Category: 875664-38-3

875664-38-3, name is 1-Bromo-4,5-difluoro-2-methylbenzene, 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. Recommanded Product: 875664-38-3

Preparation 2 (4,5-Difluoro-2-methyl-phenyl)boronic acid n-Butyl lithium (4.6 mL, 11.5 mmol) is added to the mixture of 1-bromo-4,5-difluoro-2-methylbenzene (2.0 g, 9.6 mmol) and trimethyl borate (1.5 g, 14.5 mmol) in anhydrous tetrahydrofuran (30 mL), drop wise, at -78 C. over one hour, under an atmosphere of argon. The reaction mixture is stirred for another hour at the same temperature, quenched and acidified with 1 N HCl. The resulting mixture is extracted with ethyl acetate(3*). The combined organic layer is washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated in vacuo.

The synthetic route of 875664-38-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ELI LILLY AND COMPANY; US2012/322841; (2012); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

Related Products of 875664-38-3,Some common heterocyclic compound, 875664-38-3, name is 1-Bromo-4,5-difluoro-2-methylbenzene, molecular formula is C7H5BrF2, 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.

1-47: A mixture of 2-bromo-4,5-difluorotoluene (4.00 g, 19.3 mmol), DIPEA (5.2 mL, 30.0 mmol), dichlorobis(benzonitrile)palladium(II) (269 mg, 0.700 mmol) and 1,1- bis(diphenylphosphino)ferrocene (dppf) (482 mg, 0.870 mmol) in absolute ethanol (50 mL) was placed in a sealed bomb with stirring and placed under 10 bars of carbon monoxide and heated to 135C for 4 h. The mixture was then cooled to RT, returned to atmospheric pressure and opened. The rxn mixture was concentrated and diluted with brine (100 mL) and extracted with EtOAc (3×50 mL). The combined organic layers were washed with brine (2×50 mL), dried over sodium sulfate, filtered and concentrated. The residue was purified by normal phase flash column chromatography on silica gel using 5-20% EtOAc in heptane to afford compound 1-47.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1-Bromo-4,5-difluoro-2-methylbenzene, its application will become more common.

Reference:
Patent; EXELIXIS, INC.; XU, Wei; (170 pag.)WO2017/4609; (2017); 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. 875664-38-3, name is 1-Bromo-4,5-difluoro-2-methylbenzene, A new synthetic method of this compound is introduced below., HPLC of Formula: C7H5BrF2

General procedure: To a solution of o—dibromobenzenes, N—Boc—pyrrole—2—boronic acid 2 and 1.0 M K2CO3aq. in DMF was added PdCl2(PPh3)2 (20%/mol) under a nitrogen atmosphere. Theresulting mixture was heated at 80 C for 7 h. After cooling to room temperature, themixture was extracted with a mixture of EtOAc/hexane (v/v = 1:4). The organic layerwas washed with water and brine, and then dried over Na2SO4. After removal solvent,the residue was purified by silica gel column chromatography and recrystallization todi(N—Boc—pyrrol—2—yl—benzenes).

The synthetic route of 875664-38-3 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Kuzuhara, Daiki; Miyake, Satoshi; Moriyama, Hirotake; Tamura, Yuto; Aratani, Naoki; Yamada, Hiroko; Tetrahedron Letters; vol. 56; 41; (2015); p. 5564 – 5567;,
Bromide – Wikipedia,
bromide – Wiktionary

875664-38-3, name is 1-Bromo-4,5-difluoro-2-methylbenzene, 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. Application In Synthesis of 1-Bromo-4,5-difluoro-2-methylbenzene

4′,5′-Difluoro-2′-methyl-biphenyl-4-ol To a stirred solution of 3,4-difluorotoluene (30 g, 234.1 mmol) and iron powder (0.784 g, 14.05 mmol) in methylene chloride (140 mL) in an ice bath was added bromine (12 mL, 155 mmol) slowly over 6.5 hrs. The reaction mixture was warmed to RT and stirred for an additional 60 hrs. The mixture was washed with water (200 mL), 10% Na2SO3 (3*150 mL), saturated (NaHCO3 (100 mL) and saturated NaCl. The organic layer was dried over MgSO4, filtered and concentrated in vacuo to give 40 g of crude 1-bromo-4,5-difluoro-2-methyl-benzene. Bromo-4,5-difluoro-2-methyl-benzene (30 g, 145 mmol) and 4-hydroxyphenyl-boronic acid (20.99 g, 152.2 mmol) were suspended in 725 ml of dioxane. The mixture was degassed with argon. Potassium carbonate (23.17 g, 166 mmol) in 72.5 ml water solution was added and after stirring for 10 minutes, bis(tricyclohexylphosphine)palladium(0) (2.4 g, 3.62 mmol) was added. The reaction was stirred at 80-85 C. for 19 hrs and concentrated. The mixture was diluted with ethyl acetate and water. The organic layer was washed with brine, dried and solvents were evaporated. The crude product was purified by flash chromatography, eluting with 0-7% ethyl acetate in hexanes to obtain the crude product which was further recrystallized from hexane to afford 4′,5′-difluoro-2′-methyl-biphenyl-4-ol (23.76 g, 74.5%). LR-MS (ES) calculated for C13H10F2O, 220.22. found m/z 219 [M-H].

The synthetic route of 875664-38-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Bolin, David Robert; Hamilton, Matthew Michael; McDermott, Lee Apostle; Qian, Yimin; US2011/112158; (2011); A1;,
Bromide – Wikipedia,
bromide – Wiktionary

875664-38-3, name is 1-Bromo-4,5-difluoro-2-methylbenzene, 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. SDS of cas: 875664-38-3

Preparation 2 (4,5-Difluoro-2-methyl-phenyl)boronic acid n-Butyl lithium (4.6 mL, 11.5 mmol) is added to the mixture of 1-bromo-4,5-difluoro-2-methylbenzene (2.0 g, 9.6 mmol) and trimethyl borate (1.5 g, 14.5 mmol) in anhydrous tetrahydrofuran (30 mL), drop wise, at -78 C. over one hour, under an atmosphere of argon. The reaction mixture is stirred for another hour at the same temperature, quenched and acidified with 1 N HCl. The resulting mixture is extracted with ethyl acetate(3*). The combined organic layer is washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated in vacuo.

The synthetic route of 875664-38-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ELI LILLY AND COMPANY; US2012/322841; (2012); A1;,
Bromide – Wikipedia,
bromide – Wiktionary