Synthesis of 4-Cyano Pyrroles via Mild Knorr Reactions with -Ketonitriles
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文摘
Mild methods for conducting Knorr chemistry with -ketonitriles were developed. This enabled the preparation of 4-cyano-penta-substituted pyrroles and gave access to -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptorpotentiators for biological evaluation. In addition, a series ofalkyl and aryl -ketonitriles were employed in Knorr cyclizations to probe steric tolerance and the possibility of directintroduction of aromatic moieties via Knorr chemistry.

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