Tag: M.W:100-200

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27148-03-4,Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide,as a common compound, the synthetic route is as follows.

General procedure: For 6: A solution of thiosaccharin (tsacH) (0.06 g, 0.307 mmol) in chloroform (8 cm3) was added to a solution of [PtCl2(kappa2-dppm)] (0.10 g, 0.154 mmol) in chloroform (10 cm3). A few drops of triethylamine were added and the resulting mixture was heated under reflex for 1 h. This produced a yellow solution was filtered off and reduced to half volume. Methanol (2 cm3) was added and the mixture was set a side to evaporate slowly at room temperature. The yellow crystalline solid thus formed was filtered off and dried in a vacuum oven (0.12 g, 91%)., 27148-03-4

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

55512-82-8, 3-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,55512-82-8

Intermediate I-1 (15 mg, 0.045 mmol) and 3-bromoisothiazole (10.98 mg, 0.067 mmol) were dissolved in DMF (446 muL). PdCl2(dppf)-CH2Cl2 (2.187 mg, 2.68 mumol) was added and the reaction mixture was degassed by bubbling with argon for 15 minutes. Sodium carbonate (2 M, 26.8 muL, 0.054 mmol) was added and the reaction mixture was degassed for 5 minutes, then sealed and heated to 90 ¡ãC in the microwave for 30 minutes. The reaction mixture was diluted with DMF, filtered, and purified by preparative HPLC (Method D, 35 to 80percent B in 10 minutes) to give Example 5 (5.0 mg, 0.017 mmol, 37.2percent): 1H NMR (500MHz, METHANOL-d4) delta 8.89 (d, J=4.7 Hz, 1H), 8.59 (s, 1H), 8.13 (d, J=1.9 Hz, 1H), 8.10 (d, J=4.7 Hz, 1H), 7.84-7.52 (m, 2H), 2.64 (s, 3H); LC^MS: Method H, RT = 1.08 min, MS (ESI) m/z: 293.9 (M+H)+; Analytical HPLC Method B: 97.4percent purity

As the paragraph descriping shows that 55512-82-8 is playing an increasingly important role.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; RICHTER, Jeremy M.; ZHANG, Xiaojun; PRIESTLEY, Eldon Scott; (111 pag.)WO2018/13772; (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

7716-66-7,7716-66-7, 3-Chlorobenzo[d]isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2)Preparation of 4-(1,2-benzisothiazol-3-yl)-1-piperazine3-chloro-(1,2-benzisothiazole) (14g, 200 mmol) and anhydrous piperazine (6.8g, 40 mmol) are placed in an egg type flask and heated at 125¡ãC for 24 hours.After completion of reaction, 52 ml of an ice-water mixture is added for quenching the reaction.The mixture is further added with 3.2g of 50percent NaOH solution, stirred 5 minutes and extracted with CH2Cl2 (50ml*3).The organic layer is washed with an ice-water mixture (50ml*2) and saturated saline (50ml*2), and dried over anhydrous MgSO4 to obtain 4-(1,2-benzisothiazol-3-yl)-1-piperazine.

As the paragraph descriping shows that 7716-66-7 is playing an increasingly important role.

Reference£º
Patent; Jiangsu Guohua Investment Co., Ltd; Shanghai Institute of Pharmaceutical Industry; EP2322520; (2011); 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.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

3,4-Dichloroisothiazol-5-ylcarboxylic acid (400 mg, 2.02 mmol) was dissolved in abs. dichloromethane (20 ml), and triethylamine (0.85 ml, 6.06 mmol) was added. After stirring at room temperature for 5 minutes, pyrrolidine-i-amine (209 mg, 2.42 mmol) and 2,4,6-tripropyl-1,3, 5,2,4,6-trioxatriphosphorinane 2,4,6-trioxide (1.80 ml, 3.03 mmol, 50percent solution in tetrahydrofuran) were added. The resulting reaction mixture was stirred at room temperature for a further 30 minutes, and then water, sat. sodium hydrogencarbonate solution and dichloromethane were added. The aqueous phase was repeatedly extracted vigorously with dichloromethane, and the combined organic phases were then dried over magnesium sulfate, filtered and concentrated. Final purification of the resulting crude product by colunm chromatography gave 3,4-dichloro-N-(pyr- rolidin-i-yl)-i,2-thiazole-5-carboxamide in the form of a colorless solid (520 mg, 92percent of theory). ?H-NMR (400 MHz, CDC13 oe, ppm) 3.38-3.28 (m, 2H), 2.73-2.64 (m, 2H), 2.03-1.98 (m, 4H). 3,4-Dichloro-N-(pyrrolidin- 1 -yl)-i ,2- thiazole-5-carboxamide (120 mg, 0.45 mmol) was dissolved in abs. tetrahydroffiran (5 ml) under argon, and sodium hydride (40 mg, 1.99 mmol, 60percent purity) was added at room temperature. Stirring at room temperature for 30 minutes was followed by the addition of picolyl chloride (HC1 salt, 74 mg, 0.45 mmol), and the resulting reaction mixture was stirred under reflux conditions for approx. 3 hours. After cooling to room temperature, sat. sodium hydrogencarbonate solution, water and dichloromethane were added. The aqueous phase was repeatedly extracted vigorously with dichloromethane, and the combined organic phases were then dried over magnesium sulfate, filtered and concentrated. Final purification of the resulting crude product by colunm chromatography gave 3,4-dichloro-N-(pyridin-2-yl- methyl)-N-(pyrrolidin- 1 -yl)-i ,2-thiazole-5-carboxamide in the form of a colorless solid (112 mg, 69percent of theory). ?H-NMR (400 MHz, CDC13 oe, ppm) 8.62 (m, 1H), 7.71-7.67 (m, 1H), 7.53 (m, 1H), 7.33 (m, 1H), 5.15 (s, 2H), 4.18-4.13 (m, 2H), 3.71-3.66 (m, 2H), 2.30-2.24 (m, 2H), 2.13-2.08 (m, 2H).

18480-53-0, As the paragraph descriping shows that 18480-53-0 is playing an increasingly important role.

Reference£º
Patent; Bayer CropScience Aktiengesellschaft; FRACKENPOHL, Jens; BOJACK, Guido; BRUENJES, Marco; HELMKE, Hendrik; LEHR, Stefan; BRUECHNER, Peter; TIEBES, Joerg; MOSRIN, Marc; DITTGEN, Jan; SCHMUTZLER, Dirk; DESBORDES, Philippe; (92 pag.)US2018/206498; (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.111248-89-6,1,3-Dihydrobenzo[c]isothiazole 2,2-dioxide,as a common compound, the synthetic route is as follows.

c. 1-Methyl-1,3-dihydrobenzo[c]isothiazole-2,2-dioxide To a suspension of 1,3-dihydrobenzo[c]isothiazole-2,2-dioxide (280 mg, 1.655 mmol) and potassium carbonate (229 mg, 1.66 mmol) in DMF (5 mL) was added iodomethane (414 muL, 6.62 mmol). The reaction was stirred for 6 h at rt and was then quenched with a sat. NH4Cl solution. The reaction mixture was concentrated and purified by column chromatography (CyHex/acetone) to afford the title compound as a white solid (270 mg, 89%)., 111248-89-6

111248-89-6 1,3-Dihydrobenzo[c]isothiazole 2,2-dioxide 15536009, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Merck Patent GmbH; Cancer Research Technology, Ltd.; SCHIEMANN, Kai; BLAGG, Julian; MALLINGER, Aurelie; RINK, Christian; SEJBERG, Jimmy; HONEY, Mark; (139 pag.)US2016/16951; (2016); 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

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: 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