The development of efficient synthetic strategies for the preparation of tetrasubstituted N‐H pyrrole derivatives, especially in an environmentally benign fashion, still remains momentous, yet challenging. Herein, we report a Cu(II)‐catalyzed tandem reaction of 1,3‐dipolar cycloaddition of α,β‐ynones and glycine iminoesters, followed by Cu(II)‐promoted oxidative (air) dehydrogenative aromatization, allowing de novo access to tetrasubstituted N‐H pyrroles in up to 81% yield under green reaction conditions. The possible reaction pathway is tentatively proposed. Finally, fully substituted pyrroles can be available via N‐alkylation, and the preliminary phase‐transfer catalytic asymmetric N‐alkylation is also studied to give an axially chiral pyrrole.

中文翻译：

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通过偶氮甲碱叶立德和 α,β-Ynones 的催化 1,3-偶极环加成模块化获得四取代 N-H 吡咯

开发有效的合成策略来制备四取代的 N-H 吡咯衍生物，特别是以环境友好的方式，仍然很重要，但也具有挑战性。在此，我们报道了 Cu(II) 催化的 α,β-ynones 和甘氨酸亚氨基酯的 1,3-偶极环加成串联反应，然后是 Cu(II) 促进的氧化（空气）脱氢芳构化，从而从头获得在绿色反应条件下，四取代 N-H 吡咯的收率高达 81%。初步提出了可能的反应途径。最后，可以通过N-烷基化获得完全取代的吡咯，并且还研究了初步相转移催化不对称N-烷基化以得到轴向手性吡咯。