Application of 175205-81-9, 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.175205-81-9, name is 2-Bromo-4-(trifluoromethyl)pyridine, molecular formula is C6H3BrF3N, molecular weight is 225.99, as common compound, the synthetic route is as follows.
n-Butyllithium solution (1.6 M in hexane, 0.46 mL, 0.73 mmol) was added to a flask with diethyl ether (2.0 mL) at ?78 ¡ãC, followed by the dropwise addition of 2-bromo-4-(trifluoromethyl)pyridine (0.10 mL, 0.81 mmol), and the resulting mixture was stirred at -78¡ãC for 45 mm. To the prepared aryllithium solution was added a solution of (4aS,6S)- 1 -(4-fluorophenyl)-6-(( 1-methyl- 1H-pyrazol-4-yl)thio)- 1,4,5,6,7,8-hexahydro-4aH-benzo[flindazole-4a-carbaldehyde (3d) (50 mg, 0.12 mmol) in THF (1.2 mL) dropwise and stirred at ?78 ¡ãC for 30 mm. The reaction was quenched by the addition of water (8 mL). The dry ice bath was removed and the mixture was stirred for 10 mm. Then a small amount of saturated aq. NH4C1 solution was added and the solution was extracted (3 x EtOAc). The combined organic layer was washed (brine), dried (Na2SO4), and concentrated under reduced pressure. Purification of the residue by silica gel column chromatography (12 g Si02, 1percent to 3percent MeOHIDCM, a gradient elution) provided ((4aS,6S)- 1 -(4-fluorophenyl)-6-(( 1-methyl- 1H-pyrazol-4-yl)thio)- 1,4,5,6,7, 8-hexahydro-4aH- benzo [flindazol-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanol (3e) (43 mg, 63percent) as an off-white solid. mlz (ESI, +ve ion) 556.2 [M+Hjb.
Statistics shows that 175205-81-9 is playing an increasingly important role. we look forward to future research findings about 2-Bromo-4-(trifluoromethyl)pyridine.
Reference:
Patent; ORIC PHARMACEUTICALS, INC.; DU, Xiaohui; EKSTEROWICZ, John; FANTIN, Valeria R.; REW, Yosup; SUN, Daqing; YE, Qiuping; ZHOU, Haiying; KAWAI, Hiroyuki; MOORE, Jared; PHAM, Johnny; WU, Kejia; ZHU, Liusheng; YAMASHITA, Dennis; (288 pag.)WO2018/191283; (2018); A1;,
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