METHOD AND PROCESS OF PREPARATION AND PRODUCTION OF DEUTERATED OMEGA-DIPHENYLUREA Russian patent published in 2014 - IPC C07D213/81 C07C275/30 

Abstract RU 2527037 C2

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining N-(4-chloro-3-(trifluoromethyl)phenyl)- N'-(4-(2-(N-(methyl-d3)aminoformyl)-4-pyridyloxy)phenyl)urea or its pharmaceutically acceptable salts Method includes (a) reaction of compound III with compound V in inert solvent and in presence of base with formation of said compound where X represents Cl, Br or I. Compound III is obtained in the following way: (ii) reaction of p-methoxyaniline (X) with 4-chloro-3-trifluoromethylaniline (II) or 4-chloro-3-trifluoromethylphenylisocyanate (VIII) with formation of compound XI After that, compound XI is demethylated in acidic or alkaline conditions with formation of compound III. Also claimed are versions of method, intermediate compound, method of obtaining 4-chloro-pyridyl-2-(N-(methyl-d3))carboxamide, application of intermediate compound for obtaining deuterated ω-diphenylurea and p-toluolsulphonate 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)phenoxy)-N-(methyl-d3)picolinamide.

EFFECT: invention makes it possible to obtain compounds with inhibiting activity with respect to raf-kinase, which can be applied for treatment or prevention of tumour development.

13 cl, 3 dwg, 1 tbl, 9 ex

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RU 2 527 037 C2

Authors

Fehn Vehjdun

Gao Sjaojun

Daj Sjaotszjun'

Dates

2014-08-27Published

2011-03-17Filed