发明名称 PROCESS FOR THE PREPARATION OF TAPENTADOL
摘要 Disclosed herein is an improved process for the preparation of 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-I and its pharmaceutically acceptable salt which comprises the reaction of (S)-1-(dimethylamino)-2-methylpentan-3-one of formula VIII with 3-bromo anisole of formula II under Grignard conditions to get the compound (2S,3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl pentan-3-ol of formula V followed by activation of the —OH group of the formula V to convert into sulfonate esters of formula IX, which are on reductive deoxygenation to yield (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentan-1-amine of formula VII and demethylation of formula VII to obtain the compound 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-1.
申请公布号 EP2606030(B1) 申请公布日期 2016.05.18
申请号 EP20110767301 申请日期 2011.08.16
申请人 INDOCO REMEDIES LIMITED 发明人 RAJADHYAKSHA, MANGESH, NARAYAN;NAIR, RANJEET;DESHMUKH, SANDIP KACHARU;KHABALE, SOMNATH AMBADAS;PANANDIKAR, ADITI MILIND
分类号 C07C213/00;C07C215/54 主分类号 C07C213/00
代理机构 代理人
主权项
地址