title: Solid-phase total synthesis of polymyxin B1.
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.
authors.affiliation: Oncology Department, Novartis Institute of Biomedical Research, Summit, NY 07901-1398, USA. SUSHIL.SHARMA@PHARMA.NOVARTIS.COM
authors.forename: S K
authors.initials: SK
authors.lastname: Sharma
authors.forename: A D
authors.initials: AD
authors.lastname: Wu
authors.forename: N
authors.initials: N
authors.lastname: Chandramouli
authors.forename: C
authors.initials: C
authors.lastname: Fotsch
authors.forename: G
authors.initials: G
authors.lastname: Kardash
authors.forename: K W
authors.initials: KW
authors.lastname: Bair
mesh_terms: 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*
chemical_list: D011113:Polymyxins; C121746:polymyxin B(1); D011112:Polymyxin B