Efficient and Convenient Methods for Synthesis of Some Phthalazine Derivatives and Their Evaluation of Cytotoxicity

Abstract

<div><p></p><p>A systematic study of the reaction of 1,4-dihydrazinophthalazine (DHPH) with 1,3-dicarbonyls [<i>viz.</i>, acetylacetone (acac), dibenzoylmethane (bzbz), and 1-benzoylacetone (bzac)] varying the reaction conditions was carried out to obtain the phthalazine derivatives (<b>1</b>–<b>4</b>). One-pot reaction of DHPH with acac led to the formation of two compounds <b>1</b> and <b>2</b>, with various factors such as the presence of the acid or base, amount of the acac, time of reflux, and the temperature. The reaction conditions of DHPH with bzbz or bzac are sort of different to isolate the products <b>3</b> and <b>4</b>, respectively. The derivatives (<b>1</b>–<b>4</b>) have been characterized by elemental analyses, ¹H NMR, and electrospray ionization–mass spectrometry (ESIMS) and the cytotoxic activity of the compounds <b>1</b>–<b>4</b> was evaluated on HeLa cell line.</p> <p>[Supplementary materials are available for this article. Go to the publisher's online edition of <i>Synthetic Communications</i>® for the following free supplemental resource(s): Full experimental and spectral details.]</p> </div