Design and synthesis of deuterium-labeled vorapaxar / 中国药科大学学报
Journal of China Pharmaceutical University
; (6): 295-300, 2018.
Article
in Zh
| WPRIM
| ID: wpr-704338
Responsible library:
WPRO
ABSTRACT
Vorapaxar,a novel antagonist of the protease-activated receptor 1 (PAR-1 ),can inhibit the clotting process. Deuterium-labeled vorapaxar was required for the analysis of clinical sample as an internal stand-ard. Starting for unlabeled vorapaxar,four-step reactions including hydrolysis,condensation,transesterification and hydrogen-deuterium exchange were carried out to synthesize [D8]vorapaxar effectively for the first time. All intermediates and final products were confirmed by NMR and high resolution mass spectrometry (HRMS).Impor-tantly,the prepared [D8]vorapaxar could meet the requirements of sample analysis as the internal standard.
Full text:
1
Index:
WPRIM
Language:
Zh
Journal:
Journal of China Pharmaceutical University
Year:
2018
Type:
Article