An efficient and tunable route to AG7088, a rhinovirus protease inhibitor |
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| Authors: | Dawei Ma Weiqing Xie Qiong Lei |
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| Affiliation: | a State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Lu, Shanghai 200032, China
b Department of Pharmacology, University of Minnesota, Minneapolis, MN 55455, USA |
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| Abstract: | Aldol reaction of N,N-dibenzyl valinal with propiolic acid ethyl ester derived lithium reagent provides anti-aminoalcohol 8 and syn-aminoalcohol 9, which are converted into the lactone 6 via two different routes. Alkylation of 6 followed by lactone ring opening afford the acid 2a, which is coupled with the amine 3 and 5-methylisoxazole-3-carboxylate acid 1, respectively, to deliver AG7088. |
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