- Facile solid phase synthesis of N-cycloguanidinyl-formyl peptides
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A novel strategy of solid phase synthesis of N-cycloguanidinyl-formyl peptides has been established and investigated which involved coupling orthogonal protected diaminoacid with resin bound peptide, α-amino group deprotection, guanidinylation of α-amino group by bis-Cbz-1H-pyrazole-1- carboxamidine followed by cleavage and cyclization in solution, and finally removing Cbz by palladium catalyzed hydrogenation. Through this method, cycloguanidine could be introduced to either N-terminus or sidechain of designated peptides. The reaction conditions were facile, straightforward, and totally adaptive to common solid phase peptide synthesis strategy.
- Yang, Xiaoxiao,Bai, Guoliang,Lin, Hao,Wang, Dexin
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supporting information
p. 1733 - 1735
(2014/03/21)
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