新型庚铂衍生物的合成

Synthesis of Novel Eptaplatin Derivatives

以D-酒石酸与芳香醛为起始原料,经缩合、氨解和还原反应制得中间体(4R,5R)-4,5-双(氨甲基)-1,3-二氧戊环类化合物(5a^5n);5a^5n分别与氯亚铂酸钾经配位反应合成了14个新型庚铂衍生物(6a^6n);6a^6j依次与硝酸银和丙二酸钠反应合成了10个新型庚铂衍生物,收率18.29%~50.91%,其结构经1H NMR,ESI-MS和元素分析表征。

The intermediates, （ 4R, 5R ） -4,5-bis （ aminomethyl ） -2-isopropyl-1,3-dioxolane （ 5a ~ Sn）, Were synthesized by condensation, aminolysis and reduction from D-tartaric acid and aromatic aldehydes. Fourteen novel eptaplatin derivatives（6a ~ 6n） were synthesized by coordination reaction of 5a ~ 5n with dipotassium tetraehloroplatinate. Ten novel eptaplatin derivatives with yields of 18.29% -50.91% were obtained by reaction of6a ~6j with AgNO3 and then sodium malonate. The structures were characterized by 1H NMR, ESI-MS and elemental analysis.