Efficient and stereoselective synthesis of novel cis-4-substituted proline analogues |
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| Authors: | Junyi ZhangWei Wang Chiyi XiongVictor J Hruby |
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| Institution: | a Department of Chemistry, University of Arizona, 1306 E. University Boulevard, Tucson, AZ 85721, USA
b Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA |
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| Abstract: | A series of novel cis-4-substituted proline analogues were designed and synthesized. Highly stereoselective alkylations at the γ-position of glutamic ester 2 were achieved, followed by reduction, mesylation, and cyclization to afford the title compounds 1 in good yields and high diastereoselectivity. |
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| Keywords: | proline constrained amino acids alkylation |
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