摘要
4-羟基-L-脯氨酸、半胱胺盐酸为反应材料,经过一系列的氨基保护、氧化、缩合反应,得到Teneligliptin的关键中间体(2S)-4-氧代-2-(3-噻唑烷基羰基)-1-吡咯烷羧酸叔丁酯,收率可达73.8%。开发了一种全新的合成方式,在氧化阶段进行了改进和创新,对其质量进行控制,整个路线对环境几乎没有污染,并且通过1 H NMR和ESI-MS确认了设备的结构。
4-Hydroxy-L-proline and cysteamine hydrochloric acid are the reaction materials.After a series of amino protection,oxidation and condensation reactions,the key intermediate(2S)-4-oxo-2-(of Teneligliptin is obtained.3-thiazolidinecarbonyl)-1-pyrrolidinecarboxylic acid tert-butyl ester,the yield can reach 73.8%.According to the literature,a brand-new synthesis method was summarized,and the oxidation stage was improved and innovated,and its quality was controlled.The whole route had almost no pollution to the environment,and the structure of the equipment was confirmed by 1 H NMR and ESI-MS.
作者
张少平
张爱启
李培申
漆定超
刘东玲
Zhang Shao-ping;Zhang Ai-qi;Li Pei-shen;Qi Ding-chao;Liu Dong-ling
出处
《化工设计通讯》
CAS
2021年第3期145-146,共2页
Chemical Engineering Design Communications
