Category: 113421-98-0

Adding a certain compound to certain chemical reactions, such as: 113421-98-0, name is 4-Fluoro-3-(trifluoromethoxy)aniline, belongs to ethers-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 113421-98-0, name: 4-Fluoro-3-(trifluoromethoxy)aniline

General procedure: Ethyl 4-bromo-1H-indole-2-carboxylate (1 eq), Pd2(dba)3 (0.1 eq), X-phos(0.2 eq), Cs2CO3 (3 eq) and aryl amine (3 eq) was added to a microwave tube,dissolved in 1,4-dioxane, and filled with argon gas. The microwave reaction wascarried out at 100 C for 0.5-1.5 h, and the starting material disappeared. The mixturewas cooled to room temperature and concentrated. Ethyl acetate was added todissolve the residue, and the mixture was washed with saturated brine and water, driedover anhydrous Na2SO4, and concentrated in vacuo. The crude product was purifiedby column chromatography to afford the target compound. Compounds 8m-8o, 8s,8a-3 ~ 8a-5, 8a-13, 8a-15 ~ 8a-17, 8o-1 ~ 8o-24 were prepared with method 3.

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Reference:
Article; Cui, Guonan; Lai, Fangfang; Wang, Xiaoyu; Chen, Xiaoguang; Xu, Bailing; European Journal of Medicinal Chemistry; vol. 188; (2020);,
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Reference of 113421-98-0,Some common heterocyclic compound, 113421-98-0, name is 4-Fluoro-3-(trifluoromethoxy)aniline, molecular formula is C7H5F4NO, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

General procedure: Ethyl 4-bromo-1H-indole-2-carboxylate (1 eq), Pd2(dba)3 (0.1 eq), X-phos(0.2 eq), Cs2CO3 (3 eq) and aryl amine (3 eq) was added to a microwave tube,dissolved in 1,4-dioxane, and filled with argon gas. The microwave reaction wascarried out at 100 C for 0.5-1.5 h, and the starting material disappeared. The mixturewas cooled to room temperature and concentrated. Ethyl acetate was added todissolve the residue, and the mixture was washed with saturated brine and water, driedover anhydrous Na2SO4, and concentrated in vacuo. The crude product was purifiedby column chromatography to afford the target compound. Compounds 8m-8o, 8s,8a-3 ~ 8a-5, 8a-13, 8a-15 ~ 8a-17, 8o-1 ~ 8o-24 were prepared with method 3.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Fluoro-3-(trifluoromethoxy)aniline, its application will become more common.

Reference:
Article; Cui, Guonan; Lai, Fangfang; Wang, Xiaoyu; Chen, Xiaoguang; Xu, Bailing; European Journal of Medicinal Chemistry; vol. 188; (2020);,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Adding a certain compound to certain chemical reactions, such as: 113421-98-0, name is 4-Fluoro-3-(trifluoromethoxy)aniline, belongs to ethers-buliding-blocks compound, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 113421-98-0, COA of Formula: C7H5F4NO

4-fluoro-3-(trifluoromethoxy)aniline (99i mg, 5.08 mmol) dissolved in toluene (iO mL) wasadded to 4-chlorosulfonyl-i-methyl-pyrrole-2-carbonyl chloride (i.23 g, 5.079 mmo) in toluene (65 mL) at reflux and refluxed 2 hours. The reaction mixture was filtered while still hot and concentrated yielding crude 5- [[4-fluoro-3 -(trifluoromethoxy)phenyl] carbamoyl] – i-methylpyrrole-3-sulfonyl chloride as a beige powder which was used as such.?H NMR (400 MHz, acetonitrile-d3) oe ppm 3.97 (s, 3 H), 7.27 – 7.35 (m, i H), 7.38 (d, J2.0 Hz, i H), 7.57 (ddd,J9.0, 4.0, 2.6 Hz, i H), 7.73 (d, Ji.5 Hz, i H), 7.87 – 7.94 (m, i H), 8.79 (br. s., i H).

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it.

Reference:
Patent; JANSSEN R&D IRELAND; VANDYCK, Koen; HACHE, Geerwin, Yvonne, Paul; LAST, Stefaan, Julien; MC GOWAN, David, Craig; ROMBOUTS, Geert; VERSCHUEREN, Wim, Gaston; RABOISSON, Pierre, Jean-Marie, Bernard; WO2014/184350; (2014); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Application of 113421-98-0,Some common heterocyclic compound, 113421-98-0, name is 4-Fluoro-3-(trifluoromethoxy)aniline, molecular formula is C7H5F4NO, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

4-bromo-6-acetylamino-1H-indole-2-carboxylic acid ethyl ester (100 mg, 0.31 mmol), Pd2 (dba) 3 (28 mg, 0.031 mmol), X-phos (30 mg, 0.062 mmol), Cs2CO3 (301 mg, 0.92 mmol) and 3-trifluoromethoxy-4-fluoroaniline (172 mg, 0.92 mmol) were added to a microwave tube, dissolved in 1,4-dioxane (2 mL), and filled with argon Gas-protected, microwave reaction at 100 C for 0.5h, the raw materials disappeared. Cool to room temperature, add EA (20mL), wash with saturated brine (20mL ¡Á 3), wash with water (20mL ¡Á 2), and column chromatography (P / E = 2: 1) to obtain 84mg of a white solid with a yield of 62.2% and a melting point. : 205-206 C.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Fluoro-3-(trifluoromethoxy)aniline, its application will become more common.

Reference:
Patent; Chinese Academy Of Medical Sciences Pharmaceutical Institute; Xu Boling; Chen Xiaoguang; Cui Guonan; Lai Fangfang; Zhou Jie; Ji Ming; Wang Xiaoyu; Du Tingting; Li Ling; Jin Jing; (144 pag.)CN110483366; (2019); A;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem