The Study On The C-H Indolylation And Cycloisomerization Reactions Based On Quinazoline

As a common fuse heterocyclic skeleton,quinazoline is an important structural unit in many medical and agricultural products.Quinazoline derivatives displace various biological activities,such as anticancer,anti-inflammatory,analgesic,anti-allergic and hypotensive activities.In addition,many quinazoline derivatives have excellent photophysical properties and can be used as fluorescent probes,bioimaging reagents and luminescent materials.Base on their important applications in many fields,the derivatization of quinazolines is a very interesting topic in chemistry.Most of the derivatizations of quinazolines have focused on the introduction of different substituents into the quinazoline backbone.The common cyanylation,hydroxymethylation,alkylation,amination,allylation,acetoxylation,etc.have been achieved.Based on these reported derivatization studies of quinazolines,we continued to expand the quinazoline derivatives with medicinal potential,and the main studies in this paper include the following two aspects.(1)A series of 2-arylindolylquinazoline compounds were synthesized by combining the C-H activation of quinazolines and the cyclization of o-alkynylbenzenesulfonamides under the catalytic action of Rh,which successfully introduced indole groups on the quinazoline compounds.The reaction system has the advantages of good substrate suitability and mild reaction conditions,and these synthesized compounds may have great potential in medical chemistry.(2)The 1,8-diynyl structure was introduced into the quinazoline skeleton,and the1,8-diynyl cycloisomerization of the 1,8-diynyl group was achieved by photocatalysis to synthesize pyrrolozine fused quinazoline compounds with the bridge linkage of the quinazoline as a directing gtoup.The method is simply operate without metal catalysis and provides a new and effective strategy for the synthesis of complex polycyclic compounds.