CHRISTOPHER W. DERSTINE,JOSSIAN OPPENHEIMER,MARK V.M. EMONDS,ROBERT C. CLOUSE
申请号:
BR112014015962
公开号:
BR112014015962A2
申请日:
2012.12.28
申请国别(地区):
BR
年份:
2017
代理人:
摘要:
patent summary: "methods of producing methyl 4-amino-3-chloro-6- (4-chloro-2-fluoro-3-methoxyphenyl) pyridine-2-carboxylate". The present invention relates to a method of producing methyl 4-amino-3-chloro-6- (4-chloro-2-fluoro-3-methoxyphenyl) pyridine-2-carboxylate. One method comprises adding methyl isobutyl ketone to an aqueous solution comprising 4-chloro-2-fluoro-3-methoxyphenylboronic acid to form an organic phase comprising 4-chloro-2-fluoro-3-methoxyphenylboronic acid and an aqueous phase. the organic phase and the aqueous phase are separated. 4-chloro-2-fluoro-3-methoxyphenylboronic acid is reacted with methyl 4- (acetylamino) -3,6-dichloropyridine-2-carboxylate in methyl isobutyl ketone to yield 4- (acetylamino) -3-chloro-6 Methyl (4-chloro-2-fluoro-3-methoxyphenyl) pyridine-2-carboxylate, which is deacetylated to yield 4-amino-3-chloro-6- (4-chloro-2-fluoro-3-methoxyphenyl) methyl pyridine-2-carboxylate.resumo patente de invenção: "métodos de produzir 4-amino-3-cloro-6-(4-cloro-2-fluoro-3-metoxifenil) piridina-2-carboxilato de metila". a presente invenção refere-se a método de produzir 4-amino-3-cloro-6-(4-cloro-2-fluoro-3-metoxifenil)piridina-2-carboxilato de metila. um método compreende adicionar metil isobutil cetona a uma solução aquosa compreendendo ácido 4-cloro-2-fluoro-3-metoxifenil-borônico para formar uma fase orgânica compreendendo o ácido 4-cloro-2-fluoro-3-metoxifenilborônico e uma fase aquosa. a fase orgânica e a fase aquosa são separadas. o ácido 4-cloro-2-fluoro-3-metoxifenilborônico é reagido com 4-(acetilamino)-3,6-dicloropiridina-2-carboxilato de metila em metil isobutil cetona para produzir 4-(acetilamino)-3-cloro-6-(4-cloro-2-fluoro-3-metoxifenil)piridina-2-carboxilato de metila, que é desacetilado para produzir 4-amino-3-cloro-6-(4-cloro-2-fluoro -3-metoxifenil)piridina-2-carboxilato de metila.