Solid-phase total synthesis of polymyxin B1
S K Sharma1, A D Wu, N Chandramouli
1Oncology Department, Novartis Institute of Biomedical Research, Summit, NY 07901-1398, USA. SUSHIL.SHARMA@PHARMA.NOVARTIS.COM
Abstract:
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-dioxocyclohexylidene)ethyl-(Dde). This report demonstrates that a complex peptide macrocycle can be synthesized in high yields using solid-phase synthesis. According to MS and HPLC, the synthetic peptide was identical to the naturally occurring antibiotic.
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