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US 2026/0240957 A1Published application
Process of making abaloparatide
AssigneeRadius Health, Inc.
InventorsMatt Burke, Silvio Campagna
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Abstract
Disclosed herein is an improved process for preparing abaloparatide. The process generally utilizes solid phase peptide synthesis employing an Fmoc-protection scheme. Incorporating a systematic recoupling step of a glutamine residue (Gln16) has been found to minimize the formation of an undesirable des-Gln16 abaloparatide impurity, which is often obtained in significant quantities in the conventional process.
Claims1
A process for the preparation of abaloparatide comprising:
- a) providing a peptide bound to a solid resin and having an initial N-terminus, wherein said bound peptide is NH2-Asp(OtBu)-Leu-Arg(Pbf)-Arg20-(Pbf)-Arg(Pbf)-Glu(OtBu)-Leu-Leu-Glu25(OtBu)-Lys(Boc)-Leu-Leu-Aib-Lys30-(Boc)-Leu-His(Trt)-Thr(tBu)-Ala34-Rink Amide MBHA resin;
- b) coupling a carboxyl terminus of Fmoc-(Trt)Gln16-OH to the initial N-terminus of the bound peptide in the presence of a coupling reagent;
- c) repeating step b) to ensure complete incorporation of Fmoc-(Trt)Gln16;
- d) selectively cleaving the Fmoc group with a solution comprising an amine base to provide a peptide bound to a solid resin and having a new N-terminus.
1 more element
Dependencies are inferred from the claim text.