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【结 构 式】 
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【药物名称】 【化学名称】4-(Aminomethyl)-2,6-difluorophenol 【CA登记号】220353-10-6 (hydrochloride) 【 分 子 式 】C7H7F2NO 【 分 子 量 】159.13674 |
【开发单位】AstraZeneca (Originator) 【药理作用】Pharmacological Tools, GABA(C) Receptors Antagonists |
合成路线1
Nitration of 2,6-difluorophenol (I) gave 2,6-difluoro-4-nitrophenol (II), which was reduced to the corresponding aniline (III) by hydrogenation over Pd/C. Nitrile (IV) was obtained by diazotization of (III) followed by in situ displacement of the diazonium salt with CuCN and KCN. The nitrile (IV) was finally reduced to the title benzylamine employing borane in THF.
| 【1】 Qiu, J.; Stevenson, S.H.; O'Beirne, M.J.; Silverman, R.B.; 2,6-Difluorophenol as a bioisostere of a carboxylic acid: Bioisosteric analogues of gamma-aminobutyric acid. J Med Chem 1999, 42, 2, 329. |
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