Category: 57946-63-1

Adding a certain compound to certain chemical reactions, such as: 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, belongs to bromides-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 57946-63-1, HPLC of Formula: C7H5BrF3N

Example 139 Synthesis of 5- [Acetyl- (3, 5-bis-trifluoromethyl-benzyl)-amino]-7-trifluoromethyl-2, 3,4, 5- tetrahydro-benzo [b] azepine-1-carboxylic acid tert-butyl ester. Step 1. Preparation of Methyl-3-trifluoromethyl-2-aminobenzoate Add palladium (II) acetate (1.89 g, 8.4 mmol), 1,1- bis (diphenylphosphino) ferrocene (6.83 g, 12.3 mmol), and triethyl amine (32 mL, 44.0 mmol) to a solution of 2-bromo-4-trifluoromethylanaline (10.0 g, 42.0 mmol) in dimethylsulfoxide (283 mL) and methanol (187 mL). At 100 psi of carbon monoxide, heat the mixture to 80 °C. After heating for 14-16 h cool the reaction to room temperature and filter. Dilute the organics with ethyl acetate (500 mL), wash with water (3×200 mL) and brine (200 mL). Dry the organics over sodium sulfate and filter. Remove solvent under vacuum and chromatograph the crude product using ethyl acetate/hexane (10 percent) to elute. This provides the title compound (8.0 g, 88percent) as an off white solid: H NMR (CDC13,400 MHz) 8 3.93 (s, 3H), 6.11 (bs, 2H), 6.73 (d, J = 8.4 Hz, 1H), 7.49 (dd, J = 2.0, 8.4 Hz, 1H), 8.17 (d, J = 2.0 Hz, 1H).

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; ELI LILLY AND COMPANY; WO2005/37796; (2005); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, belongs to bromides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Quality Control of 2-Bromo-4-(trifluoromethyl)aniline

Reference Example 57 4-[2-{[2-Bromo-4-(trifluoromethyl)phenyl]amino}-4-chloro-7-(1-ethylpropyl)-1H-benzimidazol-1-yl]butan-1-ol A mixture of ethyl 4-[2,4-dichloro-7-(1-ethylpropyl)-1H-benzimidazol-1-yl]butanoate (Reference Example 33; 2.24 g, 6.63 mmol), 2-bromo-4-trifluoromethylaniline (3.18 g, 13.25 mmol), p-toluenesulfonic acid monohydrate (1.35 g, 7.09 mmol) and xylene (5.0 mL) was stirred at 130° C. for 15 hr. After cooling, the reaction mixture was neutralized with aqueous saturated sodium hydrogen carbonate and extracted with ethyl acetate (*3). The combined organic layer was washed with brine, dried over anhydrous magnesium sulfate, filtered and concentrated in vacuo. The residue was purified by silica gel column chromatography eluding with a 0-15percent ethyl acetate/n-hexane gradient mixture to give crude ethyl 4-[2-{[2-bromo-4-(trifluoromethyl)phenyl]amino}-4-chloro-7-(1-ethylpropyl)-1H-benzimidazol-1-yl]butanoate. The crude material (MS Calcd.: 573; Found: 574 (M+H)) was subjected for the next step without further purification.

The synthetic route of 57946-63-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; US2009/186879; (2009); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, This compound has unique chemical properties. The synthetic route is as follows., name: 2-Bromo-4-(trifluoromethyl)aniline

To a 100-mLround-bottom flask was placed a solution of 2-bromo-4-(trifluoromethyl)aniline (4.8 g,20.00mmol) in THF (20 mL) then DMAP (488 mg,3.99 mmol) and Boc2O (8.72 g) were added. The reaction was heated to reflux overnight then concentrated under reduced pressure. The residue was purified by column chromatography eluting with EtOAc/petroleum ether (1:50) affording 7.9 g of the title compound as a white solid. 1H NMR (300 MHz,CDCl3): oe 7.89 (s,1H ),7.62-7.59 (d,J = 9.0 Hz,1H ),7.38-7.35 (d,J = 9.0 Hz,1H ),1.42 (s,9H).

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 57946-63-1.

Reference:
Patent; PROTEOSTASIS THERAPEUTICS, INC.; MUNOZ, Benito; BASTOS, Cecilia, M.; PARKS, Daniel; KOMBO, David; (301 pag.)WO2017/62581; (2017); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Reference of 57946-63-1,Some common heterocyclic compound, 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, molecular formula is C7H5BrF3N, 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.

A round-bottom flask was charged with 2-bromo-4-(trifluoromethyl)aniline (4.115 g, 17.14 mmol), l-methyl-5-(4,4,5,5-tetramethyl-l ,3,2-dioxaborolan-2-yl)-lH- pyrazole (4.64 g, 22.29 mmol), potassium phosphate (10.92 g, 51.4 mmol), and Pd(AmPhos)2Ci2 (0.607 g, 0.857 mmol). Dioxane (30 mL) and water (10 mL) were added to give a thick suspension. The flask was fitted with a reflux condenser and placed in a 90 ¡ãC oil bath for 4 h. The mixture was removed from the heat, then diluted with water and extracted with EtOAc (3x). The combined organic extracts were dried over sodium sulfate, filtered and concentrated. The residue was partially purified twice by chromatography on silica gel, first with 25 to 75percent EtO Ac/Heptane, then with 20 to70percent EtO Ac/Heptane. The partially purified material thus obtained was dissolved in methanol and loaded onto a lOg SCX-2 ion exchange column. The column was eluted with methanol, then with 2N ammonia in methanol. The basic fractions were combined and concentrated to give 2-(l-methyl-lH-pyrazol-5-yl)-4-(trifluoromethyl)aniline (0.5526 g, 2.291 mmol, 13.36 percent yield) as a tan solid. 1H NMR (400 MHz, DMSO-d6) delta = 7.52 (d, J = 1.9 Hz, 1 H), 7.43 (ddd, J = 0.5, 2.3, 8.6 Hz, 1 H), 7.26 (d, J = 1.9 Hz, 1 H), 6.88 (d, J = 8.5 Hz, 1 H), 6.32 (d, J = 1.9 Hz, 1 H), 5.62 (s, 2 H), 3.64 (s, 3 H). m/z (ESI) 242.2 (M+H)+.

The synthetic route of 57946-63-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DINEEN, Thomas; MARX, Isaac, E.; NGUYEN, Hanh, Nho; WEISS, Matthew; AMGEN INC.; WO2013/25883; (2013); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Reference of 57946-63-1,Some common heterocyclic compound, 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, molecular formula is C7H5BrF3N, 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.

Into a 50-mL round-bottom flask purged and maintained with an inert atmosphere of nitrogen, was placed a solution of 2-bromo-4-(trifluoromethyl)benzenamine (1 g, 4.17 mmol, 1.00 equiv) in DMSO (20 mL), 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1,3,2-dioxaborolane (1.58 g, 6.22 mmol, 1.50 equiv), PdCl2(dppf) (91 mg, 0.12 mmol, 0.03 equiv), potassium acetate (1 g, 10.40 mmol, 2.57 equiv). The resulting solution was stirred overnight at 80¡ã C. in an oil bath. The resulting mixture was combined with the solution of the previous batch and then diluted with 100 mL of ethyl acetate. The resulting mixture was washed with 2*100 mL of brine. The mixture was dried over anhydrous sodium sulfate and concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (1:100). This resulted in 1.2 g of 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-4-(trifluoromethyl)benzenamine as a yellow solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-Bromo-4-(trifluoromethyl)aniline, its application will become more common.

Reference:
Patent; Ardelyx, Inc.; Lewis, Jason G.; Jacobs, Jeffrey W.; Reich, Nicholas; Leadbetter, Michael R.; Bell, Noah; Chang, Han-Ting; Chen, Tao; Navre, Marc; Charmot, Dominique; Carreras, Christopher; Labonte, Eric; (323 pag.)US9301951; (2016); B2;,
Bromide – Wikipedia,
bromide – Wiktionary

Reference of 57946-63-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline belongs to bromides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below.

Heat a mixture of copper [(1)] cyanide (2.24g, 25.00 mmol), and 2-bromo-4- trifluoromethyl-phenylamine [(5.] [0G,] 20.83 mmol from Avocado) in [ L-METHYL-2-] pyrrolidinone (20 ml) to [195 ¡ãC] for four hours. Dilute the reaction mixture with 100 ml of ethyl acetate and wash the dark solution twice with 28percent aqueous ammonium hydroxide, twice with saturated aqueous sodium chloride (brine) and twice with water. Collect the organic layer, dry over sodium sulfate and remove the solvent under reduced pressure. Purify the residue via flash chromatography eluting with a step gradient starting with hexanes and going to 70percent hexanes with 30percent ethyl acetate to obtain 1. [821G] (9.78 mmol, 47percent yield) the title compound as a green amorphous solid: Mass Spectrum (m/e): 187 (M+1).

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 2-Bromo-4-(trifluoromethyl)aniline, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; ELI LILLY AND COMPANY; WO2004/14895; (2004); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps, and cheap raw materials. 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, A new synthetic method of this compound is introduced below., Recommanded Product: 57946-63-1

General procedure: Under argon condition [26], p-TsCl (p-toluenesulfonyl, 1.2 mmol) in 2 mL dichloromethane was injected to the 2 mL dichloromethane mixture of compounds 1?9 (1 mmol) and 4-dimethylaminopyridine (2.4 mmol) at reflux temperature. The aromatic amine or heteroaromatic amine (1.2 mmol) was injected to the reaction mixture 2 h later. The mixture was stirred for another 2 h. After removing solvent in vacuo, the residue was quenched with EtOAc and water, neutralized with sat. NaHCO3 solvent, the EtOAc layer was dried over anhydrous Na2SO4 and concentrated. The residue was chromatographed on silica gel (EtOAc?petroleum ether) to give target compounds. The structures of compounds 1a-9s were showed in the Supporting information.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Article; Liu, Ye; Lei, Chao; Xu, Xiao-Yong; Shao, Xu-Sheng; Li, Zhong; Chinese Chemical Letters; vol. 27; 3; (2016); p. 321 – 324;,
Bromide – Wikipedia,
bromide – Wiktionary

Application of 57946-63-1, The chemical industry reduces the impact on the environment during synthesis 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, I believe this compound will play a more active role in future production and life.

In an air atmosphere, 1.0 mmol of o-hydroxybenzyl alcohol was added to a 10 ml flask,1.3 mmol of 4-trifluoromethyl-2-bromoaniline, 0.05 mmol of p-cymene ruthenium dichloride dimer, 0.1 mmol of cuprous chloride, 0.1 mmol of 1,1′-bis (diphenylphosphine) Ferrocene, 9.0 mmol of potassium tert-butoxide,And 5ml of xylene, and then placed on a condenser with magnetic stirring with an oil bath heated to 120 ,The reaction for 12 hours. The oil bath was removed, 3 ml of water was added to the reaction mixture, the mixture was extracted three times with 5 ml of ethyl acetate,The organic phases were combined and dried over anhydrous MgSO4 for 30 minutes and filtered; the filtrate was usedThe product was concentrated on a rotary evaporator. The concentrated solid was recrystallized from dichloromethane to give pure product 6 in 87percent yield.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles, 2-Bromo-4-(trifluoromethyl)aniline, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Luoyang Normal College; Xu Chen; Li Hongmei; Wang Zhiqiang; Lou Xinhua; Fu Weijun; (11 pag.)CN105949143; (2016); A;,
Bromide – Wikipedia,
bromide – Wiktionary

These common heterocyclic compound, 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, its 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. SDS of cas: 57946-63-1

A solution of 2-bromo-4-(trifluoromethyl)aniline(5g, 20.83 mmol), tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate (6.34g, 20.83 mmol), and sodium carbonate(5.52g, 52.1 mmol) in toluene (30 ml) / water (20 ml) Ethanol (10 ml), N2 was purged for 10 mm. then Tetrakistriphenyl phosphinePd (0) (2.407g, 2.083 mmol) was charged and stirred at 95 ¡ãC for 4h. After completion of reaction as indicated by TLC, the mixture was poured into water and extracted with ethyl acetate. The organic layer was collected anddried over sodium sulphate, finally evaporated and purified by column chromatography(4.5g, 64 percent). LCMS (ESI): m/z 338.10(M+H).

The synthetic route of 2-Bromo-4-(trifluoromethyl)aniline has been constantly updated, and we look forward to future research findings.

Reference:
Patent; LUPIN LIMITED; RAMDAS, Vidya; LORIYA, Rajeshkumar, Maganlal; BANERJEE, Moloy; PATIL, Pradeep, Rangrao; JOSHI, Advait, Arun; DATRANGE, Laxmikant, Shamlal; WALKE, Deepak, Sahebrao; KHAN, Talha, Hussain; DAS, Amit, Kumar; GOTE, Ganesh, Navinchandra; KALHAPURE, Vaibhav, Madhukar; PALLE, Venkata, P.; KAMBOJ, Rajender, Kumar; (234 pag.)WO2017/37682; (2017); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Some common heterocyclic compound, 57946-63-1, name is 2-Bromo-4-(trifluoromethyl)aniline, molecular formula is C7H5BrF3N, 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. 57946-63-1

2-Bromo-4-(trifluoromethyl)aniline (3. 5g, 14.58 mmol), 1H-pyrazole (1 .98g, 29.2 mmol), N1,N2-dimethylethane-1,2-diamine (0.78 ml, 7.29 mmol), cesium carbonate (10.45g, 32.1 mmol) was added to degassed 1,4-dioxane (15 ml) in a sealed tube and copper(i) iodide (0.55g, 2.92 mmol) was added. The tube was sealed and heated at 120 ¡ãC for 72h. After the solution was cooled, the mixture was passed through a pad of celite and the filtrate was extracted with ethyl acetate. The ethyl acetate layer was washed withbrine, dried over Na2SO4 and concentrated. The crude was purified by column chromatography to obtain the product as off white solid (2.7g, 83percent). LCMS (ESI): mlz 228.39(M+H)+.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 57946-63-1, its application will become more common.

Reference:
Patent; LUPIN LIMITED; RAMDAS, Vidya; LORIYA, Rajeshkumar, Maganlal; BANERJEE, Moloy; PATIL, Pradeep, Rangrao; JOSHI, Advait, Arun; DATRANGE, Laxmikant, Shamlal; WALKE, Deepak, Sahebrao; KHAN, Talha, Hussain; DAS, Amit, Kumar; GOTE, Ganesh, Navinchandra; KALHAPURE, Vaibhav, Madhukar; PALLE, Venkata, P.; KAMBOJ, Rajender, Kumar; (234 pag.)WO2017/37682; (2017); A1;,
Bromide – Wikipedia,
bromide – Wiktionary