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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 \u03b1-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.<\/jats:p>","DOI":"10.1021\/acscombsci.7b00137","type":"journal-article","created":{"date-parts":[[2017,12,7]],"date-time":"2017-12-07T12:01:13Z","timestamp":1512648073000},"page":"70-74","source":"Crossref","is-referenced-by-count":19,"title":["Library-to-Library Synthesis of Highly Substituted\n\u03b1-Aminomethyl Tetrazoles via Ugi Reaction"],"prefix":"10.1021","volume":"20","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-0903-8174","authenticated-orcid":true,"given":"Pravin","family":"Patil","sequence":"first","affiliation":[{"name":"University of Groningen , , A. 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