FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to an improved method for preparing 4-[(1,6-dihydro-6-oxo-2- pyrimidinyl)amino]benzonitrile of formula 
. 
wherein R is C1-4alkyl. The method consists in dealkoxycarbonylation of 4-oxo-1,6-dihydropyrimidinylcarboxylic acid (II) ester with added MX salt in the appropriate inert solvent, wherein M is a metal or ammonium or substituted ammonium, and X is an anion having the nucleophilic properties. The compound of formula (II) is new and can be prepared by the reaction of a guanidine derivative of formula (III) and alkoxymethylene malonic acid ester of the ester (IV) by the following scheme: 
.
The compound (I) prepared by said method is halogenated 
to prepare the compound (C) which is used in the reaction with the compound (B) to prepare E-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile (TMC278) showing antiviral action in case of HIV infection.
EFFECT: method enables producing the high-yield and high-purity end product.
14 cl, 2 ex
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