Direct aminoalkylation of arenes and hetarenes via Ni-catalyzed Negishi cross-coupling reactions.
A direct room-temperature Ni-catalyzed cross-coupling of aminoalkylzinc halides, readily available from the corresponding aminoalkyl chlorides via Grignard reagents, with aryl and hetaryl electrophiles, allows a convenient one-step preparation of aminoalkyl (het)arenes, bearing a basic tertiary nitrogen in the side chain, including piperidine and tropane derivatives. Such aminoalkylarene scaffolds are widely present in various biologically active molecules.
Department Chemie und Biochemie, Ludwig-Maximilians-Universität München, Butenandtstrasse 5-13, Haus F, 81377 München, Germany.
Laurin
L
Melzig
Andrey
A
Gavryushin
Paul
P
Knochel
D000478:Alkylation; D002384:Catalysis; D009532:Nickel / Q000737:chemistry*
D009532:Nickel