申请人:KRKA, tovarna zdravil, d.d., Novo mesto
公开号:EP2194050A1
公开(公告)日:2010-06-09
A process for the preparation of Irbesartan or a pharmaceutically acceptable salt thereof comprising the step of coupling the 1-pentanamidocyclapentanecarboxamide of formula (V) with 4'-substituted methyl biphenyl-2-carbonitrile or 1-(4'-substituted methyl biphenyl-2-yl)-1H-tetrazole wherein tetrazole can be protected or unprotected to obtain the N-[(2'-cyanobiphenyl-4-yl)methyl]-1-pentanamidocyclopentanecarboxamide or N-[1-([2'-(1H-tetrazol-1-yl)biphenyl-4-yl]methylamino)methyl)cydopentyl]pentanamide wherein tetrazole can be protected or unprotected that is further processed to Irbesartan or a pharmaceutical acceptable salt thereof.
制备厄贝沙坦或其药用可接受盐的方法包括以下步骤:将式(V)的1-戊酰胺环戊烷羧酰胺与4'-取代甲基联苯基-2-碳腈或1-(4'-取代甲基联苯基-2-基)-1H-四唑偶联,其中四唑可以被保护或未被保护,得到N-[(2'-氰基联苯基-4-基)甲基]-1-戊酰胺环戊烷羧酰胺或N-[1-([2'-(1H-四唑-1-基)联苯基-4-基]甲基氨基}甲基)环戊基]戊酰胺,其中四唑可以被保护或未被保护,进一步处理得到厄贝沙坦或其药用可接受盐。