Scope of the organocatalysed asymmetric reductive amination of ketones with trichlorosilane
Francois‐Moana Gautier, Simon D. Jones, Xianfu Li, Stephen John Martin
Abstract
Francois‐Moana Gautier, Simon D. Jones, Xianfu Li, Stephen John Martin
Abstract
A highly active organocatalyst has been shown to affect the asymmetric reductive amination of ketones producing both aromatic and aliphatic amines. At 1 mol% catalyst loading, a series of structurally diverse chiral amines were quickly and economically prepared with good enantioselectivity and generally useful yield. The efficient synthesis of the calcimimetic (+)-NPS R-568 (67%, 89% ee) demonstrated the synthetic applicability of this methodology.
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A highly active organocatalyst has been shown to affect the asymmetric reductive amination of ketones producing both aromatic and aliphatic amines. At 1 mol% catalyst loading, a series of structurally diverse chiral amines were quickly and economically prepared with good enantioselectivity and generally useful yield. The efficient synthesis of the calcimimetic (+)-NPS R-568 (67%, 89% ee) demonstrated the synthetic applicability of this methodology.
Key concepts: Trichlorosilane, Chemistry, Reductive amination, Amination, Yield (engineering), Catalysis, Scope (computer science), Combinatorial chemistry