DIPROPOFOL PYROPHOSPHATE DIHYDROGEN ESTER AND PHARMACEUTICALLY ACCEPTABLE SALT, PREPARATION PROCESS AND APPLICATION THEREOF

摘要

Dipropofol pyrophosphate dihydrogen ester and pharmaceutically acceptable salt, preparation process and application thereof. The ester (2) is prepared by phosphorylating propofol with P2O5 as phosphorylating reagent in anhydrous organic solvent at 25-110°C for 2-8h under stirring, and condensing to obtain white solid. The title pharmaceutically acceptable salt is prepared by salifying ester (2) with base in organic solvent at 0-80°C for 1-5 h under stirring, filtering to obtain white solid. The process has the advantages of simple preparation process, high product yield and purity, low cost, and easily-accessible raw materials. The ester (2) and its pharmaceutically acceptable salt may be used to prepare the medical preparations as sedative, hypnotic and anesthetic, with stable property and good water solubility.