一种坎格列净工艺杂质的制备分离与结构鉴定

Isolation and Identification of a Process Impurity of Canagliflozin

坎格列净（canagliflozin,1）,化学名为（1S）-1,5-脱氢-1-C-[3-[[5-（4-氟苯基）-2-噻吩基]甲基]-4-甲基苯基]-D-葡萄糖醇水合物（2∶1）,是美国强生杨森制药公司和日本三菱制药株式会社共同开发研制的一种新型钠依赖性葡萄糖转运蛋白抑制剂,

The impurity was obtained in the work-up by methylsulfonic acid in MeOH of the Grignard reaction in the synthesis of canagliflozin. Its structure was identified as （2S,3S,4R,5R） -1- [3- [ [5- （4-fluorophenyl） thiophen-2- yl] methyl] -4-methylphenyl] hexane-1,2,3,4,5,6-hexaol （A） by HRMS and two-dimensional NMR.