A Convenient One-Pot Preparation of Disubstituted Phosphinic Acids Derived from Simple Amino Acids and Proline

Authors:
  • MBMarianne Borloo
    Marianne Borloo
  • XJXian-Yun Jiao
    Xian-Yun Jiao
  • HWHalina Wójtowicz
    Halina Wójtowicz
  • PRPadinchare Rajan
    Padinchare Rajan
  • CVChristophe Verbruggen
    Christophe Verbruggen
  • AHAchiel Haemers
    Achiel Haemers
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Abstract
A facile method for the preparation of both 2-pyrrolidinyl-substituted phosphinic acids and 1-aminoalkylphosphinic acids is described. Reaction of 1-pyrroline trimer or N-tritylalkanamine with bis(trimethylsilyl)phosphonite, followed by silylation with N,O-bis(trimethylsilyl)acetamide gives an intermediate which is used in a Michael addition reaction or an Arbuzov reaction.