【药物名称】
化学结构式(Chemical Structure):
参考文献No.588390
标题:1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors
作者:Coppola, G.M.; Zhang, Y.L.; Schuster, H.F.; Russell, M.E.; Hughes, T.E.
来源:Bioorg Med Chem Lett 2000,10(14),1555
合成路线图解说明:

Acylation of ethyl 3-amino-2-(3,5-dimethoxyphenyl)propionate (I) with N-phthaloylglycine (II) using EDC and HOAt afforded amide (III), which was subjected to a Bischler-Napieralski cyclization in the presence of POCl3 to produce the dihydroisoquinoline (IV). Aromatization of (IV) to the corresponding isoquinoline (V) was achieved by treatment with MnO2 in refluxing benzene. Hydrazinolysis of the phthaloyl group of (V) gave the free amine, which was purified after conversion to the N-Boc derivative (VI). Acid cleavage of the Boc group then furnished the title product.

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