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【结 构 式】 
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【药物名称】RP-463 【化学名称】Trisodium (OC-6-54)-[N-formyl-L-methionyl-L-leucyl-L-phenylalanyl-N6-[6-(diazenyl-kappaN2)pyridin-3-ylcarbonyl]-L-lysinato(2-)][N-[2-hydroxy-1,1-bis(hydroxy-kappaO-methyl)ethyl]glycinato-kappaN,kappaO][[3,3',3''-(phosphinidyne-kappaP)tris[benzenesulfonato]](3-)]technetate(3-)-99Tc 【CA登记号】244238-18-4 【 分 子 式 】C57H68N9Na3O21PS4Tc 【 分 子 量 】1542.42441 |
【开发单位】AnorMED (Originator), Bristol-Myers Squibb (Originator), McNeil Consumer Products (Originator) 【药理作用】DIAGNOSTIC AGENTS |
合成路线1
The title compound was synthesized from the known formyl tetrapeptide conjugated to 6-hydrazinonicotinic acid (I) by complexation with tricine (II), trisodium triphenylphosphine-3,3',3''-trisulfonate (III) and sodium 99mTc-pertechnetate, either in two steps by first complexation of the stannous chloride-reduced technetium with (I) and (II), and then reaction with (III), or in one step by direct reduction of Na99mTcO4 with SnCl2 in the presence of (I), (II) and (III). The compound was also formed in the absence of SnCl2.
| 【1】 Edwards, D.S.; et al.; RP463: A stabilized technetium-99m complex of a hydroazino nicotinamide derivatized chemotactic peptide for infection imaging. Bioconjugate Chem 1999, 10, 5, 884. |
| 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) | 37262 | (5S,8S,11S,14S)-11-benzyl-5-(formylamino)-14-(4-[[(6-hydrazino-3-pyridinyl)carbonyl]amino]butyl)-8-isobutyl-6,9,12-trioxo-2-thia-7,10,13-triazapentadecan-15-oic acid | C33H48N8O7S | 详情 | 详情 | |
| (II) | 37263 | 2-[[2-hydroxy-1,1-bis(hydroxymethyl)ethyl]amino]acetic acid | 5704-04-1 | C6H13NO5 | 详情 | 详情 |
| (III) | 37264 | trisodium 3-[bis(3-sulfonatophenyl)phosphino]benzenesulfonate | C18H12Na3O9PS3 | 详情 | 详情 |