METHOD OF PRODUCING 5-FLUORO-L-DOPA Russian patent published in 2024 - IPC C07C227/12 C07C229/36 C07C227/28 C07C227/32 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: present invention relates to chemistry and pharmaceutics, to production of fluorine-containing amino acids, specifically to a method of producing 5-fluoro-L-DOPA (5-fluoro-L-3,4-dihydroxyphenylalanine). Method involves producing 3-fluoro-L-tyrosine from 2-fluorophenol, pyruvic acid and ammonia with the participation of the enzyme tyrosine phenol lyase from Citrobacter freundii, nitration of 3-fluoro-L-tyrosine with concentrated nitric acid, which gives 5-nitro-3-fluoro-L-tyrosine, reduction of the latter with tin in hydrochloric acid to 5-amino-3-fluoro-L-tyrosine, reaction of 5-amino-3-fluoro-L-tyrosine with barium nitrite in sulfuric acid while cooling with ice in the presence of CuSO₄ in an inert gas medium and subsequent hydrolysis of the obtained diazo compound to form 5-fluoro-L-DOPA.

EFFECT: providing a method for synthesis of the end product in mild conditions with high stereoselectivity and high output.

1 cl, 4 ex