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      The total synthesis of (+)-migrastatin.

      Journal of the American Chemical Society
      Antineoplastic Agents, chemical synthesis, Lactones, Macrolides, Piperidones, Stereoisomerism, Streptomyces, chemistry

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          Abstract

          The first total synthesis of (+)-migrastatin, a macrolide natural product with interesting antimetastatic properties, has been accomplished. Our concise and flexible approach utilizes a Lewis acid-catalyzed diene aldehyde condensation to install the three contiguous stereocenters and the trisubstituted (Z)-alkene of migrastatin. Construction of the two remaining stereocenters and incorporation of the glutarimide-containing side chain have been achieved via an anti-selective aldol reaction, followed by a Horner-Wadsworth-Emmons olefination. Finally, the assembly of the macrocycle has been realized by a highly (E)-selective ring-closing metathesis.

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          Author and article information

          Journal
          12785819
          10.1021/ja0349103

          Chemistry
          Antineoplastic Agents,chemical synthesis,Lactones,Macrolides,Piperidones,Stereoisomerism,Streptomyces,chemistry

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