Construction Of Indolizine Derivatives Based On Carbon-Sulfur Bond Formation And Their Anticancer Activity

Indolizine is a very important aromatic nitrogen-containing heterocyclic compound widely present in structural units of natural products.With the deepening of research,it has been found that the indolizine and its derivatives have a very wide range of uses in biology,medicine,pesticides,and optoelectronic properties.Studies on the synthesis methods and biological activities of nitrogen-containing heterocyclic compounds have been receiving much attention.This paper developed a C-H bond activation strategy for transition-metal-free catalyzed indolizine and thiol,which is simple,environmentally friendly,highly efficient and controllable to synthesize 3-and 1,3-thiolated indolizine,and some of the compounds exhibited A549 inhibitory activity in human non-small cell lung cancer cells.The details are as follows:In the chapter 1,the application value and research significance of the indolizine derivatives in biology,medicine,pesticides and photoelectric properties are introduced.Then,the recent progress in the synthesis of the indolizine derivatives is reviewed.In the chapter 2,an efficient transition-metal-free?KI?catalyzed,TBHP oxidized regioselective C-H/S-H cross-coupling of indolizines with thiols has been developed for the first time to describe a workable route to dithioethers indolizine.The reaction is simple in operation,environmentally friendly,and has wide applicability and high efficiency,and provides a new path for the synthesis of 1,3-dithiolation indolizines.For the screening of anticancer activity of their derivatives,several compounds having anticancer activity were initially found.In the chapter 3,based on the research in the synthesis of dithiolation indolizines,a catalyst-free,H₂O₂ straightforward oxidation of thiol and indolizine route was developed to form the monothioethers.The method has the advantages of operationally simple,environmental friendliness,wide applicability of substrate,high selectivity,water as the only by-product.