Rapid access to pyrido[1,2,5]triazepin-4-ones through intramolecular nucleophilic aromatic substitution |
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| Authors: | Shujuan Jin Olivier St-Jean Sandra I Baltatu Vijayaratnam Santhakumar Miros?aw J Tomaszewski |
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| Institution: | Department of Medicinal Chemistry, AstraZeneca R&D Montreal, 7171 Frederick-Banting, Saint-Laurent, Quebec, Canada H4S 1Z9 |
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| Abstract: | Several 3-substituted pyrido1,2,5]triazepin-4-ones and their benzo counterparts have been prepared in three steps from commercial starting materials. The key step involves SNAr-type intramolecular nucleophilic aromatic substitution of the appropriate hydrazone substrates. |
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