The carbodiimide anions which were generated in situ from -cyano--aryl--toluenesulfonamides (NCTS) in the presence of the base participated in annulations that remain less reported to date. Herein, we have developed for the first time an efficient and environmentally friendly [4 + 2] annulation reaction of CF-substituted hetero-1,3-dienes with NCTS for the efficient synthesis of CF-substituted 4-1,3-oxazines and 2-aminopyrimidines under transition-metal-free conditions. The methodology demonstrates the advantages of readily available substrates, simple operation, good functional group tolerance, and broad substrate scope, providing a promising route to the synthesis of structurally diverse CF-substituted scaffolds. The products followed by simple transformations provide a facile route to .
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