الفهرس 
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Abstract
Pyrimidine derivatives are important type of six membered
heterocyclic compounds. Its chemical structure and reactivity has been
the subject of many synthetic and theoretical investigations.
This thesis is divided into two parts discussion and biological
activities (antimicrobial and antitumor activities). The discussion part will
deal with the synthesis of pyrimidine and thiazol derivatives. Also it will
deal with the investigation of newly synthized compounds by using mass
spectroscopy. Biological activity studies are also performed on selected
examples of the compounds obtained.
The first part of this investigation deals with the synthesis of ethyl-
aryl--cyanoacrylate (2a, b) and their reaction towards some
nucleophiles (Scheme 1). The starting material ethyl-aryl--
cyanoacrylate (2a, b) was prepared by the reaction of ethyl cyanoacetate
and aromatic aldehyde in methanol in presence of anhydrous potassium
carbonate under reflux.
Treatment of compound 2 with thiourea in the presence of anhydrous
potassium carbonate in methanol under reflux resulted in the formation of
6-aryl-5-cyano-4-hydroxy-2-mercaptopyrimidine (3a, b). .
Acetylation of 6-(5-bromo-2-hydroxyphenyl)-5-cyano-4-hydroxy-2-
mercaptopyrimidine (3a) with acetic anhydride under reflux led to the
8
Summary
formation of 6-(5-bromo-2-acetoxyphenyl)-5-cyano-4-hydroxy-2-
mercaptopyrimidine (4).
Cyclo-condensation of ethyl--(3-nitrophenyl)--cyanoacrylate (2b) with
guanidine hydrochloride in the presence of anhydrous potassium
carbonate in methanol under reflux afforded the corresponding 6-(3-
nitrophenyl)-5-cyano-4-hydroxy-2-amino pyrimidine (5).
6-(3-nitrophenyl)-5-cyano-4-hydroxy-2-(acetylamino)-pyrimidine (6)
was prepared via acetylation of (5) with acetic anhydride under reflux.
The reaction of 2-amino pyrimidine (5) with ethylchloroacetate in
presence of fused sodium acetate in acetic acid under reflux gave the
corresponding 7-(3-nitrophenyl)-6-cyano-5-hydroxy-imidazolo-[2,1-b]-
pyrimidine-1-one(7)
Treatment of ethyl –-(5-bromo-2-hydroxyphenyl)--cyanoacrylate (2a)
with thio semicarbazide in presence of anhydrous potassium carbonate in
methanol under reflux gave the corresponding