METHOD OF PRODUCING 2-FLUORO-4-BORONO-L-PHENYLALANINE AND PRECURSOR OF 2-FLUORO-4-BORONO-L-PHENYLALANINE Russian patent published in 2018 - IPC C07C229/36 C07C251/24 C07C271/22 C07F5/02 C07F7/22 C07B59/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound represented by the formula 1:

[Formula 1] .

In formula 1 R¹ is a bromo group, an iodo group or a chloro group, R² represents Sn(R⁶)₃, N=N-NR⁷R⁸, (R^14-)I⁺R¹³ or boric acid (B(OH)₂) or a boric acid ester selected from the group consisting of pinacoline, 2,2-dimethyl-1,3-propanediol, N-methyldiethanolamine, 1,8-diaminonaphthalene, N-methyliminodiacetic acid, 1,1,1-tris-hydroxymethylethane and pyrocatechol, where R⁶ represents an alkyl group, having 1–7 carbon atoms, or a benzyl group, R⁷ and R⁸ are joined together by N to form a 3- to 7-membered cyclic structure, R¹³ is a C_1-6 alkyl-substituted phenyl group, C_1-6 alkoxy-substituted phenyl group or a phenyl group or a thienyl group, R¹⁴ is a halogen, a tetrafluoroborate group, a nitrate group, a triflate group, a sulphonyloxy group, a toluenesulphonyloxy group or a perchlorate group, R³ is hydrogen, an ethyl group, a tert-butyl group or a benzyl group, R⁴ or R⁵ independently represents hydrogen, a benzyloxycarbonyl group or a t-butoxycarbonyl group, or NR⁴R⁵ are bonded to form C₆H₅(C₆H₅)C=N. Method for producing a compound of formula 2 and a method for producing ¹⁸F-labelled BPA are also disclosed.

EFFECT: invention provides a novel derivative of BPA, which may be an intermediate for synthesis ¹⁸F-labelled BPA in good yield and in a state having a good specific activity.

5 cl, 6 ex