A Simple and Highly Efficient Enantioselective Synthesis of ( S)-Rivastigmine

Abstract

A highly efficient and convenient procedure for the enantioselective synthesis of (S)-Rivastigmine, a cho-linergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease, is accomplished by the treatment of versatile, readily accessible (S)-(-)-2-methyl-2-propanesulfinamide with 3-hydroxyacetophenone. This protocol provides high yield and excellent enan-tiomeric excess in short step synthesis.