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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

The Application of Olefin Metathesis to the Synthesis of Biologically Active Macrocyclic Agents

Author(s): Pierre V. de Weghe and Jacques Eustache

Volume 5, Issue 15, 2005

Page: [1495 - 1519] Pages: 25

DOI: 10.2174/156802605775009748

Price: $65

Abstract

Recent developments of the metathesis reaction in the area of biologically active molecules are presented. Scope and limitations of ring-closing metathesis to form medium and large rings are discussed and illustrated by the epothilone synthesis. Applications of the metathesis reaction related to medicinal chemistry, including solid phase synthesis and combinatorial chemistry are presented.

Keywords: epothilone 490, combinatorial chemistry, 1,2,3,6-tetrahydropyridine, ring-closing metathesis, Type I cyclization, molybdenum-derived Schrock catalyst, proteolytic degradation


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