Process for preparation of liraglutide
AssigneeDr. Reddy's Laboratories, Inc.
InventorsSunil Kumar GANDAVADI, Sekhar NARIYAM MUNASWAMY, Karthik RAMASAMY, Rajiv Vishnukant THAKUR, Yagna Kiran Kumar KOMARAVOLU, Kishore Kumar MOVVA, Giri Babu NANDIVADA, Lavanya KOLA, Srinivas KATKAM
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Abstract
The present application relates to improved processes for the preparation of Liraglutide.
Claims11
A process for the preparation of Liraglutide comprising one or more of the following steps:
- a) introducing the spacer Nα-Palmitoyl-L-γ-glutamyl-OtBu on side chain NH2 of Lysine of fragment Fmoc-Lys(Alloc)-Glu(Otbu)-Phe-Ile-Ala-Trp(Boc)-Leu-Val-Arg(Pbf)-Gly-Arg(pbf)-Gly attached to solid support;
- b) coupling rest of the amino acid sequentially sequence from alpha amino group of Lysine of the fragment of Liraglutide obtained in step (a) to obtain Liraglutide attached to solid support;
- c) cleavage of Liraglutide from the solid support;
- d) optionally purifying the resulting Liraglutide.
A process for the preparation of Liraglutide, comprising one or more of the following steps:
- a) sequential coupling of the fragments Fmoc-Arg(pbf)-Gly-OH, Fmoc-Leu-Ala-Arg(Pbf)-OH, Fmoc-Ile-Ala-Trp(Boc)-OH, Fmoc-Glu(OtBu)-Phe-OH, Fmoc-Glu(OtBu)-Phe-OH, Fmoc-Lys-(Glu-(Palmitic Acid)-OH, Fmoc-Gly-Gln(Trt)-Ala-Ala-OH, Fmoc-Tyr(tBu)-Leu-Glu(OtBu)-OH, Fmoc-Val-SerSer(tBu)-Ser(tBu)-OH, Fmoc-Phe-Thr(tBu)-Ser(tBu)-Asp(tBu)-OH, Fmoc-Gly-Thr(tBu)-OH and Boc-His(Trt)-Ala-Glu(OtBu)-OH on Glycine that is already attached to solid support to obtain Liraglutide attached to solid support;
- b) cleavage of Liraglutide from the solid support;
- c) optionally purifying the resulting Liraglutide.
A process for the preparation of Liraglutide comprising introduction of the spacer Nα-Palmitoyl-L-γ-glutamyl-OtBu on side chain NH2 of Lysine of fragment Fmoc-Lys(Alloc)-Glu(Otbu)-Phe-Ile-Ala-Trp(Boc)-Leu-Val-Arg(Pbf)-Gly-Arg(pbf)-Gly.
Dependencies are inferred from the claim text.