Synthetic Route of 201849-17-4, These common heterocyclic compound, 201849-17-4, name is 1-Bromo-2-chloro-5-fluoro-4-methylbenzene, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A solution of isopropyl magnesium chloride in THF (2.0 M; 27.2 mL) was added dropwise to a mixture of 1-bromo-2-chloro-5-fluoro-4-methylbenzene (8.10 g) and THF (55 mL) at -10 C. under an argon atmosphere, followed by stirring at -10 C. for 45 minutes. A mixture of iodine (18.4 g) and THF (26 mL) was added dropwise to the reaction mixture at -75 C., followed by stirring at -75 C. for 3 hours. A saturated aqueous Na2S2O3 solution was added to the reaction mixture at -75 C., followed by stirring at room temperature for 15 minutes. Saturated aqueous sodium bicarbonate was added to the reaction mixture at room temperature, followed by extraction with EtOAc. The organic layer was washed with brine, dried over Na2SO4, and then concentrated under reduced pressure, thereby obtaining 1-chloro-4-fluoro-2-iodo-5-methylbenzene (9.71 g).
Statistics shows that 1-Bromo-2-chloro-5-fluoro-4-methylbenzene is playing an increasingly important role. we look forward to future research findings about 201849-17-4.
Reference:
Patent; ASTELLAS PHARMA INC.; ISHIHARA, Tsukasa; IKEGAI, Kazuhiro; KURIWAKI, Ikumi; HISAMICHI, Hiroyuki; TAKESHITA, Nobuaki; TAKEZAWA, Ryuichi; US2014/364421; (2014); A1;,
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