METHOD FOR PREPARING WATER-SOLUBLE PHOSPHONOOXYMETHYL DERIVATIVES OF ALCOHOL AND PHENOL Russian patent published in 2007 - IPC C07F9/09

Abstract RU 2310659 C2

FIELD: organic chemistry, chemical technology, pharmacy.

SUBSTANCE: invention relates to a new method for synthesis of water-soluble formulations of pharmaceutical preparations containing a blocked aromatic hydroxyl group. Invention describes a method for synthesis of water-soluble phosphonooxymethyl derivatives involving the following steps: step (1): wherein R-OH is converted to R-O-CH₂Cl, and step (2): wherein compounds synthesized in the first step is used and wherein R-O-CH₂Cl reacts with the phosphoric acid molar excess and a base in suitable polar aprotonic solvent, and wherein R-OH represents a drug containing alcohol or phenol; n = 1 or 2; R¹ means hydrogen atom, alkaline metal ion or pharmaceutically acceptable cation; R² means hydrogen atom, alkaline metal ion or pharmaceutically acceptable cation. Also, Invention describes a method for synthesis of water-soluble phosphonooxymethyl-propofol. Invention provides simplifying the process for synthesis of water-soluble formulations of pharmaceutical preparations.

EFFECT: improved method of synthesis.

26 cl, 4 ex

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RU 2 310 659 C2

Authors

Bonnevill Dzhordzh

Delakhanti Greg

Uolz Ehndrju Dzh.

Dates

2007-11-20—Published

2002-12-20—Filed