Студенттер мен жас ғалымдардың «фараби әлемі» атты халықаралық ғылыми конференциясы

«Фараби Әлемі» атты студенттер мен жас ғалымдардың халықаралық конференциясы
44 
SYNTHESIS OF SOME AMINOPHOSPHONATES BASED ON 
PYRIMIDINYLPIPERAZINE 
 
 Bissenbay D.
1,2
, 
 
Ten A.Yu.
2
 
1
Al-Farabi Kazakh National University 
2
A.B. Bekturov Institute of Chemical Sciences 
 
didy_17@mail.ru

 
α -Aminophosphonates represent a fascinating class of molecules with unique properties and 
potential biological activities. They attract attention with their wide range of biological effects such 
as antibacterial, antiviral, also act as enzyme inhibitors, herbicides, antibiotics, antifungal and 
antitumor agents. 
In this work the pyrimidinyl piperazine molecule was chosen as the main pharmacophore 
center because it has a large biopotential and it is part of some drugs of various spectrum of action. 
In this regard, the purpose of this research is focused on the synthesis new aminophosphonates of 
pyrimidinyl piperazine and identifying new effective safe medicines among synthesized derivatives. 
For this purpose, under the conditions of a three-component (pyrimidinyl 
piperazine+anisaldehyde+diethylphosphite) "one-pot" Kabachnik-Fields reaction which is boiling 
in benzene using a Dean-Stark trap to remove the resulting water from the reaction mixture, three 
derivatives of aminophosphonates were obtained with a reaction time of 32-52 hours. At the end of 
the reaction, the benzene is evaporated. The target product is separated from incompletely reacted 
initial by column chromatography on Al
2
O
3
by elution with a mixture of chloroform:hexane (1:1), 
isolating the second fraction. The resulting aminophosphonates of pyrimidinyl piperazine are white 
and yellow crystals. 
The composition and structure of the synthesized derivatives are confirmed by the results of 
elemental analysis and spectral data. Also, virtual forecasts of their possible biological activity were 
carried out using the PASS online computer program and the SwissADME web tool. According to 
the forecasts of the former program, the compounds are more likely to have thrombolytic activity 
and can be used as anticoagulants and calcium regulators, as well as in the treatment of 
atherosclerosis, Parkinson's disease, in the treatment of stroke. According to the analysis of the 
latter one, they have useful therapeutic activity, an affinity for medicines, and low acute oral 
toxicity (for rats). 

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