Development of environmentally benign organometallic catalysis for drug discovery and its application.
We have developed a novel organometallic catalysis and applied it to drug discovery. Two new catalysts were found, ruthenium hydride with a nitrogen-containing heterocyclic carbene (A) and an organopalladium catalyst supported on a sulfur-terminated semiconductor, gallium arsenide (001) (B). 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). We also describe our synthetic study of nitrogen-containing heterocycles using ring-closing metathesis (RCM), such as chiral bicyclic lactams, azacycloundecenes, axially chiral macrolactams, 1,2-dihydroquinolines and indoles, including the development of silyl-enol ether ene metathesis, selective isomerization of terminal olefin, enamide metathesis and cycloisomerization and its application to the syntheis of 4 natural products, (-)-coniceine, (S)-pyrrolam A, angustureine, and fistulosin.
Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan.
Mitsuhiro
M
Arisawa
D000818:Animals; D002384:Catalysis; D015195:Drug Design; D004787:Environmental Pollution / Q000517:prevention & control*; D006801:Humans; D009942:Organometallic Compounds / Q000737:chemistry*; D010946:Plants, Medicinal / Q000737:chemistry; D017975:Ruthenium Compounds / Q000737:chemistry
D009942:Organometallic Compounds; D017975:Ruthenium Compounds