|
【结 构 式】 
|
【药物名称】CPI-[(99m)-Tc], Tc-CPI, (99m)-Tc-CPI 【化学名称】Hexakis(carbomethoxyisopropylisonitrile)technetium[(99m)Tc](1+) 【CA登记号】109834-25-5, 109800-36-4 (non-labeled) 【 分 子 式 】C36H54N6O12Tc 【 分 子 量 】861.86478 |
【开发单位】Harvard College (Originator), Massachusetts Institute of Technology (Originator) 【药理作用】DIAGNOSTIC AGENTS, Isotopes |
合成路线1
The esterification of 2-aminoisobutyric acid (I) with methanol - HCl gives the corresponding methyl ester (II), which is formylated with formic acid - acetic anhydride or methyl formate yielding the formamide (III). Dehydration of (III) with diphosgene (DPG) or POCl3 in pyridine affords methyl 2-isocyanoisobutyrate (CPI) (IV). Finally, this compound or its ZnBr2 complex [Zn(CPI)2Br2] is treated with 99mTcO4 and sodium dithionite or SnCl2 respectively, in ethanol-water solution. The radiochemical purity was >95%.
| 【1】 Jones, A.G.; Davison, A.; Kronauge, J.; Abrams, M.J. (Harvard College; Massachusetts Institute of Technology); Carboxy, carboalkoxy and carbamile substd. isonitrile radionuclide complexes. EP 0213945 . |
| 【2】 Holman, B.L.; Sporn, V.; Jones, A.G.; et al.; Myocardial imaging with Tc-99m CPI: Initial experience in human. J Nucl Med 1987, 28, 13-18. |
| 【3】 Liu, X.-J.; Wang, X.-B.; Lahiri, A.; Prous, J.; Castaner, J.; [99m]-Tc-CPI. Drugs Fut 1990, 15, 9, 883. |
| 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) | 31173 | 2-methylalanine；2-Aminoisobutyric acid;2-Amino-2-methylpropionic acid;alpha-Aminoisobutyric acid | 62-57-7 | C4H9NO2 | 详情 | 详情 |
| (II) | 31174 | methyl 2-amino-2-methylpropanoate | C5H11NO2 | 详情 | 详情 | |
| (III) | 31175 | methyl 2-(formylamino)-2-methylpropanoate | C6H11NO3 | 详情 | 详情 | |
| (IV) | 31176 | methyl 2-isocyano-2-methylpropanoate | C6H9NO2 | 详情 | 详情 |