有机化学ChineseJournalofOrganicChemistryREVIEW*Correspondingauthor.E-mail:moeastlight@mailbox.gxnu.edu.cnReceivedJune21,2022;revisedAugust10,2022;publishedonlineSeptember1,2022.ProjectsupportedbytheNationalNaturalScienceFoundationofChina(Nos.21871062,22071035).国家自然科学基金(Nos.21871062,22071035)资助项目.130http://sioc-journal.cn/©2023ShanghaiInstituteofOrganicChemistry,ChineseAcademyofSciencesChin.J.Org.Chem.2023,43,130～155DOI:10.6023/cjoc202206035综述与进展九元氮杂环化合物合成最新研究进展覃小婷邹宁农彩梅莫冬亮*(广西师范大学化学与药学学院省部共建药用资源化学与药物分子工程国家重点实验室桂林541004)摘要九元氮杂环骨架广泛存在于天然产物和生物活性分子中,其环系的刚性结构对这类分子的生物活性及药理活性的调控具有重要的作用,是被广泛关注的中环化合物之一.由于九元环的熵和环张力的增加,其合成往往是有机合成中的难点,特别是环上取代基立体化学的有效控制更是极大挑战之一.综述了近年来九元氮杂环化合物合成的新策略和新方法,以及这些策略和方法在合成含九元氮杂环骨架天然产物和药物分子中的应用.关键词九元氮杂环;中环化合物;环化反应;环加成反应;扩环反应RecentAdvancesontheSynthesisofNine-MemberedN-HeterocyclesQin,XiaotingZou,NingNong,CaimeiMo,Dongliang*(StateKeyLaboratoryforChemistryandMolecularEngineeringofMedicinalResources,SchoolofChemistryandPharmaceuticalSciences,GuangxiNormalUniversity,Guilin541004)AbstractNine-memberedN-heterocyclescaffoldsarewidelyfoundinnaturalproductsandbiologicallyactivemolecules.Therigidstructureofthemedium-sizedringplaysimportantrolesintheregulationoftheirbiologicalandpharmacologicalactivities.Therefore,nine-memberedN-heterocycleisoneofthemostattractivemedium-sizedringcompounds.Becauseoftheincreasingentropyandringextensionofnine-memberedringskeleton,thesynthesisofnine-memberedN-heterocyclesisstilldifficult;especiallytheeffectivecontrolofsubstituentstereoselectivityforthenine-memberedringisoneofthegreatestchal-lengingtopicsThisreviewsummarizesthenovelsyntheticstrategiesofnine-memberedN-heterocyclesandtheirapplicationsinthesynthesisofnaturalproductsandpharmaceutical...
