【药物名称】
化学结构式(Chemical Structure):
参考文献No.42056
标题:Biphenyl derivs.
作者:Van Amsterdam, C.; Harting, J.; Wikstr鰉, H.V.; Liao, Y.; B鰐tcher, H. (Merck Patent GmbH)
来源:WO 0005225
合成路线图解说明:

Coupling of 4-bromobenzoyl chloride (I) with amine (II) by means of Et3N in CH2Cl2 or THF yields bromo derivative (III), which is then converted into boronic acid derivative (IV) by treatment with triisopropyloxyboron and n-BuLi in THF/hexane. Suzuki reaction between (IV) and oxadiazole (V) by means of Pd(PPd3)4 and Na2CO3 in dimethoxyethane (DME)/H2O affords compound (VI), which is finally hydrogenated over Raney-Ni in H2O/MeOH/AcOH to furnish the desired product.

参考文献No.565859
标题:New selective and potent 5-HT1B/1D antagonists: Chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides
作者:Liao, Y.; B鰐tcher, H.; Harting, J.; Greiner, H.; van Amsterdam, C.; Cremers, T.; Sundell, S.; M鋜z, J.; Rautenberg, W.; Wikstrom, H.
来源:J Med Chem 2000,43(3),517
合成路线图解说明:

Coupling of 4-bromobenzoyl chloride (I) with amine (II) by means of Et3N in CH2Cl2 or THF yields bromo derivative (III), which is then converted into boronic acid derivative (IV) by treatment with triisopropyloxyboron and n-BuLi in THF/hexane. Suzuki reaction between (IV) and oxadiazole (V) by means of Pd(PPd3)4 and Na2CO3 in dimethoxyethane (DME)/H2O affords compound (VI), which is finally hydrogenated over Raney-Ni in H2O/MeOH/AcOH to furnish the desired product.

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