【药物名称】AVP-13358
化学结构式(Chemical Structure):
参考文献No.57656
标题:Benzimidazole cpds. for modulating IgE and inhibiting cellular proliferation
作者:Sircar, J.C.; Richards, M.L.; Major, M.W. (Avanir Pharmaceuticals)
来源:EP 1368028; WO 0272090
合成路线图解说明:

The cyclization of 3,4-diaminobenzoic acid (I) with 4-nitrobenzaldehyde (II) in nitrobenzene at 160 C gives 2-(4-nitrophenyl)-1H-benzimidazole-5-carboxylic acid (III), which is condensed with 2-aminopyridine (IV) by means of CDI in DMF to yield the corresponding amide (V). The reduction of the nitro group of (V) with H2 over Pd/C in methanol affords 2-(4-aminophenyl)-N-(2-pyridinyl)-1H-benzimidazole-5-carboxamide (VI). Finally, this compound is condensed with adamantane-1-carboxylic acid (VII) to provide the target diamide.

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