Category: 936-16-3

936-16-3, 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2.To a solution of 1 (97.0 mg, 0.57 mmol) in DMF (4 mL) was added NaH (13.9 mg, 0.58 mmol) at 0¡ãC. The mixture was stirred at 0¡ãC for 30 minutes. Dichloropyrimidine 2 (100 mg, 0.48 mmol, 1.0 eq) was added, the solution was allowed to warm to 15¡ãC and stirred for 15 hours. The resulting mixture was poured into ice water (w/w = 1/1, 20 mL) and stirred for 10 minutes. The aqueous phase was extracted with EtOAc (30 mL) and the combined organic phase was washed with brine (20 mL), dried with anhydrous Na2S04, filtered, and concentrated in vacuo to afford 3 (120 mg, 72percent).

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

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

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.

2-[{1-(tert-Butyl)-5-(4-cyclohexylphenyl)-1H-pyrazol-3-yl}methyl]-2,3-dihydro[d]isothiazole 1,1-dioxide (Compound 36) (0327) To a solution of {1-(tert-butyl)-5-(4-cyclohexylphenyl)-1H-pyrazol-3-yl}methanol (101 mg, 0.323 mmol) in were added PPh3 (71.8 mg, 0.655 mmol), and CBr4 (217 mg, 0.655 mmol) at 0¡ã C., followed by stirring at the same temperature for one hour to give {1-(tert-butyl)-5-(4-cyclohexylphenyl)-1H-pyrazol-3-yl}methyl bromide. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), drops of N,N-dimethylformamide (1.5 mL) in 1,2-benzisothiazoline-1,1-dioxide (57.1 mg, 0.388 mmol) were slowly added. (0328) At the same temperature, potassium carbonate (447 mg, 3.23 mmol) was added, and the resulting solution was stirred for a day. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), water was added dropwise, after which extraction was carried out with ethyl acetate and brine. The organic layer was dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=4:1) to afford the title compound (55.4 mg, 31percent, white solid). (0329) M.P. 135.7-141.5¡ã C.; (0330) 1H NMR (300 MHz, CDCl3) delta 7.83 (d, J=7.5 Hz, 1H), 7.63-7.50 (m, 2H), 7.40 (d, J=7.5 Hz, 1H), 7.30-7.20 (m, 4H), 6.24 (s, 1H), 4.53 (s, 2H), 4.45 (s, 2H), 2.56 (brs, 1H), 1.92-1.77 (m, 5H), 1.48-1.27 (m, 14H); (0331) 13C NMR (75 MHz, CDCl3) delta 148.5, 144.3, 143.4, 135.4, 134.3, 132.5, 131.3, 130.3, 128.9, 126.2, 124.5, 121.4, 109.0, 61.1, 50.0, 44.3, 41.4, 34.4, 31.2, 26.9, 26.1

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

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

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.

To a solution of {5-(4-fluorophenyl)-1-isobutyl-1H-pyrazol-3-yl}methanol (19.4 mg, 0.078 mmol) in methylene chloride (1 mL) were added PPh3 (42.8 mg, 0.163 mmol) and CBr4 (66.3 mg, 0.200 mmol) at 0¡ã C., followed by stirring at the same temperature for 30 minute to give {5-(4-fluorophenyl)-1-isobutyl-1H-pyrazol-3-yl}methyl bromide. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), drops of 1,2-benzisothiazoline-1,1-dioxide (24.3 mg, 0.078 mmol) N,N-dimethylformamide (1.5 mL) were slowly added to the solution. (0338) Then, potassium carbonate (113 mg, 0.816 mmol) were added at the same temperature, and the resulting solution was stirred for a day. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), water was added, after which extraction was carried out with ethyl acetate and brine. 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=2:1) to afford the title compound (19.2 mg, 62percent percent, white solid). (0339) M.P. 110.8-118.2¡ã C.; (0340) 1H NMR (300 MHz, CDCl3) delta 7.61-7.52 (m, 2H), 7.46-7.33 (m, 4H), 7.18-7.12 (m, 2H), 6.41 (s, 1H), 4.56 (s, 2H), 4.41 (s, 2H), 3.91 (d, J=7.5 Hz, 2H), 2.26-2.08 (m, 1H), 0.80 (d, J=6.7 Hz, 6H); (0341) 13C NMR (75 MHz, CDCl3) delta 146.0, 144.5, 136.8, 135.2, 134.0, 133.0, 132.6, 131.0, 130.8, 129.2, 129.1, 124.8, 124.5, 121.4, 115.9, 115.6, 106.3, 56.7, 49.9, 45.7, 41.2, 29.6, 19.8

The synthetic route of 936-16-3 has been constantly updated, and we look forward to future research findings.

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

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 27. 4-(1,1-Dioxido-1,2-benzisothiazol-2(3H)-yl)-2-piperazin-1-ylquinazoline. 2,4-Dichloroquinazoline (60 mg, 0.30 mmol), 2,3-dihydro-l,2-benzisothiazole 1,1-dioxide (50 mg, 0.30 mmol) and sodium hydride (11 mg, 0.45 mmol) were dissolved in anhydrous DMF (2 ml). The mixture was heated at 60¡ã C under nitrogen atmosphere for 10 min. Piperazine (52 mg, 0.60 mmol) was added and the heating was continued for 10 minutes. 5 The reaction mixture was diluted with water (0.5 ml), filtered and purified by preparative HPLC to give the acetate of the title compound as a solid (36 mg, 27 percent). 1H NMR (400 MHz, MeOD-d4) delta ppm 8.49 (1 H3 d) 7.58 – 7.87 (6 H, m) 730 – 7.38 (1 H, m) 5.58 (2 H, s) 4.03 – 4.16 (4 H3 m) 3.15 – 3.26 (4 H3 m); ESI-MS m/z M+H+ 382.

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; ASTRAZENECA AB; WO2007/108743; (2007); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

936-16-3, 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Potassium carbonate was dissolved in DMF, and 1,2-bezeneisothiazolin-1,1-dioxide (8) (1 equiv.) in dichloromethanewas added to the reaction solution, and stirred for overnight. Then,the reaction mixture was filtered through Celite, and washed with1 N HCl and saturated sodium hydrogen carbonate solution. Residualsolution was dried over magnesium sulfate, and concentratedin vacuo, and purified by column chromatography to afford the titlecompound.

As the paragraph descriping shows that 936-16-3 is playing an increasingly important role.

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