Rapid Access to α-Alkoxy and α-Amino Acid Derivatives through Safe Continuous-Flow Generation of Diazoesters

Added on:
17 Jul, 2011

Microreactors: A highly efficient continuous-flow process has been developed for the synthesis of diazoesters from arylsulfonylhydrazones by means of in-flow Bamford–Stevens reactions. Furthermore, a range of α-alkoxy and α-amino acid derivatives have been prepared in excellent yields through rhodium(II)-mediated O[BOND]H and N[BOND]H insertions, without the need to isolate or handle the potentially hazardous diazo species (see scheme).

  • Hannah E. Bartrum1
  • David C. Blakemore2
  • Christopher J. Moody1
  • Christopher J. Hayes1
  • 1School of Chemistry, University of Nottingham, UK
  • 2Pfizer Global Research and Development, Sandwich, UK
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