Solid-phase total synthesis of polymyxin B1.
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.
Sharma
S K
SK
Oncology Department, Novartis Institute of Biomedical Research, Summit, NY 07901-1398, USA. SUSHIL.SHARMA@PHARMA.NOVARTIS.COM
Wu
A D
AD
Chandramouli
N
N
Fotsch
C
C
Kardash
G
G
Bair
K W
KW
D002851:Chromatography, High Pressure Liquid; D013058:Mass Spectrometry; D008958:Models, Molecular; D011112:Polymyxin B / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D011113:Polymyxins / Q000031:analogs & derivatives*
D011113:Polymyxins; C121746:polymyxin B(1); D011112:Polymyxin B