Category: 112110-07-3

Electric Literature of 112110-07-3 ,Some common heterocyclic compound, 112110-07-3, molecular formula is C6H5F3N2, 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.

Dissolve the amine obtained in Step 2 (380 mg, 2.35 mmol), pyridine (371 mg, 4.7 mmol) in DCM (8 mL), cool to 0 C. in ice bath. Add slowly phenyl chloroformate (403 mg, 2.35 mmol). After addition, stir the reaction at 0-5 C. for 2 hrs. Pour the mixture into water (50 mL), adjust pH to neutral with 1M HCl solution, extract with EtOAc (15 mL*3). Combine the organic layers; wash with brine (100 mL), dry over anhydrous Na2SO4, and concentrate under reduced pressure to get the crude product. Purification by chromatography (silica gel, EtOAc_PE=15:85) affords the target compound (390 mg, 59%).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,112110-07-3, its application will become more common.

Reference:
Patent; Zhang, Deyi; Zhang, Ruihao; Zhong, Boyu; Shih, Chuan; US2015/197511; (2015); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, the common compound, a new synthetic route is introduced below. Safety of 5-(Trifluoromethyl)pyridin-3-amine

To a stirred solution of Example 30A (100 mg, 0.62 mmol) and triethylamine (75 mg, 0.74 mmol) at0 C in dichloromethane (5 ml) is added ethyl malonyl chloride (108 mg, 0.65 mmol) dropwise over 15 minutes. The solution is allowed to warm to room temperature, and stirring is continued overnight (18 h). The crude reaction solution is concentrated in vacuo and the residue is purified by preparativeRP-HPLC (acetonitrile/water 1: 9 to 9: 1 gradient) to afford a colourless oil. Yield: 144.4 mg(85% of th.)HPLC (method 5): Rt = 3.80 min. , max 196 nm, 244 nm MS (ESIpos):m/z = 277[M+H] +H-NMR (300MHz, CDC13) :8 = 9.74 (s, 1H); 8.81 (s, 1H); 8.64 (s, 1H) ; 8.47 (s,1H) ; 4.30 (q, 2H); 3.53 (s, 2H);1. 35 (t, 3H) ppm.

The synthetic route of 112110-07-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BAYER HEALTHCARE AG; WO2004/20410; (2004); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. Safety of 5-(Trifluoromethyl)pyridin-3-amine

To a mixture of 2-(4-bromo-2,5-difluoro-phenyl)acetic acid (9, 2.16 g, 8.60 mmol), 5-(trifluoromethyl)pyridin-3-amine (10, 1.39 g, 8.57 mmol) and pyridine (2.09 ml, 25.8 mmol) in ethyl acetate (85 ml) was added slowly propylphosphonic anhydride (50 wt % solution in ethyl acetate, 10.1 ml, 17.2 mmol). The reaction mixture was allowed to stir at room temperature for 3 hours. The reaction was diluted with ethyl acetate and was washed with saturated aqueous ammonium chloride, water and brine. The organic layer was dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to provide 3.29 g (97% yield) of compound 11 that was used in the next step without further purification. MS ESI [M+H+]+=397.05.

With the rapid development of chemical substances, we look forward to future research findings about 112110-07-3.

Reference:
Patent; Plexxikon Inc.; Lin, Jack; Ibrahim, Prabha N.; Albers, Aaron; Buell, John; Guo, Zuojun; Pham, Phuongly; Powers, Hannah; Shi, Songyuan; Spevak, Wayne; Wu, Guoxian; Zhang, Jiazhong; Zhang, Ying; (132 pag.)US2017/267660; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. Safety of 5-(Trifluoromethyl)pyridin-3-amine

To a mixture of 2-(4-bromo-2,5-difluoro-phenyl)acetic acid (9, 2.16 g, 8.60 mmol), 5-(trifluoromethyl)pyridin-3-amine (10, 1.39 g, 8.57 mmol) and pyridine (2.09 ml, 25.8 mmol) in ethyl acetate (85 ml) was added slowly propylphosphonic anhydride (50 wt % solution in ethyl acetate, 10.1 ml, 17.2 mmol). The reaction mixture was allowed to stir at room temperature for 3 hours. The reaction was diluted with ethyl acetate and was washed with saturated aqueous ammonium chloride, water and brine. The organic layer was dried over anhydrous magnesium sulfate, filtered and concentrated under reduced pressure to provide 3.29 g (97% yield) of compound 11 that was used in the next step without further purification. MS ESI [M+H+]+=397.05.

With the rapid development of chemical substances, we look forward to future research findings about 112110-07-3.

Reference:
Patent; Plexxikon Inc.; Lin, Jack; Ibrahim, Prabha N.; Albers, Aaron; Buell, John; Guo, Zuojun; Pham, Phuongly; Powers, Hannah; Shi, Songyuan; Spevak, Wayne; Wu, Guoxian; Zhang, Jiazhong; Zhang, Ying; (132 pag.)US2017/267660; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 112110-07-3, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, molecular weight is 162.11, as common compound, the synthetic route is as follows.

Dissolve the amine obtained in Step 2 (380 mg, 2.35 mmol), pyridine (371 mg, 4.7 mmol) in DCM (8 mL), cool to 0C in ice bath. Add slowly phenyl chloroformate (403 mg, 2.35 mmol). After addition, stir the reaction at 0-5C for 2 hrs. Pour the mixture into water (50 mL), adjust pH to neutral with 1M HC1 solution, extract with EtOAc (15 mLx3). Combine the organic layers; wash with brine (100 mL), dry over anhydrous a2S04, and concentrate under reduced pressure to get the crude product. Purification by chromatography (silica gel, EtOAc_PE=15:85) affords the target compound (390 mg, 59%).

Statistics shows that 112110-07-3 is playing an increasingly important role. we look forward to future research findings about 5-(Trifluoromethyl)pyridin-3-amine.

Reference:
Patent; CROWN BIOSCIENCE INC. (TAICANG); ZHANG, Deyi; ZHANG, Ruihao; ZHONG, Boyu; SHIH, Chuan; WO2014/418; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine. This compound has unique chemical properties. The synthetic route is as follows. Quality Control of 5-(Trifluoromethyl)pyridin-3-amine

5-(Trifluoromethyl)pyridin-3 -amine (977 mg, 6.03 mmol, Anichem, P20551 , North Brunswick, NJ) was treated with THF (40 mL) and LiHMDS (1.0 M in THF, 13.26 mL, 13.26 mmol) slowly dropwise at RT and stirred at this temperature for 20 min. The solution was then cooled in an ice bath and di-tert-butyl dicarbonate (1.38 g, 6.33 mmol) was added and the solution stirred warming to RT overnight. LC-MS indicated partial conversion to bis(Boc) material (M+l =363.2). The reaction mixture was treated with additional di-tert-butyl dicarbonate (1.38 g, 6.33 mmol) and of 1M LiHMDS and stirred overnight (16 h). The reaction mixture was concentrated and the crude material was treated with 0.2M HC1 (aq., 30 mL) and extracted with EtOAc (100 mL). The organic layer was washed with a saturated solution of NaHCC>3 (aq.) and brine and dried over MgS04, filtered and concentrated. The resulting crude product was purified by silica gel chromatography (20-50% EtOAc in hexanes) to afford bis(teri-butyl (5- (trifluoromethyl)pyridin-3-yl)carbamate) (729 mg, 33 % yield) as a yellow crystalline solid. MS (ESI, pos. ion) m/z: 363.0 (M+l). .H NMR (400 MHz, CDCl3) delta ppm 8.80 (1 H, s), 8.58 – 8.64 (1 H, m), 7.75 (1 H, s), 1.44 (18 H, s). 19F NMR (377 MHz, CDCl3) delta ppm -62.36 (3 F, s).

With the rapid development of chemical substances, we look forward to future research findings about 112110-07-3.

Reference:
Patent; AMGEN INC.; D’AMICO, Derin C.; HERBERICH, Bradley J.; JACKSON, Claire L.M.; PETTUS, Liping H.; TASKER, Andrew; WANG, Hui-Ling; WU, Bin; WURZ, Ryan; WO2012/148775; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Electric Literature of 112110-07-3, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

Under a nitrogen atmosphere, 0.1 g (0.25 mmol, 1.0 eq) of JD1001-002-12 was sequentially added to a 25 mL reactor.3.2 mL (10.0 V) THF, 0.32 g (0.75 mmol, 3.1 eq) NaHCO3, 0.38 g (0.75 mmol, 3.0 eq) 2-amino-5-trifluoromethylpyridine, heated to 60 C, stirred for 3 hours, TLC The reaction of the raw materials is detected (developing agent: PE/EA=1/1,UV254), the reaction was stopped, the reaction was quenched with water and extracted with ethyl acetate. Filtration and concentration of the organic phase gave a solid, which was purified by HPLC (CH3CN/H2O = 60:40) to afford 39 mg of JD1001-2111. Yield31%.

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 112110-07-3, 5-(Trifluoromethyl)pyridin-3-amine.

Reference:
Patent; Kunming Jida Pharmaceutical Co., Ltd.; Xiao Xuzhi; Zhang Poyong; Lu Faguan; Wang Zhipeng; Chen Mengran; Guo Kun; Zhou Rui; Zhang Yun; (28 pag.)CN109593061; (2019); A;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 112110-07-3, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, molecular weight is 162.11, as common compound, the synthetic route is as follows.

1-(((Benzyloxy)carbonyl)amino) cyclopropane-1-carboxylic acid (50 mg, 0.21 mmol), 5-(trifluoromethyl)pyridin-3-amine (104 mg, 0.64 mmol), and DIPEA (111 muL, 0.64 mmol) were dissolved in DMF (1 mL), and then HATU (97 mg, 0.26 mmol) was added thereto, followed by stirring at room temperature overnight. A saturated aqueous sodium hydrogen carbonate solution was added to a reaction liquid, the mixture was stirred for a while, and then extraction was performed with ethyl acetate. A separated organic layer was washed with a saturated saline solution and dried over anhydrous sodium sulfate, an insoluble substance was filtered, and then a solvent was distilled off under reduced pressure. The obtained residue was purified by silica gel column chromatography (hexane:ethyl acetate) (concentration gradient: 40% to 60%) to obtain a crude product (white powders, 126 mg) of benzyl (1-((5-(trifluoromethyl)pyridin-3-yl)carbamoyl)cyclopropyl)carbamate.

The chemical industry reduces the impact on the environment during synthesis 112110-07-3, I believe this compound will play a more active role in future production and life.

Reference:
Patent; Nippon Chemiphar Co., Ltd.; Kinki University; TANAKA Hiroto; OOI Isao; HAYASHIDA Kohei; OGAWA Toru; KAWABATA Atsufumi; (64 pag.)EP3572403; (2019); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine, molecular formula is C6H5F3N2, molecular weight is 162.11, as common compound, the synthetic route is as follows.Quality Control of 5-(Trifluoromethyl)pyridin-3-amine

Step 5: 4-Methyl-3-(9H-pyrimido[4, 5-bJindol- 7-yl)-N-[5-(trifluoromethyl)pyridin-3-yl]benzamideTo a vial was added 4-methyl-3-(9H-pyrimido[4,5-b]indol-7-yl)benzoic acid (15.2 mg, 0.0501 mmol), DMF (0.32 mL), and AWN’N’-tetramethyl-O-(7-azabenzotriazol-l-yl)uronium hexafluorophosphate (22.9 mg, 0.0601 mmol). This mixture was stirred 15 min at RT. To the mixture was then added 5-(trifluoromethyl)pyridin-3-amine (10.6 mg, 0.0651 mmol. The resulting mixture was stirred at 70 0C for 18 h. LCMS indicated complete consumption of the activated ester (M+H 422) and showed product (M+H 448). The product was isolated by prep HPLC/MS using a 19 mm x 100 mm C18 column; 28%CH3CN-H2O (0.1% TFA), 1 min, to 48% at 6 min; 30 mL/min. The HPLC fractions containing the product were freeze dried to yield a light yellow solid, 5.6 mg, 20% yield. FMR showed that it was the mono TFA salt; and contained some residual PF6. 1H NMR (DMSOd6) delta 13.29 (s, IH, NH); 10.76 (s, IH, amide NH); 9.72 (s, IH); 9.22 (s, IH); 9.20 (s, IH); 8.69 (s, IH); 8.62 (s, IH); 8.44 (d, IH); 7.98 (m, 2H); 7.66 (s, IH); 7.56 (d, IH); 7.53 (d, IH).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,112110-07-3, 5-(Trifluoromethyl)pyridin-3-amine, and friends who are interested can also refer to it.

Reference:
Patent; INCYTE CORPORATION; WO2008/79965; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 112110-07-3, Adding some certain compound to certain chemical reactions, such as: 112110-07-3, name is 5-(Trifluoromethyl)pyridin-3-amine,molecular formula is C6H5F3N2, 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 112110-07-3.

To a 5 ml reaction vial was added 2-[4-[2-[(1-methylimidazol-4-yl)amino]pyrimidin-5-yl]phenyl]acetic acid (14, 160 mg, 0.050 mmol) followed by anhydrous NMP (1.5 ml), 5-(trifluoromethyl)pyridin-3-amine (10, 8 mg, 0.05 mmol) and pyridine (80 mul). To the mixture was slowly added propylphosphonic anhydride (50 wt % solution in ethyl acetate, 0.25 ml, 0.42 mmol). The reaction was allowed to stir at room temperature for three hours. Upon completion, the reaction was poured into water and extracted with ethyl acetate. The organic phase was washed with saturated aqueous ammonium chloride and brine, dried over anhydrous sodium sulfate and filtered. The solvent was removed under reduced pressure in the presence of silica. The resulting crude material was purified by silica gel flash column chromatography eluting with 0-15% methanol in dichloromethane. This provided compound P-0167. MS ESI [M+H+]+=452.00.

According to the analysis of related databases, 112110-07-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Plexxikon Inc.; Lin, Jack; Ibrahim, Prabha N.; Albers, Aaron; Buell, John; Guo, Zuojun; Pham, Phuongly; Powers, Hannah; Shi, Songyuan; Spevak, Wayne; Wu, Guoxian; Zhang, Jiazhong; Zhang, Ying; (132 pag.)US2017/267660; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem