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Chapter 1
Synthesis of functionalized pyrimidines
1.4. Current research work
The literature survey described above has demonstrated that the pyrimidine
derivatives possesses a variety of biological activity, among which are the analgesic,
antihypertensive, antipyretic, antiviral and anti-inflammatory activity. These agents
are also associated with nucleic acid, antibiotic, antimalarial and anti cancer drugs.
Many of the pyrimidine derivatives are reported to possess potential CNS depressant
properties. However, to our knowledge functionalized pyrimidines such as 4-
isopropyl-2,6-di-phenylsubstituted derivatives are less studied (Figure-48). The
tremendous biological potential of pyrimidine derivatives encouraged us to prepare
some novel highly functionalized pyrimidines bearing 4-isopropyl-2-6-disubstitutedphenylpyrimidine-5-carboxylate
functions.
R
O
N
O
R 1
N
ASM-4a-t
Figure-48
Herein we described a series of novel and efficient protocol for the synthesis
of diversely substituted pyrimidines. A series of chlorinated pyrimidines were
synthesized from easily available Biginelli 3,4-dihydropyrimidin-2(1H)-ones. The
chlorinated pyrimidines were subjected to the Suzuki-Miyaura coupling reactions
with various phenylboronicacid derivatives to obtain C-phenyl pyrimidines. The
newly synthesized compounds are characterized by IR, Mass, 1 H NMR, 13 C NMR
spectroscopy and elemental analysis.
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Department of Chemistry, Saurashtra University, Rajkot-360005 20