PRODUCTION OF F-FLUCYCLOWINE Russian patent published in 2018 - IPC C07B59/00 C07C227/16 C07C227/18 C07C227/20 C07C227/40 C07C269/06 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 1-amino-3-[¹⁸F]-fluorocyclobutanecarboxylic acid ([¹⁸F]-FACBC), which is used in the imaging of tumours by positron emission tomography. The process includes steps a) to e). In step a), a solid phase adsorbed compound of formula II is obtained, where PG¹ is a carboxy-protecting group and PG² is an amine-protecting group. In step b), the said adsorbed compound of formula II is reacted with an agent for removing the protective group PG¹. In step c), the agent for removing the protective group PG¹ is sent to waste after the indicated stage of interaction (b). In step d), the elution solution is passed through the said solid phase to obtain an eluted compound of formula III. In step e), the eluted compound of formula III obtained in step (d) is reacted with an agent for removing the protective group PG² to obtain a reaction mixture containing [¹⁸F]-FACBC. The invention also relates to systems and cassettes for carrying out the said method.

EFFECT: method makes it possible to simplify the purification, to remove soluble impurities from the reaction system, that are present in the solution used to remove the protection, and to improve the purity of the product obtained.

22 cl, 1 ex