936-16-3,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.
Example 88 2-[{1-(tert-Butyl)-5-(4-fluorophenyl)-1H-pyrazol-3-yl}methyl]-2,3-dihydro[d]isothiazole 1,1-dioxide (Compound 33) To a solution of 1,2-benzisothiazoline-1,1-dioxide (10.3 mg, 0.061 mmol) in N,N-dimethylformamide (0.9 mL) was added potassium carbonate (88.5 mg, 0.640 mmol) at room temperature, followed by stirring for 10 min. The solution was slowly added with drops of {1-(tert-butyl)-5-(4-fluorophenyl)-1H-pyrazol-3-yl}methyl bromide (20.9 mg, 0.067 mmol) in methylene chloride (3 mL), and stirred at room temperature for a day. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), the reaction mixture was filtered through celite. The filtrate was neutralized with 1M HCl and an aqueous saturate sodium hydrogen carbonate solution. After extraction with ethyl acetate and water, the organic layer thus formed was dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=6:1?1:1) to afford the title compound (10.2 mg, 42percent, white solid). M.P. 163.5-167.5¡ã C.; 1H NMR (300 MHz, CDCl3) delta 7.86 (d, J=7.6 Hz, 1H), 7.65-7.53 (m, 2H), 7.41 (d, J=7.5 Hz, 1H), 7.35-7.29 (m, 2H), 7.13-7.06 (m, 2H), 6.27 (s, 1H), 4.53 (s, 2H), 4.46 (s, 2H), 1.48 (s, 9H); 13C NMR (75 MHz, CDCl3) delta 164.4, 162.3, 161.1, 143.6, 142.9, 135.3, 134.2, 132.6, 132.2, 132.1, 129.9, 129.0, 124.5, 121.5, 115.0, 114.7, 109.3, 61.3, 50.0, 41.3, 31.2
936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various fields.
Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; NAM, Ghil Soo; CHOI, Kyung Il; KIM, Jung Hyun; PAE, Ae Nim; HONG, Jin Ri; LEE, Jae Kyun; (30 pag.)US2015/329533; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com