公开(公告)号：EP2882752A1

公开(公告)日：2015-06-17

申请号：EP13750356.1

申请日：2013-08-08

申请人： Cipla Limited

发明人： RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao ,  GHAGARE, Maruti ,  KADAM, Swati, Atul

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： There is provided a process for the preparation of sitagliptin or a pharmaceutically acceptable salt thereof, and a process for the preparation of intermediate compounds useful in the preparation of sitagliptin. In particular, there is provided a process comprising condensing 3-tert-butoxycarbonylamino-4-(2,4,5-trifluorophenyl) butyric acid of formula (II) with 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[l,2,4]triazolo[4,3-a] pyrazine of formula (III) or a salt thereof in presence of a catalyst to obtain (R)-tert-butyl-4-oxo-4-(3- (trifluoromethyl)-5,6-dihydro-[ 1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl)- 1 -(2,4,5- trifluorophenyl)butan-2-yl-carbamate of formula (IV) or a pharmaceutically acceptable salt thereof. The catalyst is represented by the compound of formula (V). Compound of formula (IV) or its pharmaceutically acceptable salt obtained may be deprotected to obtain a compound of formula (I).

摘要翻译： 提供了西他列汀或其药学上可接受的盐的制备方法，以及制备可用于制备西格列汀的中间体化合物的方法。 特别地，提供了一种方法，其包括将式（II）的3-叔丁氧基羰基氨基-4-（2,4,5-三氟苯基）丁酸与3-（三氟甲基）-5,6,7,8-四氢 - [1,2,4]三唑并[4,3-a]吡嗪或其盐在催化剂存在下反应，得到（R） - 叔丁基-4-氧代-4-（3- （三氟甲基）-5,6-二氢 - [1,2,4] - 三唑并[4,3-a]吡嗪-7（8H） - 基）-1-（2,4,5-三氟苯基）丁-2- （Ⅳ）的 - - - - 氨基甲酸酯或其药用盐。 催化剂由式（V）化合物表示。 可以将得到的式（IV）化合物或其药学上可接受的盐脱保护，得到式（I）化合物。