Synthesis and Stabilities of 3-Borylated Indoles

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Al-Saedy, M.A.E. ; Harrity, J.P.A. (2016)
  • Publisher: Georg Thieme Verlag

We report herein that 3-pinacol boronic esters undergo facile protodeborylation in the presence of palladium catalysts and base, and this contributes significantly to the generation of nonborylated indole byproducts in the B2Pin2-mediated palladium-catalysed borylative cyclization of 2-alkynylanilides. Suginome’s reagent provides an alternative method to access 3-borylated indoles as these compounds are less susceptible to protodeborylation.
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