The Reactions Of 1-sulfonyl-1h-indazoles And Its Applications In Thesynthesis Of Drugs

Indazoles and their derivatives represent an important class of compounds in the medicinal arena,and have found widespread application in the pharmaceutical and biological industry.This paper intends to explore the reactions of 1-tosyl-1H-indazole and its applications in the systhesis of drugs.The paper is divided into three chapters:The first chapter summarized a wide range of biological activities of indazoles as well as their representative preparations briefly.In the second chapter,we develop an efficient synthesis of indazols from readily accessible E/Z mixtures of o-haloaryl N-tosylhydrazones.A series of valuable indazole derivatives were prepared in good yields.The method has been successfully applied to the synthesis of Lonidamine,Axitinib,AF-2785 and YD-3.In the last chapter,the reactions of 1-sulfonyl-1H-indazoles under basic conditions are discussed,the direct N-alkylation reaction and the Kemp elimination reaction are reported in detail.A series of 2-(p-tosylamino)benzonitriles and N-alkyl indazoles are prepared in good yields.Moreover,the 2-(p-tosylamino)benzonitriles could be transformed to diverse important 3-amino-1H-indole and 5-amine-2,3-dihydro-1H-benzo[b]azepin derivatives in an one-pot reaction.