Angew Chem Int Ed Engl
December 2023
1-Azaspiro[3.3]heptanes were synthesized, characterized, and validated biologically as bioisosteres of piperidine. The key synthesis step was thermal [2+2] cycloaddition between endocyclic alkenes and the Graf isocyanate, ClO S-NCO, to give spirocyclic β-lactams.
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