报道了四环素C-2位与伯胺、仲胺反应形成Mannich碱的简便方法:四环素盐酸盐在甲醇和水溶液中与伯胺反应,生成二级Mannich碱;四环素在叔丁醇中与仲胺反应,生成三级Mannich碱。合成了10个化合物,其中8个未见报道,并对所合成化合物的结构进行了表征。
A simple method for synthesis of tetracycline Mannich bases by C-2 reacting with primary and secondary amine was reported. Secondary Mannich base was obtained by primary amine reacting with tetracycline hydrochloride in methanol and water. Tertiary Mannich base was obtained by the reaction of secondary amine and tetracycline in t-butanol. The structures of synthesized ten of tetracyline analogs 4 - 13 had been identified.