【药物名称】HSP-117
化学结构式(Chemical Structure):
参考文献No.31203
标题:Piperidine derivs.
作者:Tanaoue, Y.; Beppu, K.; Okayama, A.; Sakamoto, O. (Hisamitsu Pharmaceutical Co., Ltd.)
来源:EP 0826684; US 5886011; WO 9630367
合成路线图解说明:

Reductive condensation of 3-amino-2-chloropyridine (I) with 5-isopropylbenzofuran-7-carbaldehyde (II) in the presence of sodium triacetoxyborohydride provided secondary amine (III). Displacement of the chlorine atom of (III) with phenylmagnesium bromide (IV) using NiCl2 produced phenylpyridine (V), which was hydrogenated with hydrogen over PtO2 in acetic acid to give racemic piperidine (VI). Resolution of (VI) with (R)-(-)-mandelic acid yielded the (2S,3S)-isomer, which was finally isolated as the dihydrochloride salt.

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