摘要
以简单易得的光学纯的R-环氧氯丙烷为原料,经过开环、羟基保护、合成烯烃化试剂,然后在-78℃经KHMDS还原,得降血脂药物他汀(Pitavastatin)的重要中间体(R,E)-1-氯-4-(2-环丙基-4-(4-氟苯基)喹啉-3-基)丁-3-烯-2-醇,总收率达36%。与传统的不对称合成以及消旋体的拆分等方法相比降低了生产成本,提高了收率,更适合于工业化生产。
Using optically pure R-epichlorohydrin as raw material, with ring-opening, hydroxy protected, synthezed olefin reagents, and using KHMDS in -78 ℃, important intermediates ( R,E)-1-chloro-4-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)but-3-en-2-ol of cholesterol-lowering drugs statins (Pitavastatin) was synthezed, total yield was 36%. Compred to traditional asymmetric synthesis, the separation of racemic reduced production costs, improved yields, was more suitable for industrial production.
出处
《广州化工》
CAS
2015年第18期89-90,100,共3页
GuangZhou Chemical Industry