流技术实现了 C3-杂取代 1-氮杂双环[1.1.0]丁烷和氮杂环丁烷的制备：开拓了在刚性杂环化学中未探索的化学空间。
Flow technology enabled preparation of C3-heterosubstituted 1-azabicyclo[1.1.0]butanes and azetidines: accessing unexplored chemical space in strained heterocyclic chemistry.
机构信息
FLAME-Lab, Flow Chemistry and Microreactor Technology Laboratory, Department of Pharmacy - Drug Sciences, University of Bari "A. Moro" Via E. Orabona 4, 70125, Bari, Italy.
Department of Discovery, Dompé Farmaceutici S.p.A., Via Campo di Pile, L'Aquila, 67100, Italy.
出版信息
Chem Commun (Camb). 2022 May 26;58(43):6356-6359. doi: 10.1039/d2cc01641a.
The use of flow technology as an enabling tool for accessing 1-azabicyclo[1.1.0]butanes bearing strained 3-, 4-, and 5-membered O-heterocycles with C3-C2 connectivity is reported. Reactivity and chemoselectivity (N-ring O-ring) were also evaluated. New chemical space has been explored and new structural motifs such as ABB-aziridines or spiro azetidine-oxazetidines are also reported.
本文报道了使用流动技术作为一种辅助手段，来构建具有 C3-C2 连接的 3-、4-和 5-元 O-杂环并带有张力的 1-氮杂双环[1.1.0]丁烷。还评估了反应性和化学选择性（N 环-O 环）。本文还探索了新的化学空间，并报道了新的结构基序，如 ABB-氮丙啶或螺氮杂环丁烷-噁唑烷。
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