IMPROVED PROCESS FOR THE PREPARATION OF SEMAGLUTIDE

Improved process for the preparation of Semaglutide having the structural formula (I).His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys (C18 di acid mono-t-butyl-γ-Glu(AEEA-AEEA)-OtBu)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH Formula-IThe present invention relat...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Hauptverfasser:	SHAIK, Kalesha, GANDAVADI, Sunil Kumar, BEGUM, Rehana, TELAKALA, Hema Sundara Rao, SHAIK, Mohammed Sharif, JUJJURI, Pavan Kumar, MOHAMMED, Khalid Anwer, SHAIK, Shavali, LAYEK, Mohosin, SIRIPRAGADA, Mahender Rao
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
Online-Zugang:	Volltext bestellen
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Improved process for the preparation of Semaglutide having the structural formula (I).His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys (C18 di acid mono-t-butyl-γ-Glu(AEEA-AEEA)-OtBu)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH Formula-IThe present invention relates to the following fragments which are useful in the preparation of Semaglutide.Fragment-1: Boc-His(X)-Aib-Glu(OtBu)-Gly-OH; wherein X is Boc or TrtFragment-2: Fmoc-Thr(tBu)-Phe-Thr(tBu)-Ser(tBu)-Asp(OtBu)-Val-Ser(Oxa)-OHFragment-3: Fmoc-Ser(tBu)-Tyr(tBu)-Leu-Glu(OtBu)-Gly-OHFragment-4: Fmoc-Gln(Trt)-Ala-Ala-Lys(PEG-PEG-γ-Glu-octadecane dioic acid)-Glu(OtBu)-Phe-Ile-Ala-Trp(Boc)-OHFragment-5: Leu-Val-Arg(pbf)-Gly-Arg(pbf)-Gly-OtBuFragment-6: H-Gln(Trt)-Ala-Ala-Lys(C18diacid mono-t-butyl-γ-Glu(AEEA-AEEA)-OtBu)-Glu (OtBu)-Phe-Ile-Ala-Trp(Boc)-Leu-Val-Arg(Pbf)-Gly-Arg(Pbf)-Gly-OtBuFragment-7: Boc-His(X)-Aib-Glu(OtBu)-Gly-Thr(tBu)-Phe-Thr(tBu)-Ser(tBu)-Asp (OtBu)-Val-Ser(Oxa)-OH; wherein X is Boc or TrtThe present invention also relates to novel fragment-4 which is useful in the preparation of Semaglutide.Fmoc-Gln(Trt)-Ala-Ala-Lys(C18 diacid mono-t-butyl-γ-Glu(AEEA-AEEA)-OtBu)-Glu (OtBu)-Phe-Ile-Ala-Trp(Boc)-OH (fragment-4)