The Design And Synthesis Of Water-soluble Prodrug Of Propofol

Objective: The design and synthesis of water-soluble prodrug of propofol. Methods: With NMP being the starting material, the ring cleavage was conducted under alkaline condition to form N-methyl-γ-aminobutyrate, which was then protected with (Boc)2O to form N-(tert-butyloxycarbonyl)- N-methyl-γ-aminobutyric acid, and then reacted with propofol with the presence of DCC and DMAP to form 2,6-diisopropylphenyl N-(tert-butyl- oxycarbonyl)-N-methyl-γ-aminobutyrate, which was finally deprotected under hydrogen chloride atmosphere to form the target compound (2,6- diisopropylphenyl N-methyl-γ-aminobutyrate hydrochloride). Results: The target molecule was identified by infrared spectrum, mass spectrum and NMR. Conclusion: The target compound showed a good water-solubility and chemical stability, and the initial Experiments on the pharmacodynamics confirmed its nice narcotic activity.