一种富马酸沃诺拉赞杂质的制备及表征

Preparation and characterization of an impurity of vonoprazan fumarate

目的制备富马酸沃诺拉赞合成工艺中产生的一个杂质,加强其质量控制。方法以5-(2-氟苯基)-1H-吡咯-3-甲醛为起始原料,按照原研路线合成富马酸沃诺拉赞,富马酸沃诺拉赞经高温降解得到目标杂质:N-[5-(2-氟苯基)-1-(吡啶-3-基磺酰基)-1H-吡咯-3-基]甲基-N-甲基天冬氨酸,通过制备液相得到该杂质纯品。结果与结论目标杂质的结构经HR-MS和NMR谱确证,使得富马酸沃诺拉赞的杂质研究更加全面和深入,为其工艺研究提供一定的帮助。

An impurity of vonoprazan fumarate,N-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]methyl-N-methyl aspartic acid,was prepared,and its structure was confirmed by HR-MS and NMR.It was easily produced by addition reaction in the salt formation and crystallization steps,which directly affected the quality of vonoprazan fumarate.This study introduced a method to prepare this impurity and reduce its amount,which will provide helps for the quality control of vonoprazan fumarate in the industrial production.■.