【药物名称】A-160621
化学结构式(Chemical Structure):
参考文献No.41278
标题:Retroviral protease inhibiting cpds.
作者:Chen, X.; Mohammadi, F.; Norbeck, D.W.; Kempf, D.J. (Abbott Laboratories Inc.)
来源:WO 9959994
合成路线图解说明:

Intermediate (III) was prepared by condensation of epoxide (I) with piperazine (II). After removal of the carbobenzoxy protecting group of (III) by catalytic hydrogenation, the resulting amine (IV) was coupled to the valine derivative (V) using EDC to afford amide (VI). Subsequent cleavage of the Boc protecting group of (VI) under acidic conditions gave (VII), which was finally alkylated with the benzodioxolylmethyl halide (VIII) to provide the target compound.

参考文献No.483521
标题:Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands
作者:Chen, X.; Kempf, D.J.; Sham, H.L.; Green, B.E.; Molla, A.; Korneyeva, M.; Vasavanonda, S.; Wideburg, N.E.; Saldivar, A.; Marsh, K.C.; McDonald, E.; Norbeck, D.W.
来源:Bioorg Med Chem Lett 1998,8(24),3531
合成路线图解说明:

Intermediate (III) was prepared by condensation of epoxide (I) with piperazine (II). After removal of the carbobenzoxy protecting group of (III) by catalytic hydrogenation, the resulting amine (IV) was coupled to the valine derivative (V) using EDC to afford amide (VI). Subsequent cleavage of the Boc protecting group of (VI) under acidic conditions gave (VII), which was finally alkylated with the benzodioxolylmethyl halide (VIII) to provide the target compound.

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