Abstract

Olayinka O. Ajani¹, Oluwatosin Y. Audu¹, Markus W. Germann² and Babatunde L. Bello²

DOI : http://dx.doi.org/10.13005/ojc/330203

Quinazoline and quinazolinone derivatives are well-known bioactive heterocycles owing to their therapeutic diversity and extensive medicinal application in drug design and pharmaceutics. A series of 2-methyl-3-substituted quinazolin-4(3H)-one derivatives 8a-q was herein synthesized from synthetic conversion of anthranilic acid to 2-methyl-4H-3,1-benzoxazi-4-one, 7 which was subsequently transformed to the targeted 2,3-disubstituted quinazolin-4(3H)-one derivatives 8a-q by reacting with some notable amino-containing moieties via an ameliorable pathway. The catalyst-free synthesis was successful achieved by careful reaction optimization study using solvent choice and reaction temperature variability as key parameters. The chemical structures of the synthesized compounds were confirmed by IR, UV, ¹H-NMR, ¹³C-NMR and DEPT-135 as well as analytical data.

Solvent-dependent synthesis; spectral study; quinazolin-4(3H)-one; DEPT-135 analysis

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