PREPARATION OF AND FORMULATION COMPRISING A MEK INHIBITOR Russian patent published in 2018 - IPC C07D235/06 

Abstract RU 2669391 C2

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to a process for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2- hydroxyethyoxy)-amide (Compound A), comprising a) reacting a compound of formula (I) with a suitable base followed by reacting an acid to form an intermediate of formula (V) and crystallizing an intermediate of formula (V); and b) reacting said intermediate of formula (V) with a compound of formula (II) in the presence of a coupling agent and a proton source to form a compound of formula (III) or a hydrate thereof, wherein P1 is t-butyl; c) deprotecting said compound of formula (III) or a hydrate thereof with a suitable deprotecting reagent in a suitable polar aprotic solvent, followed by reacting the deprotected compound with a suitable base to provide compound A. Invention also relates to an intermediate compound. Compound A, Formula (I), Formula (V), Formula (II), Formula (III).

EFFECT: process for preparing compound A having an improved purity profile with low levels of palladium is developed.

6 cl, 1 tbl, 5 ex

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RU 2 669 391 C2

Authors

Krell Kristof Maks

Misun Marian

Nedereer Daniel Andreas

Pakhinger Verner Khejnts

Volf Mari-Kristin

Tsimmermann Daniel

Lyu Vejdun

Stendzhel Piter Dzh.

Nikols Pol

Dates

2018-10-11Published

2013-10-18Filed