SHEKHAR SHASHANK,FRANCZYK THADDEUS S.,BARNES DAVID M.,DUNN TRAVIS B.,HAIGHT ANTHONY R.,CHAN VINCENT S.
申请号：
NZ60576711
公开号：
NZ605767A
申请日:
2011.07.15
申请国别(地区):
NZ
年份:
2015
代理人:
摘要：
Disclosed is a process for the preparation of dasabuvir (N-(6-(3-tert-butyl-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-2-methoxyphenyl)naphthalen-2-yl)methanesulfonamide) or a salt thereof, wherein the process comprises: sulfonamidating 1-(3-tert-butyl-5-(6-tosyl-naphthalen-2-yl)-4-methoxyphenyl)-2,4-dioxo-3,4-dihydropyrimidine, or an analogue thereof (such as 1-(3-tert-butyl-5-(6-perfluorobutanesulfonyl-naphthalen-2-yl)-4-methoxyphenyl)-2,4-dioxo-3,4-dihydropyrimidine) with methanesulfonamide, preferably using a palladium catalyst and a phosphine ligand. Also disclosed are useful intermediates such as 1-(3-tert-butyl-5-(6-perfluorobutanesulfonyl-naphthalen-2-yl)-4-methoxyphenyl)-2,4-dioxo-3,4-dihydropyrimidine and 1-(3-tert-butyl-5-(6-hydroxy-naphthalen-2-yl)-4-methoxyphenyl)-2,4-dioxo-3,4-dihydropyrimidine.
