Convenient Approach to 2-Substituted (Thio)morpholin-3-ones from alpha-Diazoacetates via X-H Carbene Insertion - Lactamization Sequence

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    Abstract

    Stepwise coupling of N-Boc-protected beta-aminoethanols or beta-mercaptoethylamines with various alpha-diazoacetates provides a new, unified approach to constructing (thio)morpholin-3-ones. The process involves a Rh-2(esp)(2)-catalyzed X-H insertion reaction, Boc group removal and ambient-temperature lactamization and is conveniently conducted in one-pot format.

    Original languageEnglish
    Number of pages8
    JournalEuropean Journal of Organic Chemistry
    Issue number45
    Early online date11 Oct 2019
    DOIs
    Publication statusPublished - 18 Nov 2019

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