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.,936-16-3
General procedure: [1-(tert-Butyl)-5-{4-(piperidin-1-yl)phenyl}-1H-pyrazol-3-yl]methanol (54.9 mg, 0.18 mmol) was reacted with tripheny phosphine(93.1 mg, 0.36 mmol) and carbontetrabromide (121 mg,0.37 mmol) for 1 h. at 0 C. Without purification, the reaction mixturewas added to compound 8 (27.3 mg, 0.16 mmol) in DMF, andstirred for overnight. Then the reaction mixture was extracted withethyl acetate. The organic layer was dried over magnesium sulfate,filtered, concentrated in reduced pressure, and purified by columnchromatography (Hex: EtOAc = 4: 1 then 1: 1) to give title compound(15.2 mg, 20percent). 1H NMR (300 MHz, CDCl3) d 7.89 (d, J = 7.9 Hz, 1H), 7.64?7.52(m, 2H), 7.40 (d, J = 7.1 Hz, 1H), 7.30?7.17 (m, 2H), 6.29 (d,J = 8.7 Hz, 2H), 6.22 (s, 1H), 4.52 (s, 2H), 4.46 (s, 2H), 3.26?3.23(m, 4H), 1.79?1.74 (m, 4H), 1.67?1.63 (m, 2H), 1.49 (s, 9H).; 13CNMR (75 MHz, CDCl3) d 151.9, 144.4, 143.3, 135.4, 134.3, 132.5, 131.1, 128.9, 124.5, 123.7, 121.4, 114.9, 109.0, 61.0, 50.0, 41.4,31.2, 25.7, 24.3.
936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.
Reference£º
Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com