Reference of 74784-70-6, 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.74784-70-6, name is 5-(Trifluoromethyl)pyridin-2-amine, molecular formula is C6H5F3N2, molecular weight is 162.1125, as common compound, the synthetic route is as follows.
Sodium hydride (60% in paraffin oil, 0.0907 g, 2.27 mmol) was washed twice under Ar with n-hexane (2 ml). A solution of 2-amino-5-chloropyridine (0.250 g, 1.51 mmol) in 2-MeTHF (2.0 ml) was added slowly. The brown-red suspension was stirred until no more gas evolution was observed and then 3-methyl-2-oxazolidinone (0.3 12 g, 3.02 mmol) wasadded. The resulting reaction mixture was stirred at room temperature for 20 h. The reaction was quenched by careful addition of water and diluted with EtOAc. Phases were separated and aqueous phase was extracted with EtOAc (2x). The combined organic layers were washed with brine, dried over anhydrous Na2504 and evaporated under reduced pressure to afford a crude residue (0.457 g). Quantitative 1H NMR analysis using trimethoxy benzeneas an internal standard indicated purity of 45% (52% chemical yield). The crude product was purified by silica gel chromatography (eluting with 1-4% MeOH in DCM) to afford 1-(2- hydroxyethyl)-1 -methyl-3-[5-(trifluoromethyl)-2-pyridyl]urea (0.177 g, 99% purity, 44%) as a pale yellow solid.1H NMR (400MHz, d6DMSO) 69.56 (br, 1H), 8.56 (dd, J = 1.5, 0.7 Hz, 1H), 8.03 (dd, J =9.0, 2.6 Hz, 1H), 7.97-7.93 (m, 1H), 5.42 (br, 1H), 3.62 (q, J = 4.9 Hz, 2H), 3.46-3.38 (m,2H), 2.96 (s, 3H).
The chemical industry reduces the impact on the environment during synthesis 74784-70-6, I believe this compound will play a more active role in future production and life.
Reference:
Patent; SYNGENTA PARTICIPATIONS AG; SMITS, Helmars; GHORAI, Sujit, Kumar; (25 pag.)WO2017/186624; (2017); A1;,
Pyridine – Wikipedia,
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