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Research demonstrates efficient aldol reactions in an eco-friendly manner, suggesting new pathways for synthesizing important pharmaceuticals.
By modifying Dixon's ligands, cinchona-derived amide adamantylphosphine ligands were synthesized. When combined with silver salts, these ligands enabled highly efficient asymmetric aldol reactions using isocyanoacetates as eco-friendly C-N synthons. The catalytic system operated under mild conditions with accelerated kinetics, affording chiral oxazolines in up to 99% ee and >99:1 dr. Broad substrate scope was demonstrated with both aryl and alkyl aldehydes, and the method enabled atom-economical synthesis of key intermediates for thiamphenicol and chloramphenicol.
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Jiang et al. (2026) studied this question.
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