A new synthetic route of (3-Bromo-5-(trifluoromethyl)phenyl)methanol

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,172023-97-1, its application will become more common.

Electric Literature of 172023-97-1, 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 172023-97-1 as follows.

Step 2: 3-bromo-5-(trifluoromethyl)benzyl 4-((tert-butoxycarbonyl)amino)piperidine-1-carboxylate To a stirred solution of (3-bromo-5-(trifluoromethyl)phenyl)methanol (567 mg, 2.223 mmol) in DMF (5 mL) at RT under nitrogen was added CU (360 mg, 2.223 mmol) and the reaction mixture heated at 50 C. for 20 hours. Tert-butyl piperidin-4-yl carbamate (445 mg, 2.223 mmol) was added and the reaction mixture stirred at 50 C. for 3 hours. On cooling to RT the mixture was diluted with DCM and washed with a saturated solution of sodium bicarbonate, a saturated solution of brine, and the organic portion was dried over MgSO4 filtered and concentrated under reduced pressure. Purification was carried out by chromatography on silica using 0-100% EtOAc in Hexanes as eluent to afford the title product; LC-MS: Rt 1.59 mins; MS m/z 427.2 [M-tBu]+; Method 2minLowPHv03

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,172023-97-1, its application will become more common.

Reference:
Patent; Novartis AG; Legrand, Darren Mark; Furminger, Vikki; Thomson, Christopher; Hughes, Owen Rhys; Stanley, Emily; US2014/171403; (2014); A1;,
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