SSR-69071
2-[[6-甲氧基-4-(1-甲基乙基)-1,1-二氧并-3-氧代-1,2-苯并异噻唑-2(3H)-基]甲氧基]-9-[2-(1-哌啶基)乙氧基]-4H-吡啶并[1,2-a]嘧啶-4-酮Chemical Name: 2-(4-Isopropyl-6-methoxy-1,1,3-trioxo-2,3-dihydro-1,2-benzisothiazol-2-ylmethoxy)-9-[2-(1-piperidinyl)ethoxy]-4H-pyrido[1,2-a]pyrimidin-4-one
CAS No. 344930-95-6, 344930-98-9 (benzoate), 344930-99-0 (citrate), 344930-97-8 (fumarate), 344930-96-7 (hydrochloride), 344931-13-1 (tartrate)
项目整合开发状态: Discontinued
项目研究机构: Sanofi-Aventis (Originator), Chinoin (Codevelopment)
合成路线: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.
📌 参考资料/链接:
参考文献标题:Saccharin derivs.as orally active elastase inhibitors
文献作者: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-Synthabo)
参考来源:WO 0144245