ABSTRACT
Diverse compounds such as anti-biotics, alkaloids, vitamins, essential amino acids, hormones, hemoglobin, and various dyes and synthetic drugs contain heterocycles as core skeletons. Reduction of β-nitroamine products to 1,2-diamines provided substrates for selective intramolecular nitrogen (N)-arylations to yield both five- and six-membered ring heterocycles. This synthesis was used to produce an array of 1,2-diamine containing fused heterocycles. The chapter discusses the preparation of many quinoxalines and quinolines due to immense biological properties associated with them. Some substituted quinolines exhibit potent anti-breast cancer activity. 4-Carboxyl quinoline derivative acts as a selective cyclooxygenase inhibitor with greater potency than reference drug celecoxib. The 2-methylquinolines were yielded via palladium-catalyzed aza-Wacker oxidative cyclization. Many of syntheses of 3-aminotetrahydroquinolines reported in the literature utilized a reduction of α-aminoamides to form the desired 1,2-diamine. Good yields of isoquinolines were obtained by extrusion of nitrogen followed by an isomerization-aromatization with release of excessive allene and extended heating.
