Convenient Synthesis of Polyaza-2-(heteroaryl)pyridine Derivatives
Vo l 5 5
Ghada S. Masaret
Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, Mecca, Saudi Arabia
Received August 13, 2017
Published online 10 January 2018 in Wiley Online Library (wileyonlinelibrary.com).
A simple and efﬁcient method for the synthesis of new heterocyclic compounds containing pyridine and
1,3-pyrimidine units has been developed. It is based on the reaction of the appropriate enaminone with some
J. Heterocyclic Chem., 55, 610 (2018).
Enaminones are chemical compounds consisting of an
amino group linked through a C═C to a carbonyl group.
They are versatile synthetic intermediate that combine the
ambident nucleophilicity of enamines with the ambident
electrophilicity of enones.
Enaminone derivatives are highly reactive intermediates
extensively used for synthesis of heterocyclic compounds.
On the other hand, a great deal of interest has been focused
on the synthesis of the functionalized pyridine derivatives
due to their biological activity [1,2]. Some 2-pyridine
derivatives are considered as cardiotonic agents such as
milrinone and as potential human immunodeﬁciency
virus 1-speciﬁc transcriptase inhibitors [3,4]. Moreover, it
has been reported that there are many review articles that
deal with the synthesis of pyridine derivatives from
In view of our interest in developing efﬁcient synthesis
of 2-pyridine derivatives by utilizing the enaminones as
starting material, we report here several approaches to the
synthesis of pyridine derivatives using compound 2 as a
RESULTS AND DISCUSSION
Firstly, 2-pyridylacetophenone was formed by the
reaction of α-picoline with benzonitrile or ethyl acetate in
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