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Regioselective α-Cyanation of Unprotected Alicyclic Amines

Fuchao Yu, Daniel A. Valles, Weijie Chen, Scott D. Daniel, Ion Ghiviriga, Daniel Seidel

2022Organic Letters18 citationsDOIOpen Access PDF

Abstract

Secondary alicyclic amines are converted to α-aminonitriles via addition of TMSCN to their corresponding imines, intermediates that are produced in situ via the oxidation of amine-derived lithium amides with simple ketone oxidants. Amines with an existing α-substituent undergo regioselective α'-cyanation even if the C-H bonds at that site are less activated. Amine α-arylation can be combined with α'-cyanation to generate difunctionalized products in a single operation.

Topics & Concepts

CyanationAlicyclic compoundRegioselectivityChemistryCombinatorial chemistryOrganic chemistryCatalysisCatalytic C–H Functionalization MethodsRadical Photochemical ReactionsSynthesis and Catalytic Reactions
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