Design of Phosphorus Ligands with Deep Chiral Pockets: Practical Synthesis of Chiral β-Arylamines by

来源 :The 24th International Society of Heterocyclic Chemistry Con | 被引量 : 0次 | 上传用户:lnfssg
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Chiral β-arylamines exist in numerous biologically interesting natural products and therapeutic agents.They also serve as pivotal structural units for many active pharmaceutical ingredients.We have successfully developed a novel C2-symmetric P-chiral bisphosphorus ligands WingPhos with a deep and well-defined chiral pocket that have shown high efficiency in rhodium-catalyzed asymmetric hydrogenation of (E)-β-aryl-N-acetyl enamides, cyclic β-arylenamides, and heterocyclic β-arylenamides.A series of chiral β-arylisopropylamines, 2-aminotetralines, and 3-aminochromans can be synthesized in excellent ee values at high s/c ratios (up to 10,000 TON).
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