Asymmetric Synthesis of 1-Heteroaryl-1-arylalkyl Tertiary Alcohols and 1-Pyridyl-1-arylethanes by Lithiation-Borylation Methodology

作者：Watson Charlotte G; Aggarwal Varinder K^*

来源：Organic Letters, 2013, 15(6): 1346-1349.

DOI：10.1021/ol400289v

The synthesis of highly enantioenriched alpha-heterocyclic tertiary alcohols has been achieved via lithiation-borylation of a configurationally stable lithiated carbamate and heterocyclic pinacol boronic esters followed by oxidation. Protodeboronation of the alpha-heterocyclic tertiary boronic esters using TBAF center dot 3H(2)O or CsF gave highly enantioenriched 1-pyridyl-1-arylethanes in high er.

• 出版日期2013-3-15