SUBSTITUTED BENZIMIDAZOLES AND METHODS OF PREPARING Russian patent published in 2011 - IPC C07D401/14 

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to a method of preparing a compound of formula

or its tautomer, stereoisomer, or pharmaceutically acceptable salt, consisting in the fact that: (a) compound of formula

is introduced into a reaction with a compound of formula

to produce a compound of formula

, where Q means NO₂; one of L¹ or L² means halogen, and the other of L¹ or L² means OH or its anion; Z means a cyano group or COOR⁵ where R⁵ means hydrogen or a hydroxy-protecting group; (b) when in the compound of formula (IV), Z means a cyano group or COOR⁵, said compound is transformed into the compound of formula (IV) where Z means CHO; (c) when in the compound of formula (IV) Z means CHO, said compound is introduced into a reaction with a compound of formula

to produce a compound of formula (VI) where R^4p and R^4q in formula (Vb) mean independently H or C_1-6alkyl provided at least one of R^4p and R^4q means C_1-6alkyl, and X^b means =O or =NHOH; (d) when in the compound of formula

Q means NO₂, said compound is transformed into the compound of formula (VI) where Q means NH₂; (e) the compound of formula (VI) where Q means NH₂ is introduced into a reaction with a compound of formula

to produce the compound of formula (VIII) or its tautomer; (f) a compound of formula

or its tautomer is introduced into a reaction with a desulphating agent to produce the compound of formula (I); (g) optionally, the compound of formula (I) or its tautomer is introduced into a reaction with an to produce a first pharmaceutically acceptable salt; (h) optionally, the first pharmaceutically acceptable salt of the compound of formula (I) or its tautomer is transformed into a second pharmaceutically acceptable salt. Also, the invention refers to alternative methods of producing the compound of formula I.

EFFECT: new improved methods of producing the compound of formula I are implemented.

19 cl, 1 tbl, 82 ex