An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines |
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Authors: | Deodialsingh Guiadeen Shankaran Kothandaraman Lihu Yang Sander G. Mills Malcolm MacCoss |
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Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA |
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Abstract: | 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 scope of the microwave methodology developed herein was extended to other ketones. |
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Keywords: | Difluoromethoxy Trifluoromethoxy Microwave |
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