PROCESS FOR PREPARING WATER-SOLUBLE PHOSPHONOOXYMETHYL DERIVATIVE OF ALCOHOL AND PHENOL

摘要

PROBLEM TO BE SOLVED: To provide water-soluble prodrugs of a hindered aromatic hydroxy group-containing pharmaceutical. SOLUTION: A water-soluble phosphonooxymethyl ether group is introduced into pharmaceuticals containing a hindered alcohol and phenol, such as camptothecin, propofol, etoposide, Vitamin E and Cyclosporin A. The process for preparing phosphonooxymethyl derivatives comprises the steps of formula (i) and formula (ii), wherein R-OH represents an alcohol- or phenol-containing drug, n represents an integer of 1 or 2, R1is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation, and R2is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation. COPYRIGHT: (C)2009,JPO&INPIT