A Novel Methodology for the Synthesis of Fumarates and Maleates
Autor: | Michael R. Jorgensen, Steven Fletcher, Andrew D. Miller, Wayne S. Price |
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Rok vydání: | 2006 |
Předmět: | |
Zdroj: | Synlett. 2006:1933-1937 |
ISSN: | 1437-2096 0936-5214 |
DOI: | 10.1055/s-2006-948166 |
Popis: | The stereoselectivity of both the Wittig and the Homer-Wadsworth-Emmons reactions allows for the synthesis of orthogonally protected fumarates and maleates, respectively, from α-keto esters. This methodology has been shown to be useful in the synthesis of a derivative of the pH sensitive cis-aconitic linker, important for prodrug approaches in drug delivery. We have incorporated this linker into a cholesterol-based PEGylated lipid, for its potential use in liposomal drug and gene delivery. The synthesized lipids have also been shown to be pH degradable using HPLC analyses. |
Databáze: | OpenAIRE |
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