New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof

Download or read book New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof written by Nicolas Winssinger and published by . This book was released on 2000 with total page 852 pages. Available in PDF, EPUB and Kindle. Book excerpt: The complexity of natural products and the inherent challenges imposed by target synthesis were used as a platform to develop new strategies and linkers for solid phase organic synthesis. This research led to the development of two cyclorelease reaction involving an olefin metathesis and a Stille reaction. Our interest in linkers also led to the development of three new linkers; a simplified photolabile linker, a very versatile selenium linker and a new safety-catch linker. The utility of these developments were illustrated by the solid phase synthesis of heptasaccharide phytoalexin elicitor (HPE), epothilone A, zearalenone, sarcodictyins and vancomycin (Figure 1). Libraries of the promising anticancer agents epothilone and sarcodictyins provided valuable information towards the structure-activity relationship of these molecules as well as several compounds with improved biological activity.