Synthesis of potential UDP‐glucuronosyltransferase inhibitors containing a diphosphate function

Abstract

AbstractThe synthesis of potential inhibitors of UDP‐glucuronosyltransferase, in which the β‐phosphate moiety of uridine 5′‐diphosphate is linked to phenolic or alcoholic hydroxyl groups, is described. Key intermediates in the formation of the diphosphate function are S‐(4‐methylphenyl) 2‐cyanoethyl phosphorothioate triesters which, after conversion into the corresponding S‐(4‐methylphenyl) phosphorothioate diesters, react with phosphate monoesters, in the presence of iodine, to give the target molecules.