Journal
TETRAHEDRON
Volume 69, Issue 10, Pages 2352-2356Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2012.12.086
Keywords
Boronic acids; Azides; Multicomponent reactions; Cyclization; 1,4,5-Trisubstituted 1,2,3-triazoles
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Funding
- National Natural Science Foundation of China [21072057, 21272070]
- Key Project in the National Science & Technology Pillar Program of China in the twelfth five-year plan period [2011BAE06B01-15]
- National Basic Research Program of China (973 Program) [2010CB126101]
- National High Technology Research and Development Program of China (863 Program) [2011AA10A204]
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A series of 1-aryl-5-trifluoromethyl (or difluoromethyl)-1,4,5-trisubstituted 1,2,3-triazoles were synthesized in high yield by a novel one-pot three-component reaction of arylboronic acids, sodium azide, and active methylene ketones, such as ethyl 4,4-difluoroacetoacetate or ethyl 4,4,4-trifluoroacetoacetate in the presence of Cu(OAc)(2) and piperidine using a DMSO/H2O (10/1) mixture as solvent. (C) 2013 Elsevier Ltd. All rights reserved.
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