The first cascade diastereoselective synthesis of oxazoloisoindolinones via the palladium-catalyzed decarboxylative ortho-acylation of N-benzoyl α-amino acid derivatives followed by double intramolecular cyclizations has been demonstrated. This reaction, using α-amino acids as directing groups and α-oxocarboxylic acids as the acylation source, features a broad substrate scope, good functional group tolerance, high regioselectivity, and excellent diastereoselectivity.

This study demonstrates a novel method for the synthesis of oxazoloisoindolinones using palladium-catalyzed decarboxylative ortho-acylation of N-benzoyl -amino acid derivatives and double intramolecular cyclizations

The Journal of organic chemistry

Diastereoselective Synthesis of Oxazoloisoindolinones via Cascade Pd-Catalyzed ortho-Acylation of N-Benzoyl α-Amino Acid Derivatives and Subsequent Double Intramolecular Cyclizations.

Paper

Diastereoselective Synthesis of Oxazoloisoindolinones via Cascade Pd-Catalyzed ortho-Acylation of N-Benzoyl α-Amino Acid Derivatives and Subsequent Double Intramolecular Cyclizations.

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