With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111248-89-6,1,3-Dihydrobenzo[c]isothiazole 2,2-dioxide,as a common compound, the synthetic route is as follows.
4f. 5-bromo-1 ,3-dihydrobenzo[c]isothiazole 2,2-dioxide 1,3-Dihydro-benzo[c]isothiazole 22-dioxide (0.50 g, 3.14 mmol, 1.00 eq.)was solubilized in acetic acid (5 mL) at RT under nitrogen atmosphere.Bromine (0.45 g, 3.14 mmol, 1.00 eq.) in acetic acid (5 mL) was added dropwise over 5 minutes and the reaction mixture was stirred for 0.5 h. Potassium, acetate (0.28 g, 3.14 mmol, 1.00 eq.) was added and the reaction mixture was concentrated to dryness. The residue was taken in 2 % NaHCO3 solution and stirred for 10 minutes. This solution wasacidified to pH 2 using conc. HCI (2.5 mL) and extracted with MTBE (50 mL). The MTBE layer was washed with water (50 mL), brine solution (25 mL), dried over Na2SO4 and concentrated to get the crude product as brown solid. The crude product was triturated with petroleum ether (10 mL), filtered to a light brown solid (HPLC purity app. 86 %) which was further purified by column chromatography using 60-1 20 mesh silica gel, 15 %ethyl acetate in petroleum ether as eluent to get a yellow solid (HPLC purity app.90 %). The resulting product was then triturated with ethanol (5 mL), filtered and dried to get the title compounds as light yellow solid (0.35 g, 47.7 %, 94% purity).
111248-89-6, The synthetic route of 111248-89-6 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; MERCK PATENT GMBH; CANCER RESEARCH TECHNOLOGY LIMITED; SCHIEMANN, Kai; STIEBER, Frank; CALDERINI, Michel; BLAGG, Julian; MALLINGER, Aurelie; WAALBOER, Dennis; RINK, Christian; CRUMPLER, Simon Ross; (127 pag.)WO2015/144290; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com