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Synthetic Entry into 1‑Phosphono-3-azabicyclo[3.1.0]hexanes

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Figshare2016-02-18 更新2026-04-29 收录
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3-Azabicyclo­[3.1.0]­hex-2-en-1-yl phosphonates were prepared in a five-step reaction route from β-ketophosphonates. The key steps in this sequence are an atom-transfer radical cyclization and an unforeseen lithium–halogen exchange with n-BuLi. The cyclization reaction proceeds with excellent diastereoselectivity. The resulting cyclic imines were reduced, and 3-azabicyclo[3.1.0]­hexan-1-yl phosphonates were obtained.

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2016-02-18
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