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Rapid, one-pot synthesis of α,α-disubstituted primary amines by the addition of Grignard reagents to nitriles under microwave heating conditions

✍ Scribed by Brian T. Gregg; Kathryn C. Golden; John F. Quinn; Hong-Jun Wang; Wei Zhang; Ruifang Wang; Francis Wekesa; Dmytro O. Tymoshenko

Publisher
Elsevier Science
Year
2009
Tongue
French
Weight
488 KB
Volume
50
Category
Article
ISSN
0040-4039

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✦ Synopsis

A series of a,a-disubstituted amines have been prepared in a simple and efficient one-pot procedure by the addition of Grignard reagents to a series of aliphatic, aromatic, and heteroaromatic nitriles. Key to this reported procedure is the unprecedented addition of the Grignard reagent to the nitrile under heating by microwave irradiation which both significantly improves reaction yields and reduces reaction times. In general, the Grignard addition reaction is complete within 5-10 min at 100 °C followed by rapid reduction with sodium borohydride to give the target amines.

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