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【结 构 式】

【药物名称】Amorolfine hydrochloride, MT-861, Ro-14-4767/000(free base), Ro-14-4767/002, Pekiron, Bekiron, Loceryl

【化学名称】(±)-cis-4-[3-[4-(1,1-Dimethylpropyl)phenyl]-2-methylpropyl]-2,6-dimethylmorpholine hydrochloride

【CA登记号】78613-35-1 (free base), 67467-83-8 (free base non-specified stereoch.)

【 分 子 式 】C21H36ClNO

【 分 子 量 】353.98017

【开发单位】Roche (Originator), Galderma (Not Determined), Kyorin (Licensee), Maruho (Codevelopment), Shiseido (Codevelopment)

【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY

合成路线1

By condensation of 3-(4-tert-amylphenyl)propionaldehyde (I) with 2,6-dimethylmorpholine (II) by heating at 100 C in toluene, followed by hydrogenation with H2 over Pd/C in the same solvent.

1 Pfiffner, A.; Bohnen, K. (Roche); Piperidines morpholines, etc., and fungicidal compsns. Thereof. US 4202894; US 4241058 .
2 Blancafort, P.; Castaner, J.; Serradell, M.N.; RO-144,767/002. Drugs Fut 1982, 7, 7, 492.
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) 37122 (2R,6S)-2,6-dimethylmorpholine;cis-2,6-dimethylmorpholine 6485-55-8 C6H13NO 详情 详情
(II) 37123 2-methyl-3-[4-(tert-pentyl)phenyl]propanal C15H22O 详情 详情
Extended Information