METHOD OF PRODUCING NONAPEPTIDES Russian patent published in 2016 - IPC C07K1/04 C07K7/06 A61K38/08 A61P7/10 

Abstract RU 2592282 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a solid-phase method of producing nonapeptides of the following formula I-III: R - A r g 1 - L y s 2 - L y s 3 - T y r 4 - L y s 5 - T y r 6 - A r g 7 - X a a 8 - L y s 9 - N H 2 , where R=H, Xaa=L-Arg (I); R=Me, Xaa=L-Arg (II); R=H, Xaa=D-Axg (III). Nonapeptides synthesis as per formula I-III is carried out by serial growth of the peptide chain, starting with the C-terminal amino acid covalently bound with the polymer matrix using Nα-protected derivatives of arginine, for blocking the guanidine function of which protonating is used. For the guanidine function protonation 1-hydroxybenzotriazole, hexafluorophosphate or tetrafluoroborate is used. Obtained nonapeptidilpolymer is processed with an unblocking agent for removing the protective groups and the polymeric matrix and in 1 stage the end product is given out by means of HELC.

EFFECT: method increases the output of end products, simplifies and lowers the cost of their production process.

4 cl, 5 dwg, 5 tbl, 3 ex

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Authors

Azmuko Andrej Andreevich

Arzamastsev Evgenij Veniaminovich

Baldin Mikhail Ivanovich

Kapelko Valerij Ignatevich

Kudryavtseva Elena Vitalevna

Molokoedov Aleksandr Sergeevich

Ovchinnikov Mikhail Vladimirovich

Samovilova Nelya Nikolaevna

Sidorova Mariya Vladimirovna

Shirinskij Vladimir Pavlovich

Dates

2016-07-20Published

2015-06-19Filed