公开(公告)号：US07884214B2

公开(公告)日：2011-02-08

申请号：US12064150

申请日：2006-07-19

申请人： Satyanarayana Chava ,  Seeta Ramanjaneyulu Gorantla ,  Sai Prasanna Bhagya Lakshmi Ginjupalli

发明人： Satyanarayana Chava ,  Seeta Ramanjaneyulu Gorantla ,  Sai Prasanna Bhagya Lakshmi Ginjupalli

IPC分类号： C07D403/02

CPC分类号： C07D235/20

摘要： The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4′-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan.

摘要翻译： 本发明包括用于制备替米沙坦的方法，其包括通过替米沙坦二盐酸盐包括i）使4-甲基-2-正丙基-1H-苯并咪唑-6-羧酸与N-甲基-O-苯二胺二盐酸盐冷凝，得到4 - 甲基-6（1-甲基苯并咪唑-2-基）-2-正丙基1H-苯并咪唑ii）处理4-甲基-6-（1-甲基苯并咪唑-2-基）-2-正丙基-1H- 苯并咪唑与4' - （溴甲基）-2-联苯基-2-羧酸叔丁酯在碱的存在下在有机溶剂中反应，并将酯分离为酸加成盐iii）将酯酸加成盐转化为替米沙坦二盐酸盐，和iv）将替米沙坦二盐酸盐转化为 替米沙坦