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中文摘要：
具有重要生理活性的天然产物一直是化学科学和生物医药科学关注的焦点之一，包括从我国特有自然资源中发现的喜树碱等天然产物已经成为全球药物研发的基本化学骨架。本项目拟选取若干具有代表性的重要生理活性天然产物作为研究目标，设计、发展和优化高效合成方法和合成策略，开展全合成研究。具体研究内容包括结构新颖但天然来源稀缺而导致进一步研究困难的抗癌活性海洋二萜Clavulactone和Plumisclerin A；具有显著抗肿瘤活性、结构中含有恶唑等结构单元的大环海洋天然产物Jaspisamides A-C；具有明确药用发展前景但目前自然资源日渐贫乏紧缺、全合成技术路线尚不够理想的生物碱喜树碱和石杉碱甲。本项目将争取实现若干生理活性天然化合物的全合成，发展新方法、新路线，为开展新的化学结构拓展研究，将这些重要天然产物的最终推向创新药物奠定基础。
英文摘要：
natural product；total synthesis；asymmetric synthesis；synthesis economy；natural product-like chemistry
结论摘要：
本项目针对一些具有显著生理活性和独特结构特点的天然产物开展了全合成研究。通过四年的项目工作，除了海洋二萜Plumisclerin A的全合成尚未收尾发表，其余计划内容全部完成，具体包括海洋二萜Clavulactone、大环型海洋天然产物IKD-8344、药用生物碱喜树碱和石杉碱甲。此外，该项目还扩展完成了石松生物碱Lanotinidine B、Lycoposerramine-V和5-epi-Lycoposerramine-V；醚类离子载体类抗生素Demethyl Cezomycin；复杂环肽Chlorofusin；高张力笼状结构海洋天然产物Azonazine以及高度N/O-甲基化海洋环酯肽Coibamide A文献归属结构的全合成，共计12例天然产物。同时，针对天然产物核心结构的化学键形成问题，设计并发展了三例独特的高效率合成方法学。多项天然产物全合成工作为国际上首次实现，发表之后获得了国内外同行的积极评价，形成了较好的学术影响和反馈。通过本项目还获得了一批较多数量的天然产物类似物、衍生物和稳定中间体，为进一步工作的深入和拓展建立了坚实基础。本项目总共发表标注基金号的SCI学术论文61篇（其中3项天然产物全合成和1项天然产物目标导向的方法学工作分别发表在J. Am. Chem. Soc.和Angew. Chem. Int. Ed.上）；参加国内外学术会议并作邀请报告31人次；培养毕业博士研究生18名（含2名联合培养博士生），硕士研究生18名（含8名联合培养硕士生），出站博士后2名。
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期刊论文
Asymmetric Annulation of 3？Alkynylacrylaldehydes with Styrene-Type Olefins by Synergetic Relay Catal
Regio- and stereoselective C10beta-H functionalization of sinomenine: an access to more potent immun
CuCl2-Promoted 6-endo-dig Chlorocyclization and Oxidative Aromatization Cascade: Efficient Contructi
Three-component Reactions of IsochromenyliumTetrafluoroborates via Non-classical [4+2]-Intermediates
Assembly of PentacyclicPyrido[4,3,2-mn]acridin-8-ones via a Domino Reaction Initiated by Au(I)-Catal
Sinomenine derivatives with embedment of nitrogen-containing heterocycles exhibiting potent TNF-？ in
A simple selective protocol for continuous two-stage fluorescent sensing of both MeHg+ and anti-MeHg
Electronically unfavorable addition of electron-deficient olefins to isochromenyliumtetrafluoroborat
Dual-Functional abeo-Taxane Derivatives Destabilizing Microtubule Equilibrium and Inhibiting NF-κB A
Unified Flexible Total Synthesis of Chlorofusin and Artificial Click Mimics as Antagonists against p
Total Synthesis of 7-Ethyl-10-hydroxycamptothecin (SN38) and Its Application to the Development of C
Synthesis of the Anti-melanogenic Glycerol Fatty Acid Ester Isolated from the Tuber-barks of Colocas
Concise synthesis of zanamivir and its C4-thiocarbamido derivatives utilizing a [3+2]-cycloadduct de
Synthesis and Absolute Configuration of the 7-Phenylhepta-4,6,diyne-1,2-diol Isolated from Bidenspil
Asymmetric Michael addition of 4H-thiopyran-4-one to nitroolefins catalyzed by diamine mono-N-sulfon
Asymmetric cascade annulation based on enantioselective oxa Diels-Alder cycloaddition of in situ gen
Facile Assembly of 11H-Indolo[3,2-c]quinoline by a Two-Step Protocol Involving a Regioselective 6-en
Regio-selective reduction of the C-C double bonds in α,β-unsaturated acyl 4-substituted oxazolidin-2
Access to some UV chromophore-containing antimalrailtrioxanes using hydrogen peroxide as source of t
Target-oriented multifunctional organocatalysis for enantioselective synthesis of bicyclo[3.3.1]nona
Br？nsted acid-promoted dimerization of o-alkynylbenzaldehydes: a one-step synthesis of functionalize
Assembly of Fused Indenes via Au(I)-Catalyzed C1-C5 Cyclization of Enediynes Bearing an Internal Nuc
Synthesis of 2-Vinyl-2H-benzotriazoles via NIS-Promoted Regio/Stereoselective Addition of 1H-Benzotr
Asymmetric Cascade Annulation Based on EnantioselectiveOxa Diels？Alder Cycloaddition of in Situ Gene
Organocatalytic enantioselective conjugate addition of 2-nitrocyclohexanone to acrylaldehyde: a conc
Total Synthesis of Proposed Structure of Coibamide A, A Highly N-and O-Methylated Cytotoxic Marine C
Ge, H. M.; Zhang, L.-D.; Tan, R. X.; Yao, Z.-J.* Protecting Group-Free Total Synthesis of (-)-Lannot
Yang, Z.-Y.; Liao, H.-Z.; Sheng, K.; Chen, Y.-F.; Yao, Z.-J.* Enantioselective Total Synthesis of Ma
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