Journal
MOLECULES
Volume 27, Issue 23, Pages -Publisher
MDPI
DOI: 10.3390/molecules27238488
Keywords
acetylenes; amino acids; C-H activation; annulation; catalysis; isoquinolones
Funding
- Russian Science Foundation
- [21-13-00328]
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A convenient method has been developed for the synthesis of a new series of alpha-CF3-substituted alpha-amino acid derivatives bearing pharmacophore isoquinolone core. The method involves the [4+2]-annulation of N-(pivaloyloxy) aryl amides with orthogonally protected internal acetylene-containing alpha-amino carboxylates under Rh(III)-catalysis. The resulting annulation products can be easily transformed into valuable isoquinoline derivatives through a successive aromatization/cross-coupling operation.
A convenient pathway to a new series of alpha-CF3-substituted alpha-amino acid derivatives bearing pharmacophore isoquinolone core in their backbone has been developed. The method is based on [4+2]-annulation of N-(pivaloyloxy) aryl amides with orthogonally protected internal acetylene-containing alpha-amino carboxylates under Rh(III)-catalysis. The target annulation products can be easily transformed into valuable isoquinoline derivatives via a successive aromatization/cross-coupling operation.
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