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【结 构 式】 
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【药物名称】HIPDM 【化学名称】N,N,N'-Trimethyl-N'-(2-hydroxy-3-methyl-5-iodobenzyl)-1,3-propanediamine dihydrochloride 【CA登记号】84718-97-8 【 分 子 式 】C14H25Cl2IN2O 【 分 子 量 】435.17855 |
【开发单位】State University of New York, Buffalo (Originator) 【药理作用】DIAGNOSTIC AGENTS, Radiopharmaceuticals, Radiopharmaceuticals for Brain Imaging |
合成路线1
The 5-methylsalicylaldehyde (I) is prepared by a tin (IV) chloride-catalyzed formylation. Iodination of the aldehyde with ICl in glacial acetic acid gives good yield of 3-methyl-5-iodobenzylaldehyde (III). The iodinated salicylaldehyde is reductively aminated with N,N,N'-trimethylpropane-1,3-diamine and sodium borohydride to give N,N,N'-trimethyl-N'-(2-hydroxy-3-methyl-5-iodobenzyl)-1,3-propanediamine (HIPDM) (III) in excellent yield.
| 【1】 Blau, M.; Tramposch, K.M.; Kung, H.F.; Radioiodine-labeled N,N-dimethyl-N'-(2-hydroxy-3-ankyl-5-iodobenzyl)-1,3.propanediamines for Brain Perfusion Imaging. J Med Chem 1983, 28, 2, 121-125. |
| 【2】 Kung, H.F.; Hostyniak, P.J.; HIPDM. Drugs Fut 1985, 10, 9, 742. |