【药物名称】SSR-69071
化学结构式(Chemical Structure):
参考文献No.49874
标题:Saccharin derivs. as orally active elastase inhibitors
作者:Hermecz, I.; Kapui, Z.; Ar醤yi, P.; B醫ori, S.; Varga, M.; Dessilla, S.; L関ai, F.; Mikus, E.; Pascal, M.; Simonot, B.; Urb醤 Szab? K.; Vasv醨in?Debreczy, L.; T. Nagy, L. (Sanofi-Synth閘abo)
来源:WO 0144245
合成路线图解说明:

2-Amino-3-hydroxypyridine (I) is alkylated with N-(2-chloroethyl)piperidine (II) under phase transfer conditions to provide ether (III). Subsequent cyclization of aminopyridine (III) with bis-trichlorophenyl malonate (IV) in refluxing acetone leads to the pyridopyrimidine (V). This is finally condensed with the N-(bromomethyl)saccharin derivative (VI) to furnish the title compound.

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