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Ester linkage (s) is a key chemical connector in organic chemistry, including natural products, peptides, and synthetic polymers. We herein describe a straightforward method for the efficient formation of ester linkage (s) on solid‐phase. This method simply involves the use of amide coupling reagents under microwave irradiation. The robustness of this method relies on the use of classical solid‐phase...
Ohne die dreidimensionale Gesamtstruktur zu beeinflussen, hat eine Substitution von Amid‐ gegen Esterfunktionen im Molekülgerüst deutliche Auswirkungen auf das Konformationsgleichgewicht des RGD‐Cyclopeptids Cilengitid und seiner Derivate (siehe Bild; RGD=Arg‐Gly‐Asp). Die geeignete Substitution stabilisiert die Rezeptor‐komplementären Konformationen und verbessert die biologische Aktivität dieses...
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