Asymmetric Synthesis of alpha-Aryl Amino Acids; Aryne-Mediated Diastereoselective Arylation

作者:Jones Elizabeth P; Jones Peter; Barrett Anthony G M*
来源:Organic Letters, 2011, 13(5): 1012-1015.
DOI:10.1021/ol1030469

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.

  • 出版日期2011-3-4