Patent ID: 8377891
Filing Date: 2013-02-19
Classification: A61K,C07K

Abstract:
1. A process for preparing octreotide of formula comprising the following steps: i) using H-Cys (Trt)-2-chlorotrityl resin as the starting material, coupling of various selected amino acid residues using coupling agent in polar aprotic solvent to give the straight chain peptide resin compound of formula 2 ii) cleaving the product of step i with a solution comprising of TFA in dichloromethane or acetic acid in dichloromethane to give straight chain peptide of formula 3 iii) coupling of threoninol to the C-terminal in the presence of benzotriazole to give linear protected octapeptide of the formula 4 iv) deprotecting the product of step iii with TFA, triisopropylsilane and water to give linear deprotected octapeptide with a yield >95% of formula 5 v) oxidizing the deprotected octapeptide of step iv at an acidic pH in the range of 2.5 to 6.5 in the presence of hydrogen peroxide to yield octreotide of formula 1; vi) purifying the crude octreotide of step v by chromatography to a purity of >99%; vii) converting the pure octreotide of step vi to acetate salt; viii) concentrating the acetate salt of octreotide of step vii and lyophilizing the same.