Aromatic Nitrogen heterocycles are a very important class of organic compounds,of which 1,8-naphthyridone is the parent structure of several marketed small molecule drugs.The currently reported synthetic methods have problems with lengthy steps and low atom efficiency.Using inexpensive and readily available methyl nicotinate as the starting material,1,8-naphthyridone is prepared through Claisen condensation,oxidation,activating reagent mediated C-H amination and acid catalyzed cyclization.The oxidant has been optimized and the effect of different activating reagents on the amination reaction has been investigated.The optimized process is used to achieve a gram scale reaction of the synthesis route,and the target product is synthesized in a total yield of about 20%through four steps.
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