ANZALONE, Luigi,VILLANI, Frank J.,TELEHA, Christopher Allan,FEIBUSH, Penina,FEGELY, Barry
申请号：
ES08781434
公开号：
ES2567077T3
申请日:
2008.07.07
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A method of preparing a crystalline zwitterion of 5 - ({[2-amino-3- (4-carbamoyl-2,6-dimethyl-phenyl) propionyl] - [1- (4-phenyl-1 H -imidazol 2- yl ) ethyl] amino} methyl) -2-methoxy-benzoic acid comprising the steps of: the combination of a strong ionizable acid 5 - ({[2- tert-butoxycarbonylamino-3- (4-carbamoyl-2,6-dimethyl -phenyl) propionyl] - [1- (4-phenyl-1H-imidazol-2- yl) ethyl] amino} methyl) -2-methoxy-benzoic acid to prepare a salt of 5 - ({[2-amino-3 - (4-carbamoyl-2,6-dimethyl-phenyl) -propionyl] - [1- (4-phenyl-1 H -imidazol-2-yl) ethyl] amino} methyl) -2-methoxy-benzoic acid； and washing said salt of 5 - ({[2-amino-3- (4-carbamoyl-2,6-dimethyl-phenyl) propionyl] - [1- (4- phenyl-1 H -imidazol-2-yl) -ethyl ] -amino} -methyl) -2-methoxy-benzoic acid with an inorganic base to obtain zwitterion of 5 - ({[2-amino-3- 10 (4-carbamoyl-2,6-dimethylphenyl) propionyl] - [1 - (4-Phenyl-1H-imidazol-2-yl) -ethyl] amino} methyl) -2-methoxy-benzoic acid.Un método de preparación de una zwitterion cristalina de 5 - ({[2-amino-3- (4-carbamoil-2,6-dimetil-fenil ) propionil] - [1- (4-fenil-1H-imidazol 2- il) etil] amino} metil) -2-ácido metoxi-benzoico que comprende las etapas de: la combinación de un ácido fuerte ionizable 5 - ({[2- terc-butoxicarbonilamino-3- (4-carbamoil-2,6-dimetil-fenil) propionil] - [1- (4-fenil-1H- imidazol-2- il) etil] amino} metil) -2-ácido metoxi-benzoico para preparar una sal de 5 - ({[2-amino-3- (4-carbamoil-2,6-dimetil-fenil ) -propionil] - [1- (4-fenil-1H-imidazol-2-il) etil] amino} metil) -2-metoxi-benzoico； y lavar dicha sal de 5 - ({[2-amino-3- (4-carbamoil-2,6-dimetil-fenil) propionil] - [1- (4- fenil-1H-imidazol-2-il) -etil] -amino} -metil) -2-ácido metoxi-benzoico con una base inorgánica para obtener zwitterion de 5 - ({[2-amino-3- 10 (4-carbamoil-2,6-dimetilfenil) propionil] - [1- (4-fenil-1H-imidazol-2-il) - etil] amino} metil) -2-ácido metoxi-benzoico.
