jo8b02509_si_002.cif (173.44 kB)
Diastereoselective Synthesis of Oxazoloisoindolinones via Cascade Pd-Catalyzed ortho-Acylation of N‑Benzoyl α‑Amino Acid Derivatives and Subsequent Double Intramolecular Cyclizations
dataset
posted on 2018-12-04, 00:00 authored by Kun Jing, Xiang-Nan Wang, Guan-Wu WangThe
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.