化学学报 ›› 1980, Vol. 38 ›› Issue (1): 67-77. 上一篇    下一篇

论文

“酞丁安”的合成研究

赵知中, 王琳, 蒋湘君, 王子厚, 魏征   

  1. 中国医学科学院药物研究所 北京
  • 投稿日期:1978-03-15 发布日期:2013-06-03

SYNTHESIS OF TAI-DING-AN

ZHAO ZHI-ZHONG, WANG LIN, JIANG XIANG-YUN, WANG ZI-HOU, WEI ZHENG   

  1. Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing
  • Received:1978-03-15 Published:2013-06-03

3-酞酰亚胺-2-氧-正丁醛双缩硫代氨基脲(5)具有明显的抑制沙眼衣原体、细菌和大鼠瓦克癌256的作用。对各型沙眼和某些病毒性皮肤病均有肯定的疗效。本文报道了该化合物的合成方法,即以丁酮为原料经溴化得到了3-溴代丁酮-(2)(1),1与酞酰亚胺钾盐缩合得2,再经溴化得3。由于溴化反应条件不同,可得其它的溴化物(6,8,9)。3用二甲基亚砜氧化成α-酮醛(4)。我们对氧化反应进行了一些探讨,除酞丁安(5)外,还分到三个副产物,经鉴定分别为:α-酞酰基丙酰甲基二甲基溴化锍(10),三甲基溴化锍(11)及酞酰亚胺。4可不经分离直接与硫代氨基脲缩合而得酞丁安。

3-phthalimido-2-ono-butyraldehyde bisthiosemicarbazone (6) (namely Tai-Ding-An,V 6133) exhibited marked inhibiting activity against Chlamydozoa trachamatis and some species of bacteria in vitro as well as against Walker 256 carcinoma in animals.It showed definite therapeutic e}caoy in the treatment of various Chlamydoazoa trachomatis and some virus infected skin diseases in clinical trials.