Scheme 3.
Synthesis of cystathionine-containing compstatin analogues 2, 3 and 5.a,b
a Reagents and conditions: a) SPPS; b) Pd(PPh3)4, PhSiH3, DMF; c) piperidine, DMF; d) PyBOP, HOAt, iPr2EtN, DMF; e) CF3CO2H, H2O, iPr3SiH, HS(CH2)2SH. b An asterisk indicates standard Fmoc-orthogonal side chain protection: Gln(Trt), Asp(OtBu), Trp(Boc), His(Trt), Arg(Pbf), Thr(tBu).
