Synthesis of Quinolines N_Acetyl Dioxoisoindolins and Sulfonamide Urea Derivatives

Abstract

The core adjective of this submitting effort is to design, synthesis and biological assessment (Anti cancer activity) of new pyrazoles, indolidinones and sulfonamide derivatives. In addition and pharmaceutically functional scaffolds have been developed C-N and C-C coupling reactions by using new synthetic procedures. The thesis is divided into five chapters newlineCHAPTER-I: Heterocycles are important in organic chemistry because they constitute the fundamental structure inside countless natural products and furthermore due to their expansive scope of biological properties in medicinal chemistry (Preston.,2009).Moreover the condensed heterocycles considers as synthetic building blocks and pharmacophores. Heterocycles contain a group of natural operators with especially fascinating pharmacological properties identified with planarity of the framework and subsequently to its DNA-chain intercalating capacity, which make them appropriate for hostile to neoplastic and mutagenic applications (Hudson and Barton., 1998); (Fewell and Woolford., 1999); (Bailly., 2000). Because of their useful applications in the biological field, synthesis of fused heterocycles has attracted the interest in modern drug discovery (Alvarez-Corral et al., 2008); (Balme et al., 2003); (Zeni and Larock., 2006).The pharmacophore of hetero atoms are mostly act as a anti cancer drugs, the moreover ancho products are heterocycle scaffolds newlineCHAPTER-II: 4-Nitropheny1 cyclopropy1carbamate was deployed as a novel synthon for the synthesis of anticancer drug Lenvatinib. 4-nitrohenyl cyclopropylcarbamate was prepared by the reaction of 4-nitrophenyl chloroformate and cyclopropy1 amine in acetonitrile at room temperature. Furthermore, Lenvatinib was synthesized by reacting 4-(4-amino-3-chloro phenoxy)-7-methoxy quinoline-6- carboxamide with 4-nitro phenyl cyclopropylcarbamate in good yields. newline