創薬を指向した環境調和型有機金属触媒の開発とその応用

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  • Development of Environmentally Friendly Organometallic Catalysis for Drug Discovery and Its Application to Heterocyclic Chemistry
  • ソウヤク オ シコウシタ カンキョウ チョウワガタ ユウキ キンゾク ショクバイ ノ カイハツ ト ソノ オウヨウ

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  Two new catalysts, ruthenium hydride with a nitrogen-containing heterocyclic carbene (A) and an organopalladium catalyst supported on a sulfur-terminated semi-conductor, gallium arsenide (001) (B) were discovered. Both catalysts are environmentally benign, because A can yield indole derivatives with good atom economy, and B can catalyze the Mizoroki-Heck reaction more than 10 times with only trace amounts of leached palladium (ppb level). Substituted 1,2-dihydroquinoline, indole and 3-methylene-2,3-dihydroindole were also prepared selectively from the common starting material, N-allyl-o-vinylaniline, and catalyst by slight modification of the reaction conditions. These procedures address an important issue in diversity-oriented synthesis. These methods utility were demonstrated by application to biologically active natural products synthesis.<br>

収録刊行物

  • 薬学雑誌

    薬学雑誌 127 (9), 1383-1398, 2007-09-01

    公益社団法人 日本薬学会

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