中文摘要：

西他列汀是首个二肽基肽酶-4（DPP-4）抑制剂的II型糖尿病治疗药,该药物的制备技术主要经历了三代工艺路线的发展。本文主要综述了西他列汀的制备技术,以及生物催化法应用于西他列汀的合成工艺路线,并对今后西他列汀制备技术的发展方向进行了展望。

英文摘要：

Sitagliptin is the first dipeptidyl peptidase-4（DPP-4） inhibitor type II diabetes drug. The development of this drug after the market has gone through three generations of the development process line. In this paper, the preparation technology of sitagliptin and the biocatalytic method applied in the synthesis of sitagliptin were mainly introduced. The future development of sitagliptin preparation technology was also discussed.