METHOD FOR SYNTHESIS OF 5-(METHYL-1H-IMIDAZOL-1-YL)-3-(TRIFLUOROMETHYL) BENZAMIDE Russian patent published in 2012 - IPC C07D401/04 

FIELD: chemistry.

SUBSTANCE: invention relates to versions of an improved method for synthesis of 5-(methyl-1H-imidazol-1-yl)-3-(trifluoromethyl) benzamide of formula (I), for example compound (1a). The obtained compounds can be used to treat neoplastic diseases such as leukaemia. The method involves reaction of a compound of formula (II)

,

with 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)benzamine of formula (IVa):

, .

R1 denotes 5-(4-methyl-1H-imidazol-1-yl)-3-(trifluoromethyl)phenyl; R2 denotes hydrogen; R4 denotes hydrogen, lower alkyl or halogen; and R3 denotes lower alkyl, phenyl, phenyl-lower alkyl or substituted phenyl. The reaction takes place in an organic solvent in the presence of a base as a catalyst, selected from a group comprising a metal hydride, (volumetric) alkyllithium, metal alkoxide, metal bis-(trimethylsilyl)amide and lithium dialkylamide.

EFFECT: method simplifies synthesis of desired products by excluding expensive compounds and obtaining products with stable high output.

5 cl, 4 dwg, 1 ex