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Journal ArticleDOI

Eine neue Methode zur Synthese von Peptiden: Aktivierung der Carboxylgruppe mit Dicyclohexylcarbodiimid unter Zusatz von 1‐Hydroxy‐benzotriazolen

Wolfgang König, +1 more
- 01 Mar 1970 - 
- Vol. 103, Iss: 3, pp 788-798
TLDR
In this article, the authors show that 1-Hydroxy-benzotriazol and 1-hydroxy-acetyl carbodiimid-methode eignen sich als Zusatze bei der Dicyclohexylcarbodiimids-Methode zur Synthese von Peptiden, verhindern die N-Acyl-harnstoffbildung and fuhren in hoher Ausbeute.
Abstract
1-Hydroxy-benzotriazol sowie verschiedene kernsubstituierte 1-Hydroxy-benzotriazole eignen sich als Zusatze bei der Dicyclohexylcarbodiimid-Methode zur Synthese von Peptiden. Ihr Einflus auf die Racemisierung bei Peptidsynthesen wurde unter Anwendung des gaschromatographischen Racemisierungstests von Weygand u. Mitarbb.2) untersucht. Die neuen Zusatze senken die Racemisierung, verhindern die N-Acyl-harnstoffbildung und fuhren in hoher Ausbeute zu sehr reinen Peptiden.

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Modulation of the activity and assessment of the receptor selectivity in a series of new RGD-containing peptides.

TL;DR: One of the short linear peptides investigated, in which the piperidine carboxylic group was attached to the N-terminus of KGDW, not only strongly inhibited platelet aggregation, but also selectively abolished cell adhesion mediated by GPIIb-IIIa without effect on the vitronectin receptor.
Journal ArticleDOI

Application of cyclic ketones in MCR: Ugi/amide coupling based synthesis of fused tetrazolo[1,5-a][1,4]benzodiazepines

TL;DR: Azido-Ugi reaction involving cyclic ketone, primary amine, isonitrile, and azide afforded substituted tetrazole derivatives 5. These intermediates were hydrolyzed to corresponding acid derivatives as discussed by the authors.
Journal ArticleDOI

Efficient approach to synthesis of two-chain asymmetric cysteine analogs of receptor-binding region of transforming growth factor-α

TL;DR: An approach to the synthesis of two-chain analogs containing an intermolecular disulfide linked A-chain and the 17-residue carboxyl fragment (C-fragment) possessing receptor-binding activity using the Boc-benzyl protecting group strategy is described.
Journal ArticleDOI

Synthesis of ribonucleoside 3′,5′‐cyclic phosphorothioates using a modified hydroxybenzotriazole phosphotriester approach

TL;DR: In this paper, a 3-5-dihydroxyl ribonucleosides with O-(2-chlorophenyl) O, O-bis[6-(trifluoromethyl)-1-benzotriazolyl] phosphorothioate, followed by addition of N-methyl-imidazole and removal of protecting groups, gives ribon nucleosides 3 −5−5−cyclic (3 −5 −cyclic) cyclic (cyclic).
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