手性缩醛的催化不对称合成研究进展

Catalytic Asymmetric Synthesis of Chiral Acetals

缩醛是许多药物和天然产物分子中常见的结构单元,研究发现手性缩醛的生物活性通常优于其消旋体.由于手性缩醛存在消旋化倾向,其催化不对称合成具有挑战性,近年来才引起关注.综述了目前手性N,N-缩醛、N,O-缩醛、N,S-缩醛、O,O-缩醛的催化不对称合成研究进展,及其在含缩醛骨架手性药物合成中的应用.

Acetals are common building blocks of many drugs and natural product molecules. It was found that the biological activity of chiral acetals is usually superior to their racemates. The catalytic asymmetric synthesis of chiral acetals is challenge for its racemization and attracts attention until recent years. In this review, the recent studies on catalytic asymmetric synthesis of chiral aminals, N,O-acetals, N,S-acetals, O,O-acetals, as well as its application in synthesis of chiral drugs containing acetal moieties are reviewed.