A facile and regioselective synthesis of rimonabant through an enamine-directed 1,3-dipolar cycloaddition |
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| Authors: | Sean R Donohue Christer Halldin |
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| Institution: | a Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Building 10, Rm B3 C346A, 10 Center Drive, Bethesda, MD 20892, USA
b Karolinska Institutet, Department of Clinical Neuroscience, Psychiatry Section, Karolinska Hospital, S-17176 Stockholm, Sweden |
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| Abstract: | Rimonabant is a high-potency cannabinoid type-1 (CB1) receptor inverse agonist that has recently been approved in the European Union as a treatment for obesity. Current methods of synthesis require several steps that have long reaction times and/or lack regioselectivity. Here we present a novel, regioselective synthesis of rimonabant though an enamine-directed 1,3-dipolar cycloaddition. In addition, we present a new and more reactive hydrazonoyl halide for the generation of the requisite nitrile imine dipole. |
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| Keywords: | CB1 Receptor 1 5-Diarylpyrazole Rimonabant 1 3-Dipolar cycloaddition |
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