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Rui Wang, Ping Tian and Guoqiang Lin Stereoselective Total Synthesis of Tubulysin V Chinese Journal of Chemistry 31

Article first published online: 11 DEC 2012 | DOI: 10.1002/cjoc.201200984

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The total synthesis of tubulysin V was accomplished in 1.0% overall yield with linear 13 steps. Our synthetic strategy featured the following two reactions. One is zinc-mediated aza-Barbier reaction of (R)-N-tert-butanesulfinyl imine 8 with β-ester group functionalized allylic bromide 9 to afford the chiral homo-allylic amine 7; the other is to employ the methodology of aqueous indium-mediated aza-Barbier reaction previously developed by our group, giving the chiral homo-allylic amine 13 with high efficiency.

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