With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.936-16-3,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide,as a common compound, the synthetic route is as follows.
Step 2. Solution of 1 (97 mg, 0.053 mmol) in DMF (4 mL) was cooled to 0¡ãC and NaH (13.9 mg, 0.058 mmol) was added. The mixture was stirred at 0¡ãC for 30 minutes followed by addition of 10 (100 mg, 0.48 mmol). The solution was allowed to stir 15 hours at 0¡ãC. The resulting mixture was poured into water (20 mL) and stirred for 10 minutes. The aqueous phase was extracted with ethyl acetate (30 mL). The combined organic layer was washed with brine (20 mL), dried with anhydrous sodium sulfate, filtered, and concentrated. Purification with prep- HPLC (0.04percentNH3.H2O/ ACN/ H20 system) resulted in Compound 114 (20 mg) as a white solid. 1H NMR (DMSO-d6, 400MHz) delta 8.56 (d, 1H), 8.51-8.46 (m, 2H), 8.06 (d, 1H), 7.88- 7.82 (m, 1H), 7.81-7.67 (m, 3H), 7.50 (dd, 8.2 Hz, 1H), 7.09 (d, 1H), 5.17 (s, 2H); LCMS (ESI+): m/z 341 (M+H).
The synthetic route of 936-16-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; NUMERATE, INC.; RAIMUNDO, Brian; KOLTUN, Elena S.; GRIFFIN, John; STANGELAND, Eric; (93 pag.)WO2018/49324; (2018); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com