Some common heterocyclic compound, 220227-21-4, name is 2,4,5-Trifluorobenzene-1-sulfonyl chloride, molecular formula is C6H2ClF3O2S, 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. Safety of 2,4,5-Trifluorobenzene-1-sulfonyl chloride
A mixture of 46-1 (1.12g. 10 mmol), 41-1 (2.3g. 10 mmol), pyridine (4g. 50 mmol) and DCM (30 mL) was stirred at room temperature under nitrogen overnight. H20 (30 mL) was added into the mixture which was extracted with DCM. The combined organic layers were washed with brine, dried over Na2504, filtered and the filtrate was concentrated. The residue was purified by column chromatography on silica gel (PE: EtOAc = 5:1) to give 46-2. 1H NMR (400 MHz CD3OD) delta 7.98 (dd, J = 15.6, 8.8 Hz, 1H), 7.75 (dd, J = 16.0, 8.0 Hz, 1H), 7.34~7.41 (m, 1H), 6.90 (t, J = 1.2 Hz, 1H), 6.60 (dd, J = 8, 2 Hz, 1H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 220227-21-4, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; LI, Dansu; LAYTON, Mark, E.; ROECKER, Anthony, J.; EGBERTSON, Melissa; JONES, Kristen, L. G.; WANG, Xiu; PENG, Xuanjia; WO2015/80988; (2015); A1;,
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