发明名称 Process for the preparation of letrozole
摘要 The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
申请公布号 US7705159(B2) 申请公布日期 2010.04.27
申请号 US20060482228 申请日期 2006.07.06
申请人 SICOR, INC. 发明人 MACDONALD PETER LINDSAY;BIGATTI ETTORE;ROSSETTO PIERLUIGI;HAREL ZVI
分类号 C07D249/08 主分类号 C07D249/08
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