【药物名称】Zaprinast, M&B-22948
化学结构式(Chemical Structure):
参考文献No.47603
标题:Pharmaceutical compositions comprising azapurinones useful in treating allergic respiratory disorders
作者:Broughton, B.J.; et al. (May & Baker, Ltd.)
来源:DE 2162096; FR 2118078; GB 1338235; US 3987160
合成路线图解说明:

By reduction of 2-propoxybenzamidoxime (I) with H2 over Raney-Ni in ethanol to give 2-propoxybenzamidine (II), m.p. 170-1 C, which was condensed with ethyl alpha-nitrosocyanacetate (A) by means of sodium methoxide in methanol yielding 4-amino-2-(2-propoxyphenyl)-5-nitrosopyrimid-6-one (III), m.p. 215-6 C. This compound was reduced with sodium dithionite in water to give 4,5-diamino-2-(2-propoxyphenyl)- pyrimid-6-one (IV), m.p. 162-4 C, which was finally cyclized with sodium nitrite in aqueous HCl.

参考文献No.62081
标题:M&B 22,948
作者:Ryan, M.P.; Casta馿r, J.
来源:Drugs Fut 1977,2(1),35
合成路线图解说明:

By reduction of 2-propoxybenzamidoxime (I) with H2 over Raney-Ni in ethanol to give 2-propoxybenzamidine (II), m.p. 170-1 C, which was condensed with ethyl alpha-nitrosocyanacetate (A) by means of sodium methoxide in methanol yielding 4-amino-2-(2-propoxyphenyl)-5-nitrosopyrimid-6-one (III), m.p. 215-6 C. This compound was reduced with sodium dithionite in water to give 4,5-diamino-2-(2-propoxyphenyl)- pyrimid-6-one (IV), m.p. 162-4 C, which was finally cyclized with sodium nitrite in aqueous HCl.

参考文献No.607982
标题:Antiallergic activity of 2-phenyl-8-azapurin-6-ones
作者:Broughton, B.J.; Chaplen, P.; Knowles, P.; Lunt, E.; Marshall, S.M.; Pain, D.L.; Wooldridge, K.R.
来源:J Med Chem 1975,18(11),1117-22
合成路线图解说明:

By reduction of 2-propoxybenzamidoxime (I) with H2 over Raney-Ni in ethanol to give 2-propoxybenzamidine (II), m.p. 170-1 C, which was condensed with ethyl alpha-nitrosocyanacetate (A) by means of sodium methoxide in methanol yielding 4-amino-2-(2-propoxyphenyl)-5-nitrosopyrimid-6-one (III), m.p. 215-6 C. This compound was reduced with sodium dithionite in water to give 4,5-diamino-2-(2-propoxyphenyl)- pyrimid-6-one (IV), m.p. 162-4 C, which was finally cyclized with sodium nitrite in aqueous HCl.

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