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Synthesis of novel HIV-1 protease inhibitors via diastereoselective Henry reaction with nitrocyclopropane |
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| Authors: | Michael L. Mitchell Lianhong Xu Zachary E. Newby Manoj C. Desai |
| Affiliation: | 1. Gilead Sciences, Inc., Department of Medicinal Chemistry, 333 Lakeside Drive, Foster City, CA 94404, United States;2. Gilead Sciences, Inc., Department of Structural Chemistry, 333 Lakeside Drive, Foster City, CA 94404, United States |
| Abstract: | Novel reaction and work-up conditions were developed for the unprecedented Henry reaction using nitrocyclopropane in the key step towards the synthesis of HIV-1 protease inhibitors. This procedure may find application in the preparation of diverse compounds of potential biological interest. |
| Keywords: | Henry reaction Nitro-aldol reaction Nitrocyclopropane HIV-1 protease inhibitor |
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