Convenient synthesis of a head-to-tail cyclic peptide containing an expanded ring

Citation
M. Cudic et al., Convenient synthesis of a head-to-tail cyclic peptide containing an expanded ring, TETRAHEDR L, 41(23), 2000, pp. 4527-4531
Citations number
16
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
41
Issue
23
Year of publication
2000
Pages
4527 - 4531
Database
ISI
SICI code
0040-4039(20000612)41:23<4527:CSOAHC>2.0.ZU;2-4
Abstract
Here we describe a rapid and efficient solid-phase synthesis of a 29-mer cy clic antibacterial peptide 1, currently under pharmaceutical development. T he linear peptide was assembled by standard Fmoc chemistry on an Fmoc-Asp(r esin)-ODmab carrier. Intramolecular on resin head-to-tail cyclization was e nabled after selective deprotection of the Asp alpha-carboxy protecting gro up with 2% hydrazine-DMF at room temperature. (C) 2000 Elsevier Science Ltd . All rights reserved.