Abstract

Common and novel synthesized active methylene compounds as well as heterocycles bearing active methyl or having an active methine were used in the syntheses of a wide variety of substituted and fused five-, six- and seven-membered nitrogenous heterocyclic systems of interesting medical and pharmaceutical importance such as triazoles, pyridazines, triazines, and diazepines. Carbothiosemicarbazides, carbothiohydrazones and 2-hydrazinoazaherterocycles were used as suitable starting materials for triazole formation. The preparation of tetrazoles showed a valence ring-chain tautomerism. The key starting materials for the synthesis of pyridazines were acetohydrazide derivative, activated enones, enaminones, and aryl hydrazones. The reaction of 2-chloro or 2-hydrazinoazaheterocycles and thiocarbohydrazones with different reagents under suitable reaction conditions led to the formation of triazines. Diazepines were obtained via treatment of enones with 1,2-diamino derivatives. Also, the antimicrobial activities of some selected synthesized heterocyclic compounds were reported.

摘要

常见的和新颖的合成的活性亚甲基化合物以及带有活性甲基或具有亚甲基的杂环被用于各种具有医学和药物重要性的取代和稠合的五，六和七元含氮杂环系统的合成中例如三唑，哒嗪，三嗪和二氮杂s。碳硫半脲，碳硫hydr和2-肼基氮杂杂环化合物被用作形成三唑的合适原料。四唑的制备显示价环互变异构。合成哒嗪的关键起始原料是乙酰肼衍生物，活化的烯酮，烯胺酮和芳基。在合适的反应条件下，2-氯或2-肼基氮杂杂环和硫代碳杂azo与不同的试剂反应导致形成三嗪。通过用1,2-二氨基衍生物处理烯酮获得二氮杂ze。此外，还报道了一些选定的合成杂环化合物的抗菌活性。