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A convenient one-pot Negishi coupling of amino-heteroaryl chlorides and alkyl bromides
Authors:Iain A.S. Walters
Affiliation:AstraZeneca R&D Charnwood, Medicinal Chemistry, Bakewell Road, Loughborough LE11 5RH, UK
Abstract:A simple Ni-catalysed cross-coupling protocol for amino-heteroaryl chlorides with alkylzinc reagents has been developed. The alkylzinc reagents can be commercially available dialkylzincs or alkylzinc halides, or can be conveniently generated in situ from diethylzinc and primary alkyl bromides in the presence of the same inexpensive Ni catalyst used to effect the subsequent coupling reaction.
Keywords:Negishi coupling   Nickel   Halogen-zinc exchange   Alkyl-aminopyrazine
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