Application of cyclic ketones in MCR: Ugi/amide coupling based synthesis of fused tetrazolo[1,5-a][1,4]benzodiazepines |
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| Authors: | Swapnil G Yerande Kiran M Newase Bhawani Singh André Boltjes Alexander Dömling |
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| Institution: | 1. Acoris Research (A Division of Hikal Ltd), 3A, International Biotech Park, Hinjewadi, Pune 411 057, Maharashtra, India;2. Department of Pharmaceutical Chemistry, P.E. Society’s, Modern College of Pharmacy, Sector 21, Yamunanagar, Nigdi, Pune 411 044, Maharashtra, India;3. Organic Research Laboratory, Department of Chemistry, Banasthali University, Banasthali 304 022, India;4. Dept. of Pharm. Chemistry (PG), Chair of Drug Design, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands |
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| Abstract: | Azido-Ugi reaction involving cyclic ketone, primary amine, isonitrile, and azide afforded substituted tetrazole derivatives 5. These intermediates were hydrolyzed to corresponding acid derivatives. EDAC/HOBt mediated amide bond formation of 5 gave fused tetrazolo1,5-a]1,4]benzodiazepine 6 in high yield and good diversity. |
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| Keywords: | Cyclic ketone Ugi multi component reaction Ugi/amide coupling Fused tetrazole-ketopiperazine |
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