- Transition metal-free direct C–H trifluoromethyltion of (hetero)arenes with Togni's reagent
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A new transition-metal-free direct C–H trifluoromethylation reaction of (hetero)arenes with Togni's reagent was developed. This transformation proceeded smoothly under mild conditions and exhibited good tolerance of many synthetically relevant functional groups. It provided an alternative approach for the synthesis of trifluoromethylated (hetero)arenes.
- Chen, Xiaoyu,Ding, Licheng,Li, Linlin,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
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supporting information
(2019/12/30)
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- Preparation method of trifluoromethylated aniline compound
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The invention provides a preparation method of a trifluoromethylated aniline compound shown in a formula (IIA) or a formula (IIB). The method comprises the following steps: by taking a mixed solvent of DMF and water in a volume ratio of 1:(1-4) as a reaction medium, adding an aniline compound shown in a formula (IA) or a formula (IB), 1-(trifluoromethyl)-1,2-benziodoxol-3-(1H)-one and a photocatalyst, and reacting for 2-6 hours at room temperature under blue light; and carrying out post-treatment on the obtained reaction mixture to obtain the trifluoromethylated aniline compound as shown in the formula (IIA) or the formula (IIB). According to the method, by the photocatalyst, the reaction is driven to be carried out under the irradiation of visible light, the reaction conditions are mild,the site selectivity is high, the reaction is efficient, green and environment-friendly, the reaction yield can reach 90%, and the product can be prepared by only one step.
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Paragraph 0104-0112
(2020/12/30)
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- Nickel-Catalyzed Direct C-H Trifluoromethylation of Free Anilines with Togni's Reagent
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An efficient nickel-catalyzed C-H trifluoromethylation for the synthesis of trifluoromethylated free anilines using Togni's reagent has been developed. This approach exhibits a good functional group tolerance, good regioselectivity, and chemoselectivity under mild conditions. The newly developed economical one-step method is a better alternative to synthesize trifluoromethylated free anilines.
- Gao, Xianying,Geng, Yang,Han, Shuaijun,Liang, Apeng,Li, Jingya,Zou, Dapeng,Wu, Yusheng,Wu, Yangjie
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supporting information
p. 3732 - 3735
(2018/07/22)
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- Preparation method of trifluoromethylamine
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The invention relates to a preparation method of trifluoromethylamine. The method includes the following steps that aromatic amine shown in the formula (1) and a trifluoromethyl reagent shown in the formula (2) react in a solvent under the condition that an alkali and/or nickel compound exists, and the trifluoromethylamine compound shown in the formula (3) is generated. According to the preparation method of trifluoromethylamine, aromatic amine and 1-trifluoromethyl-1,2-iodobenzoyl-3(H)-ketone serve as raw materials and react under the condition that the alkali and/or nickel compound exists through the amino positioning effect on aromatic nucleus. The synthesis steps of the method are simple, the cost of the raw materials is low, the production cost of trifluoromethylamine can be greatly reduced, and large-scale industrialized production is promoted.
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Paragraph 0150-0154
(2018/09/28)
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- A for the preparation of ortho-trifluoromethyl-aniline or its derivatives (by machine translation)
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The invention discloses a method for preparing o-trifluoromethyl phenylamine and derivatives thereof. According to the method, phenylamine or a phenylamine derivative serving as raw material reacts with a trivalent iodine reagent compound 2 in a solution under the protection of argon or nitrogen and illumination condition in the presence of tri(2-phenylpyridine)-iridium [Ir(ppy)3] serving as a catalyst to produce o-trifluorophenylamine or derivatives thereof 3, wherein the trivalent iodine reagent compound 2 has a structure shown in the specification. The method is mild in reaction conditions, the amino does not need to be protected, and trifluoromethyl substituted phenylamine or phenylamine derivatives can be directly obtained.
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Paragraph 0025-0026
(2016/10/24)
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- Visible-light-promoted radical C-H trifluoromethylation of free anilines
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The trifluoromethyl-substituted anilines are biologically active compounds and useful building blocks. In this communication, we have developed the first visible-light-induced radical trifluoromethylation of free anilines with the commercially available and easily handled Togni reagent at room temperature. The resulting products were successfully transformed into a variety of valuable fluorine-containing molecules and heterocyclic compounds. This protocol provides an economical and powerful route to trifluoromethylated free anilines.
- Xie, Jin,Yuan, Xiangai,Abdukader, Ablimit,Zhu, Chengjian,Ma, Jing
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supporting information
p. 1768 - 1771
(2014/04/17)
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- Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents
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This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
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