915395-01-6Relevant articles and documents
A novel methodology for the synthesis of fumarates and maleates
Price, Wayne S.,Fletcher, Steven,Jorgensen, Michael R.,Miller, Andrew D.
, p. 1933 - 1937 (2008/02/08)
The stereoselectivity of both the Wittig and the Horner-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. Georg Thieme Verlag Stuttgart.
