| 摘要 |
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 |
