申请人:Chemagis Ltd.
公开号:EP1127873A2
公开(公告)日:2001-08-29
The present invention provides a process for preparing a compound of the general formula (I):
wherein R1 to R5 are independently selected from hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C1-6 alkoxy, all optionally substituted by one or more of halogen, hydroxy and aryl groups, as well as being independently selected from amino, mono- or disubstituted amino, alkenyloxy, acyl, acyloxy, cyano, nitro, aryl and alkylthio groups, which process comprises reacting a compound of the general formula (II):
wherein R1 to R5 are as defined in formula (I), with aminoguanidine bicarbonate in a mixture of a water-soluble solvent and polyphosphoric acid.
本发明提供了一种制备通式(I)化合物的工艺:
其中 R1 至 R5 独立地选自氢、卤素、C1-6 烷基、C2-6 烯基、C2-6 炔基或 C1-6 烷氧基,它们均任选被卤素、羟基和芳基中的一个或多个基团取代,以及独立地选自氨基、一取代或二取代氨基、烯氧基、酰基、酰氧基、氰基、硝基、芳基和烷硫基,该工艺包括将通式(II):
其中 R1 至 R5 如式 (I) 所定义,与氨基胍碳酸氢盐在水溶性溶剂和多磷酸的混合物中反应。