METHOD OF PRODUCING O-(2'-[F]FLUOROETHYL)-L-TYROSINE Russian patent published in 2016 - IPC C07C227/18 C07C229/36 C07B59/00 

FIELD: chemistry.

SUBSTANCE: invention relates to method of producing O-(2′-[¹⁸F]fluoroethyl)-L-tyrosine, which can be used in synthesis of radiopharmaceuticals for positron emission tomography. Proposed method is implemented in synthesis module with vessels for reagents, reaction vessel, capillaries and column with sorbent C18. Method involves nucleophilic fluorination of precursor Ni-(S)-BPB-(S)-TyrO-CH₂CH₂OX (X=Ms, Ts, Tf; BPB=[N-2-(N′-benzyl-prolyl)amino]benzophenone) in the presence of interphase catalyst in reaction vessel, hydrolysis of fluorinated precursor and cleaning of the end product by means of column with sorbent C18 to produce preparation and subsequent purification of module. Method is characterised by fact that final semi-finished product is further purified from residue formed during neutralisation of reaction mass after hydrolysis of fluorinated precursor by means of coarse and fine purification filters arranged between reaction vessel and column with sorbent C18. Cleaning of synthesis module is performed in two steps with removal of formed during synthesis nickel compounds and organic impurities using deionised water, acetonitrile and one molar hydrochloric acid at the first stage and trace amounts of water and hydrochloric acid by means of acetonitrile, deionised water and ethanol - at the second. At that given solutions are arranged in the module in eight vessels for reagents.

EFFECT: method enables to obtain end product with stable high radiochemical yield and high radiochemical and enantiomeric purity, as well as provides complete automation of synthesis.

3 cl, 3 dwg, 1 ex