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【结 构 式】 
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【药物名称】DuP-654 【化学名称】2-Benzyl-1-naphthol 【CA登记号】36441-32-4 【 分 子 式 】C17H14O 【 分 子 量 】234.30053 |
【开发单位】Bristol-Myers Squibb (Originator) 【药理作用】Antiinflammatory Drugs, Lipoxygenase Inhibitors |
合成路线1
Alkylation of the sodium salt of 1-naphthol with benzyl bromide provides DuP-654. Alternatively, condensation of 1-tetralone (I) with benzaldehyde (II) in the presence of potassium hydroxide yields 2-benzylidene-1-tetralone (III), which may be isomerized to DuP-654 using rhodium chloride or a soluble iridium complex. A mixture of (I) and (II) may also be directly converted to DuP-654 by treating with potassium tert-butoxide in refluxing tert-butanol.
| 【1】 Batt, D.G. (E.I. Du Pont de Nemours & Co.); 2-Substituted-1-naphthols as 5-lipoxygenase inhibitors. AU 8657186; EP 0201071; ES 8801780; US 4833164 . |
| 【2】 Harris, R.R.; Batt, D.G.; Galbraith, W.; Gans, K.R.; Jaffee, B.D.; Kerr, J.S.; Ackerman, N.R.; Mackin, W.M.; DuP-654. Drugs Fut 1989, 14, 11, 1040. |
Extended Information