Highly Diastereoselective Alkylation of Aziridine-2-carboxylate Esters:Enantioselective Synthesis of LFA-1 Antagonist BIRT-377

摘要

Aziridines are important synthons in organic chemistry as they provide convenient entry to optically pure amines,alpha-amino acids,amino alcohols,diamines,and a variety of other amino compounds that are useful both in industrial and academic endeavors.In the past,most optically pure azir-idines were derived from acyclic members of the chiral pool,however,methods are emerging for the direct synthesis of optically pure aziridines through catalytic asymmetric reac-tions.