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匹伐他汀关键手性中间体的立体选择性合成

Stereoselective Synthesis of Statins Chiral Allyl Alcohol Structure
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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.
机构地区 江南大学药学院
出处 《广州化工》 CAS 2015年第18期89-90,100,共3页 GuangZhou Chemical Industry
关键词 他汀类药物 中间体 合成 Statins intermediates synthetic
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参考文献6

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