| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Outline of Final Research Achievements |
Ring-opening cyclization of spirocyclopropanes for the construction of a benzofuran skeleton was developed. The reaction of aryl-substituted spirocyclopropanes with acid catalysts proceeded smoothly to provide tetrahydrobenzofuran-4-ones in high yields. However, the reactions of non-substituted and electron-withdrawing group-substituted spirocyclopropanes using acid catalyst did not occur. After considerable experimentation, we found that iodide ion was an effective catalyst for these reactions.
We also developed the divergent synthesis of highly substituted indoles via the common synthetic intermediates tetrahydroindol-4-ones, which was prepared by the ring-opening cyclization of spirocyclopropanes with amines.
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