SIMPLE METHOD OF PRODUCING PRECURSOR COMPOUND Russian patent published in 2016 - IPC C07B59/00 C07C227/18 C07C269/06 C07C303/28 

FIELD: pharmaceutics.

SUBSTANCE: invention relates to method of producing radiopharmaceutical precursors for positron emission tomography, specifically to method of producing compound of formula (II). Proposed method comprises steps (a)-(d). At step (a) debenzylation of compounds of formula Ia is carried out to obtain compound of formula Ib. Step (b) involves conversion of compound of formula Ib obtained directly at step (a), into compound of formula I, wherein above conversion is realised by reacting of said compound of formula Ib with suitable form of X, where said compound of formula I is obtained in amount of 100 g or more. At step (b) reacting of compound of formula I, obtained at step (b) is carried out with suitable source of ¹⁸F-fluoride to obtain compound of formula IIa. Step (d) involves removing protection from compound of formula IIa obtained at step (b) to remove R³¹ and R³². In said formulae x, v, w, n and y are an integer from 0 to 4; R¹¹, R²¹, R¹ and R³¹ represent C_1-5alkyl group with straight or branched chain; R¹², R²², R² and R³² represent amino-protective group; X is leaving group selected from halogen or group -O-SO₂-R³, where R³ represents halogen, C_1-10alkyl with straight-chain or branched chain, C_1-10haloalkyl with straight-chain or branched chain and C_6-10aryl.

EFFECT: proposed method allows to carry out process without cleaning substance obtained at debenzylation step, and is suitable for simple production of relatively large amounts of target product.

15 cl, 8 ex