【药物名称】Lanicemine hydrochloride, AR-R15896AR, FPL-15895AR((-)-enantiomer), FPL-15035AR(racemate), ARL-15896, FPL-15896AR(former code)
化学结构式(Chemical Structure):
参考文献No.22124
标题:Enantiomeric 1-phenyl-2-(2-pyridinyl)ethylamine for the treatment of neurodegenerative disorders
作者:Griffith, R.C.; Murray, R.J.; Balestra, M. (Celltech Group plc)
来源:EP 0633879; JP 2000319259; WO 9320052
合成路线图解说明:

Addition of lithium bis(trimethylsilyl)amide to a cooled solution of benzaldehyde (I), followed by treatment with the lithiated anion of 2-picoline (II), gave rise to the silylated amino intermediate (III), which, upon acidic quenching, yielded the racemic alpha-phenyl-2-pyridineethanamine (IV). Resolution of amine (IV) with S-(+)-mandelic acid in EtOAc provided the target (S)-amine mandelate salt (V). Liberation of the free amine with NaOH and subsequent treatment with HCl in EtOAc furnished the corresponding dihydrochloride

参考文献No.25061
标题:(S)-Alpha-phenyl-2-pyridineethanamine (S)-malate and its use as a medicament
作者:Murray, R.J.; Mathisen, D.; Balestra, M. (Celltech Group plc)
来源:EP 0691957; EP 0691958; JP 1996508292; JP 1996508475; WO 9422831; WO 9422832
合成路线图解说明:

Addition of lithium bis(trimethylsilyl)amide to a cooled solution of benzaldehyde (I), followed by treatment with the lithiated anion of 2-picoline (II), gave rise to the silylated amino intermediate (III), which, upon acidic quenching, yielded the racemic alpha-phenyl-2-pyridineethanamine (IV). Resolution of amine (IV) with S-(+)-mandelic acid in EtOAc provided the target (S)-amine mandelate salt (V). Liberation of the free amine with NaOH and subsequent treatment with HCl in EtOAc furnished the corresponding dihydrochloride

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