Efficient and concise synthetic protocol to benzo- and pyrazolo-fused medium-sized N,S-heterocycles (e.g,. thiazocinones, thiazoninones, thiazecinones, thiecinones, and thioninones) is developed. The process involves the AlCl₃/MeNO₂, TfOH or polyphosphoric acid mediated cyclization of pyrazole-based carboxylic acids or esters into tricyclic ketones under mild conditions. The designed protocol offers easy access to biologically and pharmaceutically promising pyrazoles in good yields. The structure elucidation of all new compounds without stereochemical assignments has been carried out by spectral and elemental analysis.

中文翻译：

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通过Friedel-Crafts闭环方法靶向合成功能性吡唑并稠合的中等尺寸N，S-杂环

有效和简洁的合成方案于苯并吡唑并和-稠合中型N，S-杂环（例如，。 thiazocinones，thiazoninones，thiazecinones，thiecinones和thioninones）显影。该方法涉及在温和条件下由AlCl ₃ / MeNO ₂，TfOH或多磷酸介导的吡唑基羧酸或酯环化为三环酮。设计的方案可轻松获得高收率的生物学和药学上有前景的吡唑。通过光谱和元素分析已经完成了所有没有立体化学分配的新化合物的结构解析。