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WATER-SOLUBLE PROPOFOL DERIVATIVES AND USES THEREOF

机译:水溶性丙泊酚衍生物及其用途

摘要

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I): wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is W 1 or W 2 ; W 1 is NR 1 R 2 ·A or R 1 and R 2 are each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, W 2 is COOM 1/t or OPO 3 (M) 2/t or PO 3 (M) 2/t ; M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M.
机译:本发明公开了一类水溶性丙泊酚衍生物,其制备方法,使用其的麻醉方法,其作为前药的用途及其在静脉麻醉剂制备中的用途。水溶性丙泊酚衍生物具有通式(I):其中X为H或F,Y为F或被一个或多个F取代的烷基,n为1、2、3、4、5或6,W为W 1或W 2; W 1为NR 1 R 2·A或R 1和R 2各自独立地为H,任选被苯基取代的烷基或环烷基,m为0、1、2或3,A为药学上可接受的酸,W 2为COOM 1 / t或OPO 3(M)2 / t或PO 3(M)2 / t; M是可以与酸根形成盐的金属离子,铵离子或碱性氨基酸阳离子。 t是M的电荷数。

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