申请人:KOHJIN CO. Ltd.
公开号:EP0452504A1
公开(公告)日:1991-10-23
A method of directly producing N-(3',4'-dimethoxycinnamoyl)anthranilic acid readily in a high yield without being accompanied by the formation of difficultly separable by-products, which comprises either reacting 3',4'-dimethoxycinnamic acid with anthranilic acid in an aprotic polar solvent in the presence of both a specified inorganic salt and an iminium salt which can be quantitatively prepared from dimethylformamide and an inexpensive acyl halide reagent, or reacting 3',4'-dimethoxycinnamic acid with the iminium salt and then with an anthranilic acid-inorganic salt complex which is a new compound not found in any literature. This method makes it possible to produce an objective compound at a high yield without the necessity for using a basic substance or an amine in a large amount sufficient for neutralizing an acid to be generated as a by-product in the condensation unlike known methods, and is scarcely accompanied by the formation of by-products, especially those which are difficult to separate.
一种高产率地直接生产 N-(3',4'-二甲氧基肉桂酰基)氨茴酸而不伴有难以分离的副产物形成的方法,该方法包括使 3'.4'-二甲氧基肉桂酸与氨茴酸在非沸腾极性溶剂中在指定的无机盐和亚氨基盐的存在下反应、4'-二甲氧基肉桂酸与蚁酸在特定的无机盐和亚胺盐(可从二甲基甲酰胺和廉价的酰基卤化试剂中定量制备)的存在下,在非沸腾极性溶剂中反应,或者将 3',4'-二甲氧基肉桂酸与亚胺盐反应,然后与蚁酸-无机盐复合物反应,该复合物是一种未在任何文献中发现的新化合物。与已知方法不同的是,这种方法无需大量使用碱性物质或胺来中和缩合过程中产生的副产物酸,就能以高产率生产出目标化合物,而且几乎不会产生副产物,尤其是难以分离的副产物。