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Medchem & Toxicology 2018
Page 83
Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123
A n n u a l C o n g r e s s o n
Medicinal Chemistry,
Pharmacology and toxicology
J u l y 3 0 - 3 1 , 2 0 1 8
Am s t e r d a m , N e t h e r l a n d s
S
ubstituted pyrimidines are very important biologically and pharmaceutically active agents in the medicinal chemistry and drug
discovery processes. A multicomponent reaction (MCRs) is ideal synthetic strategy to construct diverse molecular scaffolds
of tetrazolopyrimidines starting from a few simple materials or intermediates. In connection with our continuous interest in
design of new efficient and green protocols of synthesis of new biologically active compounds, we developed sonochemical
approach for the one-pot four-component synthesis of 5-methyl-7-aryl-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylic esters,
obtained in the reaction of 2-cyano-guanidine, sodium azide, various aromatic aldehydes and methyl or ethyl acetoacetates in
the presence of a catalytic amount of new functionalized hybrid organic-inorganic nanoparticle magnetic metal oxide core shell
based catalyst Fe
2
O
3
@SiO
2
-(CH
2
)
3
NHC(O)(CH
2
)
2
PPh
2
. This is the first design, preparation, full characterization and application
of the present nanomaterial and also the first ultrasound irradiated synthesis of the biologically and pharmaceutically important
heterocyclic compounds in water used as a green solvent. The novel protocol offers several advantages such as high yields,
short reaction times, mild reaction conditions and environment friendly reaction media, easily isolation of the products, simple
preparation, and recoverability of the nanocatalyst by an external magnet and reusing several times without significant loss of
activity. The details of our studies, which describe a scope and generality of the one-pot, simple and high atom economy strategy
of synthesis of tetrazolopyrimidine derivatives with respect to various starting materials, will be presented
.
Oleh.Demchuk@UMCS.Lublin.plSynthesis of pharmaceutically active
tetrazolopyrimidines catalysed by new magnetic
nanoparticles
Oleg M Demchuk
1
, A Maleki,
2
J Rahimi,
2
and A Z Wilczewska
3
1
Maria Curie-Skłodowska University, Lublin, Poland
2
Iran University of Science and Technology, Tehran, Iran
3
University of Białystok, Białystok, Poland\
J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C3-009
Cat
.
( 5 mol%)
,
H
2
O
Cat
. :
Ultrasonic
irradiation
15
-
20 min ,
80
-
90%
Fe
2
O
3
O
O
O
Si
HN P
SiO
2
O
+
H
O
3
4
+
O
O
O
R
2
R
1
N
H
N
N
N
N
OR
2
O
R
1
1
2
NH
2
NH
2
N
N
NaN
3
+
5
Figure.
Synthesis of tetrazolo[1,5-a]pyrimidines