A general, enantioselective synthesis of

Autor: Timothy J, Senter, Matthew C, O'Reilly, Katherine M, Chong, Gary A, Sulikowski, Craig W, Lindsley
Rok vydání: 2016
Předmět:
Zdroj: Tetrahedron letters
ISSN: 0040-4039
Popis: A short, high-yielding protocol involving the enantioselective α-chlorination of aldehydes has been developed for the enantioselective synthesis of C2-functionalized aziridines and N-alkyl terminal azetidines from a common intermediate. This methodology allows for the rapid preparation of functionalized aziridines in 50–73% overall yields and 88–94% ee, and azetidines in 22–32% overall yields and 84–92% ee. Moreover, we developed a scalable and cost-effective route to the key organocatalyst (54% overall yield, >95% dr).
Graphical Abstract
Databáze: OpenAIRE
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