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.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or ##STR00001##
R.sup.1 and R.sup.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.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.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. ##STR00002##

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.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or ##STR00001##
R.sup.1 and R.sup.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.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.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. ##STR00002##

The present invention provides compounds, compositions thereof, and methods of using the same.

The present invention provides compounds, compositions thereof, and methods of using the same.

The present invention discloses a class of carboxylic acid derivatives and use thereof in preparation of prodrugs. The carboxylic acid derivatives have the general formula (I), wherein R.sup.1 is H or alkyl; X is H or F; Y is F or fluoroalkyl; n is 0, 1, 2, 3, 4, 5, or 6; W is W.sup.1 or W.sup.2; W.sup.1 is NR.sup.2R.sup.3, NR.sup.2R.sup.3.A,

##STR00001##

R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, or a protecting group for amino; m is 0, 1, 2, or 3; A is an acid; W.sup.2 is COOR.sup.4, OPO(OR.sup.4).sub.2, or PO(OR.sup.4).sub.2; R.sup.4 is H, or a protecting group for carboxyl or hydroxyl in phosphoric acid.

##STR00002##

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.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or

##STR00001##

R.sup.1 and R.sup.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.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.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.

##STR00002##

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.sup.1 or W.sup.2; W.sup.1 is NR.sup.1R.sup.2.A or

##STR00001##

R.sup.1 and R.sup.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.sup.2 is COOM.sub.1/t or OPO.sub.3(M).sub.2/t or PO.sub.3(M).sub.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.

##STR00002##

The present invention provides compounds, compositions thereof, and methods of using the same.

The present invention provides compounds, compositions thereof, and methods of using the same.

The present disclosure describes an L-S2-amino-4-halobutyric acid derivative-L-tartrate salt. The present disclosure also describes a method of preparing L-S-amino-4-halobutyric acid derivative-L-tartrate salt, comprising the following steps: using D, L-S2-amino-4-halobutyric acid derivative enantiomeric mixture as the raw material, using L-tartrate as the resolution agent, and obtaining L-S2-Amino-4-halobutyric acid derivative-L-tartrate by resolution reaction, crystallization and filtration in the same resolution agent system; or the enantiomeric mixture of D, L-S2-amino-4-halobutyric acid derivatives is used as raw material, L-tartrate is used as resolution agent under aromatic aldehyde catalysis or aromatic aldehyde and organic acid co-catalysis, and dynamic resolution reaction is carried out in the same resolution agent system, further comprising crystallization and filtration to obtain L-S2-amino-4-halobutyric acid derivative-L-tartrate.