Verbesserte Synthese von tert.-Butyloxycarbonyl-aminosäuren durch pH-Stat-Reaktion
作者:Eugen Schnabel
DOI:10.1002/jlac.19677020123
日期:1967.3.21
teilgeschützten Derivate mit tert.-Butyloxy-carbonylazid führt bei kontrolliertem pH in guten Ausbeuten zu den tert.-Butyloxycarbonyl-Derivaten. Auch sterisch gehinderte Aminosäuren reagieren glatt. Durch die Wahl der pH-Werte lassen sich die günstigsten Bedingungen für eine rasche und weitgehende Umsetzung bequem ermitteln.
1-(1-Adamantyl)-1-methylethoxycarbonyl (Adpoc) fluoride, a useful reagent for synthesis of a new class of protected amino-acids with advantageous properties for peptide synthesis
作者:Hubert Kalbacher、Wolfgang Voelter
DOI:10.1039/c39800001265
日期:——
Amino protection of amino-acids with the new, acid-labile Adpoc group is achieved by acylation with Adpoc fluoride, a very reactive and stable compound; the reagent allows the introduction of the Adpoc group under mild conditions and in high yields.
Novel conjugates of polysaccharides and uses thereof
申请人:Lapidot Aviva
公开号:US20060166867A1
公开(公告)日:2006-07-27
Novel conjugates composed of a saccharide-containing moiety (e.g., aminoglycosides) covalently linked to a moiety containing two or more basic amino acid residues (e.g., a polyarginine) and processes of preparing same are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses of these conjugates as antiviral and antibacterial agents.
[EN] DIPEPTIDYL PEPTIDASE INHIBITORS<br/>[FR] INHIBITEURS DE DIPEPTIDYLE PEPTIDASE
申请人:AIC
公开号:WO2004076433A1
公开(公告)日:2004-09-10
The present invention relates to novel inhibitors of serine type peptidases in general and of serine type dipeptidyl peptidases in particular. The present invention further relates to the use of the dipeptidyl peptidase inhibitors for selective inhibition of dipeptidyl peptidases. The present invention also relates to pharmaceutical compositions comprising these novel dipeptidyl peptidase inhibitors. The present invention further relates to the use of the novel inhibitors in therapy, diagnosis and research.
A tri-carbobenzoxy-arginine represented by the following formula (2):
is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof:
by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.