New method achieves up to 98% yield of 3,4-dihydroquinazolinones using metal-free [4 + 2] cycloadditions with isocyanates, indicating a safer alternative to current techniques.
3,4‐dihydroquinazolin‐2( 1H )‐one (3,4‐DHQ) is a key structural motif found in many biologically active molecules. Although several synthetic methods have been developed to date, harsh reaction conditions, and/or metal toxic reagents are often required. In this work, a general, metal‐free methodology for the synthesis of 3,4‐DHQs is described. This novel protocol relies on a formal [4 + 2] cycloaddition of in situ formed aza‐ ortho ‐quinone methides and isocyanates leading to a wide variety of 3,4‐DHQs in yields up to 98%.
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Torres‐Oya et al. (2025) studied this question.
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