majun_an68@tju.edu.cn
有机化学
未公开
教授
基于糖结构的新型双功能手性硫脲有机小分子催化剂设计合成及相关不对称反应和应用研究

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微生物多细胞体系的设计与合成

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含氟有机化合物不对称控制合成

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新型螺环手性季铵盐相转移催化剂设计合成及其应用于相关手性氨基酸的催化不对称构建

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端联炔及烯炔参与的不对称1,2-加成反应及相关药物研究

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碗烯类分子的药物传输特性研究

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自由基脱羧和氟代反应研究

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基于1,3-端联炔构筑含氟合成砌块的反应、机理及应用研究
含联萘轴手性螺环季膦盐相转移催化剂及其制备方法

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3,3’-位联芳基联萘轴手性亚磷酰胺配体及其制备方法

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含糖氨基脲和硫脲双功能手性催化剂及其制备方法与在不对称反应中的应用

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N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-反式-2,4-戊二烯酰胺

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联萘轴手性功能基的4-二甲胺基吡啶有机小分子催化剂及其制备方法

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5-芳基-3-三氟甲基-1H-吡唑类化合物制备方法

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(R)-r,r,r-三氟-β-羟基丁酸苯酚酯的制备方法

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含联萘轴手性双螺环季铵盐相转移催化剂及其制备方法

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一种如式（I）所示的N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-反式-2,4-戊二烯酰胺衍生物以及其作为EGFR抑制剂的制备和应用，该化合物具有可抑制突变体L858R EGFR、T790M EGFR及外显子-19缺失激活突变体的活性。因此将式（I）所示的化合物及其药学上可接受的盐作为EGFR调谐子用于治疗或预防癌症。

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本发明涉及一类5-芳基-3-三氟甲基-1H-吡唑化合物的新制备方法是：将2-芳基-1-乙炔于0oC至50oC温度，在催化剂及碱的作用下，于有机溶剂中，以DABCO作为添加剂，与2,2,2-三氟甲基重氮乙烷完全反应后，经洗涤、萃取、分离，得到目标5-芳基-3-三氟甲基-1H-吡唑类化合物；2-取代基-1-乙炔、催化剂、碱、DABCO及2,2,2-三氟甲基重氮乙烷的摩尔配比为1/1-3/1-3/0.1-1/2-10。

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-将丙二酸单苯酚酯、三氟乙醛半缩醛、金属铜盐及手性双噁唑配体加入反应瓶中，加入有机溶剂将这些化合物完全溶解，于0-5oC温度反应2－24小时后，经洗涤、萃取、分离，得到目标(R)-γ, γ, γ-三氟-β-羟基丁酸苯酚酯。提供的合成方法不需要无水、无氧处理，也不需要低温制冷，因此操作简单，反应条件温和；而且反应完全彻底，目标产物收率高；所得目标产物的ee值高达95%，与已有合成方法相比，本发明提供的合成方法对映选择性最高。

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Direct amide synthesis via Ni-mediated aminocarbonylation of arylboronic acids with CO and nitroarenes

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Construction of Chiral beta-Trifluoromethyl Alcohols Enabled by Catalytic Enantioselective Aldol-Type Reaction of CF3CHN2

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Catalytic Enantioselective Cyclopropenation of Internal Alkynes: Access to Difluoromethylated Three-Membered Carbocycles

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silver-catalyzed[3+2] dipolar cycloaddition of trifluorodiazoethane and glycine imines

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Use of a Traceless Activating and Directing Group for the Construction of Trifluoromethylpyrazoles: One-Pot Transformation of

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Copper-triggered three-component reaction of CF3CHN2, nitriles, and aldehydes: highly diastereoselective synthesis of CF3-sub

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Core-structure-inspired asymmetric addition reactions: enantioselective synthesis of dihydrobenzoxazinone- and dihydroquinazo

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Silver-Catalyzed Regioselective [3 + 2] Cycloaddition of Arene-diazonium Salts with 2,2,2-Trifluorodiazoethane (CF3CHN2): A F

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Brine-Stabilized 2,2,2-Trifluorodiazoethane and Its Application in the Synthesis of CF3？Substituted Cyclopropane α-Amino Acid

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Copper-Catalyzed One-Pot Denitrogenative-Dehydrogenative-Decarboxylative Coupling of beta-Ketoacids with Trifluorodiazoethane

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Lithium Binaphtholate-Catalyzed Enantioselective Enyne Addition to Ketones: Access to Enynylated Tertiary Alcohols

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Nucleophilic Lewis Base Dependent Addition Reactions of Allenoates with Trifluoromethylated Cyclic Ketimines

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Cyclic Aldimines as Superior Electrophiles for Cu-Catalyzed Decarboxylative Mannich Reaction of beta-Ketoacids

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A Direct Copper-Promoted Three-Component Entry to Trifluoromethylketoximes

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Copper-Catalyzed One-Pot Denitrogenative-Dehydrogenative-Decarboxylative Coupling of beta-Ketoacids with Trifluorodiazoethane

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Copper-Catalyzed One-Pot Denitrogenative-Dehydrogenative-Decarboxylative Coupling of beta-Ketoacids with Trifluorodiazoethane

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Cyclic Aldimines as Superior Electrophiles for Cu-Catalyzed Decarboxylative Mannich Reaction of β-Ketoacids with a Broad Scop

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Regioselective Cycloaddition of Trifluorodiazoethane with Electron-Deficient Allenic Esters and Ketones: Access to CF3-

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Regioselective Cycloaddition of Trifluorodiazoethane with Electron-Deficient Allenic Esters and Ketones: Access to CF3？Substi

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Hydrogen-Bond-Directed Enantioselective Decarboxylative Mannich Reaction of -Ketoacids with Ketimines

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Bisphosphine-Triggered One-Pot Sequential [3 + 2]/[3+ 2] Annulation of Allenoates with Cyclic Ketimines

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Silver-Mediated Cycloaddition of Alkynes with CF3CHN2 : Highly Regioselective Synthesis of 3-Trifluoromethylpyrazoles

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BETA-KETO ACIDS; ASYMMETRIC CATALYSIS; MICHAEL ADDITION; AROMATIC KETONES; ALDOL REACTION; TRIFLUOROMETHYLATION; ALKALOIDS; B

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A Facile Parallel Synthesis of Trifluoroethyl-Substituted Alkynes

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Reversal of Enantioselectivity by Tuning the Conformational Flexibility of Phase-Transfer Catalysts

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Chiral Bifunctional Thiourea-Catalyzed Enantioselective Michael Addition of Ketones to Nitrodienes

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Brønsted Acid-catalyzed Efficient Strecker Reaction of Ketones, Amines and Trimethylsilyl Cyanide

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Chiral Brønsted Acid-Catalyzed Enantioselective Arylation of Ethyl Trifluoro-acetoacetate and Ethyl Trifluoropyruvate

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A perfect double role of CF3 groups in activating substrates and stabilizing adducts: the chiral Brøsted acid-catalyzed direct arylation of trifluoromethyl ketones

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Chiral Brønsted Acid-Mediated Enantioselective Organocatalytic Three-component Reaction for the Construction of Trifluoromethyl-containing Molecules

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Stereoselective Construction of Fluorinated Indanone Derivatives via a Triple Cascade Lewis Acid-Catalyzed Reaction

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Highly Enantioselective Michael Addition of Aromatic Ketones to Nitroolefins Promoted by Chiral Bifunctional Primary Amine-thiourea Catalysts Based on Saccharides

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Catalytic Stereoselective Synthesis of Highly Substituted Indanones via Tandem Nazarov Cyclization and Electrophilic Fluorination Trapping

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Catalytic Asymmetric Synthesis of α- and β-Amino Phosphonic Acid Derivatives

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Catalytic asymmetric tandem transformations triggered by conjugate addition