【药物名称】
化学结构式(Chemical Structure):
参考文献No.37650
标题:CRF antagonistic quino- and quinazolines
作者:Huang, C.; Chen, C.; McCarthy, J.R.; Haddach, M.; Wilcoxen, K.M. (Janssen Pharmaceutica NV; Neurocrine Biosciences Inc.)
来源:EP 0977737; WO 9847874
合成路线图解说明:

Suzuki coupling of 2-bromoaniline (I) with boronic acid (II) in the presence of a palladium catalyst gave biphenyl (III). Subsequent condensation of (III) with ethyl acetoacetate (IV) afforded enamine (V), which was cyclized to hydroxyquinoline (VI) in refluxing diphenyl ether. Chlorination of (VI) in boiling POCl3 produced the corresponding 4-chloroquinoline (VII). This was finally condensed with N-(cyclopropylmethyl)-N--propylamine (VIII) to provide the target aminoquinoline.

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