Catalytic Enantioselective Allylic Amination of Olefins for the Synthesis of ent-Sitagliptin.

ABSTRACT: The presence of nitrogen atoms in most chiral pharmaceutical drugs has motivated the development of numerous strategies for the synthesis of enantioenriched amines. Current methods are based on the multi-step transformation of pre-functionalized allylic electrophiles into chiral allylic amines. The enantioselective allylic amination of unactivated olefins represents a more direct and attractive strategy. We report the enantioselective synthesis of ent-sitagliptin via an allylic amination of an unactivated terminal olefin.

SUBMITTER: Bao H 

PROVIDER: S-EPMC4219538 | biostudies-literature | 2013 Nov

REPOSITORIES: biostudies-literature