Day: August 24, 2020

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1. 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-isothiazole. To an oven dried schlenck flask charged with 6-bromo-isothiazole (0.5 g, 3.1 mmol), 4,4,5,5,4,4,5,5?-octamethyl-[2,2?]bi[[1,3,2]dioxaborolanyl] (0.85 g, 3.4 mmol), tri(dibenyzlideneacetone)dipalladium(0) (0.28 g, 0.31 mmol), tricyclohexylphosphine 20 (0.17 g, 0.61 mmol), potassium acetate (0.9 g, 9.14 mmol), followed by 1,4-dioxane (20 mL) was degassed for 5 min. under an atmosphere of nitrogen. The reaciton was heated at 100 C overnight, and cooled at rt. The reaction was diluted with dichloromethane, filtered through celite, washed with 1N sodium carbonate solution, water and brine, dried over sodium sulfate, and concentrated to give the product. LCMS m/z = 212 (M + 1).

24340-77-0 4-Bromoisothiazole 5200358, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; CEPHALON, INC.; HUDKINS, Robert L.; ZULLI, Allison L.; WO2015/100117; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-isothiazolecarboxylic acid (500 mg, 3.87 mmol, commercially available from e.g. Fluorochem or Astatech) in dry Dichloromethane (DCM) (12.9 ml) was stirred at room temperature under an atmosphere of argon. EDC (891 mg, 4.65 mmol) and HOBt (296 mg, 1.936 mmol) were added to the stirred solution. The resulting solution was stirred at room temperature under an atmosphere of argon for 1/2 hour. After this time, 1 ,1-dimethylethyl hydrazinecarboxylate (614 mg, 4.65 mmol) was added and the solution was stirred for a further 18 hours at room temperature (overnight). The solution was diluted with DCM (approx 30 ml) and washed with water (2 x 20ml). The organics were dried over MgSO4, filtered and concentrated under reduced pressure to give a brown coloured oil. The oil was chromatographed [Sitheta2, EtOAc/Hexane 0-100%] to give a thick, yellow-coloured oil which solidified on standing to afford the product in 480 mg. The residue was used directly in the next step. LCMS [M+H]+ 244.14 (at) 0.66 min (2 min run).

As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; DEAN, David Kenneth; MUNOZ-MURIEDAS, Jorge; SIME, Mairi; STEADMAN, Jon Graham Anthony; THEWLIS, Rachel Elizabeth Anne; TRANI, Giancarlo; WALTER, Daryl Simon; WO2010/125102; (2010); 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.

Step 2. A mixture of 23 (180 mg, 0.70 mmol), 1 (60 mg, 0.35 mmol), CsF (107 mg, 0.70 mmol), Cs2CO3 (458 mg, 1.41 mmol) in DMF (3 mL) was degassed and purged with N2 (3X). The mixture was stirred at 80¡ãC for 1 h, filtered, and then purified by prep-HPLC to give Compound 143 (15 mg, 5percent) as a light yellow solid. 1H NMR (DMSO-d6, 400MHz) delta 7.97 (d, 1H), 7.81 (s, 1H), 7.72 (d, 1H), 7.43 (s, 1H), 7.31 (s, 2H), 7.18 (s, 2H), 5.09 (s, 2H), 2.33 (s, 3H); LCMS (ESI): m/z 356.0 (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

87691-88-1, 3-Piperazinobenzisothiazole hydrochloride is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3. Preparation of ZPR in water/Na3CO . Na2SO4. In a three necked flask was charged BITP HC1 (lOg), CEI (10.35g) Na2C03 (14.1 g, ), Na2SO4 (40g) and water (50. 7g) and the reaction mixture was heated at reflux for 9 hours. After 9 hours reflux, the ziprasidone peak is No.71% area from the reaction mixture.; 6. Preparation of ZPR in the presence of Na2SO4. In a 250g three necked flask was charged water (25ml), Na2C03 (6.91g), Na2S04 (19.72g), BITP HCl (4.9g) and CEI (4.68g). The mixture was stirred at-100C for 12 hours. The isolated solid weights after drying 7.77g (purity by HPLC 85.15%).

The synthetic route of 87691-88-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/40160; (2005); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a 250 ml round bottom flask in water are sequentially added methanol 80 ml, 3,4-dichloro-thiazole-5-carboxylic acid (10.7 g, 53.8 mmol), gradually under the condition ice bath adds by drops two chlorine Asia sulphone (9.6 g, 80.7 mmol), the drop finishes heated to 40 degree c stirring 5 hours, after the reaction is complete to concentrate, add ethyl acetate to dissolve the filter, the filtrate of the distilled water are used to, saturated NaHCO3saturated NaCl wash again, anhydrous magnesium sulphate dried, concentrated, vacuum drying the white solid obtained 11.2 g, yield 98percent

18480-53-0 3,4-Dichloroisothiazole-5-carboxylic acid 49837, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Nankai University; Fan, Zi Jin; Zong, guangning; Li, Feng Yun; Li, yuedong; Li, Juan Juan; Ji, xiaotian; Chen, Lai; Zhu, Yu Jie; Liu, chaolun; Cheng, shengming; (21 pag.)CN103497182; (2016); B;,
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

Example 83 2-((5-Isobutyl-1-phenyl-1H-pyrazol-3-yl)methyl)-2,3-dihydrobenzo[d]isothiazole-1,1-dioxide (Compound 28) To a solution of 1,2-benzisothiazoline-1,1-dioxide (51.8 mg, 0.306 mmol) in N,N-dimethylformamide (1.0 mL) was added potassium carbonate (423 mg, 3.06 mmol), followed by stirring for 10 min. This solution was added with (5-isobutyl-1-phenyl-1H-pyrazol-3-yl)methyl bromide (108 mg, 0.367 mmol) in methylene chloride, and stirred for a day. Dilution was carried out in ethyl acetate before filtration. The filtrate was extracted with 1N HCl and an aqueous saturate sodium hydrogen carbonate solution. The organic layer was dried over magnesium sulfate, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=3:1?2:1) to afford the title compound (99.8 mg, 85.5percent). 1H NMR (400 MHz, CDCl3) delta 7.81-7.79 (m, 2H), 7.58-7.33 (m, 8H), 6.35 (s, 1H), 4.54 (s, 2H), 4.39 (s, 2H), 2.50 (d, J=7.06 Hz, 2H), 1.84-1.77 (m, 1H), 0.84 (d, J=6.56 Hz, 6H) 13C NMR (100 MHz, CDCl3) delta 147.2, 144.7, 139.7, 135.1, 134.0, 132.6, 129.2, 129.0, 128.1, 125.7, 124.6, 121.3, 106.0, 50.0, 41.3, 35.2, 28.3, 22.4

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

822-82-2, Isothiazole-4-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of l-[4-[methyl(tetrahydropyran-4-yl)amino]-5-oxido-6,7-dihydro- thieno[3,2-d]pyrimidin-5-ium-2-yl]azetidin-3-ol (5.0 mg, 15 muiotatauiotaomicronIota) in DCE (0.2 mL) was added solutions of 4-isothiazolecarboxylic acid (3.6 mg in 0.2 mL DCE, 28 muiotatauiotaomicronIota), DMAP (3.4 mg in 0.1 mL DCE, 28 muiotatauiotaomicronIota) and EDAC (5.3 mg in 0.2 mL DCE, 28 muiotatauiotaomicronIota) . The mixture was shaken at 50 C for 1 hour before it was concentrated in vacuo. Prep HPLC purification (acidic) afforded the title compound. 1H NMR (DMSO-d6) delta: 9.81 (s, 1H), 9.00 (s, 1H), 5.53 – 5.44 (m, 1H), 4.93 – 4.79 (m, 1H), 4.48 (dd, J = 10.4, 6.7 Hz, 2H), 4.16 (dd, J = 10.7, 3.8 Hz, 2H), 4.01 – 3.93 (m, 2H), 3.53 – 3.45 (m, 1H), 3.43 – 3.37 (m, 2H), 3.25 – 3.20 (m, 1H), 3.19 (s, 3H), 3.10 – 2.97 (m, 2H), 1.92 – 1.79 (m, 2H), 1.69 – 1.54 (m, 2H).HPLC-Retention time (XE Metode 7 CM) : 1.88 minutes.Detected “M + l”-mass: 450.12.

As the paragraph descriping shows that 822-82-2 is playing an increasingly important role.

Reference£º
Patent; LEO PHARMA A/S; LARSEN, Jens; (110 pag.)WO2019/57806; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

822-82-2, Isothiazole-4-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of Example 9b (0.19 M in N,N-dimethylacetamide, 237 muL, 0.045 mmol), N,N-diisopropylethylamine (0.21 M in N,N-dimethylacetamide, 262 muL, 0.055 mmol), HATU (0.21 M in N,N-dimethylacetamide, 238 muL, 0.05 mmol), and isothiazole-4-carboxylic acid (0.4M in N,N-dimethylacetamide, 125 muL, 0.05 mmol) were aspirated from their respective source vials, mixed through a perfluoroalkoxy alkanes mixing tube (0.2 mm inner diameter), and loaded into an injection loop. The reaction segment was injected into the flow reactor (Hastelloy coil, 0.75 mm inner diameter, 1.8 mL internal volume) set at 100 C., and passed through the reactor at 180 muL min-1 (10 minute residence time). Upon exiting the reactor, the reaction was loaded directly into an injection loop and purified using preparative HPLC to yield the title compound (9.95 mg, 49.50% yield). Samples were purified by preparative HPLC on a Phenomenex Luna C8 (2) 5 mum 100 AXIA column (50 mm¡Á21.2 mm). A gradient of acetonitrile (A) and 0.1% trifluoroacetic acid in water (B) was used, at a flow rate of 30 mL/min (0-0.5 minutes 5% A, 0.5-6.5 minutes linear gradient 5-60% A, 6.5-7.0 minutes linear gradient 60-100% A, 7.0-8.9 minutes 100% A, 8.9-9.0 minutes linear gradient 100-5% A, 9.0-10 minutes 5% A). A sample volume of 1.0 mL was injected directly from the flow reactor stream to the HPLC system. A custom purification system was used, consisting of the following modules: Gilson 305 and 306 pumps; Gilson 806 Manometric module; Gilson UV/Vis 155 detector; Gilson 506C interface box; Gilson FC204 fraction collector; Agilent G1968D Active Splitter; Thermo MSQ Plus mass spectrometer. The system was controlled through a combination of Thermo Xcalibur 2.0.7 software and a custom application written in-house using Microsoft Visual Basic 6.0. 1H NMR (400 MHz, DMSO-d6) delta 4.69 (d, J=3.9 Hz, 2H), 5.62 (s, 2H), 6.43 (s, 1H), 6.84 (d, J=2.0 Hz, 1H), 7.51 (d, J=2.0 Hz, 1H), 8.18 (s, 1H), 8.32 (s, 1H), 8.96 (s, 1H), 9.59 (s, 1H). MS (APCI) m/z 439.1 [M+H]+.

The synthetic route of 822-82-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; AbbVie Inc.; Dai, Yujia; McClellan, William; Michaelides, Mike; Sweis, Ramzi; Wilson, Noel; Dietrich, Justin; (90 pag.)US2017/174688; (2017); 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.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

a) 5-Isothiazolecarboxylic acid was prepared from isothiazole, n-BuLi and dry ice according to the method of step a of Example 258.

The synthetic route of 288-16-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Monsanto Company; US5498630; (1996); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

After 10 g of 50 mmol of 3,4-dichloro-isothiazole carboxylic acid II was added to 100 ml flask was added 30 ml of thionylchloride, refluxed for 5 hours, thionyl chloride was distilled off at atmospheric pressure, the residue was water pump vacuumdistillation at 100-110 degrees C compound fraction collected between 10.6 g yellow solid 3,4-dichloro-isothiazole carboxylicacid chloride III, a yield of 96.3percent, 3,4-dichloro-isothiazole carboxylic acid chloride III prepared a pro rata amount of expanded orreduced, the volume of the reaction vessel according to the corresponding scaled up or down, a commercially availablecompound II has the same effect.

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

Reference£º
Patent; Jiangxi Tianren Ecology Co., Ltd.; Nankai University; Chen, Xiaoyan; Liu, Xiping; Fan, Zhijin; Liang, Xiaowen; Li, Yuedong; Mao, Wutao; Li, Juanjuan; Wang, Dun; Wang, Shuhua; Zhou, Lifeng; Ji, Xiaotian; HUA, XUEWEN; (23 pag.)CN102942565; (2016); B;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com