yield and purity, and suitable for industrial production.

关 键 词：帕博西尼 2-氯-8-环戊基-5-甲基-8H-吡啶并[2 3-d]嘧啶-7-酮 合成 

分 类 号：TQ463[化学工程—制药化工]