发明名称 PROCESS FOR PREPARATION OF ALBENDAZOLE
摘要 The present invention discloses a novel, cost-effective process for preparation of a benzimidazole carbamates compound. Specifically, it relates to the process for the preparation of anti-parasite bulk drug albendazole. The process comprises a) thiocyanating 2-nitroaniline of formula VI with ammonium thiocyanated in presence of a halogen to obtain 2-nitro-4-thiocyanoaniline of formula V; b)propylating 2-nitro-4-thiocyanoaniline of formula V with propylbromide in presence of n-propanol and a base in absence of a phase transfer catalyst to obtain 4-propylthio-2-nitroaniline of formula III; C) reducing the nitro group of 4-propylthio-2-nitroaniline prepared in step b) by reacting an aqueous alkali metal sulphide or an alkaline metal sulphide to obtain 4-propylthio-o-phenylenediamine of formula II; and d)condensing 4-propylthio-o-phenylenediamine of formula II with alkali or alkaline earth metal salt of methylcyano carbamate in presence of an acid to form Albendazole of formula I.
申请公布号 US2013303782(A1) 申请公布日期 2013.11.14
申请号 US201113989497 申请日期 2011.11.23
申请人 RANE RAMKRISHNA APPAJI;NAITHANI SUSHIL;NATIKAR RAJENDRA DEVENDRA;VERMA SUDHAKAR;ARULMOLI THANGAVEL;SEQUENT SCIENTIFIC LIMITED 发明人 RANE RAMKRISHNA APPAJI;NAITHANI SUSHIL;NATIKAR RAJENDRA DEVENDRA;VERMA SUDHAKAR;ARULMOLI THANGAVEL
分类号 C07D235/32 主分类号 C07D235/32
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