journal article·2020-08Open access

Photoredox Catalytic Trifluoromethylation and Perfluoroalkylation of Arenes Using Trifluoroacetic and Related Carboxylic Acids

Dehang Yin, Dengquan Su, Jian Jin

Cell Reports Physical Science· Volume 1· Issue 8

Abstract

Trifluoroacetic acid (TFA) is among the most attractive trifluoromethylation reagents with respect to its low prices, ease of handling, and availability in large quantities. However, because of its exceedingly high oxidation potential, harsh conditions are required for the direct oxidation of TFA to the trifluoroacetate radical, which after prompt CO2 extrusion, affords the desired CF3 radical. Therefore, mild and efficient protocols for the direct conversion of TFA to the CF3 radical are still in high demand. Here, we report a mild and practical method that allows for the direct C–H trifluoromethylation, perfluoroalkylation, and chlorodifluoromethylation of (hetero)arenes using TFA and the related carboxylic acids. A diverse array of arenes and heteroarenes were successfully transformed into valued fluoroalkylated compounds. The combination of photoredox catalysis and a diaryl sulfoxide provides a platform for the facile generation of fluoroalkyl radicals from the corresponding fluoroalkyl carboxylic acids under mild conditions.
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Research context

OpenAlex topics: Fluorine in Organic Chemistry · Inorganic Fluorides and Related Compounds

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

References (84)

Show source-provided references
1. Fluorine in pharmaceuticals: looking beyond intuition10.1126/science.1131943 ↗
2. Fluorine in medicinal chemistry10.1039/B610213C ↗
3. Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001-2011)10.1021/cr4002879 ↗
4. Next Generation of Fluorine-Containing Pharmaceuticals, Compounds Currently in Phase II-III Clinical Trials of Major Pharmaceutical Companies: New Structural Trends and Therapeutic Areas10.1021/acs.chemrev.5b00392 ↗
5. Catalysis for fluorination and trifluoromethylation10.1038/nature10108 ↗
6. Introduction of fluorine and fluorine-containing functional groups10.1002/anie.201206566 ↗
7. Late-Stage Fluorination: From Fundamentals to Application10.1021/op400349g ↗
8. Modern carbon-fluorine bond forming reactions for aryl fluoride Modern carbon-fluorine bond forming reactions for aryl fluoride synthesis10.1021/cr500366b ↗
9. Facile C-F Bond Formation through a Concerted Nucleophilic Aromatic Substitution Mediated by the PhenoFluor Reagent10.1021/acs.accounts.7b00413 ↗
10. Aromatic trifluoromethylation with metal complexes10.1021/cr1004293 ↗
11. Carbon trifluoromethylation reactions of hydrocarbon derivatives and heteroarenes10.1021/cr500368h ↗
12. Facile Ar-CF3 bond formation at Pd. Strikingly different outcomes of reductive elimination from [(Ph3P)2Pd(CF3)Ph] and [(Xantphos)Pd(CF3)Ph]10.1021/ja064935c ↗
13. Active trifluoromethylating agents from well-defined Copper(I)-CF3 complexes10.1021/ja802946s ↗
14. The palladium-catalyzed trifluoromethylation of aryl chlorides10.1126/science.1190524 ↗
15. Aryl-CF(3) bond-forming reductive elimination from palladium(IV)10.1021/ja100955x ↗
16. Copper-mediated trifluoromethylation of heteroaromatic compounds by trifluoromethyl sulfonium salts10.1002/anie.201006823 ↗
17. Mechanistic and computational studies of oxidatively-induced aryl-CF3 bond-formation at Pd: rational design of room temperature aryl trifluoromethylation10.1021/ja201726q ↗
18. A broadly applicable copper reagent for trifluoromethylations and perfluoroalkylations of aryl iodides and bromides10.1002/anie.201100633 ↗
19. A broadly applicable [18F]trifluoromethylation of aryl and heteroaryl iodides for PET imaging10.1038/nchem.1756 ↗
20. Rapid and efficient trifluoromethylation of aromatic and heteroaromatic compounds using potassium trifluoroacetate enabled by a flow system10.1002/anie.201306094 ↗
21. A radical approach to the copper oxidative addition problem: trifluoromethylation of bromoarenes10.1126/science.aat4133 ↗
22. Copper-mediated oxidative trifluoromethylation of boronic acids10.1021/ol1023135 ↗
23. Room temperature aryl trifluoromethylation via copper-mediated oxidative cross-coupling10.1021/jo1023377 ↗
24. Copper-catalyzed trifluoromethylation of aryl boronic acids using a CF3+ reagent10.1039/c1cc10359h ↗
25. Copper-catalyzed trifluoromethylation of aryl and vinyl boronic acids with an electrophilic trifluoromethylating reagent10.1021/ol2005903 ↗
26. Merging visible-light photocatalysis and transition-metal catalysis in the copper-catalyzed trifluoromethylation of boronic acids with CF3I10.1021/ja301553c ↗
27. Practical method for the Cu-mediated trifluoromethylation of arylboronic acids with CF3 radicals derived from NaSO2CF3 and tert-butyl hydroperoxide (TBHP)10.1021/ol3022726 ↗
28. Copper-catalyzed trifluoromethylation of aryl- and vinylboronic acids with generation of CF3-radicals10.1039/c2cc36554e ↗
29. Copper-mediated trifluoromethylation using phenyl trifluoromethyl sulfoxide10.1021/ol5034018 ↗
30. Trifluoromethylation of Arylsilanes with [(phen)CuCF3 ]10.1002/anie.201601163 ↗
31. Copper-promoted Sandmeyer trifluoromethylation reaction10.1021/ja404217t ↗
32. Silver-mediated trifluoromethylation of aryldiazonium salts: conversion of amino group into trifluoromethyl group10.1021/ja4056239 ↗
33. Sandmeyer trifluoromethylation of arenediazonium tetrafluoroborates10.1002/anie.201304276 ↗
34. Trifluoromethylation of arenediazonium salts with fluoroform-derived CuCF3 in aqueous media10.1039/C4CC04930F ↗
35. Pd(II)-catalyzed ortho-trifluoromethylation of arenes using TFA as a promoter10.1021/ja909522s ↗
36. Palladium-catalyzed oxidative trifluoromethylation of indoles at room temperature10.1002/chem.201100283 ↗
37. Ortho-trifluoromethylation of Functionalized Aromatic Triazenes10.1002/anie.201107414 ↗
38. Copper-catalyzed direct C-H oxidative trifluoromethylation of heteroarenes10.1021/ja209992w ↗
39. Pd(II)-catalyzed ortho trifluoromethylation of arenes and insights into the coordination mode of acidic amide directing groups10.1021/ja305259n ↗
40. Exceedingly fast copper(II)-promoted ortho C-H trifluoromethylation of arenes using TMSCF310.1002/anie.201404822 ↗
41. Aryl Sulfonium Salts for Site-Selective Late-Stage Trifluoromethylation10.1002/anie.201906672 ↗
42. Metal-Free Photoredox-Catalysed Formal C–H/C–H Coupling of Arenes Enabled by Interrupted Pummerer Activation10.1038/s41929-019-0415-3 ↗
43. A “Renaissance” in radical trifluoromethylation10.1002/anie.201202624 ↗
44. Rapid trifluoromethylation and perfluoroalkylation of five-membered heterocycles by photoredox catalysis in continuous flow10.1002/cssc.201301282 ↗
45. Condensed-phase, halogen-bonded CF3I and C2F5I adducts for perfluoroalkylation reactions10.1002/anie.201410954 ↗
46. Nickel-Catalyzed C–H Trifluoromethylation of Electron-Rich Heteroarenes10.1002/adsc.201600702 ↗
47. Strongly Reducing, Visible-Light Organic Photoredox Catalysts as Sustainable Alternatives to Precious Metals10.1002/chem.201702926 ↗
48. Palladium-Catalyzed Trifluoromethylation of (Hetero)Arenes with CF3 Br10.1002/anie.201511131 ↗
49. Trifluoromethylation of arenes and heteroarenes by means of photoredox catalysis10.1038/nature10647 ↗
50. Graphitic carbon nitride polymer as a recyclable photoredox catalyst for fluoroalkylation of arenes10.1002/chem.201405505 ↗
51. Trifluoromethanesulfonic Anhydride as a Low-Cost and Versatile Trifluoromethylation Reagent10.1002/anie.201803566 ↗
52. Catalyst-Free and Redox-Neutral Innate Trifluoromethylation and Alkylation of Aromatics Enabled by Light10.1021/jacs.7b08685 ↗
53. Rhenium-Catalyzed Trifluoromethylation of Arenes and Heteroarenes by Hypervalent Iodine Reagents10.1021/cs300089y ↗
54. Electrophilic trifluoromethylation by use of hypervalent iodine reagents10.1021/cr500223h ↗
55. Direct Aromatic C-H Trifluoromethylation via an Electron-Donor-Acceptor Complex10.1002/chem.201500896 ↗
56. Nickel(IV)-Catalyzed C-H Trifluoromethylation of (Hetero)arenes10.1021/jacs.9b06383 ↗
57. Silver-mediated trifluoromethylation of arenes using TMSCF310.1021/ol202174a ↗
58. Silver-catalysed trifluoromethylation of arenes at room temperature10.1039/c3cc41829d ↗
59. Innate C-H trifluoromethylation of heterocycles10.1073/pnas.1109059108 ↗
60. Simple and Clean Photoinduced Aromatic Trifluoromethylation Reaction10.1021/jacs.6b02782 ↗
61. Sunlight decatungstate photoinduced trifluoromethylations of (hetero)aromatics and electron-poor olefins10.1039/c7pp00179g ↗
62. Visible-Light-Induced Trifluoromethylation of Highly Functionalized Arenes and Heteroarenes in Continuous Flow10.1055/s-0036-1588527 ↗
63. Organic semiconductor photocatalyst can bifunctionalize arenes and heteroarenes10.1126/science.aaw3254 ↗
64. Electrophotocatalytic Undirected C-H Trifluoromethylations of (Het)Arenes10.1002/chem.201905774 ↗
65. Practical and innate carbon-hydrogen functionalization of heterocycles10.1038/nature11680 ↗
66. Radical C-H functionalization of heteroarenes under electrochemical control10.1002/anie.201407948 ↗
67. Trifluoromethylation of Aromatic Compounds with Bis(trifluoroacetyl)10.1016/S0022-1139(00)82927-9 ↗
68. Metal-free Radical Perfluoroalkylation of (Hetero)arenes10.1039/C4RA13430C ↗
69. A scalable and operationally simple radical trifluoromethylation10.1038/ncomms8919 ↗
70. Photochemical Perfluoroalkylation with Pyridine N-Oxides: Mechanistic Insights and Performance on a Kilogram Scale10.1016/j.chempr.2016.08.002 ↗
71. Visible-Light Photoredox Decarboxylation of Perfluoroarene Iodine(III) Trifluoroacetates for C–H Trifluoromethylation of (Hetero)arenes10.1021/acscatal.7b03990 ↗
72. Direct Perfluoalkylation Including Trifluoromethylation of Aromatics with Perfluoro Carboxylic Acids Mediated by Xenon Difluoride10.1021/jo00254a033 ↗
73. Trifluoromethylation of Aromatic Compounds via Kolbe Electrolysis in Pure Organic Solvent. Study on Laboratory and Pilot Scale10.1039/a901305i ↗
74. Silver-catalyzed C-H trifluoromethylation of arenes using trifluoroacetic acid as the trifluoromethylating reagent10.1021/ol503189j ↗
75. A New Approach to the Photochemical Trifluoromethylation of Aromatic Compounds10.1039/c39930001359 ↗
76. Photo-driven redox-neutral decarboxylative carbon-hydrogen trifluoromethylation of (hetero)arenes with trifluoroacetic acid10.1038/ncomms14353 ↗
77. Ligand-Accelerated Iron Photocatalysis Enabling Decarboxylative Alkylation of Heteroarenes10.1021/acs.orglett.9b01439 ↗
78. Visible Light-Promoted Aliphatic C-H Arylation Using Selectfluor as a Hydrogen Atom Transfer Reagent10.1021/acs.orglett.9b01635 ↗
79. Green Oxidant H2O2 as a Hydrogen Atom Transfer Reagent for Visible Light-Mediated Minisci Reaction10.1039/C9NJ03106E ↗
80. Transition-Metal-Free Dehydrogenative N–N Coupling of Secondary Amines with KI/KIO410.1002/ejoc.201900763 ↗
81. Decarboxylative C–C and C–N Bond Formation by Ligand-Accelerated Iron Photocatalysis10.1002/ejoc.201901381 ↗
82. Intramolecular Aromatic C-H Acyloxylation Enabled by Iron Photocatalysis10.1021/acs.orglett.0c00002 ↗
83. Visible light photoredox catalysis with transition metal complexes: applications in organic synthesis10.1021/cr300503r ↗
84. Radical Chlorodifluoromethylation: Providing a Motif for (Hetero)arene Diversification10.1021/acs.orglett.8b01249 ↗