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【结 构 式】 
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【药物名称】NSC-350602, PHIC 【化学名称】cis-(1,2-Diaminocyclohexane)(isocitrato) platinum (II) disodium salt dihydrate 【CA登记号】 【 分 子 式 】C12H24N2Na2O10Pt 【 分 子 量 】597.40208 |
【开发单位】CNRS (Originator) 【药理作用】Oncolytic Drugs, Platinum Complexes |
合成路线1
PHIC is prepared from the diaquo derivative cis-[Pt(diaminocyclohexane)(H2O)2](NO3)2 (II), which is obtained by addition of a stoichiometric amount of silver nitrato to cis-[PtCl2(diaminocyclohexane)] (I). Then isocitrate trisodium salt is added to the diaquo species (II) (1:1), and the mixtures heated to 60 C in the dark for 20 h. The yellow solution is concentrated. then treated with cold ethanol acetona (1:1) to give white PHIC precipitate. After the usual workup, PHIC is obtained (85%). The binding sites of the isocitrate ion to the platinum: diamino cyclohexane moiety have not been characterized.
| 【1】 Ross, W.C.J.; Khokkar, A.R.; Connors, T.A.; Jones, M.; Braddock, P.D.; Tobe, M.L.; New platinum complexes with anti-tumor activity. Chem Biol Interact 1972, 5, 415-424. |
| 【2】 Speer, R.J.; Zapata, A.; Hill, J.M.; Stewart, D.P.; Ridgway, H.; Hall, L.M.; Sulfato 1,2-diaminocyclohexane platinum (II): A potencial new antitumor agent. J Clin Hematol Oncol 1977, 7, 210-219. |
| 【3】 Macquet, J.P.; Armand, J.P.; Cros, S.; Pharmacological and preclinical toxicological studies of 1,2-diaminocyclohexane(isocitrato)platinum (II). Cancer Res 1984, 44, 9, 3736. |
| 【4】 Chang, P.; PHIC. Drugs Fut 1985, 10, 10, 827. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (I) | 12824 | 2-Aminophenylamine; o-Phenylenediamine; 1,2-Benzenediamine | 95-54-5 | C6H8N2 | 详情 | 详情 |
| (II) | 29737 | Phenylene-1,2-diamine dichloroplatinum complex | C6H8Cl2N2Pt | 详情 | 详情 | |
| (III) | 29738 | Phenylene-1,2-diamine diaqua platinum complex dinitrate | C8H14N2Pt | 详情 | 详情 | |
| (IV) | 29739 | trisodium 1-hydroxy-1,2,3-propanetricarboxylate | C6H5Na3O7 | 详情 | 详情 |