Facile synthesis of octahydrobenzo[h]isoquinolines: Novel and highly potent D1 dopamine agonists |
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Authors: | Lisa A Bonner Benjamin R Chemel Val J Watts David E Nichols |
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Institution: | Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907, United States |
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Abstract: | The octahydrobenzoh]isoquinoline scaffold is of interest as a conformationally-restricted phenethylamine that may be useful for constructing biologically active products. Surprisingly, however, no tractable synthesis of this ring system has been reported. We now describe a facile method for obtaining this framework, and illustrate that our approach is easily amenable to substitutions at the 5-position. Importantly, we demonstrate that the 7,8-dihydroxy-5-phenyl-substituted ligand is an extremely potent, high-affinity, full D1 dopamine receptor-selective agonist. |
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