d-生物素全合成研究进展

Advance Research in Total Synthesis of d-Biotin

d-生物素目前大生产工艺以Sternbach合成路线为基础,加以不断优化形成以富马酸为起始原料,经溴代、苄胺化、环合、缩合、还原、水解、硫代、格氏、氢化、脱苄、精制得生物素。基于原料手性池的不对称合成方法发展迅速,取代Sternbach合成路线有望成为可能。

The main route of synthesis of d-biotin is based on Sternbach synthetic approach at present. After much study of process optimizing, we get an optimal process. This process started with fumaric acid, then bromination, amination, cyclization, condensation, reduction, hydrolyzation, Phosphorthioate, Grignard reaction, hydrogenation, debenzylation and refining, then d-biotin was got. With the development of the asymmetric synthesis which based on the chiral pool, it may replace Sternbach synthetic approach.