A Practical Entry to β‐Aryl‐β‐alkyl Amino Alcohols: Application to the Synthesis of a Potent BACE1 Inhibitor.

The 1,2-addition of alkyl Grignard reagents to readily available N-tert-butanesulfinyl ketimines, bearing an α-silyloxy substituent, proceeds in high yields and excellent diastereocontrol. The utility of the present method was demonstrated by the synthesis, in enantiomerically pure form, of one recently disclosed β-secretase (BACE1) inhibitor.