Synthesis of phosphinopeptides via the Mannich ligation.

  title={Synthesis of phosphinopeptides via the Mannich ligation.},
  author={Bonan Li and Shuzong Cai and Da-Ming Du and Jiaxi Xu},
  journal={Organic letters},
  volume={9 12},
Phosphinopeptides are a class of unnatural peptides containing a tetrahedral phosphorus atom and have potential for use as enzyme inhibitors. A series of phosphinopeptides were synthesized via the Mannich-type reaction of aryldichlorophosphines, aldehydes, and N-protected amino amides or peptide amides and subsequent aminolysis with amino esters or peptide esters. The current method named the Mannich ligation is an efficient route to synthesis of phosphinopeptides through convergent… CONTINUE READING

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