Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 128071-98-7, name is 4-Bromo-2-fluoropyridine. This compound has unique chemical properties. The synthetic route is as follows. Safety of 4-Bromo-2-fluoropyridine
The stirred solution of 4-bromo-2-fluoropyridine (10.0 g, 56.82 minol), phenylmethanethiol (7.3 mL, 62.50 minol), Pd2(dba)3 (2.60 g, 2.84 minol), Xanthophos (3.28 g, 5.68 minol) andDIPEA (19.4 mL, 113.64 minol) in dioxane (150 mL) was degassed with argon for 15 min The resulting reaction mixture was heated to reflux for 16 h under argon atmosphere. The reaction mixture was cooled to rt, filtered through celite bed, the celite bed was washed with EtOAc and the combined filtrate was concentrated to dryness under reduced pressure. The crude was purified by flash column chromatography (40 g SiliCycle column, 2-3% EtOAc inHexane elution) to provide the title compound as yellow oil (12.0 g, 96.3%). LC/MS, ESIMS( ): 219.5. 1H NMR (400 MHz, CDCI3) O ppm 7.99 (d, J= 5.2 Hz, 1H), 7.43-7.30 (m, 5H), 7.00 -6.98 (m, 1 H), 6.74 -6.73 (m, 1 H).
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Reference:
Patent; NOVARTIS AG; PHILLIPS, Dean Paul; AZIMIOARA, Mihai; CHEN, Bei; EPPLE, Robert; NIKULIN, Victor Ivanovich; RODRIGUEZ, Rodrigo A.; PATEL, Sejal; HONDA, Ayako; (295 pag.)WO2018/42316; (2018); A1;,
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