4.7 Article

Kilogram-Scale Asymmetric Ruthenium-Catalyzed Hydrogenation of a Tetrasubstituted Fluoroenamide

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ADVANCED SYNTHESIS & CATALYSIS
卷 353, 期 18, 页码 3367-3372

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201100195

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amines; enantioselectivity; fluorine; high-throughput screen (HTS); homogeneous catalysis; hydrogenation; ruthenium; tetrasubstituted ss-fluoroenamides

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Ruthenium-catalyzed asymmetric homogeneous hydrogenation (AHH) is used as the key step of a multi-kilogram scale synthesis of an enantiomeric fluoropiperidine. The AHH of a tetrasubstituted beta-fluoroenamide is carried out under mild conditions using a Ru/Josiphos catalyst with high ee (98%).

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