Propofol hydroxy acid ester compound with ester constitutional terminal, preparation method for same and application thereof

Abstract

Disclosed are a propofol hydroxy acid ester compound with an ester constitutional terminal, a preparation method for the same and application thereof. As shown in the constitutional formula (I) of the compound, Y refers to a C1-4 linear carbon chain, and R refers to acetyl or propiono. The propofol hydroxy acid ester compound can be prepared by utilizing corresponding propofol hydroxy acid ester as raw materials and is obtained by means of esterification reaction with corresponding acid anhydride. As experiments show, the compound is stable in vitro but capable of quickly releasing propofol with sedation and hypnogenesis and / or narcotism in blood plasma. Since hydroxy in propofol hydroxy butyric ester molecules is protected by means of shielding, heat stability of the propofol hydroxy acid ester compound is improved, and self-decomposition of the propofol hydroxy acid ester compound caused by lactonization is reduced.

Description

technical field [0001] The invention relates to a derivative of propofol, specifically a propofol hydroxy ester compound with an ester structure terminal, a preparation method thereof and an application in pharmacy. Background technique [0002] Propofol, whose chemical name is 2,6-diisopropylphenol, is a sedative drug widely used clinically for the induction, maintenance and intensive care of general anesthesia. features. Since the first clinical report of this compound was made in 1977, it has gradually been promoted and applied all over the world. In addition to its pharmacological effects in anesthesia, propofol has also been found to have other pharmacological effects, such as anti-epilepsy, treatment of migraine, etc. Therefore, research on oral propofol derivatives has become a research hotspot. Since propofol has a very significant first-pass effect, it needs to be modified to reduce the first-pass effect. However, if the modified propofol derivatives cannot rapi...

AI Technical Summary

Problems solved by technology

However, if the modified propofol derivatives cannot quickly release the original drug of propofol, they will not be able to play the desired pharmacological effect.