Cis-platinum coordination compound and preparation method thereof
A complex, cisplatin technology, applied in the field of cisplatin complex and its preparation, can solve the problems of poor polymer biocompatibility, limited application, inability to degrade, etc., achieve good stability, improve curative effect, and avoid cisplatin sudden release effect
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[0055] The invention provides a kind of preparation method of cisplatin complex, comprising the following steps:
[0056] Cisplatin and a block copolymer having a structure of formula (III) or formula (IV) cooperate in an aqueous medium to generate a cisplatin complex;
[0057]
[0058] In formula (III) and formula (IV), R 1 independently selected from hydrogen, alkyl or substituted alkyl;
[0059] R 2 independently selected from -NH- or -R 4 (CH 2 ) r NH-, where, R 4 is -O-, -OCONH-, -OCO-, -NHCOO- or -NHCO-, 1≤r≤8;
[0060] R 3 independently selected from hydrogen or hydrophobic groups;
[0061] m is the degree of polymerization, 40≤m≤250; n is the degree of polymerization, 1≤n≤200; y is the degree of polymerization, 0≤y≤100.
[0062] In the present invention, the block copolymer with the structure of formula (III) or formula (IV) is a carrier for carrying cisplatin, and the Pt in cisplatin and the carboxyl group of the block copolymer form a seven Member ring s...
Embodiment 1
[0083] The block copolymer having the structure of formula (V-a), m=45 and x=10 is denoted as mPEG 45 -b-PPLG 10 .
[0084] Add 0.2003g mPEG to the dry reaction vial 45 -b-PPLG 10 , after stirring and dissolving with 5mL N,N-dimethylformamide, blow nitrogen for 0.5 hours, add 14.0mg benzoin dimethyl ether and 0.6543g mercaptosuccinic acid at room temperature under the condition of nitrogen protection, and react with 365nm ultraviolet light for 2h, The product was obtained; the product was dialyzed for 72 hours, the water was changed 12 times, and freeze-dried to obtain a block copolymer freeze-dried powder having a structure of formula (III-a).
[0085] The nuclear magnetic resonance test was carried out on the block graft copolymer, and the grafting rate was calculated to be 61.8%, and the reaction conversion rate was 30.2%. The block copolymer with the structure of formula (III-a) m=45, n=6, y=4, denoted as mPEG 45 -b-PPLG 10 -g-MSA 12 .
Embodiment 2
[0087] A block copolymer having a knot of formula (V-a), m=113 and x=25, denoted as mPEG 113 -b-PPLG 25 .
[0088] Add 0.2008g mPEG to the dry reaction vial 113 -b-PPLG 25 , after stirring and dissolving with 5mL N,N-dimethylformamide, blow nitrogen gas for 0.5 hours, add 14.0mg benzoin dimethyl ether and 1.3201g mercaptosuccinic acid at room temperature under the condition of nitrogen protection, and react with 365nm ultraviolet light for 2h, The product was obtained; the product was dialyzed for 72 hours, the water was changed 12 times, and freeze-dried to obtain a block copolymer freeze-dried powder having a structure of formula (III-a).
[0089] The nuclear magnetic resonance test was carried out on the block graft copolymer, and the calculated graft rate was 60.0%, and the reaction conversion rate was 16.1%. The block copolymer with the structure of formula (III-a) m=113, n=15, y=10, denoted as mPEG 113 -b-PPLG 25 -g-MSA 30 .
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