| Literature DB >> 31437394 |
Olena Savych1,2, Yuliya O Kuchkovska1,3, Andrey V Bogolyubsky1, Anzhelika I Konovets1, Kateryna E Gubina3, Sergey E Pipko4, Anton V Zhemera1, Alexander V Grishchenko1, Dmytro N Khomenko3, Volodymyr S Brovarets2, Roman Doroschuk3, Yurii S Moroz3,4, Oleksandr O Grygorenko1,3.
Abstract
Two protocols for the combinatorial synthesis of 5-(dialkylamino)tetrazoles were developed. The best success rate (67%) was shown by the method that used primary and secondary amines, 2,2,2-trifluoroethylthiocarbamate, and sodium azide as the starting reagents. The key steps included the formation of unsymmetrical thiourea, subsequent alkylation with 1,3-propane sultone and cyclization with azide anion. A 559-member aminotetrazole library was synthesized by this approach; the overall readily accessible (REAL) chemical space covered by the method exceeded 7 million feasible compounds.Entities:
Keywords: 2,2,2-trifluoroethylthiocarbamate; REAL (readily accessible) compounds; heterocyclization; tetrazoles; thiourea
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Year: 2019 PMID： 31437394 PMCID： PMC7297054 DOI： 10.1021/acscombsci.9b00120
Source DB: PubMed Journal: ACS Comb Sci ISSN： 2156-8944 Impact factor: 3.784