Synthesis of integerrimide A by an on-resin tandem Fmoc-deprotection-macrocyclisation approach.

@article{Kumarn2013SynthesisOI,
  title={Synthesis of integerrimide A by an on-resin tandem Fmoc-deprotection-macrocyclisation approach.},
  author={Sirirat Kumarn and Nitirat Chimnoi and Somsak Ruchirawat},
  journal={Organic & biomolecular chemistry},
  year={2013},
  volume={11 44},
  pages={7760-7}
}
A solid-phase total synthesis of integerrimide A (1) is reported. This work employs a safety-catch linker which enables head-to-tail cyclisation of the required linear peptide 6 as a method of cleaving the peptide from the solid support, and highlights a new tandem approach to direct macrocyclisation. It provides access to useful quantities of 1 in 16 steps and 19% overall yield, based on the manufacturer's stated resin substitution from commercially available materials, and also verifies the… CONTINUE READING