Electric Literature of 210532-25-5,Some common heterocyclic compound, 210532-25-5, name is 3,5-Difluorobenzene-1-sulfonyl chloride, molecular formula is C6H3ClF2O2S, 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.
To a suspension of 3-amino-4,5,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-2-carboxylic acid ethyl ester hydrochloride (36.2 g, 127.8 mmol) in anhydrous dichloromethane (1 L), at 0-5C, N,N-diisopropylethylamine (111.3 mL, 639 mmol) was added. To the resulting solution, 3,5-difluorobenzenesulfonyl chloride (27.17 g, 127.8 mmol) was added portionwise. The mixture was stirred at 0-5C for 1 hour then at room temperature for 3 hours. The organic phase was washed with NaHCC>3 satured solution, water and brine, dried over sodium sulfate filtered and evaporated. The crude, was triturated with diethylether (500 mL) to obtain the title compound as yellowish solid (45.48 g, 92%). IH-NMR (400 MHz), delta (ppm, DMSOtZ6): 7.71 (m, IH), 7.51 (m, 2H), 6.38 (bs, 2H), 4.34 (q, J=7.1 Hz, 2H), 3.99 (s, 2H), 3.44 (m, 2H), 2.58 (m, 2H), 1.30 (t, J= 7.1 Hz, 3H).
The synthetic route of 210532-25-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; NERVIANO MEDICAL SCIENCES S.r.l.; WO2007/68619; (2007); A1;,
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