Abstract Reported herein is a straightforward and enantiodivergent synthesis of both enantiomers of trifluoromethylated analogues of calcimimetic NPS R-569 in a highly estereoselective manner. The synthesis features a diastereoselective synthesis of the N- (isopropylsulfinyl) imine unit by the “DAG methodology” and a diastereoselective addition of Ruppert–Prakash's reagent to the imine as the key steps. No protecting groups were ...