手性噁唑啉-2-酮类化合物是不对称有机合成中应用最广泛的手性辅基之一。通常以光学活性的氨基酸为起始原料,经过羧基的还原、一碳基团酰化、环化等单元反应合成该类化合物。由于制备该类化合物过程中涉及到的试剂价格昂贵、工艺要求较高、产物分离较复杂等原因,手性噁唑啉-2-酮的价格一直相当昂贵。上海有机化学研究所开发了一条新的合成路线,使用的试剂价廉易得且使用方便,每一环节都有明显优势,成本大幅度降低,具有较好的发展前景。 Chiral oxazoline-2-ones are one of the most widely used chiral prosthetic groups in asymmetric organic synthesis. Usually optically active amino acids as the starting material, after reduction of the carboxyl group, a carbon group acylation, cyclization and other unit reaction synthesis of these compounds. The price of chiral oxazolin-2-ones has been quite expensive due to expensive reagents, high process requirements and complicated product separation involved in the preparation of such compounds. Shanghai Institute of Organic Chemistry has developed a new synthetic route, the reagents used cheap and easy to use, each link has obvious advantages, significantly reduce costs, with good prospects for development.