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Abstract
Name: Doaa Abdallah Zaki Ismail Title: New Synthetic Approaches to Some Novel Fused Heterocyclic Derivatives Containing Nitrogen and / or Sulfur Degree: (Ph. D.) Thesis, Chemistry Department, Faculty of Science, Menofia University, 2016.
Versatile 3-aminopyrrolopyridine-2-carboxylate and -2-
carboxylic acid derivatives 2a,b were obtained based on an ortho
functionalized pyrrole derivative 1. Initially cyclization of ester 2a
followed by formylation to obtain a tricyclic chloroaldehyde
derivative 4, which on further treatment with hydroxylamine
hydrochloride yielded the corresponding oxime 5a. The latter
product was subsequently dehydrated forming the tricyclic 2-
cyanopyrimidine derivative 5b. Other different 2-functionalized
tricyclic derivatives of N-3-substituted pyrimidine were synthesized,
for toxicological assessment, starting from the key precursors 2a,b
through convenient methods. All condensed tricyclic pyrimidine
derivatives with the common 7,9-diphenyl-8-(4-methoxyphenylazo)
2
substitution pattern were evaluated for their toxicity on the 4th larval
instar of the mosquitoes, Culex pipiens. The compounds under
investigation displayed different levels of toxicological effects. In
general, chloro compounds 4, 5a and 5b that have a chlorine atom as
a substituent on the C-4 atom of the pyrimidine ring, showed high
insecticidal activity, with compound 5b showing essentially the
highest toxicological effect. The lethal concentration at LC50 of the
latter compound 5b is very significant (0.22%). Our results may
provide some guidance for development of some novel
chloropyrimidine-based insecticidal lead structures. The detailed
synthesis and biological screening data were reported.