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中文摘要：
由于氟原子的特性，含氟有机化合物在含氟医(农)药的研制和生命科学的研究中起到越来越重要的作用。发展向有机分子选择性引入氟原子和含氟基团(主要是三氟甲基和二氟亚甲基)的方法和分子设计与合成具有生物活性的含氟有机化合物已成为有机氟化学和药物化学的热点研究领域。本项目将包括三方面的研究内容（1）从我国已商品化的含氟有机原料出发，应用金属有机和不对称反应探索立体选择性制备含氟有机化合物的合成方法学；（2）利用本项目发展的含氟合成子，分子设计与合成多种类型的含氟生物活性物质， 如含氟核苷，含氟糖和具有重要生理活性的复杂天然产物的含氟类似物等；（3） 对合成的含氟化合物进行生物活性研究，从而得到结构与性能的关系， 特别是研究氟原子（含氟基团）对生物活性影响的根本原因. 通过本项目的开展， 将推动有机氟化学的发展; 更为重要的是，期望能发现具有抗肿瘤和抗病毒等活性的先导化合物。
英文摘要：
organofluorine chemistry；organic reaction；biological active compounds；；
结论摘要：
由于氟原子的特性，含氟有机化合物在含氟医(农)药的研制和生命科学的研究中起到越来越重要的作用。发展向有机分子选择性引入氟原子和含氟基团(主要是三氟甲基和二氟亚甲基)的方法和分子设计与合成具有生物活性的含氟有机化合物已成为有机氟化学和药物化学的热点研究领域。本项目主要开展了含氟有机化合物的反应规律、导向含氟生物活性分子的合成方法学、分子设计与合成多种类型的含氟生物活性物质的研究。 取得的主要研究结果为1）提出和实现了向有机分子引入含氟基团的新思想和新方法氧化氟烷基化反应。探索出新型的氧化三氟甲基化反应、氧化二氟亚甲基化反应、氧化三氟甲硫基化反应。2）系统地研究了含氟碳负离子参与的氟烷基化反应的相关规律发展出新型的二氟卡宾试剂、二氟甲基化试剂、单氟烯烃化反应、二氟烯烃化反应等。3）较系统地研究了过渡金属催化的多氟芳烃C-H键的直接官能团化反应探索出多氟芳烃C-H键的烯基化反应、烯丙基化反应、与芳杂环的偶联反应。4）分子设计与合成了环腺苷二磷酸核糖(cADPR)和环二鸟苷酸(c-di-GMP)的含氟类似物，对所合成的氟代类似物进行了生物活性研究。5）分子设计与合成了Dapagliflozin含氟类似物。生物活性测试发现部分Dapagliflozin含氟类似物对SGLT2具有选择抑制活性。本项目共发表SCI论文112篇，其中J. Am. Chem. Soc. 8篇，Angew. Chem. Int. Ed. 10篇。项目执行期间培养博士研究生18名, 在国内外学术会议上做请报告25次。
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期刊论文
Stereoselective Reformatskii-Claisen rearrangement: synthesis of 2 ';,3 ';-dideoxy-6 ';,6 ';-difluor
Methyl carboniumion migration during the reaction of 4-chloro-5-methoxyl-3(2H)-pyridazinone with tri
Nucleophilic Difluoromethylation of N,N-Acetals with TMSCF2SO2Ph Reagent Promoted by Trifluoroacetic
Synthesis of Photochromic 1,2-Dithienylethene Derivative with a 2,2,5,5-Tetrafluoro-2,5-dihydrofuran
Coupling of sterically hindered aldehyde with fluorinated synthons: Stereoselective synthesis of flu
Difluoromethylation of O-, S-, N-, C-Nucleophiles Using Difluorotri(n-butyl)ammonium Chloride as a N
From Difluoromethyl 2-Pyridyl Sulfone to Difluorinated Sulfonates: A Unique Protocol for Nucleophili
Highly Diastereoselective Synthesis of Quaternary ?-Trifluoromethyl ?-Amino Acids by Addition of Ben
Studies on the synthesis of nicotinamide nucleoside and nucleotide analogues and their inhibitions t
Synthesis of ?-monofluorinated goniothalamin analogous via regio- and stereoselective ring-opening h
Palladium-catalyzed cross-coupling of ethyl -fluoro- -bromoacetate with arylboronic acids: facile sy
Benzoyl peroxide (BPO)-promoted oxidative trifluoromethylation of tertiary amines with trimenthyl(tr
Diastereoselective Synthesis of Propargylic Fluorides and Its Application in Preparation of Monofluo
Highly Diastereoselective Synthesis of Quaternary ?-Trifluoromethyl ?-Amino Acids from Chiral Imines
Highly diastereoselective synthesis of ?-trifluoromethylated ?-propargylamines by acetylide addition
Synthesis of 2 ';,3 ';-dideoxy-6 ';-fluorocarbocyclic nucleosides via Reformatskii-Claisen rearrange
Pd-Catalyzed Highly Regio- and Stereocontrolled Direct Alkenylation of Electron-deficient Polyfluoro
Pd-Catalyzed Direct Cross-Coupling of Electron-Deficient Polyfluoroarenes with Heteroaromatic Tosyla
Synthesis of gem-Difluorinated Cyclopropanes and Cyclopropenes：Trifluoromethyltrimethylsilane as a D
Derivatization of beta-dicarbonyl compound with 2,4-dinitrophenylhydrazine to enhance mass spectrome
Highly Diastereoselective Zinc/SnCl2-Mediated gem-Difluoroallylation of Chiral Hydrazones: Synthesis
Difluoromethylenated polyhydroxylated pyrrolidines: facile synthesis, crystal structure and biologic
Copper-mediated oxidative cross-coupling reaction of terminal alkynes with ?-silyldifluoromethylphos
Copper and Phosphine Ligand-Free Palladium-Catalyzed Direct Allylation of Electron-Deficient Polyflu
Copper-Mediated Fluoroalkylation Reactions with [(Phenylsulfonyl) difluoromethyl] trimethylsilane: S
Synthesis and biological evaluation of nicotinamide adenine dinucleotides analogues as inhibitors of
Palladium-Catalyzed Allylation of 2,2,2-Trifluoroethyl Phenyl Sulfone: A Potential 2,2,2-Trifluoroet
Synthesis of fluoroalkylated allylic amine derivatives via palladium-catalyzed Overman rearrangement
Regio- and Diastereoselective Nickel-Catalyzed Allylation of Aromatic Aldehydes with alpha-Halo-beta
Palladium-catalyzed direct ?-arylation of ?-fluoroketones: A straightforward route to ?-fluoro--aryl
Difluoro(phenylchalcogen)methylation of aldehydes, ketones, and imines with S-, Se-, and Te-containi
Synthesis and biological evaluation of SGLT2 inhibitors: gem-difluoromethylenated Dapagliflozin anal
Copper-Catalyzed Difluoromethylation of, -Unsaturated Carboxylic Acids: An Efficient Allylic Difluor
Copper-Catalyzed Oxidative Trifluoromethylation of Terminal Alkenes Using Nucleophilic CF3SiMe3: Eff
Sequential Electrophilic Trifluoromethanesulfanylation-Cyclization of Tryptamine Derivatives: Synthe
From Olefination to Alkylation: In-Situ Halogenation of Julia-Kocienski Intermediates Leading to For
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