替格瑞洛两种代谢物的合成

Synthesis of Two Metabolites of Ticagrelor

为控制替格瑞洛的产品质量和进行药物体内代谢研究,合成了替格瑞洛的两种代谢物,AR-C133913XX[化学名:(1S,2S,3R,5S)-3-[7-氨基-5-丙硫基-3H-1,2,3-三唑并[4,5-d]嘧啶-3-基]-5-(2-羟乙氧基)环戊烷-1,2-二醇]和ARC124910XX[化学名:(1S,2R,3S,4R)-4-[7-[(1R,2S)-2-(3,4-二氟苯基)环丙胺基]-5-丙硫基-3H-1,2,3-三唑[4,5-d]嘧啶-3-基]环戊烷-1,2,3-三醇],并通过核磁、质谱对其进行结构确证。

To perform the quality control of ticagrelor and study the metabolic pathway of the drug in vivo, two metabolites of ticagrelor, AR-C 133913XX [ （ 1S,2S,3R,5S） -3- E7-amino-5-propylthio-3H- 1,2,3-triazolo [4,5-d] pyrimidin- 3-yl） -5- （2-hydroxyethoxy） cyclopentane- 1,2-diol] and AR-C 124910XX [ （1S,2R,3S,4R） -4- [7- [ （1R,2S） -2- （3,4-difluorophenyl） cyclopropylamino] -5 -propylthio-3H- 1,2,3-triazolo [4,5-d] pyrimidin-3-yl]cyclopentane- 1,2,3-triol] were prepared. Their structures were confirmed by NMR and ESI-MS.