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US 2022/0033440 A1Published application
An improved process for the preparation of plecanatide
AssigneeEnzene Biosciences Limited
InventorsSandip ADAK, Manoj BONTE, Chandrakant KULKARNI, Veeranarayana SWAMY, Nivrutti JOGDAND, Himanshu GADGIL
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Abstract
A process for the preparation of plecanatide. Specifically, an improved process for preparation of plecanatide using a non-linear solid phase peptide synthesis. In particular, the process for preparation of plecanatide involves solid phase synthesis of peptide fragments of five amino acid units using 2-chlorotrityl chloride (2-ClTrt) resin and eleven amino acid unit using Wang resin.
Claims17
1-16. (canceled)
A process for preparing plecanatide comprising the steps of:
- (a) Monocyclizing of a linear chain of formula (I), H2N-Asn1-Asp2-Glu3-Cys4-Glu5-Leu6-Cys(Acm)7-Val8-Asn9-Val10-Ala11-Cys12-Thr13-Gly14-Cys(Acm)15-Leu16-OH with a suitable reagent to obtain a monocyclic peptide of formula (VI),
- (b) purifying the monocyclic peptide of formula (VI) obtained in step (a) using reverse phase column chromatography,
- (c) dicyclizing the monocyclic peptide of formula (VI) obtained in step (b) with suitable reagents to obtain dicyclic peptide of formula (VII),
- and
- (d) purifying and desalting the dicyclic peptide of formula (VII) obtained in step (c) using reverse phase column chromatography to obtain pure plecanatide.
2 more elements
Dependencies are inferred from the claim text.