| Summary: | 碩士 === 高雄醫學大學 === 醫藥暨應用化學系碩士在職專班 === 105 === An efficient method for the synthesis of 1-benzyl/arylindazole 2-oxides via a bis(dibenzylideneacetone)palladium(0) (Pd(dba)2)/tert-butyl nitrite (TBN)-catalyzed reaction of o-alkynylaniline derivatives with TBN is reported. The overall transformation involved the formation of three new bonds via N-nitrosation (N-NO), 5-exo-dig cyclization (C-N) and oxidation (C=O). The notable features were the mild reaction conditions, broad substrate scope and dual role of TBN as a NO source and redox co-catalyst. This strategy was implemented for the synthesis of indazole-3-carbaldehyde derivatives and the formal syntheses of pharmaceutically active YC-1, an anticancer agent (lonidamine), and the male contraceptive experimental drugs AF-2785 and adjudin (AF-2364).
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