Category: 58458-10-9

Adding a certain compound to certain chemical reactions, such as: 58458-10-9, name is 3-Amino-2-bromobenzotrifluoride, 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 58458-10-9, Product Details of 58458-10-9

A mixture of 2-bromo-3-(tri r1uoromethyl)benzenamine (9.6 g; 40 mmol), 3,6-dihydro- 4-(4.4.5.5-tetramethyl- 1.3.2-dioxaborolan-2-yl )- 1.1-dimethylethylester- 1(2H)- pyridinecarboxilic acid (14.84 g; 48 mmol ). [l. l “-bis|bis( 1.1- dimethylethyl )phosphinoJferrocene]dichloro-palladium (652 mg; 1 mmol) and sodium carbonate (16.96 g; 160 mmol) in water (100 ml .) and THF (300 ml, ) was heated at reflux overnight. The solvent was removed under reduced pressure and the residue was solubilized with EtOAc and H20. The organic layer was separated, dried over MgSO.i, filtered and evaporated. The residue was purified by chromatography over silica gel (eluent: from 100% petrol ether to 50% petrol ether, 50% EtOAc). The pure fractions were collected and the solvent was evaporated to give 12 g (95%, white crystals) of intermediate 152

At the same time, in my other blogs, there are other synthetic methods of this type of compound, 3-Amino-2-bromobenzotrifluoride, and friends who are interested can also refer to it.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; MEVELLEC, Laurence, Anne; MEERPOEL, Lieven; COUPA, Sophie; PONCELET, Virginie, Sophie; PILATTE, Isabelle, Noelle, Constance; PASQUIER, Elisabeth, Therese, Jeanne; BERTHELOT, Didier, Jean-Claude; QUEROLLE, Olivier, Alexis, Georges; MEYER, Christophe; ANGIBAUD, Patrick, Rene; DEMESTRE, Christophe, Gabriel, Marcel; MERCEY, Guillaume, Jean, Maurice; (302 pag.)WO2016/97347; (2016); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

These common heterocyclic compound, 58458-10-9, name is 3-Amino-2-bromobenzotrifluoride, 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. category: bromides-buliding-blocks

An ice-cold solution of NaNO2 (0.15 g) in water (0.5 mL) is added to a mixture of 2-bromo-3-trifluoromethyl-aniline (0.48 g), concentrated H2SO4 (2 mL), and water (1.8 mL) at ca. 5 C. The mixture is stirred in the cooling bath for 20 min and then poured into a solution of KI (0.56 g) and I2 (0.56 g) in water (0.5 mL). After gas evolution ceases, the mixture is heated to 40 C. and stirred at this temperature for 1 h. The mixture is cooled to room temperature and aqueous Na2SO3 solution is added. The resulting mixture is extracted with ethyl acetate, and the combined extracts are dried (Na2SO4) and concentrated. The solvent is evaporated and the residue is chromatographed (cyclohexane/ethyl acetate 95:5?90:10) to give the title compound.

The synthetic route of 3-Amino-2-bromobenzotrifluoride has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; ECKHARDT, Matthias; US2014/221349; (2014); A1;,
Bromide – Wikipedia,
bromide – Wiktionary