The treatment of N-alkyl-5,7-dibromoisatin derivatives through the copper-catalyzed sequential processes consisting of intra/intermolecular alkoxylation/amination or double alkoxylation provided the pyrrolo[1, 2,3-de]-1,4-benzoxazine derivatives. Moreover, the alkoxylation/arylation process proceeded in a one-pot fashion under tandem copper-palladium catalysis affording 5-(hetero)aryl substituted hetero-tricyclic systems. Biological evaluation of the synthesized compounds showed antiproliferative activity on the low micromolar range.
Copper-Catalyzed Alkoxylation as Key Step to Convert Isatin to Oxazinoindol-2-one Derivatives
Broggini, Gianluigi;
2018-01-01
Abstract
The treatment of N-alkyl-5,7-dibromoisatin derivatives through the copper-catalyzed sequential processes consisting of intra/intermolecular alkoxylation/amination or double alkoxylation provided the pyrrolo[1, 2,3-de]-1,4-benzoxazine derivatives. Moreover, the alkoxylation/arylation process proceeded in a one-pot fashion under tandem copper-palladium catalysis affording 5-(hetero)aryl substituted hetero-tricyclic systems. Biological evaluation of the synthesized compounds showed antiproliferative activity on the low micromolar range.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.