METHOD FOR PRODUCTION OF TETRASUBSTITUTED IMIDAZOLE DERIVATIVES AND NEW CRYSTALLINE STRUCTURES THEREOF Russian patent published in 2006 - IPC C07D401/04 C07D213/51 

FIELD: organic chemistry.

SUBSTANCE: invention relates to method for production of tetrasubstituted imidazole derivatives of formula I , wherein R¹ represents phenyl optionally substituted with halogen atom or trifluorimethyl; R² represents heteroaryl, namely 5 or 6 membered monocyclic aromatic ring system containing one heteroatom, such as nitrogen; R³ represents hydrogen or aryl(C₁-C₅)-alkyl; R⁴ represents group of formula wherein p = 0-9, integer represents hydroxy; or pharmaceutically acceptable salts thereof. Claimed method includes reaction of compound of formula VIII , wherein L¹ and L² are independently C₁-C₄-alkyl and R¹ and R² are as mentioned above; with compound of formula X , wherein R³ has abovementioned meanings to produce respective compound of formula XI , wherein R¹, R², R³, R⁴, L¹ and L² have abovementioned meanings; cycling of XI in acidic conditions at pH approximately 7 to produce respective compound of formula XII , wherein R¹, R² and R³ have abovementioned meanings; reaction of XII with POBr₃ PBr₅ or mixture thereof to produce respective compound of formula XIII , wherein R¹, R² and R³ have abovementioned meanings; bromine substitution in XIII by reaction thereof with compound of formula XIV: H-R⁴ to produce respective compound of formula I. Method for production of intermediated and crystal form of compound of formula II also are disclosed.

EFFECT: new compound with p38 kinase inhibiting activity.

20 ck, 2 tbl, 12 ex