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,936-16-3

Step 2. A mixture of 12 (100 mg, 0.40 mmol), 1 (67 mg, 0.40 mmol), potassium carbonate (55 mg, 0.40 mmol), Cul (3.8 mg, 0.019 mmol), and L-proline (2.3 mg, 0.019 mmol) in dioxane (4 mL) was stirred at 110¡ãC for 16 hours under an inert atmosphere. Upon completion, water (40 mL) was added and the reaction mixture was extracted with EtOAc (90 mL). The organic phase was washed with brine (50 mL) and concentrated under reduced pressure. Purification with prep-HPLC (0.075percent TFA/CH3CN/H20 system) resulted in Compound 121 (40 mg, 29percent) as yellow solid and TFA salt. 1H NMR (DMSO-d6, 400MHz) delta 8.69-8.68 (d, 1H), 8.53-8.52 (d, 1H), 7.99-7.94 (m, 3H), 7.77 (m, 1H), 7.67-7.62 (m, 3H), 7.07-7.05 (d, 1H), 6.83-6.81 (d, 1H), 4.95 (s, 2H); LCMS (ESI): m/z 340.1 (M+H).

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; 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

936-16-3, 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.

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

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

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.

Intermediate 30Ethyl 1 -[4-(1 ,1 -dioxido-1 ,2-benzisothiazol-2(3H)-yl)phenyl]-3-[[(frapis-4- methylcyclohexyl)carbonyl](1-methylethyl)amino]-1H-pyrazole-4-carboxylateA solution of Intermediate 5 (108 mg), 2,3-dihydro-1 ,2-benzisothiazole 1 ,1 -dioxide (35 mg), copper (I) iodide (4 mg), potassium carbonate (58 mg) and (IR^RJ-lambda/./V-dimethyl-i ^- cyclohexanediamine (12 mg) in DMF (4 mL) was heated in a microwave at 100¡ã C, 300 W for 1 h and then evaporated to dryness. The residue was dissolved in ethyl acetate and washed sequentially with aqueous sodium bicarbonate solution, water and 2M HCI, dried using a EPO hydrophobic frit and evaporated to dryness. The crude product was then purified by MDAP HPLC to give the title compound. MS calcd for (C30H36N4O5 + H)+: 565 MS found (electrospray): (M+H)+ = 565

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

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/39146; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

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

936-16-3, 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.

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

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

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

936-16-3, Step2. A mixture of compound 17 (300 mg, 1.18 mmol), 1 (240 mg, 1.42 mmol), Cs2CO3 (769 mg, 2.36 mmol), Cul (67 mg, 0.35 mmol) and 2-(dimethylamino)acetic acid hydrochloride (49 mg, 0.354 mmol) in dioxane (20 mL) was degassed and purged with N2 for (3X). The mixture was stirred at 100¡ãC for 12 hrs, filtered, and then diluted with ethyl acetate (50 mL). The solution was washed with saturated brine (50 mL), dried over anhydrous sodium sulfate, filtered, and concentrated to give 18 as a dark brown oil which was used without further purification.

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

2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, cas is 936-16-3, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,936-16-3

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 rapid development of chemical substances, we look forward to future research findings about 936-16-3

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

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, To a solution of {1-(tert-butyl)-5-(4-piperidin-1-yl-phenyl)-1H-pyrazol-3-yl}methanol (54.9 mg, 0.175 mmol) in methylene chloride (1.5 mL) were added PPh3 (93.1 mg, 0.355 mmol) and CBr4 (121 mg, 0.365 mmol) at 0¡ã C., followed by stirring at the same temperature for one hour to give {1-(tert-butyl)-5-(4-piperidin-1-yl-phenyl)-1H-pyrazol-3-yl}methyl bromide. When the reaction was completed as measured by TLC(Hexane:EtOAc=2:1), 1,2-benzisothiazoline-1,1-dioxide (27.3 mg, 0.161 mmol) in N,N-dimethylformamide (1.5 mL) was added dropwise. At the same temperature, potassium carbonate (228 mg, 1.65 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, after which extraction was carried out with ethyl acetate and brine. The organic layer thus formed was dried over anhydrous magnesium sulfate, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=4:1?1:1) to afford the title compound (15.2 mg, 20percent, white solid). (0324) M.P. 150.4-165.2¡ã C.; (0325) 1H NMR (300 MHz, CDCl3) delta 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 (brs, 4H), 1.79-1.74 (brs, 4H), 1.67-1.63 (brs, 2H), 1.49 (s, 9H); (0326) 13C NMR (75 MHz, CDCl3) delta 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

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

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

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

936-16-3, Example 86 2-[{1-(2,6-Dichlorophenyl)-5-isobutyl-1H-pyrazol-3-yl}methyl]-2,3-dihydro[d]isothiazole 1,1-dioxide (Compound 31) To a solution of N,N-dimethylformamide (1 mL) in 1,2-benzisothiazoline-1,1-dioxide (31.4 mg, 0.186 mmol) was added potassium carbonate (255 mg, 1.85 mmol) at room temperature, followed by stirring for 10 min. This solution was slowly added with drops of {1-(2,6-dichlorophenyl)-5-isobutyl-1H-pyrazol-3-yl}methyl bromide (73.3 mg, 0.202 mmol) in methylene chloride (2 mL), and stirred for a day at room temperature. When the reaction was completed as measured by TLC (Hexane:EtOAc=4:1), 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=2:1) to afford the title compound (61.9 mg, 74percent, white solid). M.P. 130.2-139.2¡ã C.; 1H NMR (300 MHz, CDCl3) delta 7.84 (d, J=7.7 Hz, 1H), 7.62-7.30 (m, 6H), 6.40 (s, 2H), 4.57 (s, 2H), 4.38 (s, 2H), 2.24 (d, J=7.3 Hz, 2H), 1.92-1.79 (m, 1H), 0.89 (d, J=6.6 Hz, 6H); 13C NMR (75 MHz, CDCl3) delta 148.3, 146.4, 135.4, 135.2, 135.1, 134.2, 131.0, 129.0, 128.8, 124.6, 121.4, 105.4, 49.6, 41.3, 34.8, 27.5, 22.5

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

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,936-16-3

General procedure: To the mixture of the precursor 10(2.26 g, 10.1 mmol, 1.5 equiv) and tert-butyl 1,2,5-thiadiazolidine-2-carboxylate 1,1-dioxide (1.50 g, 6.75 mmol, 1.0 equiv) in dry DMF(10 mL), was added Cs2CO3 (6.60 g, 20.25 mmol, 3.0 equiv). Themixture was stirred at room temperature overnight, and thenextracted with ethyl acetate. The organic phase was washed withsaturated NaHCO3 and brine, dried over anhydrous Na2SO4, filteredand concentrated. The resulting residue was purified via silica gelchromatography to give 11a as colorless oil (1.96 g, 79%).

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

Reference£º
Article; Chen, Shulun; Guo, Wei; Liu, Xiaohua; Sun, Pu; Wang, Yi; Ding, Chunyong; Meng, Linghua; Zhang, Ao; European Journal of Medicinal Chemistry; vol. 179; (2019); p. 38 – 55;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com