The Efficient Total Synthesis of Bioactive Microbial Natural Products.

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  • Sunazuka Toshiaki
    School of Pharmaceutical Science, Kitasato University Research Center for Biological Function, The Kitasato Institute

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  • 微生物由来生物活性天然物の効率的な全合成
  • ビセイブツ ユライ セイブツ カッセイ テンネンブツ ノ コウリツテキ ナ ゼンゴウセイ

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Abstract

We have been working on finding new bioactive microbial metabolites at the Kitasato Institute. Their microbial natural products have a variety of unique and complex skeletones with many chiral centers and functional groups, and biological activities. We also have been working on total synthesis of them, which is effective and concise convergent approach, designed to afford easy access to both the natural products and a variety of analogs to clarify the structure-activity relationships. We have succeeded the efficient total syntheses of bioactive microbial metabolites; pyripyropene A (1) and E, arisugacin (2), paspalicine (3) and paspalinine (4), lactacystin (5), macrosphelide (6), and madindoline (7). We also have succeeded to create better analogs of pyripyropene A (1) and lactacystin (5).

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