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Methodology to rapidly and efficiently assemble 8-trifluoromethyltetrahydro-6H-pyrido [1,2-a] pyrazine-6-one (11) has been developed and its general applicability has been demonstrated.
An expeditious and concise synthesis of 3-(difluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines is described. Starting from N-benzyl piperidone, the key intermediates leading to these two biologically desirable synthones were rapidly assembled by inverse electron demand Diels–Alder (IEDA) reaction utilizing microwave irradiation. The...
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