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Pure intermediate for preparing letrozole
专利权人:
GENERICS [UK] LIMITED
发明人:
GORE VINAYAK GOVIND,SHUKLA VINAY KUMAR,MEKDE SANDEEP,HASBE SURESH,BHANDARI SHREYAS,SHINDE DHANANJAY,PATIL MADHUKAR SHALIGRAM
申请号:
NZ60742811
公开号:
NZ607428A
申请日:
2011.08.26
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed is the oxalic acid addition salt of 4-[(1,2,4-triazol-1-yl)methyl]benzonitrile (III). Further disclosed is a process for the preparation of 4-[(1,2,4-triazol-1-yl)methyl]benzonitrile (III), comprising the purification of the oxalic acid addition salt of 4-[(1,2,4-triazol-1-yl)methyl]benzonitrile (III), and subsequent liberation of 4-[(1,2,4-triazol-1-yl)methyl]benzonitrile (III) from the purified salt. Also disclosed is a process for the preparation of letrozole (4-[1-(4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]-benzonitrile), or a pharmaceutically acceptable salt thereof, wherein the process comprises the conversion of 4-[(1,2,4-triazol-1-yl)methyl)]benzonitrile (III) or the oxalic acid addition salt prepared as defined herein into Letrozole or a pharmaceutically acceptable salt thereof, wherein the 4-[(1,2,4-triazol-1-yl)methyl)]benzonitrile (III) or the salt thereof is reacted with 4-fluorobenzonitrile (IV) in the presence of a base.
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