)-H arylation / heteroarylation of free amines
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United States of America Patent
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Sep 1, 2020
Grant Date -
Aug 8, 2019
app pub date -
Oct 19, 2017
filing date -
Oct 24, 2016
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Abstract
Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
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