FIELD: chemistry.
SUBSTANCE: disclosed is a method of producing octreotide or pharmaceutically acceptable salts thereof, such as octreotide diacetate, in which a linear peptide sequence is synthesised automatically on a Rink polymer, modified with a N-Fmoc-threoninol-p-carboxybenzacetal linker, Fmoc-amino acid is activated with hydroxybenzotriazole/O-(benzotriazole-N,N,N,N-tetramethyluronium hexafluorophosphate)/diisopropyl-ethylamine (HOBt/HBTU/DIEA) in a dimethyl formamide medium, splitting from the polymer with simultaneous removal of all protective groups is carried out under the action of acid mixture and the completely deblocked linear octapeptide is oxidised using iodine.
EFFECT: high efficiency of the method.
2 cl, 1 ex
Title | Year | Author | Number |
---|---|---|---|
PROTECTED DERIVATIVES OF OCTREOTIDE | 2001 |
|
RU2196144C1 |
METHOD FOR THERAPEUTIC PEPTIDES SYNTHESIS | 2012 |
|
RU2625793C2 |
CYCLIC OCTAPEPTIDE, RADIOPHARMACEUTICAL AGENT BASED THEREON AND METHOD OF USING RADIOPHARMACEUTICAL AGENT TO PRODUCE MEDICINAL (PHARMACEUTICAL) AGENTS FOR TREATING NEOPLASMS EXPRESSING SOMATOSTATIN RECEPTORS | 2013 |
|
RU2528414C1 |
PROCESS FOR PREPARATION OF GLYCOPEPTIDE HAVING SIALYLATED SUGAR CHAIN, AND METHOD FOR PRODUCING SIALYL GLYCOASPARAGINE | 2012 |
|
RU2586524C2 |
METHOD FOR PRODUCING CYCLIC PEPTIDE-OCTREOTIDE | 2010 |
|
RU2435780C1 |
METHOD OF PRODUCING PEPTIDE | 2008 |
|
RU2478105C2 |
PEPTIDE FOR INHIBITING FRACTALKINE-STIMULATED MIGRATION OF MONOCYTIC CELLS | 2011 |
|
RU2461565C1 |
POLYPEPTIDES OR THEIR SALTS, PHARMACEUTICAL COMPOSITION SHOWING ANTIVIRAL ACTIVITY WITH RESPECT TO HUMAN IMMUNODEFICIENCY VIRUS | 1991 |
|
RU2073685C1 |
N-2-(4-NITROPHENYLSULFONYL)-ETHOXYCARBONYL-AMINO ACIDS AS N-PROTECTED AMINO ACIDS FOR SOLID PHASE SYNTHESIS OF PEPTIDES | 1995 |
|
RU2079491C1 |
ALPHA-CONOTOXIN PnIA ANALOGUE SHOWING HIGH AFFINITY AND SELECTIVITY TO ACETYLCHOLINE-BINDING PROTEIN FROM APLYSIA CALIFORNICA | 2011 |
|
RU2458068C1 |
Authors
Dates
2013-09-27—Published
2010-12-29—Filed