Samenvatting
α-Aminomethyl tetrazoles, recently made accessible by an Ugi multicomponent reaction (MCR), were shown to be excellent starting materials for a further Ugi MCR, yielding substituted N-methyl-2-(((1-methyl-1H-tetrazol-5-yl)methyl)amino)acetamides having four points of diversity in a library-to-library approach. The scope and limitations of the two-step sequence was explored by conducting more than 50 reactions. Irrespective of electron-rich and electron-deficient oxo-components and the nature of the isocyanide component, the reactions give excellent yields. Sterically less hindered α-aminomethyl tetrazoles give better yields of in further Ugi MCR. The target scaffold has four points of diversity and is finding applications to fill screening decks for high-throughput screening (HTS) in the European Lead Factory and in structure-based drug design.
Originele taal-2 | English |
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Pagina's (van-tot) | 70-74 |
Aantal pagina's | 5 |
Tijdschrift | Acs combinatorial science |
Volume | 20 |
Nummer van het tijdschrift | 2 |
DOI's | |
Status | Published - 12-feb.-2018 |
Datasets
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CCDC 1484776: Experimental Crystal Structure Determination
Patil, P. (Contributor), Kurpiewska, K. (Contributor), Kalinowska-Tłuścik, J. (Contributor) & Dömling, A. (Contributor), University of Groningen, 12-jun.-2016
DOI: 10.5517/ccdc.csd.cc1lv10h
Dataset
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CCDC 1485017: Experimental Crystal Structure Determination
Patil, P. (Contributor), Mishra, B. (Contributor), Sheombarsing, G. (Contributor), Kurpiewska, K. (Contributor), Kalinowska-Tluścik, J. (Contributor) & Dömling, A. (Contributor), University of Groningen, 13-jun.-2016
DOI: 10.5517/ccdc.csd.cc1lv8sh
Dataset
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CCDC 1484779: Experimental Crystal Structure Determination
Patil, P. (Contributor), Mishra, B. (Contributor), Sheombarsing, G. (Contributor), Kurpiewska, K. (Contributor), Kalinowska-Tluścik, J. (Contributor) & Dömling, A. (Contributor), University of Groningen, 12-jun.-2016
DOI: 10.5517/ccdc.csd.cc1lv13l
Dataset