Abstract

An organocatalytic version of the inverse‐electron‐demand Diels–Alder (IEDDA) reaction of 1,3,5‐triazines was successfully developed. Hydrazine was used an effective organocatalyst for the direct IEDDA reaction of ketones with 1,3,5‐triazines. This reaction has an expanded substrate scope relative to other 1,3,5‐triazine IEDDA reactions and is also more operationally simple; thus, it is a succinct, economical, and green approach for the preparation of highly functionalized pyrimidines from readily available ketones.

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