富马酸沃诺拉赞有关物质的合成和结构确定

Preparation and Structural Confirmation of the Related Substances of Vonoprazan Fumarate

为控制富马酸沃诺拉赞的质量,根据其结构特征和合成工艺合成了7个有关物质:二[2-[2-(2-氟苯基)-2-氧代乙基]]丙二腈、2-氨基-5-(2-氟苯基)呋喃-3-腈、5-(2-氟苯基)-1H-吡咯-3-甲酸、5-(2-氟苯基)-1-(3-吡啶基磺酰基)-1H-吡咯-3-甲醇、N,N-二[5-(2-氟苯基)-1-(3-吡啶基磺酰基)-1H-吡咯-3-甲基]甲胺富马酸盐、5-(2-氟苯基)-N-甲基-1H-吡咯-3-甲胺富马酸盐和N,N-二[5-(2-氟苯基)-1H-吡咯-3-甲基]甲胺富马酸盐,并进行了结构确证。为富马酸沃诺拉赞质量标准的建立奠定了基础。

To perform the quality control of vonoprazan fumarate, according to the structural characteristics and synthetic process, seven related substances including： di [2- E2- （2-fluorophenyl） -2-oxoethyl] ] propanedinitrile, 2-amino- 5- （2-fluorophenyl） furan-3-carbonitrile, 5- （2-fluorophenyl） -1H-pyrrole-3-carboxylic acid, [5- （2-fluorophenyl） -1- （3- pyridinylsul fonyl） - 1H-pyrrole-3-yl] methanol, N,N-di E E5- （2-fluorophenyl） - 1- （3-pyridinylsulfonyl） - 1H-pyrrole-3- yl]methyll methanamine fumarate, E5-（2-fluorophenyl）-N-methyl-lH-pyrrole-3-yl]methanamine fumarate and N,N- di [[5-（2-fluorophenyl）-1H-pyrrole-3-yl]methyl]methanamine fumarate, were synthesized and their structures were confirmed by 1H NMR and MS.