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Palladium-Catalyzed Regio- and Stereoselective Synthesis of Aryl and 3-Indolyl Substituted-4-Methylene- isoquinolin-1(2H)-ones [post]

Valeria Nori, Antonio Arcadi, Armando Carlone, Fabio Marinelli, Marco Chiarini
2020 unpublished
Cascade cyclocarbopalladation of the readily available aryl/alkyl-substituted propargylic amides containing an aryl iodide moiety, followed by Suzuki-Miyaura coupling with arylboronic acids, allowed an efficient regio- and stereoselective synthesis of tetrasubstituted-4-methylene-isoquinolin-1(2H)-ones. Moreover cascade cyclocarbopalladation, followed by reaction with 2- alkynyltrifluoroacetanilides, accomplished a double cyclization, to afford challenging 4-methylene-isoquinolin-1(2H)-ones
more » ... olin-1(2H)-ones bearing a 3-indolyl substituent, through aminopalladation/reductive elimination
doi:10.3762/bxiv.2020.8.v1 fatcat:m7wnaqlpufhqvkr73eitd4ebru