A novel and efficient strategy for the synthesis of 4-chloro quinolines via the TMSCl-mediated cascade cyclization of easily prepared ortho-propynol phenyl azides is developed. This reaction proceeds smoothly in moderate to excellent yields with a wide range of substrate compatibility. TMSCl acted not only as a promoter, but also as a chloro source in this transformation. Moreover, the obtained 4-chloro quinolines could be further derivated in an array of palladium-catalyzed coupling and nucleophilic substitution reactions to construct potential biologically active and pharmaceutical molecules.

中文翻译：

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通过TMSCl介导的邻丙炔酚苯叠氮化物级联环化反应制备 4-氯喹啉的有效方法†

通过易于制备的邻-丙炔醇苯基叠氮化物的TMCSI介导的级联环化反应，开发了一种新颖而有效的合成4-氯喹啉的策略。该反应以中等至极好的收率顺利进行，并具有广泛的底物相容性。TMSC1在该转化中不仅充当启动子，而且充当氯源。而且，获得的4-氯喹啉可以在钯催化的偶联和亲核取代反应的阵列中进一步衍生，以构建潜在的生物活性和药物分子。