The invention relates to a novel method for producing robenidine and salts thereof of the general formula
1
wherein X denotes a halogen atom. The method uses hydrazine hydrate and a cyano compound as the starting materials, and the starting materials are first reacted in a C
1-4
alcohol or a C
1-4
alcohoVwater mixture as solvent or in an aprotic organic solvent, to produce a diaminoguanidine of the general formula
2
wherein Y denotes a halogen atom or tosyl. This diaminoguanidine is then converted directly, without isolation, by reacting with a p-halobenzaldehyde of the general formula
3
in a C
1-4
alcohol or a C
1-4
alcohol/water mixture as solvent or in a mixture of water and an aprotic polar organic solvent to produce the robenidine and salts thereof of general formula I.
本发明涉及一种生产通式为 1 的罗贝尼定及其盐类的新方法。
1
其中 X 表示卤素原子。该方法使用
水合
肼和
氰基化合物作为起始原料,起始原料首先在 C
1-4
醇或 C
1-4
醇
水混合物为溶剂或在无相有机溶剂中反应,生成通式为
2
其中 Y 表示卤素原子或
甲苯基。然后不经分离,通过与通式 3 的对卤代
苯甲醛反应,直接转化这种
二氨基胍。
3
在 C
1-4
醇或 C
1-4
醇/
水混合物作为溶剂,或在
水和钝极性有机溶剂的混合物中,制得通式 I 的罗宾苷及其盐类。