Category: 2106-18-5

Electric Literature of 2106-18-5, These common heterocyclic compound, 2106-18-5, name is 2-(Trifluoromethoxy)fluorobenzene, 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.

Example 20: 4-[2-FLUORO-3-(TRIFLUOROMETHOXY)PHENYL]-1-PROPYLPIPERIDIN-4-OL To a solution of 1-fluoro-2-(trifluoromethoxy)benzene (1.22 g, 6.77 mmol) in dry tetrahydrofurane (30 ml) at-78 C, under nitrogen, lithium diisopropylamide (2.5 M in hexane, 3.0 ml, 7.45 mmol) was added dropwise. The mixture was stirred for 1 h after which a solution of newly distilled 4-propyl-1-piperidone (0.96 g, 6.77 mmol) in dry tetrahydrofuran (20 ml) was added drop wise. The resulting mixture was stirred at-78 C for 30 min and then brought to ambient temperature. Water (100 ml) was added and the mixture was extracted with ethylacetate (3×100 ml). The combined organic phases was dried (MgS04), filtered and evaporated to dryness. The oily residue was purified by flash column chromatography (ethylacetate/methanol, 1: 1) to give the title compound (0.83 g). MS m/z (rel. intensity, 70 eV) 321 (M+, 5), 293 (14), 292 (bp), 274 (25), 207 (10).

Statistics shows that 2-(Trifluoromethoxy)fluorobenzene is playing an increasingly important role. we look forward to future research findings about 2106-18-5.

Reference:
Patent; A. CARLSSON RESEARCH AB; WO2005/121092; (2005); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Related Products of 2106-18-5, These common heterocyclic compound, 2106-18-5, name is 2-(Trifluoromethoxy)fluorobenzene, 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.

To a 500 mL three-necked flask, concentrated sulfuric acid (20 mL, 0.35 mol, 3.5 eq)The raw material o-fluorotrifluoromethoxybenzene (18 g, 0.1 mol, 1 eq) was added portionwise with stirring,After stirring for half an hour the solution is clear,Cool to -5 C with ice-salt bath,Concentrated nitric acid (6.6 mL, 0.1 mol, 1 eq) was slowly added dropwise,The reaction is exothermic, the dropping rate to maintain the internal temperature does not exceed 0 ,After the addition is completed,After stirring at 0 C for 1 hour,Heated to 40 C and stirred for 12h,After the reaction solution was cooled to room temperature,Slowly poured into crushed ice, and constantly stirring,A large number of yellow solid precipitation, suction filtration,The filter cake was washed three times with water, drained,Dried under vacuum to give a yellow solid 18g, yield 80%, HPLC purity 95%.

The synthetic route of 2106-18-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Wuxi Jiehua Pharmaceutical Technology Co., Ltd.; Bao Liang; Gu Shuyin; (7 pag.)CN106986886; (2017); A;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 2106-18-5 as follows. Quality Control of 2-(Trifluoromethoxy)fluorobenzene

To a solution of 1-fluoro-2-(trifluoromethoxy)benzene [2106-18-5] (20.0 g, 111 mmol) in dry THF (200 mL), cooled to -78C, was added dropwise n-BuLi (2.5 M solution in n-hexane; 65 mL, 160 mmol) and subsequently TMEDA (60 mL). The reaction mixture was stirred for additional 60 min at -78C, followed by addition of a solution of iodine (30.2 g, 120 mmol) in dry THF (50 mL). The resulting mixture was stirred for 1 h and then quenched by addition of a saturated aqueous NH4CI solution (20 mL). The organic layer was washed with 1 N HCI, water and brine, and dried over MgS04. Volatiles were removed in vacuo to afford the title compound as yellow oil. The product was used in the next reaction step without further purification. MS (LC/MS): 306.0 [M+H]+.

According to the analysis of related databases, 2106-18-5, the application of this compound in the production field has become more and more popular.

Reference:
Patent; NOVARTIS AG; ALTMANN, Eva; HOMMEL, Ulrich; LORTHIOIS, Edwige Liliane Jeanne; MAIBAUM, Juergen Klaus; OSTERMANN, Nils; QUANCARD, Jean; RANDL, Stefan Andreas; SIMIC, Oliver; VULPETTI, Anna; ROGEL, Olivier; WO2012/93101; (2012); A1;,
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Synthetic Route of 2106-18-5, These common heterocyclic compound, 2106-18-5, name is 2-(Trifluoromethoxy)fluorobenzene, 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.

Example 20: 4-[2-FLUORO-3-(TRIFLUOROMETHOXY)PHENYL]-1-PROPYLPIPERIDIN-4-OL To a solution of 1-fluoro-2-(trifluoromethoxy)benzene (1.22 g, 6.77 mmol) in dry tetrahydrofurane (30 ml) at-78 C, under nitrogen, lithium diisopropylamide (2.5 M in hexane, 3.0 ml, 7.45 mmol) was added dropwise. The mixture was stirred for 1 h after which a solution of newly distilled 4-propyl-1-piperidone (0.96 g, 6.77 mmol) in dry tetrahydrofuran (20 ml) was added drop wise. The resulting mixture was stirred at-78 C for 30 min and then brought to ambient temperature. Water (100 ml) was added and the mixture was extracted with ethylacetate (3×100 ml). The combined organic phases was dried (MgS04), filtered and evaporated to dryness. The oily residue was purified by flash column chromatography (ethylacetate/methanol, 1: 1) to give the title compound (0.83 g). MS m/z (rel. intensity, 70 eV) 321 (M+, 5), 293 (14), 292 (bp), 274 (25), 207 (10).

Statistics shows that 2-(Trifluoromethoxy)fluorobenzene is playing an increasingly important role. we look forward to future research findings about 2106-18-5.