6533b837fe1ef96bd12a1cfc

RESEARCH PRODUCT

ChemInform Abstract: Synthesis of 1,2-Disubstituted Indoles from α-Aminonitriles and 2-Halobenzyl Halides.

Anne-katrin BachonTill Opatz

subject

Primary (chemistry)DeprotonationChemistryIntramolecular forceHalidechemistry.chemical_elementGeneral MedicineMedicinal chemistryCopper

description

The α-alkylation of deprotonated Strecker products derived from primary amines and aromatic aldehydes with 2-halobenzyl halides furnishes intermediates that can be cyclized to 1,2-disubstituted indoles in moderate to high yields (up to 94% over two steps) by microwave-assisted copper- or palladium-catalyzed intramolecular cross-coupling.

https://doi.org/10.1002/chin.201629146