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【结 构 式】 
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【药物名称】AP-5280 【化学名称】cis-Diammine platinum complex polymer composed of an HMPA copolymer bound to an amidomalonate chelator through a Gly-Phe-Leu-Gly linker 【CA登记号】 【 分 子 式 】C81H139N16NaO27Pt 【 分 子 量 】1987.18178 |
【开发单位】Access Pharmaceuticals (Originator) 【药理作用】Antineoplastic Enhancing Agents, Modulators of the Therapeutic Activity of Antineoplastic Agents, ONCOLYTIC DRUGS, Ovarian Cancer Therapy, DNA Alkylating Drugs, Platinum Complexes |
合成路线1
The known N-(2-hydroxypropyl)-methacrylamide copolymer (I) which has a p-nitrophenyl peptide side chain is coupled to ethyl aminomalonate (II) in the presence of Et3N in DMF to give the corresponding amide (III). Alkaline hydrolysis of the diethyl malonate ester groups of (III) affords the sodium carboxylate salt (IV). This is then complexed with the platinum species, generated in situ from cisplatin (V) and silver nitrate, to produce the title polymer-linked platinum complex.
| 【1】 Duncan, R.; Evagorou, E.G.; Buckley, R.G.; Gianasi, E. (Access Pharmaceuticals, Inc.); Polymer-platinum cpds.. WO 9847537 . |