Base-Promoted (3 + 2) Cycloaddition of Trifluoroacetohydrazonoyl Chlorides with Imidates En Route to Trifluoromethyl-1,2,4-Triazoles

Quadruple Functionalized Pyrazole Pharmacophores via One‐pot Regioselective [3 + 2] Cycloaddition of Fluorinated Nitrile Imines and Dicyanoalkenes

(2022) Yin Zhou et al.   Chemistry-An Asian Journal

Trifluoromethylated Pyrazoles via Sequential (3 + 2)-Cycloaddition of Fluorinated Nitrile Imines with Chalcones and Solvent-Dependent Deacylative Oxidation Reactions

(2022) Anna Kowalczyk et al.   ORGANIC LETTERS

Direct Synthesis of Biphenyl-2-carbonitriles by Rh(III)-Catalyzed C–H Hiyama Cross-Coupling in Water

(2022) Xiuqi Zhang et al.   ORGANIC LETTERS

Regioselective Synthesis of 3‐Trifluoromethyl 4‐Subtituted Pyrazoles by [3+2] Cycloaddition of Trifluoroacetonitrile Imines and Nitroalkenes

(2022) Ke‐Hu Wang et al.   Asian Journal of Organic Chemistry

Regioselective Decarboxylative Cycloaddition Route to Fully Substituted 3‐CF 3 ‐Pyrazoles from Nitrilimines and Isoxazolidinediones

(2021) Yu‐Chen Tian et al.   ADVANCED SYNTHESIS & CATALYSIS

Modular Chemical Synthesis of Streptogramin and Lankacidin Antibiotics

(2021) Lingchao Cai et al.   ACCOUNTS OF CHEMICAL RESEARCH

Triazines: Syntheses and Inverse Electron-demand Diels–Alder Reactions

(2021) Fa-Guang Zhang et al.   CHEMICAL REVIEWS

Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity

(2021) Yingjie Yu et al.   CHINESE CHEMICAL LETTERS

Regioselective Synthesis of 3-Trifluoromethylpyrazole by Coupling of Aldehydes, Sulfonyl Hydrazides, and 2-Bromo-3,3,3-trifluoropropene

(2020) Chuanle Zhu et al.   ORGANIC LETTERS

Cycloaddition of Trifluoroacetaldehyde N-Triftosylhydrazone (TFHZ-Tfs) with Alkynes for Synthesizing 3-Trifluoromethylpyrazoles

(2020) Hongwei Wang et al.   ORGANIC LETTERS

Fluorine-containing drugs approved by the FDA in 2019

(2020) Haibo Mei et al.   CHINESE CHEMICAL LETTERS

Cu‐Catalysed Three‐Component Reaction of Aryldiazonium Salts with Fluorinated Diazo Reagents and Nitriles: Access to Difluoro‐ and Trifluoromethylated N1‐Aryl‐1,2,4‐triazoles

(2020) Xing Peng et al.   ADVANCED SYNTHESIS & CATALYSIS

Aryl Diazonium Salt‐Triggered Cyclization and Cycloaddition Reactions: Past, Present, and Future

(2020) Fa‐Guang Zhang et al.   CHINESE JOURNAL OF CHEMISTRY

A straightforward access to 3-trifluoromethyl-1H-indazoles via (3+2)-cycloaddition of arynes with nitrile imines derived from trifluoroacetonitrile

(2020) Anna Kowalczyk et al.   JOURNAL OF FLUORINE CHEMISTRY

Highly fluorinated 2,3-dihydro-1,3,4-thiadiazole derivatives via [3+2]-cycloadditions of tertiary thioamides with nitrile imines derived from trifluoroacetonitrile

(2020) Greta Utecht-Jarzyńska et al.   JOURNAL OF FLUORINE CHEMISTRY

Palladium-catalyzed tandem cyclization of fluorinated imidoyl chlorides with 2-bromophenylboronic acid: Synthesis of 6-fluoroalkyl-phenanthridines

(2019) Yinwei Bao et al.   TETRAHEDRON

Silver-Catalyzed [3 + 3] Dipolar Cycloaddition of Trifluorodiazoethane and Glycine Imines: Access to Highly Functionalized Trifluoromethyl-Substituted Triazines and Pyridines

(2019) Zhen Chen et al.   ACS Catalysis

Trapping of trifluoroacetonitrile imines with mercaptoacetaldehyde and mercaptocarboxylic acids: An access to fluorinated 1,3,4-thiadiazine derivatives via (3+3)-annulation

(2019) Greta Utecht-Jarzyńska et al.   JOURNAL OF FLUORINE CHEMISTRY

Metal‐Free Synthesis of 5‐Trifluoromethyl‐1,2,4‐Triazoles from Iodine‐Mediated Annulation of Trifluoroacetimidoyl Chlorides and Hydrazones

(2019) Sipei Hu et al.   ADVANCED SYNTHESIS & CATALYSIS

Deconstructive Oxygenation of Unstrained Cycloalkanamines

(2019) Jian-Wu Zhang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Polysubstituted 3-trifluoromethylpyrazoles: regioselective (3 + 2)-cycloaddition of trifluoroacetonitrile imines with enol ethers and functional group transformations

(2018) Greta Utecht et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Transition-Metal-Free [3 + 2] Cycloaddition of Nitroolefins and Diazoacetonitrile: A Facile Access to Multisubstituted Cyanopyrazoles

(2018) Zhen Chen et al.   ORGANIC LETTERS

A Straightforward Access to Trifluoromethylated Spirobipyrazolines through a Double (3+2)-Cycloaddition of Fluorinated Nitrile Imines with Alkoxyallenes

(2018) Marcin Jasiński et al.   SYNLETT

Expeditious Synthesis of 6-Fluoroalkyl-Phenanthridines via Palladium-Catalyzed Norbornene-Mediated Dehydrogenative Annulation

(2018) Zhuo Wang et al.   ORGANIC LETTERS

First (3+2)-Cycloadditions of Thiochalcones as C=S Dipolarophiles: Efficient Synthesis of 1,3,4-Thiadiazoles via Reactions with Fluorinated Nitrile Imines

(2017) Grzegorz Mlostoń et al.   SYNTHESIS-STUTTGART

Fluoroalkyl-Substituted Diazomethanes and Their Application in a General Synthesis of Pyrazoles and Pyrazolines

(2016) Lucas Mertens et al.   CHEMISTRY-A EUROPEAN JOURNAL

Trifluoromethylated 2,3-dihydro-1,3,4-thiadiazoles via the regioselective [3+2]-cycloadditions of fluorinated nitrile imines with aryl, hetaryl, and ferrocenyl thioketones

(2016) Grzegorz Mlostoń et al.   JOURNAL OF FLUORINE CHEMISTRY

2-(Trifluoromethyl)indoles via Pd(0)-Catalyzed C(sp3)–H Functionalization of Trifluoroacetimidoyl Chlorides

(2016) Julia Pedroni et al.   ORGANIC LETTERS

I2-Catalyzed Oxidative Coupling Reactions of Hydrazones and Amines and the Application in the Synthesis of 1,3,5-Trisubstituted 1,2,4-Triazoles

(2016) Zhengkai Chen et al.   ORGANIC LETTERS

Bond-shift isomers: the co-existence of allenic and propargylic phenylnitrile imines

(2015) Cláudio M. Nunes et al.   CHEMICAL COMMUNICATIONS

Silver-catalyzed regioselective [3+2] cycloaddition of arene-diazonium salts with 2,2,2-trifluorodiazoethane (CF3CHN2): a facile access to 2-aryl-5-trifluoromethyltetrazoles

(2015) Zhen Chen et al.   CHEMICAL COMMUNICATIONS

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Three-component synthesis of fluorinated pyrazoles from fluoroalkylamines, NaNO2 and electron-deficient alkynes

(2015) Pavel K. Mykhailiuk   ORGANIC & BIOMOLECULAR CHEMISTRY

Chemoselectivity in 1,3-Dipolar Cycloaddition Reactions of Nitrilimines with Multifunctionalized Dipolarophiles

(2014) Ahmad S. Shawali   CURRENT ORGANIC CHEMISTRY

One-Pot Synthesis of CF3-Substituted Pyrazolines/Pyrazoles from Electron-Deficient Alkenes/Alkynes and CF3CHN2Generated in situ: Optimized Synthesis of Tris(trifluoromethyl)pyrazole

(2014) Evgeniy Y. Slobodyanyuk et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Microwave-assisted synthesis of 1-aryl-5-(trifluoromethyl)-1H-tetrazoles

(2014) Fariba Rahmani et al.   JOURNAL OF FLUORINE CHEMISTRY

Palladium-catalyzed intramolecular C−H bond functionalization of trifluoroacetimidoyl chloride derivatives: Synthesis of 6-trifluoromethyl-phenanthridines

(2014) Mei Zhu et al.   JOURNAL OF FLUORINE CHEMISTRY

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

(2014) Fa-Guang Zhang et al.   ORGANIC LETTERS

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

(2013) Feng Li et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Visible-Light-Induced Radical Cyclization of Trifluoroacetimidoyl Chlorides with Alkynes: Catalytic Synthesis of 2-Trifluoromethyl Quinolines

(2013) Xichang Dong et al.   CHEMISTRY-A EUROPEAN JOURNAL

Synthesis of 6-(Trifluoromethyl)phenanthridines via Palladium-Catalyzed Tandem Suzuki/C–H Arylation Reactions

(2013) Wen-Ying Wang et al.   JOURNAL OF ORGANIC CHEMISTRY

Au(I)-Catalyzed Intramolecular Hydroamination of the Fluorinated N′-Aryl-N-Propargyl Amidines: Mild Conditions for the Synthesis of 2-Fluoroalkyl Imidazole Derivatives

(2012) Shan Li et al.   ORGANIC LETTERS

An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

(2011) Marcus Baumann et al.   Beilstein Journal of Organic Chemistry

Celecoxib

(2011) Paul L. McCormack   DRUGS

An efficient method to access 2-fluoroalkylbenzimidazoles by PIDA oxidation of amidines

(2011) Jiangtao Zhu et al.   JOURNAL OF FLUORINE CHEMISTRY

Efficient Synthesis of 2-Fluoromethylated Quinolines via Copper-Catalyzed Alkynylation and Cyclization of Fluorinated Imidoyl Iodides

(2010) Shan Li et al.   ADVANCED SYNTHESIS & CATALYSIS

Palladium catalyzed synthesis of 2-trifluoromethylquinolines through a domino Sonogashira–alkyne carbocyclization process

(2010) Zixian Chen et al.   CHEMICAL COMMUNICATIONS

Synthesis and Biological Evaluation of 3-Biphenyl-4-yl-4-phenyl-4H-1,2,4-triazoles as Novel Glycine Transporter 1 Inhibitors

(2010) Takashi Sugane et al.   JOURNAL OF MEDICINAL CHEMISTRY

Copper-Catalyzed Thiolation Annulations of 1,4-Dihalides with Sulfides Leading to 2-Trifluoromethyl Benzothiophenes and Benzothiazoles

(2010) Chun-Lin Li et al.   JOURNAL OF ORGANIC CHEMISTRY

A General and Straightforward Method for the Synthesis of 2-Trifluoromethylbenzothiazoles

(2010) Jiangtao Zhu et al.   ORGANIC LETTERS

Palladium-Catalyzed Chloroimination of Imidoyl Chlorides to a Triple Bond: An Intramolecular Reaction Leading to 4-Chloroquinolines

(2008) Akira Isobe et al.   ORGANIC LETTERS

Fluorine in medicinal chemistry

(2007) Sophie Purser et al.   CHEMICAL SOCIETY REVIEWS