CAJ | 학술논문

匹伐他汀是第三代他汀类药物。该药不仅具有较强的3-羟基-3-甲基戊二酰辅酶A还原酶抑制作用,而且呈肝细胞选择性,已被制药界誉为是＂超级他汀＂。本文通过7条合成路线,分别从拆分法和不对称合成法介绍了降血脂药匹伐他汀钙的合成,并详细分析了这些路线的优缺点。得出结论：不对称合成法优于拆分法,手性（3R,5S）立体构型是合成的难点和重点。
필벌타정시제삼대타정류약물。해약불부구유교강적3-간기-3-갑기무이선보매A환원매억제작용,이차정간세포선택성,이피제약계예위시＂초급타정＂。본문통과7조합성로선,분별종탁분법화불대칭합성법개소료강혈지약필벌타정개적합성,병상세분석료저사로선적우결점。득출결론：불대칭합성법우우탁분법,수성（3R,5S）입체구형시합성적난점화중점。
Pitavastatin was the third-generation statin.It not only had a stronger HMG-CoA reductase inhibition,but also had liver selective action,thus was regarded as ＂superstatins＂.The seven synthesis routes of plasma lipid regulators pitavastatin calcium were reviewed,and the advantages and disadvantages of these routes were analyzed in detail.These routes belonged to racemate resolution and asymmetric synthesis,respectively.Asymmetric synthesis method was better than resolution,and the synthesis of chiral（3R,5S） stereoconstruction was important and difficulty.