Category: 884495-22-1

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. 884495-22-1, name is 5-Bromo-2-fluoropyridin-3-amine, molecular formula is C5H4BrFN2, 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. Computed Properties of C5H4BrFN2

N-{5-r3-(Dimethylamino)propyl1-2-fluoropyridin-3-yl)guanidine; Step 1 : 5-[3-(Dimethylamino)prop-l-yn-l-yl]-2-fluoropyridin-3-amine; A mixture of 5-bromo-2-fluoropyridin-3-amine (1.00 g, 5.24 mmol), N,N-dimethylprop-2-yn-1-amine (0.68 mL, 6.28 mmol), and cesium carbonate (3.41 g, 10.5 mmol) in DMF (25 mL) was degassed with argon for 15 min. To this slurry were added bis(acetonitrile)palladium(II) chloride (0.068 g, 0.26 mmol) and Xphos (0.324 g, 0.68 mmol). The suspension was allowed to stir at 50 0C for 4 h under an atmosphere of nitrogen and was then concentrated. The residue was purified by column chromatography to give 5-[3-(dimethylamino)prop-l-yn-l-yl]-2-fluoropyridin-3-amine (0.46 g, 45%).

With the rapid development of chemical substances, we look forward to future research findings about 884495-22-1.

Reference:
Patent; MILLENNIUM PHARMACEUTICALS, INC.; BHARATHAN, Indu, T.; DUFFEY, Matthew, O.; ELDER, Amy, M.; GUO, Jianping; LI, Gang; REYNOLDS, Dominic; SOUCY, Francois; VOS, Tricia, J.; WO2010/65134; (2010); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 884495-22-1, 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.884495-22-1, name is 5-Bromo-2-fluoropyridin-3-amine, molecular formula is C5H4BrFN2, molecular weight is 191.0011, as common compound, the synthetic route is as follows.

General procedure: To a solution of 76 (120 mg, 0.37 mmol) in dry pyridine (12 mL) under N2 at RT, was added 2,4-difluorobenzenesulphonyl chloride (159 mg, 0.74 mmol) in CH2Cl2 (1.5 mL) dropwise over 5 min. The mixture was stirred at 45 C under N2 for 16 , and the solvent then removed under reduced pressure. The reaction was quenched with a little water and the resulting solid collected by filtration and washed with water and Et2O. Purification was carried out by trituration with hot CH2Cl2/MeOH solution to give 4 as a pale brown solid (65%).

The chemical industry reduces the impact on the environment during synthesis 884495-22-1, I believe this compound will play a more active role in future production and life.

Reference:
Article; Spicer, Julie A.; Miller, Christian K.; O’Connor, Patrick D.; Jose, Jiney; Huttunen, Kristiina M.; Jaiswal, Jagdish K.; Denny, William A.; Akhlaghi, Hedieh; Browne, Kylie A.; Trapani, Joseph A.; European Journal of Medicinal Chemistry; vol. 137; (2017); p. 139 – 155;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 884495-22-1, name is 5-Bromo-2-fluoropyridin-3-amine. A new synthetic method of this compound is introduced below., category: pyridine-derivatives

2-Fluoro-5-morpholinopyridin-3-amine A stirred mixture of 3-amino-5-bromo-2-fluoropyridine (0.96 g, 5.02 mmol), L-proline (0.12 g, 1.01 mmol), potassium carbonate (1.39 g, 10.1 mmol), copper(I) iodide (0.096 g, 0.50 mmol), and morpholine (1.31 mL, 15.04 mmol) in dry DMSO (3.0 mL) was purged three times with argon and placed under vacuum three times, then the mixture was heated to 90 C. After 21.5 h, the reaction was cooled to rt, then treated with water. After extracting twice with EtOAc, the organics were combined and dried over anhydrous sodium sulfate. After filtration and concentration the residue was purified on basic alumina (10-50% EtOAc in hexanes) to afford a white solid as 2-fluoro-5-morpholinopyridin-3-amine. 1H NMR (400 MHz, DMSO-d6) delta ppm 6.96 (1H, t, J=2.6 Hz), 6.75 (1H, dd, J=9.6, 2.7 Hz), 5.25 (2H, br. s.), 3.80 (4H, m), 3.08 (4H, m). Mass Spectrum ESI (pos.) m/e: 198.1 (M+H)+.

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, 884495-22-1, 5-Bromo-2-fluoropyridin-3-amine.

Reference:
Patent; AMGEN INC.; US2010/331293; (2010); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Related Products of 884495-22-1, 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 884495-22-1 as follows.

To 5-bromo-2-fluoropyridin-3-amine (400 mg, 2.094 mmol) was added DMSO (2.5 ml) and morpholine (912 mg, 10.47 mmol). The reaction mixture was stirred at 110- 115 C for 40 hours. The reaction was cooled to room temperature and 200 ml of ethyl acetate was added. The mixture was washed with saturated sodium bicarbonate (2x), water (lx), brine (lx), dried with sodium sulfate, filtered and concentrated to yield 535 mg of the title compound as free base which was used without further purification.LCMS (m/z): 258.0/260.0 (MH+), retention time = 0.52 mm.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,884495-22-1, its application will become more common.

Reference:
Patent; NOVARTIS AG; ANTONIOS-MCCREA, William, R.; BARSANTI, Paul, A.; HU, Cheng; JIN, Xianming; MARTIN, Eric, J.; PAN, Yue; PFISTER, Keith, B.; SENDZIK, Martin; SUTTON, James; WAN, Lifeng; WO2012/66070; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem