Solid-phase synthesis of hydroxamic acid based TNF-alpha convertase inhibitors

Authors
Barlaam, B Koza, P Berriot, J
Citation
B. Barlaam et al., Solid-phase synthesis of hydroxamic acid based TNF-alpha convertase inhibitors, TETRAHEDRON, 55(23), 1999, pp. 7221-7232
Citations number
26
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON
ISSN journal
00404020 → ACNP
Volume
55
Issue
23
Year of publication
1999
Pages
7221 - 7232
Database
ISI
SICI code
0040-4020(19990604)55:23<7221:SSOHAB>2.0.ZU;2-Q
Abstract
An acid-sensitive linker for the solid phase synthesis of hydroxamic acids is described. Hydroxamic acid based TNF alpha inhibitors have been prepared by solid phase synthesis: derivatisation of N-2-[4-(N-oxyamino)-2R-isobuty l-3S-aminosuccinyl]-L-tert-leucine-N-1-methylamide grafted on Sasrin((R)) r esin and subsequent acidic cleavage afforded hydroxamic acids in good yield s and with good purity. (C) 1999 Elsevier Science Ltd. All rights reserved.