Journal
TETRAHEDRON LETTERS
Volume 52, Issue 31, Pages 3963-3968Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2011.05.025
Keywords
Suzuki-Miyaura coupling; Biaryl; Piperazine; Microwave
Categories
Funding
- Novartis
- BP
- EPSRC
- University of Greenwich and the School of Science
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Boc-protected (piperazin-1-ylmethyl)biaryls have been synthesised from (Boc-piperazin-1-ylmethyl) phenylboronic acid pinacol esters via a microwave-mediated Suzuki-Miyaura coupling with aryl bromides viz. 1-bromo-, 2-, 3- or 4-nitrobenzene or 2-bromo-5-nitropyridine. Judicial removal of the protecting group on the piperazine, or facile reduction of the nitro group on the biaryl system enabled the manipulation of two points of functionality in order to diversify the scope of the resulting biaryl library. (C) 2011 Elsevier Ltd. All rights reserved.
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