Tripeptide macrocyclic derivative as well as preparation method and application thereof

The invention provides a tripeptide macrocyclic derivative as well as an optical isomer, a pharmaceutically acceptable salt or a solvent compound thereof. A preparation method comprises the followingsteps: by taking a carboxyl protected compound as an initial raw material, condensation with an acid,...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: ZHOU YUBO, HU YONGZHOU, LI JIA, LI DAQIANG, HONG DUIDUI, DONG XIAOWU, XU LEI, ZHANG XIAOTUAN, LIU TAO, GAO LIXIN
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention provides a tripeptide macrocyclic derivative as well as an optical isomer, a pharmaceutically acceptable salt or a solvent compound thereof. A preparation method comprises the followingsteps: by taking a carboxyl protected compound as an initial raw material, condensation with an acid, performing olefin ring closing metathesis, removing carboxyl, condensing Boc protected amino acidwith an epoxy ketone segment, removing an amino protection group, and further condensing with an intermediate of which the carboxyl is removed, so as to obtain a target product. Experiments show thatthe derivative which has a completely novel framework and relatively good proteasome inhibition activity has a very good propagation inhibition function on multiple myeloma such as RPMI 8226, and MM.1S. The compound provided by the invention is easy in raw material obtaining, reasonable in route design, gentle in reaction condition, simple and convenient to operate and applicable to industrial production. The derivative is