Ram V J
Medicinal Chemistry Division, Central Drug Research Institute, Lucknow.
Arch Pharm (Weinheim). 1991 Nov;324(11):837-9. doi: 10.1002/ardp.2503241103.
Synthesis of 5-cyano-6-(3-pyridyl)-2-thiouracil (1) has been described from 3-pyridinecarboxaldehyde, thiourea, and ethyl cyanoacetate. Alkylation of 1 with mono- and dihaloalkanes under different conditions, provided 2a,b, 3a,b, and 4a-i. Halogenation of 4g with POCl3 yielded 5 which underwent nucleophilic substitution with amines to give 6a-g. Fusion of 4a with aromatic and heterocyclic amines at 160 degrees C gave the substitution products 7a-c. Some of the compounds were screened for antileishmanial activity but only one of them (6d) demonstrated very significant activity.
5-氰基-6-(3-吡啶基)-2-硫脲嘧啶(1)的合成方法已由3-吡啶甲醛、硫脲和氰基乙酸乙酯进行了描述。在不同条件下，1与单卤代和二卤代烷烃进行烷基化反应，得到了2a、b，3a、b和4a-i。4g用POCl₃进行卤化反应得到5，5再与胺进行亲核取代反应生成6a-g。4a与芳香胺和杂环胺在160℃下熔融得到取代产物7a-c。对其中一些化合物进行了抗利什曼原虫活性筛选，但只有其中一个(6d)表现出非常显著的活性。
