FIELD: chemistry.
SUBSTANCE: invention relates to an improved method for producing ethambutol of formula
used in medicine as an anti-tuberculosis preparation. According to the invention, ethambutol is obtained from racemic 2-aminobutane-1-ol, the method includes protecting its amino group by reacting carboxybenzyl chloride in the presence of NaOH to obtain the N-carbobenzoxy derivative of 2-aminobutane-1-ol, which is stereoselectively acylated by hydroxy group with ethyl acetate, during catalysis by lipase PPL, by chromatography on silica gel. (S)-enantiomer is then recovered by reduction to obtain (S)-2-aminobutane-1-ol, which is alkylated with 1,2-dichloroethane to form the end product. Initial 2-aminobutane-1-ol is obtained by condensing paraform with 1-nitropropane and subsequent reduction of formed 2-nitrobutan-1-ol.
EFFECT: disclosed is an improved method for producing ethambutol.
1 cl, 5 ex
