FIELD: chemistry.
SUBSTANCE: present invention relates to a method of producing montelukast of formula or its pharmaceutically acceptable salt or solvate, including a hydrate, in which a compound of formula , where R1 is selected from a group comprising (C1-C4)-alkyl, phenyl and phenyl which is mono- or disubstituted with a (C1-C4)-alkyl radical, is initially reacted with a cyanide of an alkali metal with formation and subsequent extraction of a compound of formula in form of a free base or its salt, and then optional hydrolysis of the obtained formula (III) compound with formation and subsequent extraction of a compound of formula from the reaction medium. Further, the formula (II) or formula (III) compound obtained at any of the preceding steps is hydrolysed to form montelukast of formula (I), and after that the formula (I) montelukast formed is optionally treated with a pharmaceutically acceptable base to obtain the corresponding salt. The invention also relates to compounds of formulae IV, , and salts of compounds of formula III.
EFFECT: new efficient method of producing montelukast currently used to treat asthma, inflammation and other diseases, from novel intermediate compounds which are obtained with high output.
20 cl, 23 ex
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Authors
Dates
2010-10-27—Published
2006-11-03—Filed