摘要
以N ,N′ 二甲基脲为原料 ,经氰乙酸环合、乙醇胺脱氨、二氯亚砜氯化 3步反应合成了关键中间体 6 (2 氯乙基 )胺基 1,3 二甲基 嘧啶二酮 (7)。 7再与N (2 羟乙基 ) 3 (4 硝基苯基 )丙胺反应得抗心律失常药盐酸尼非卡兰 ,总收率为 4 8.0 % (以N ,N′ 二甲基脲计 ) 。
Chloroethyl)amino-1,3-dimethylpyrimidinedione(7), as a key intermediate, was prepared in three steps by condensation of N,N′-dimethylurea successively with cyanoacetic acid and ethanolamine, and then chlorination with thionyl chloride. Nifekalant hydrochloride, an antiarrhythmic drug, was synthesized by amination of 7 with N-(2-hydroxylethyl)-3-(4-nitrophenyl)propylamine, the total yield could reach up to 48.0%. The structure of nifekalant hydrochloride was confirmed by NMR and MS.
出处
《合成化学》
CAS
CSCD
2004年第4期388-390,J004,共4页
Chinese Journal of Synthetic Chemistry
