| Budget Amount *help |
¥18,850,000 (Direct Cost: ¥14,500,000、Indirect Cost: ¥4,350,000)
Fiscal Year 2013: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2012: ¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2011: ¥10,140,000 (Direct Cost: ¥7,800,000、Indirect Cost: ¥2,340,000)
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| Research Abstract |
In this research project, we focused on the total synthesis of perophoramidine and caprazamycin B. Concerning perophoramidine, we have developed the SmI2-mediated cyclization of unsaturated lactams or amidines bearing a carbodiimide moiety as well as the dearomatizing conjugate addition to quinoline derivatives including a lactam or amidine, to construct a spirocyclic quaternary carbon center and a five-membered amidine ring. By using these original synthetic tools, total synthesis of dehaloperophoramidine was achieved. For the caprazamycin synthesis, we explored the organocatalyzed asymmetric syntheses of fatty acid side chains and hydroxyamino acids bearing a uridine. Furthermore, diazepanone rings were also synthesized by using an Au- or Pt-catalyzed hydroamidation or Mitsunobu reaction. As a result, we succeed in the introduction of the fatty acid side chain into a model compound bearing a diazepanone ring as well as the transformation into the protected caprazol derivative.
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