This invention relates to quinolone- and naphthyridone derivatives represented by the general formula VII, and a process for their preparation using Baylis-Hillman adducts from substituted aromatic or hetero-aromatic aldehydes and amines of interest as the starting materials. After the tandem Aza-Michael addition and SNAr cyclization, the resulting 4-hydroxy-1,2,3,4-tetrahydroquinoline or 4-hydroxy-1, 2,3,4- tetrahydro-1,8-naphthyridine derivative was subjected to oxidation to get the quinolone or naphthyridone skeleton in one step in good to excellent yields.
本发明涉及通式VII所代表的
喹诺酮和
萘啶酮衍
生物,以及使用取代芳香族或杂
芳香族醛和感兴趣的胺作为起始材料,从Baylis-Hillman加合物开始制备它们的过程。在串联的Aza-Michael加成和SNAr环化之后,所得的
4-羟基-
1,2,3,4-四氢喹啉或
4-羟基-
1,2,3,4-四氢-1,8-萘啶衍
生物被氧化,从而在一步中以良好至优异的收率得到
喹诺酮或
萘啶酮骨架。