Process for preparing water-soluble phosphonooxymethyl...

Details Process for preparing water-soluble phosphonooxymethyl... Process for preparing water-soluble phosphonooxymethyl...

A - Human Necessities

61

K

A61K 31/66 (2006.01) C07F 9/09 (2006.01) C07F 9/655 (2006.01) C07F 9/6561 (2006.01) C07K 7/64 (2006.01)

Patent

CA 2470423

A process for making water-soluble phosphonooxymethyl ethers of hindered alcohol and phenol containing pharmaceuticals, such as camptothecin, propofol, etoposide, Vitamin E and Cyclosporin A. In particular, the process for preparing water-soluble phosphonooxymethyl derivatives comprises the steps of Formula (i) and Formula (ii); R-OH represents an alcohol- or phenol-containing drug, n represents an integer of 1 or 2, R1 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation, and R2 is hydrogen, an alkali metal ion, or a pharmaceutically acceptable cation.

L'invention concerne un procédé de fabrication d'éthers de phosphonooxyméthyle hydrosolubles de produits pharmaceutiques contenant de l'alcool et du phénol empêchés, tels que camptothécine, propofol, étoposide, vitamine E et cyclosporine A. Plus spécifiquement, ce procédé de préparation de dérivés de phosphonooxyméthyle hydrosolubles comprend les étapes représentées par les formules (i) et (ii), dans lesquelles, R-OH représente un médicament contenant de l'alcool ou du phénol, n représente un nombre entier 1 ou 2, R?1¿ représente hydrogène, un ion de métal alcalin, ou un cation pharmaceutiquement acceptable, et R?2¿ représente hydrogène, un ion de métal alcalin ou un cation pharmaceutiquement acceptable.

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