We report herein a facile approach to tetrahydropyridazines, a scaffold found in many natural products and biologically active entities, via Pd‐catalyzed carboamination of readily available alkenyl hydrazones with aryl and alkenyl halides. Preliminary studies showed its promise for enantioselective synthesis. This work offers an expedient access to the tetrahydropyridazine scaffold bearing substitution patterns, thus significantly increasing the availability of these derivatives for downstream evaluation.

中文翻译：

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Pd催化烯基Hy的碳氨化反应合成四氢哒嗪

我们在此报告了一种简便的方法，对四氢哒嗪，一种在许多天然产物和生物活性实体中发现的支架，通过Pd催化将易得的烯基hydr与芳基和烯基卤化物进行碳氨化反应。初步研究表明其有望实现对映选择性合成。这项工作为四氢哒嗪支架的替代模型提供了一种方便的途径，从而显着提高了这些衍生物用于下游评估的可用性。