These common heterocyclic compound, 202925-07-3, name is 2-Chloro-1-fluoro-4-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. Application In Synthesis of 2-Chloro-1-fluoro-4-methoxybenzene
To 2-chloro-1-fluoro-4-methoxybenzene (5 g) in methylene chloride (30 ml) solution, titanium tetrachloride (5.8 ml) and alpha,alpha-dichloromethylmethylether (2.8 ml) were added under ice cooling, the mixture was stirred at 2C for 11.5 hours, then the reaction solution was poured into ice. Next, the methylene chloride layer was separated, washed with saturated saline, dried over with anhydrous sodium sulfate, and concentrated. The obtained residue was recrystallized from ethylether. The thus obtained 4-chloro-5-fluoro-2-methoxybenzaldehyde (3.41 g) was used instead of the starting material in Reference Example 2, that is, the compound S1, for successively the similar procedure as in Reference Example 2 to Reference Example 6 to obtain the title compound. NMR (CDCl3): delta7.96(1H, s), 7.37(1H, d, J=9.0Hz), 7.06(1H, br), 6.96(1H, d, J=5.9Hz), 4.33(2H, d, J=6.1Hz), 3.84(3H, s) MS: 378(M+Na)+
The synthetic route of 2-Chloro-1-fluoro-4-methoxybenzene has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Asubio Pharma Co., Ltd.; Daiichi Sankyo Company, Limited; EP2025672; (2009); A1;,
Chloride – Wikipedia,
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