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Synfacts 2009(9): 0951-0951  
DOI: 10.1055/s-0029-1217616
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of µ-Opioid Selective Ligands

Contributor(s): Philip Kocienski
C. Dockendorff, S. Jin, M. Olsen, M. Lautens*, M. Coupal, L. Hodzic, N. Spear, K. Payza, C. Walpole, M. J. Tomaszewski*
University of Toronto, AstraZeneca R&D Montréal, Canada and AstraZeneca Pharmaceuticals, Wilmington, USA
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Publikationsdatum:
21. August 2009 (online)

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Significance

The Lautens rhodium-catalyzed ring opening of oxa- and aza-benzonorbornadienes A and H was used to synthesize libraries of 1-aminotetralin scaffolds which were screened against human opioid receptors. Compound G was a high-affinity selective µ-opioid receptor ligand.