CAJ | 학술논문

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。
이간단역득적광학순적R-배양록병완위원료,경과개배、간기보호、합성희경화시제,연후재-78℃경KHMDS환원,득강혈지약물타정(Pitavastatin)적중요중간체(R,E)-1-록-4-(2-배병기-4-(4-불분기)규람-3-기)정-3-희-2-순,총수솔체36%。여전통적불대칭합성이급소선체적탁분등방법상비강저료생산성본,제고료수솔,경괄합우공업화생산。
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.