Accessing Medicinally Relevant O-Benzofused Heterocycles through C-X Activation: Recent Trends

In this Review, we address the recent advances in the elaboration of medicinally relevant oxygen benzofused heterocycles by palladium and copper catalyzed C-X activation of halo arene precursors. This attractive transformation has shown remarkable versatility and efficiency as a synthetic toolkit leading to the construction of numerous scaffolds with high structural diversity in an atom-economical manner. We covered recent examples that considered the application of this strategy using miscellaneous coupling partners and conditions. The haloarene motif has proven to be an exceptional candidate principally due to its availability and cost, and in this review, we showcase relevant and appropriate examples of its use in catalytic reactions leading to medicinally important targets.

Automated summary

In this review, we discuss the recent advances in the synthesis of medicinally relevant oxygen benzofused heterocycles through the palladium and copper catalyzed C-X activation of haloarene precursors. This transformation has demonstrated remarkable versatility and efficiency, allowing for the construction of diverse scaffolds in a cost-effective manner. The haloarene motif, due to its availability and low cost, has emerged as an exceptional candidate for catalytic reactions leading to medicinally important targets.