Fast and selective synthesis of novel cyclic sulfamide HIV-1 protease inhibitors under controlled microwave heating |
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| Authors: | Henrik Gold Lotta Vrang Anders Karlén Mats Larhed |
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| Institution: | a Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, Uppsala University, Uppsala Biomedical Centre, PO Box-574, SE-75123 Uppsala, Sweden
b Medivir AB, Lunastigen 7, SE-141 44 Huddinge, Sweden |
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| Abstract: | A novel and highly selective silver-promoted monobenzylation method was developed to promote synthesis of nonsymmetrical sulfamide-based HIV-1 inhibitors. Microwave-accelerated palladium-catalyzed N-amide arylation- and aminocarbonylation reactions were employed for rapid and reliable compound generation. With this class of inhibitory agents, six active inhibitors were identified, the most potent inhibitor possessing a Ki-value of 20 nM. |
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| Keywords: | Microwave Aminocarbonylation Goldberg HIV-1 protease inhibitor |
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