Asymmetric Synthesis of α-Aryl Amino Acids; Aryne-Mediated Diastereoselective Arylation
摘要:
An aryne-mediated alpha-arylation reaction of Schollkopf's bis-lactim ether is described. Arynes were generated via an ortho-lithiation approach, affording syn-arylated products in up to 94:6 dr with moderate to good yields and excellent regioselectivities. Hydrolysis provided a variety of substituted arylglycines containing a range of functional groups without racemization.
Asymmetric Synthesis of α-Aryl Amino Acids; Aryne-Mediated Diastereoselective Arylation
摘要:
An aryne-mediated alpha-arylation reaction of Schollkopf's bis-lactim ether is described. Arynes were generated via an ortho-lithiation approach, affording syn-arylated products in up to 94:6 dr with moderate to good yields and excellent regioselectivities. Hydrolysis provided a variety of substituted arylglycines containing a range of functional groups without racemization.
[EN] 2-AMINOHYDROQUINONE DERIVATIVE AND TAU AGGREGATION INHIBITOR<br/>[FR] DÉRIVÉ DE 2-AMINOHYDROQUINONE ET INHIBITEUR D'AGRÉGATION DE TAU<br/>[JA] 2-アミノヒドロキノン誘導体及びタウ凝集阻害剤