【结 构 式】 |
【药物名称】[18F]-FEDAA-1106 【化学名称】N-[2-(2-[18-F]-Fluoroethoxy)-5-methoxybenzyl]-N-(5-fluoro-2-phenoxyphenyl)acetamide 【CA登记号】 【 分 子 式 】C24H23F2NO4 【 分 子 量 】426.45361 |
【开发单位】Japan Science and Technology (Originator), National Institute Radiological Sciences (Originator) 【药理作用】Diagnostic Agents, Drugs Acting on GABA-Mediated Transmission |
合成路线1
Reaction of 2-bromoethyl triflate (I) with [18F]fluoride in boiling o-dichlorobenzene leads to the radiolabeled 1-bromo-2-fluoroethane (II). The known peripheral benzodiazepine receptor ligand (III) is then alkylated with bromide (II) in the presence of NaH in hot DMF to furnish the title compound.
【1】 Zhang, M.-R.; Maeda, J.; Furutsuka, K.; Yoshida, Y.; Ogawa, M.; Suhara, T.; Suzuki, K.; [18F]FMDAA1106 and [18F]FEDAA1106: Two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR). Bioorg Med Chem Lett 2003, 13, 2, 201. |
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) | 63201 | 2-bromoethyl trifluoromethanesulfonate | C3H4BrF3O3S | 详情 | 详情 | |
(II) | 28769 | 1-bromo-2-fluoroethane | 762-49-2 | C2H4BrF | 详情 | 详情 |
(II) | 63202 | 1-bromo-2-fluoroethane | C2H4BrF | 详情 | 详情 | |
(III) | 63200 | N-(5-fluoro-2-phenoxyphenyl)-N-(2-hydroxy-5-methoxybenzyl)acetamide | C22H20FNO4 | 详情 | 详情 |
Extended Information