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US 2019/0055278 A1Published application
Process for the preparation of guanylate cyclase 2c agonist
AssigneeCipla Limited
InventorsDharmaraj Ramachandra RAO, Geena MALHOTRA, Venkata Srinivas PULLELA, Parag Shankar KURLE, Rakesh MENDHE
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Abstract
The present invention relates to an improved process for the preparation of Linaclotide of Formula I. The process disclosed in the present invention is simple, economical and eco-friendly with reduced reaction times.
Claims20
1) A process for the preparation of Linaclotide of Formula I,
- the said process comprising;
- a) elongation of a peptide with sequential addition of amino acids by solid phase synthesis to obtain a protected peptide resin;
- b) cleaving and deprotecting the resin simultaneously to obtain the linear Linaclotide of Formula (II);
- 1 2 3 4 5 6 7 8 9 10 11 12 13 14
- H-Cys-Cys-Glu-Tyr-Cys-Cys-Asn-Pro-Ala-Cys-Thr-Gly-Cys-Tyr-OH
- Formula (II)
- c) oxidizing the linear Linaclotide of Formula (II) to obtain Linaclotide of Formula (I).
4 more elements
4) The process according to any of the preceding claims, for the preparation of protected peptide resin, which comprises the following steps, a) cleavage of Fmoc −group from F-moc protected amino acids to obtain fragments;
- and b) coupling of fragments by a solid phase synthesis to obtain a protected peptide resin.
Dependencies are inferred from the claim text.