An Efficient Synthesis of a (−)‐Physostigmine's Library for Identifying Potential Anti‐Alzheimer's Agents

An efficient route for the synthesis of (−)‐physostigmine analogs 1a – 1g and 2a – 2k is described. Analogs 1a – 1g were synthesized via copper(I)‐catalyzed cycloaddition between the optically pure azide 10 and a variety of alkynes. Similarly, analogs 2a – 2k were prepared through ‘three‐component Huisgen cycloaddition’ using various amines, propargyl bromine, and 10 in H 2 O. Facile preparation of 10 via MacMillan 's organocatalysis has made it possible to generate a great diversity of natural product‐like compounds that can be screened for anti‐ Alzheimer 's effects.