| abstract |
Disclosed is a water-soluble prodrug of a pharmaceutical product containing an aromatic hydroxyl group which is hindered. Water-soluble phosphonooxymethyl ether groups have been introduced into pharmaceuticals containing sterically hindered alcohols and phenols such as camptothecin, propofol, etoposide, vitamin E and cyclosporin A. The preparation method of the phosphonooxymethyl derivative comprises the steps of formula (i) and formula (ii), wherein R—OH represents a drug containing alcohol or phenol and n represents an integer of 1 or 2. , R 1 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation, and R 2 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation. [Selection figure] None |