The total solid-phase synthesis of polymyxin B1 (PMB1) has been achieved in
20% yield using the orthogonal protecting group N-1-(4,4-dimethyl-2,6-diox
ocyclohexylidene)ethyl-(Dde). This report demonstrates that a complex pepti
de macrocycle can be synthesized in high yields using solid-phase synthesis
. According to MS and HPLC, the synthetic peptide was identical to the natu
rally occurring antibiotic.