Abstract

Thiadiazine and thiazoles have attracted importance due to their broad applicability as biologically active compounds. New thiadiazines and thiazoles are prepared via the simple reaction of an α-haloketohydrazonoyl with thiocarbohydrazone derivatives in a basic medium under reflux. A S-alkylated intermediate forms through nucleophile substitution involving the hydrazonoyl halogen and thiocarbohydrazone thiol. In situ cyclization via the condensation between the carbonyl and NH₂ or NH moieties of the intermediate forms 1,3,4-thiadiazine and thiazole derivatives, respectively. This method employs inexpensive, commercially available reagents and facile reaction conditions to afford novel thiadiazine/thiazole derivatives in good yields.

摘要

噻二嗪和噻唑因其作为生物活性化合物的广泛适用性而受到重视。新的噻二嗪和噻唑是通过α-卤代酮腙酰基与硫代羰腙衍生物在碱性介质中回流下的简单反应制备的。通过涉及腙酰基卤素和硫代羰腙硫醇的亲核取代形成 S-烷基化中间体。通过羰基和NH _{2之间的缩合进行}原位环化中间体的 NH 或 NH 部分分别形成 1,3,4-噻二嗪和噻唑衍生物。该方法采用廉价、可商购的试剂和简便的反应条件，以良好的收率提供新型噻二嗪/噻唑衍生物。