KI-60606
Chemical Name: Hexalithium tris(trans-cyclohexane-1,2-diamine-kappaN,kappaN')[mu3-[2,4,6-tris[(1S)-1,3-di(carboxy-kappaO)propylamino]-2,4,6-tris[(1S)-1,3-dicarboxypropylamino]-1,3,5,2,4,6-triazatriphosphorinato(12-)]]triplatinate(6-)
CAS No. 297735-33-2
项目整合开发状态: Preclinical
项目研究机构: Il-Yang (Originator), Korea Inst. Sci. Technol. (Originator), Korea Res. Inst. Chem. Technol. (Originator)
合成路线:Treatment of hexachlorocyclotriphosphazene (I) with L-glutamic acid diethyl ester (II) in toluene in the presence of Et3N provides the ethyl glutamate derivative of cyclotriphosphazene (III),which is then subjected to saponification with LiOH in H2O to furnish compound (IV) (alternatively,the same procedure can be followed by performing the reaction between (I) and L-glutamic acid dimethyl ester (V) to afford the methyl glutamate derivative of cyclotriphosphazene (VI),which is saponified under the same conditions as (III)).Finally,the target product is obtained by reaction of intermediate (IV) with platinum derivative (VII) by means of Ag2SO4 in water,followed by treatment with BaCl2.H2O and precipitation in acetone.
📌 参考资料/链接：
参考文献标题:Platinum complex conjugated to cyclotriphosphazene,its preparation,and anticancer agent comprising the same
文献作者:Lee,C.O.; Sohn,Y.S.; Baek,H.G.(Il-Yang Pharmaceutical Co.,Ltd.; Korea Institute of Science and Technology)
参考来源:EP 1082331; US 6221906; WO 0058321
📄 详细内容
合成路线:Treatment of hexachlorocyclotriphosphazene (I) with L-glutamic acid diethyl ester (II) in toluene in the presence of Et3N provides the ethyl glutamate derivative of cyclotriphosphazene (III),which is then subjected to saponification with LiOH in H2O to furnish compound (IV) (alternatively,the same procedure can be followed by performing the reaction between (I) and L-glutamic acid dimethyl ester (V) to afford the methyl glutamate derivative of cyclotriphosphazene (VI),which is saponified under the same conditions as (III)).Finally,the target product is obtained by reaction of intermediate (IV) with platinum derivative (VII) by means of Ag2SO4 in water,followed by treatment with BaCl2.H2O and precipitation in acetone.
参考文献标题:Synthesis and antitumor activity of cyclotriphosphazene - (diamine)platinum (II) conjugates
文献作者:Baek,H.; Cho,Y.; Lee,C.O.; Sohn,Y.S.
参考来源:Anti-Cancer Drugs 2000,11(9),715