Application of 261762-56-5, These common heterocyclic compound, 261762-56-5, name is 1-Chloro-2-fluoro-3-methoxybenzene, 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.
2-Chloro-3-fluoro-4-methoxybenzaldehyde 1g (6.2 mmol) 3-Chloro-2-fluoroanisole in 20 ml THF was cooled to -70C and 2.7 ml of a 2.5 M n-butyl lithium solution in hexane were added. After one hour at -70 3.93 ml DMF in 7 ml THF were added at -70C and the mixture is stirred another hour at -70C. 15 ml of a 1 M aqueous hydrochloric acid were added and the reaction was warmed to ambient temperature over 18 hours. The reaction mixture was partitioned between diethyl ether and water. The aqueous phase was extracted with diethyl ether, the combined organic phases were washed with brine, dried over sodium sulfate and evaporated. The crude product was purified by chromatography on silica gel to yield 0.25 g 2-chloro-3-fluoro-4-methoxybenzaldehyde. 1H-NMR (CDCl3); delta = 3.98 (s, 3H), 6.98 (dd, 1H), 7.75 (dd, 1H), 10.30 (s, 1H).
The synthetic route of 261762-56-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Bayer Schering Pharma Aktiengesellschaft; AstraZeneca AB; EP2149558; (2010); A1;,
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