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In this chapter, we highlight several aspects concerning the hydroformylation reaction, including the mechanism of rhodium-catalyzed hydroformylation (still considered the “metal of choice” due to its high activity and selectivity), the development and evolution of new metal catalysts and phosphorus ligands in a historical perspective, some strategies related to the synthesis of reusable catalysts for use in alternative media and the utilization of less toxic solvents and alternative metals. Finally, a set of selected examples of the applications of catalytic hydroformylation in the synthesis of relevant synthons and drug intermediates is presented.

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