METHOD OF PRODUCING DERIVATIVES OF N2-ALKYL- AND N2,N2-DIALKYLISOCYTOSINE Russian patent published in 2018 - IPC C07D239/47 C07D413/04 C07D401/04 

FIELD: chemistry.

SUBSTANCE: present invention relates to the chemistry of heterocyclic compounds, particularly to a process for the preparation of new functional isocytosine derivatives that are bioisosteric analogs of non-nucleoside reverse transcriptase inhibitors of HIV. Technical result is achieved in a process for the preparation of N²-alkyl- and N²,N²dialkylisocytosine of general formula derivatives: , where R=H, R'=c-C₅H₉, 4-CH₃OC₆H₄CH₂, C₆H₅(CH₂)₃, 1-AdCH₂; R+R'=(CH₂)₅, (CH₂CH₂)₂O, by boiling 2-butoxy-6-[1-(2,6-difluorophenyl)cyclopropyl]-5-methylpyrimidin-4(3H)-one or 2-methoxy-6-[1-(2,6-difluorophenyl)cyclopropyl]-5- methylpyrimidin-4(3H)-one with an amine selected from the group of cyclopentylamine, 4-methoxybenzylamine, 3-phenylpropan-1-amine, (adamantane-1-yl)methanamine, piperidine or morpholine, taken in the molar ratios of pyrimidinone:amine=1:5–19.3, in a 1-butanol medium, taken in a volume ratio to an amine of 10:3–5, allows the desired products to be obtained in high yield and purity.

EFFECT: technical result is an increase in the yield of the target compounds, along with simplification of the process of their preparation and isolation in pure form.

1 cl, 12 ex