Synthesis and synthetic process optimization of a specific dipeptidyl peptidase-Ⅳinhibitor vildagliptin

VernacularTitle: 特异性二肽基肽酶-Ⅳ抑制剂维达列汀的合成与合成工艺优化
Author: Cai-Hua HONG ¹
Author Information

1. School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology
Publication Type:Journal Article
Keywords: Diabetes; Dipeptidyl peptidase-Ⅳ(DPP-Ⅳ)inhibitor; Process optimization; Vildagliptin
From: Journal of International Pharmaceutical Research 2020;47(8):677-682
CountryChina
Language:Chinese
Abstract: Objective: To investigate and optimize the synthetic process of specific dipeptidyl peptidase-Ⅳ(DPP-Ⅳ)inhibitor vitagliptin. Methods: The aimed synthetic route was conceived by the literature survey according to the advantages and disadvantages of the reported synthetic routes. The key process parameters were determined by the orthogonal test or single factor test for the main intermediates in the speed limiting step. Results: The structures of intermediates and target compound were confirmed by MS and 1H NMR data. The overall yield of the target compound was 38.5%. Conclusion: The synthetic process has the advantages of lower cost, simple operation and mild reaction condition, and the yield has been improved by optimizing the crystallization solvent, which should be more suitable for industrial production.