【药物名称】
化学结构式(Chemical Structure):
参考文献No.531837
标题:Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists
作者:Beck, J.P.; Arvanitis, A.G.; Curry, M.A.; Rescinito, J.T.; Fitzgerald, L.W.; Gilligan, P.J.; Zaczek, R.; Trainor, G.L.
来源:Bioorg Med Chem Lett 1999,9(7),967
合成路线图解说明:

4-Hydroxy-6-methyl-3-nitro-2-pyridone (I) was treated with phosphoryl chloride in boiling N,N-diethylaniline, and the resulting dichloropyridine (II) was condensed with n-butyl ethylamine (III) to afford a regioisomeric mixture of 4- (IV) and 2-amino (V) pyridines. After chromatographic separation, the desired isomer (IV) was coupled with 2-bromo-4-isopropylaniline (VI) at 140 C to provide (VII). Reduction of the nitro group of (VII) using sodium hydrosulfite and ammonia yielded diamine (VIII). Subsequent cyclization of (VIII) with phosgene in refluxing toluene gave imidazopyridinone (IX), which was finally N-methylated by means of CH3I and KOH in acetone.

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