瑞舒伐他汀钙的合成工艺改进  

Synthesis of Rosuvastatin Calcium

作　　者：李泽标 邹林 林燕峰 严军 

机构地区：[1]南通常佑药业科技有限公司,江苏南通226407

出　　处：《精细化工中间体》2016年第6期50-52,55,共4页Fine Chemical Intermediates

摘　　要：以(4R-cis)-6-醛基-2,2-二甲基-1,3-二氧己环-4-乙酸环戊酯和[4-[4-氟苯基-6-(1-甲基乙基)-2-[N-甲基-(N-甲磺酰基)氨基]]-5-嘧啶基]甲基溴化三苯基磷为起始原料,经维悌希反应、水解、成盐等反应制备瑞舒伐他汀钙,产品纯度99.2%,总收率为79.2%,其结构经ESI-MS、1H NMR确证。Rosuvastatin calcium was synthesized using cyclopentyl（4R-cis）-6- [（acetyloxy）methyl]-2,2-dimethyl- 1,3-dioxane-4-acetate and [[4-（4-fluorophenyl）-6-（1-methylethyl）-2-[N-methyl-（N-methylsulfonyl）amino]-5- pyrimidinyl]methyl]triphenylphosphonium bromid as the starting materials through a series of reactions including Witting reaction, hydrolysis, salination. The structure of Locaserln hydrochloride and some intermediates were confirmed by ESI-MS and 1H NMR, and the total yield of the product was 79.2%.

关 键 词：(4R-cis)-6-醛基-2 2-二甲基-1 3-二氧己环-4-乙酸环戊酯 [4-[4-氟苯基-6-(1-甲基乙基)-2-[N-甲基-(N-甲磺酰基)氨基]]-5-嘧啶基]甲基溴化三苯基磷 瑞舒伐他汀钙 

分 类 号：R973.2[医药卫生—药品]