New discoveries in chemical research and development in 2021. As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world.7343-33-1, name is 5-Bromo-1H-1,2,4-triazole belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. category: Triazoles
To a suspension of 3-bromo-1H-i,2,4-triazole (lOg, 67.6mM) and phenylboronic acid (16.5g, 135.2mM) in 500 mL of DCM, was added the following: pyridine; (i0.9mL, i0.7g, 135.2mM), copper (II) acetate; (1 8.4g, 101.5mM) and powdered 4A molecular sieves (45g). The resulting blue colored suspension was stined at room temperature for 10 days open to the air. Additional DCM (500mL) was added to the reaction and the mixture filtered through a pad of diatomaceous earth, washing the cake with DCM, 10percent MeOH/DCM, and finally DCM. The filtrates were collected and concentrated under reduced pressure to provide a viscous residue, which was partitioned between ethyl acetate and iN HC1. The organic phase was washed with water (2x), brine (ix) then dried over anhydrous sodium sulphate. Suction filtered the organic layer to remove particulates and evaporated under reduced pressure to give the crude product which was purified on CombiFlash (240g column) 5i02 eluting with 25percent ethyl acetate /heptanes. Combined clean fractions and reduced the volume of the fractions under reduced pressure until crystals formed. Isolated crystals via suction filtration, washed with additional heptanes and air dried to yield 3-bromo-i-phenyl-1H-i,2,4-triazole as a white crystalline solid (5.ig, 34percent yield). ?H NMR (400 MHz, DMSO-d6) oe 9.32(s, 1H), 7.92 – 7.79 (m, 2H), 7.58 (dd, J=ii.3, 4.5Hz, 2H), 7.51-7.41 (m, 1H) ppm. ESI-MS m/z calc. 222.9745, found 224.0 (M+i)+; Retention time: 0.75 minutes.
We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 5-Bromo-1H-1,2,4-triazole ,and how the biochemistry of the body works.
Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; DAVIES, Robert, J.; CAO, Jingrong; COCKERILL, Meghan, Elise; COLLIER, Philip, Noel; DENINNO, Michael, Paul; DOYLE, Elisabeth; FRANTZ, James, Daniel; GAO, Huai; GOLDMAN, Brian, Anthony; GREY, Ronald, Lee; GRILLOT, Anne-laure; GU, Wenxin; HENDERSON, James, A.; IRARRAZAVAL, Raul Eduardo, Krauss; KOLPAK, Adrianne, Lynn; LIAO, Yusheng; MAGAVI, Sanjay Shivayogi; MALTAIS, Francois; MESSERSMITH, David; PIERCE, Albert, Charles; PEROLA, Emanuele; RYU, Elizabeth Jin-Sun; SYKEN, Joshua; WANG, Jian; (706 pag.)WO2016/197009; (2016); A1;,
1,2,3-Triazole – Wikipedia,
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