Simple , Enantiocontrolled Azetidine Library Synthesis via Strain-Release Functionalization of 1-Azabicyclobutanes

ABSTRACT: Herein we describe a new enantioselective route for the synthesis of all stereoisomers of 2,3-disubstituted azetidines. This approach uses simple strain release functionalization of preformed 1-azabicyclobutanes (ABBs), which enables installation of a wide array of nucleophiles at the C3-position. Chemical proteomic profiling of stereoisomeric sets of cysteine-reactive acrylamides derived from the new azetidine library reveals ligandable protein sites distinct from those of azetidine probes synthesized using C–H arylation.

INSTRUMENT(S):

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Cell Suspension Culture, Lymphocyte Of B Lineage

SUBMITTER: Hayden Sharma  

LAB HEAD: Dr. Benjamin F. Cravatt

PROVIDER: PXD055926 | Pride | 2026-06-29

REPOSITORIES: Pride