These common heterocyclic compound, 210532-25-5, name is 3,5-Difluorobenzene-1-sulfonyl chloride, 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. SDS of cas: 210532-25-5
General procedure: To a solution of intermediate 13 (10mmol) and triethylamine (15mmol) in dichloromethane (20ml), a solution of appropriate acyl chlorides or sulfonyl chlorides (1.05 eq) in dichloromethane (3ml) was added dropwise at room temperature overnight. The mixture was washed with saturated aqueous sodium bicarbonate and brine. After removing the solvent under reduced pressure, the crude product was purified by flash chromatography on silica gel to yield the intermediates 14a-n, 15a-k, 16a-h, 17a-m. Subsequently, to a solution of the above intermediates (2mmol) in methanol/H2O (75%, 10ml) was added lithium hydrate (2.4mmol). The resulting mixture was allowed to warm up to 60C for 4h. The reaction mixture was allowed to cool to room temperature and concentrated under pressure to remove methanol. The resulting mixture was diluted by water and acidified with aqueous HCl (1mol/L) till pH=3. The white solid was collected by filtration, washed with water three times and dried to give the target compounds.
The synthetic route of 3,5-Difluorobenzene-1-sulfonyl chloride has been constantly updated, and we look forward to future research findings.
Reference:
Article; Guo, Yongzhi; Zhao, Yuqian; Wang, Guan; Chen, Yi; Jiang, Yingnan; Ouyang, Liang; Liu, Bo; European Journal of Medicinal Chemistry; vol. 143; (2018); p. 402 – 418;,
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