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A highly enantioselective organocatalytic synthesis of piperidines is reported. The reaction is catalyzed by simple and commercially available secondary amines, affording the corresponding adducts with high yields and enantioselectivities. Moreover, this reaction is used for the formal synthesis of (−)-Paroxetine, a blockbuster drug, in only three steps.
The first examples of highly enantioselective organocatalytic Mannich reactions of ferrocenecarbaldehyde are disclosed. The reaction is catalyzed by simple amino acids and gives access to β-arylamino-β-ferrocenylketones in high yields and with up to 99% ee.
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