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

✍ Scribed by Yi Wu; Fusheng Wang; Hao Song; Yong Qin

Publisher
John Wiley and Sons
Year
2011
Tongue
German
Weight
263 KB
Volume
94
Category
Article
ISSN
0018-019X

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✦ Synopsis

Abstract

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.

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