Keywords: Oxidative Kinetic Resolution; Enantioselective Synthesis; Steglich Reaction; Mitsunobu Reaction; Kinetic Resolution

Abstract

A practical and efficient procedure for the synthesis of potent calcimimetics (+)-NPS R-568 was developed. This procedure includes palladium-catalyzed oxidative kinetic resolution of benzylic alcohol with molecular oxygen and (-)-sparteine, as a source of chirality. The synthesis was achieved in six steps from commercially available 3-methoxyacetophenone at 18.58% overall yield and the final compound, calcimimetics (+)-NPS R-568 1 had 87% enantioselectivity.