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【结 构 式】 
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【药物名称】S-20928 【化学名称】N-[2-(1-Naphthyl)ethyl]cyclobutanecarboxamide 【CA登记号】152302-33-5 【 分 子 式 】C17H19NO 【 分 子 量 】253.34708 |
【开发单位】ADIR (Originator) 【药理作用】Melatonin Antagonists |
合成路线1
Reduction of 1-naphthylacetonitrile (1) by catalytic hydrogenation using Raney Nickel in a NH3 saturated EtOH solution afforded 2-(1-naphthyl)ethylamine, which was then converted to hydrochloride salt (II). Further condensation with cyclobutanecarbonyl chloride (III) in the presence of K2CO3 provided the target amide.
| 【1】 Leclerc, V.; Fourmaintraux, E.; Depreux, P.; Lesieur, D.; Morgan, P.; Howell, H.E.; Renard, P.; Caignard, D.H.; Pfeiffer, B.; Delagrange, P.; Guardiola-Lemaitre, B.; Andrieux, J.; Synthesis and structure-activity relationships of novel naphthalenic and bioisosteric related amidic derivatives as melatonin receptor ligands. Bioorg Med Chem 1998, 6, 10, 1875. |
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