瑞舒伐他汀侧链(3R,5S)-6-R-取代基-3,5-二羟基己酸叔丁酯合成研究进展

Research advance in synthesis of the rosuvastatin side chain intermediate tert-butyl(3R,5S)-6-R-substituent-3,5-dihydroxyhexanoate

瑞舒伐他汀是一种高效的羟甲戊二酰辅酶A(HMG-CoA)还原酶抑制剂,能有效降低低密度脂蛋白(LDL)胆固醇,且无副作用,被称为"超级他汀".瑞舒伐他汀是由疏水性母核和开环侧链构成,其手性侧链是合成中的难点.目前,化学法和生物酶法合成瑞舒伐他汀关键手性侧链(3R,5S)-6-R-取代基-3,5-二羟基己酸叔丁酯受到研究者广泛的关注.主要介绍了不对称还原合成(3R,5S)-6-R-取代基-3,5-二羟基己酸叔丁酯的研究进展.

Rosuvastatin is an effective 3-hydroxy-3-methyl-glutaryl CoA（HMG-CoA）reductase inhibitor.Regarded as ＂super-statin＂,rosuvastatin effectively reduces low-density lipoprotein（LDL）cholesterol without additional adverse effects. Rosuvastatin is composed of the hydrophobic parent nucleus and the side chain,while the the preparation of side chain is the bottleneck for the whole synthesis.Chemical and enzymatic synthesis of the rosuvastatin side chain intermediate tert-butyl（3R,5S）-6-R-substituent-3,5-dihydroxyhexanoate has attracted increasing attentions.Research progress in synthesis of tert-butyl（3R,5S）-6-R-substituent-3,5-dihydroxyhexanoate was reviewed in this paper.