文档介绍：中氮茚及其类似物的合成和抗肿瘤活性的研究摘要中氮茚(indolizine)是一类具有10兀电子体系的吲哚异构体,它的母核系统命名为 pyrrolo[1,2一a]pyridine。其生物活性主要有抗肿瘤、抗菌、抗病毒、杀螨虫、抗炎、抗心律失常、抗高血压等。吡咯[2,】噻唑和吡咯【l,2一以】,也是许多具有生物活性天然产物和药物的重要组成结构。本论文对中氮茚及其类似物的合成和抗肿瘤活性进行了研究。 ,在三乙***作用下得到叶立德,与缺电子烯烃进行1,,在氧化剂TPCD作用下,芳构化得到中氮茚衍生物。研究了1,;测定了中氮茚衍生物的抗Hep-G2 增殖活性,并研究了构效关系。 .***咪唑的鲦盐在三乙***和TPCD作用下,经1,【2,】噻唑和吡咯【1,]咪唑衍生物。初步研究了其中部分化合物的抗 。本论文共合成了37个化合物,其中36个为新化合物,并用FTIR、NMR、MS 和EA进行了结构鉴定。生物活性研究表明,部分化合物具有和5.***尿嘧啶相当的抗 。活性关键词:中氮茚;吡咯【2,】噻唑;吡咯【1,】咪唑;1,3一偶极环加成;抗肿瘤 SYNT髓SIS AND ANTITUMOR ACTIVITY OF n寸DOLIZINES AND ANALOGUES AB STRACT Indolizine has ten peripheral兀electrons and isisoelectronic with isalso named pyrrolo[1,2一a] derivatives have a diversity of biological activity, such as antitumour,antiinflammatory, and antimicrobial activities. Pyrrolo[2,1一b]thiazole and pyrrolo[1,2一a]imidazole ponents of various biologically activesubstances,which alsocontain N-fused pyrrole ,the synthesis andantitumoractivity ofindolizines and theiranalogues were studied. were synthesized by one pot reactions ofpyridinium ylide with alkene inthepresence ofthe mild oxidant reactions consisted of a 1,3-dipolar cycloaddition ofN—ylides toalkenes,followed by an of 1,3一dipolar cycloaddition reaction Was activity against Hep。G2 cell lines was tested and 5-fluorouracil Was used as —activity relationship(SAR)was explored. [2,1一b]thiazole and pyrrolo[1,2-a]imidazole were synthesized by the reactions ofthecorresponding N··ylidesand electron--deficient alkenes inthepresence of thebaseEtaN and oxidant TPCD via 1, antitumor activity of pounds Wasexamined. Totally were synthesized and characterized byFTIR,1H and MR,MS and ofthem were not reported study of b