Preparation of N(G)-substituted L-arginine analogues suitable for solid phase peptide synthesis.
A high-yielding and concise preparation of N(G)-substituted L-arginine analogues, suitably protected for use in solid phase peptide synthesis, is reported. The synthesis of each analogue employed an activated thiourea intermediate that was converted under mild conditions to the desired L-arginine analogue (10 examples, each in near quantitative yield). Subsequent allyl group removal provided each analogue in a form ideally suited for use in solid phase peptide synthesis.
Martin
Nathaniel I
NI
Department of Medicinal Chemistry & Chemical Biology, University of Utrecht, Sorbonnelaan 16 3584 CA Utrecht, The Netherlands. n.i.martin@uu.nl
Liskamp
Rob M J
RM