分子構造特性を基盤とする新反応の開発並びに薬学的応用研究
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The author and his group have been developing new reactions based on molecular structure characteristics; σ-symmetric bifunctional molecules, dipole-dipole repulsion, active amide structures, latent active species, orbital-orbital interactions, nonbonded interactions, strained structures, allenic structures, etc. Various new reactions such as asymmetric aminolyses and Dieckmann-type cyclizations of prochiral σ-symmetric dicarboxylic diamides, asymmetric aldol-type reactions onto γ-hydroxybutenolides and asymmetric imine alkylations onto ω-acetoxy lactams using chiral Sn(II)enolates, asymmetric Pummerer-type reactions, cascade reactions and endo-mode cyclizations exploiting α, β-unsaturated allenic esters and ketones, base- and palladium-promoted ring-expansion reactions, and syntheses of α-substituted serines and 1-azabicyclo[1.1.0]butane have been achieved. These new reactions were applied to the synthetic development of new seed and lead compounds(SH-enzyme inhibitors, tumor inhibitors, and antibiotics)with the aim of synthesizing new drugs. Asymmetric syntheses of(+)-Prelog-Djerassi lactonic acid methyl ester, (+)-carbacyclin, ISP-I(myriocin), (+)-conagenin, Geissman-Waiss lactone, biapenem(a new carbapenem antibiotic), thienamycin-like γ-lactam, and bicyclic alkaloids were also achieved by utilizing these reactions. Evaluation and molecular design of the seed and model compounds for angiotensin II receptor antagonists, tumor inhibitors, and antibiotics have been investigated on the basis of QRSA and/or nonbonded S…X(X=O, N, S, halogens)interaction concepts.
- 2002-01-01
著者
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