A process for preparing an anticorrosion component for an antifreeze by oxidizing an oxydiol of the formula (I) ##STR00001##
with molecular oxygen at a temperature of 20 to 100 C. and a partial oxygen pressure of 0.01 to 2 MPa in the presence of water and of a heterogeneous catalyst. The catalyst contains platinum to form an oxydicarboxylic acid of the formula (II) ##STR00002##
The process has the steps of conducting the oxidation
(a) at a molar ratio of
0.002n(Pt)/[n(oxydiol (I))+n(oxydicarboxylic acid (II))]0.019;
(b) at a concentration of water of 50% to 95% by weight in the liquid phase; and
(c) at a pH of 1 to 7.

A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture. ##STR00001##

A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture. ##STR00001##

A process for preparing an anticorrosion component for an antifreeze by oxidizing an oxydiol (I)

##STR00001##

in which x is 0 (zero) or a positive integer from 1 to 10 with molecular oxygen at a temperature of 20 to 100 C. and a partial oxygen pressure of 0.01 to 2 MPa in the presence of water and of a heterogeneous catalyst comprising platinum to form an oxydicarboxylic acid (II)

##STR00002##

in which y is 0 (zero) or a positive integer from 1 to 10, in which the oxidation is conducted
(a) at a molar ratio of

0.002n(Pt)/[n(oxydiol (I))+n(oxydicarboxylic acid (II))]0.019 where n(Pt) Is the molar amount of platinum, n(oxydiol (I)) is the molar amount of oxydiol (I) and n(oxydicarboxylic acid (II)) Is the molar amount of oxydicarboxylic acid (II);
(b) at a concentration of water of 50% to 95% by weight in the liquid phase; and
(c) at a pH of 1 to 7.

A process for preparing an anticorrosion component for an antifreeze by oxidizing an oxydiol (I)

##STR00001##

in which x is 0 (zero) or a positive integer from 1 to 10 with molecular oxygen at a temperature of 20 to 100 C. and a partial oxygen pressure of 0.01 to 2 MPa in the presence of water and of a heterogeneous catalyst comprising platinum to form an oxydicarboxylic acid (II)

##STR00002##

in which y is 0 (zero) or a positive integer from 1 to 10, in which the oxidation is conducted
(a) at a molar ratio of

0.002n(Pt)/[n(oxydiol (I))+n(oxydicarboxylic acid (II))]0.019 where n(Pt) Is the molar amount of platinum, n(oxydiol (I)) is the molar amount of oxydiol (I) and n(oxydicarboxylic acid (II)) Is the molar amount of oxydicarboxylic acid (II);
(b) at a concentration of water of 50% to 95% by weight in the liquid phase; and
(c) at a pH of 1 to 7.

This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 m to about 90 m, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia.

This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 m to about 90 m, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia.

This present invention provides gemcabene pharmaceutically acceptable salts having a PSD90 of 35 m to about 90 m, methods for purifying crude gemcabene, pharmaceutically acceptable salts of purified gemcabene, pharmaceutical compositions of a gemcabene pharmaceutically acceptable salt and therapeutic and prophylactic methods useful for various conditions, including dyslipidemia.

Being used for drug modification, the multi-arm single molecular weight polyethylene glycol and an active derivative thereof provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the active derivative of the multi-arm single molecular weight polyethylene glycol provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.

Being used for drug modification, the multi-arm single molecular weight polyethylene glycol and an active derivative thereof provided herein can effectively improve the solubility, stability, and immunogenicity of the drugs, improve the absorption of the drugs in vivo, prolong the half-life of the drugs, and increase bioavailability, enhance efficacy, and reduce toxic and side effects of the drugs. A gel formed from the active derivative of the multi-arm single molecular weight polyethylene glycol provided herein can be used for the preparation of controlled release drugs so as to prolong the action time of the drugs, thereby reducing the number of administrations and improving patient compliance.