Category: 5908-62-3

As a common heterocyclic compound, it belongs to thiazolidine compound, name is 1,1-Dioxo-isothiazolidine, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

(1S,2S)-N1,N2-Dimethylcyclohexane-1,2-diamine (46.1 mg, 0.30 mmol) and copper iodide (56.3 mg, 0.30 mmol) were added to a mixture of 2,3-dichloro-5-nitropyridine (571 mg, 2.96 mmol), isothiazolidine 1,1-dioxide (430 mg, 3.55 mmol) and potassium carbonate (817.5 mg, 5.92 mmol) in dioxane (6 mL) under N2. The reaction mixture was stirred at 100 C. for 16 h. The mixture was filtered, and the filtrate was extracted with ethyl acetate. The organic extracts were dried over Na2SO4, filtered, and the filtrate concentrated under reduced pressure. The resultant crude product was purified by flash chromatography (petroleum ether/ethyl acetate=100:0 to petroleum ether/ethyl acetate=50:50) to afford compound 58a as a white solid (600 mg, 73%).

With the complex challenges of chemical substances, we look forward to future research findings about 5908-62-3,belong thiazolidine compound

Reference£º
Patent; Janssen Biotech, Inc.; Lu, Tianbao; Allison, Brett Douglas; Barbay, Joseph Kent; Connolly, Peter J.; Cummings, Maxwell David; Diels, Gaston; Edwards, James Patrick; Kreutter, Kevin D.; Philippar, Ulrike; Shen, Fang; Thuring, Johannes Wilhelmus John Fitzgerald; Wu, Tongfei; (412 pag.)US2018/170909; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

5908-62-3,1,1-Dioxo-isothiazolidine, cas is 5908-62-3, it is a common heterocyclic compound, the thiazolidine compound, its synthesis route is as follows.

100 mg (0.231 mmol) of (¡À)-1-(4-bromophenyl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide (Example 49A), 33.6 mg (0.278 mmol) of 1,2-thiazolidine 1,1-dioxide (CAS [5908-62-3]), 64 mg (0.46 mmol) of potassium carbonate and 13 mg (0.023 mmol) of allylchloropalladium dimer (CAS [12012-95-2]) are charged in 3 ml of 2-methyltetrahydrofuran and the suspension is degassed with argon for 10 min. Then 39 mg (0.093 mmol) of di-tert-butyl(2?,4?,6?-triisopropylbiphenyl-2-yl)phosphane (CAS [564483-19-8]) are added, degassing with argon is carried out again, and the mixture is heated at 80 C. for 16 h. The crude mixture is filtered, and then the solvent is removed and the residue obtained is purified by preparative HPLC. This gave 32 mg (29% of theory) of the desired product as a solid.

As the rapid development of chemical substances, we look forward to future research findings about 5908-62-3

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; SIEGEL, STEPHAN; BAURLE, STEFAN; CLEVE, ARWED; HAENDLER, BERNARD; FERNANDEZ-MONTALVAN, AMAURY ERNESTO; MONNING, URSULA; KRAUSE, SABINE; LEJEUNE, PASCALE; SCHMEES, NORBERT; BUSEMANN, MATTHIAS; HOLTON, SIMON; KUHNKE, JOACHIM; (434 pag.)JP2015/529192; (2015); A;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

Name is 1,1-Dioxo-isothiazolidine, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

A Schlenk tube was charged with 5-[5-({3-[(1 R,5S/1 S,5R)-1-(4-bromophenyl)-3- azabicyclo[3.1.0]hex-3-yl]propyl}thio)-4-methyl-4H-1 ,2,4-triazol-3-yl]-2-methylquinoline (cf. Example 2; 0.15 g), isothiazolidine 1 ,1 -dioxide (46 mg), tris(dibenzylideneacetone)- dipalladium(O) (6 mg), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (10 mg), cesium carbonate (130 mg) and 1 ,4-dioxane (2 mL). The Schlenk tube was sealed with a teflon screwcap and the reaction mixture was stirred at 100 0C for 12 h. The reaction mixture was allowed to cool to room temperature, diluted with dichloromethane (10 mL), filtered EPO and concentrated in vacuo. The crude product was purified by flash chromatography (dichloromethane to 10% MeOH in dichloromethane) to give 50 mg of the free base of the title compound. To a solution of this material in dichloromethane (0.3 mL) was added HCI (0.087 mL, 1 M in Et2O), the solvent evaporated in vacuo and the material thus obtained triturated with Et2O to give 52 mg of the title compound as a white solid.NMR (1H, DMSO): delta 10.57 (bs,1 H), 8.27 (bd, 1 H), 8.19 (d, 1 H), 7.94 (t, 1 H), 7.82 (d, 1 H), 7.55 (d, 1 H)1 7.32 (d, 2H), 7.18 (d, 2H), 4.03 (dd, 1H), 3.72 (m, 3H), 3.60/3.20 (bm, 8H), 3.45 (s, 3H), 2.75 (s, 3H), 2.41 (m, 2H), 2.25 (m, 2H), 2.14 (m, 1 H), 1.66/1.10 (t/m, 2H). MS (ml z) 575 [MH]+.

With the complex challenges of chemical substances, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

Reference£º
Patent; GLAXO GROUP LIMITED; WO2007/22980; (2007); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belongs to thiazolidine compound, name is 1,1-Dioxo-isothiazolidine, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

Intermediate 6 (0.090 g, 0.093 mmol) was combined with isothiazolidine 1,1-dioxide (0.112 g, 0.926 mmol) in anhydrous dichloromethane (0.93 mE). paraToluenesulfonic acid monohydrate (1.761 mg, 9.26 tmol) was added in one portion. The reaction was stirred at room temperature for 100 minutes.10510] The entire reaction mixture was purified by silica gel flash column chromatography (0-40% acetone-heptane, gradient elution, 24 g silica column, TEC in 40% acetoneheptane, visualize under UV) to give a mixture of Example 18 and residual unreacted isothiazolidine 1,1-dioxide.10511] The mixed material was again purified by silica gel flash column chromatography (0-50% acetonitrile-dichloromethane, gradient elution, 24 g column, TEC in 30% acetonitrile-dichloromethane, visualize under UV) to give Example 18 (0.02 1 g, 0.019 mmol, 20.4% yield) as a white solid.Example 1810512] ESIMS [M+NH4] 1078.9, [M-H] 1059.9.10513] HRMS: calculated for C57H92N2014SNa sodiumadduct-1083.6167. Found 1083.6151.10514] ?H NMR (600 MHz, Chloroform-d) oe 6.45 (dd,J=14.5, 11.0 Hz, 1H), 6.21 (dd, J=14.6, 10.7 Hz, 1H), 6.14(dd, J=14.8, 10.8 Hz, 1H), 5.98 (d, J=10.9 Hz, 1H), 5.35 (dd,J=14.8, 9.8 Hz, 1H), 5.20 (d, J=5.8 Hz, 1H), 5.09 (d, J=9.8Hz, 1H), 4.72 (d, J=12.1 Hz, 1H), 4.61 (m, 1H), 4.46 (s, 1H),4.10 (d, J=6.9 Hz, 1H), 3.96 (t, J=11.4 Hz, 1H), **373 (t,J=5.5 Hz, 2H), 3.68 (d, J=6.9 Hz, 1H), 3.59 (m, 4H), 3.53(m, 2H), 3.46 (s, 3H), 3.28 (s, 3H), 3.21 (m, 1H), 3.13 (m,1H), 3.07 (m, 2H), 3.05-2.99 (m, 1H), 2.97 (q, J=8.0 Hz,1H), 2.78 (dq, J=14.4, 7.1 Hz, 1H), 2.44-2.33 (m, 1H), 2.31(m, 2H), 2.27-2.19 (m, 1H), 2.19-2.12 (m, 2H), 2.07-1.94 (m, 2H), 1.88 (s, 3H), 1.83 (d, J=12.9 Hz, 1H), 1.74 (m, 3H),1.66 (m, 7H), 1.56-1.44 (m, 1H), 1.43 (m, 2H), 1.41-1.15(m, 12H), 1.04 (m, 7H), 0.91 (m, 8H), 0.84 (d, J=6.7 Hz,3H), 0.70 (q, J=12.0 Hz, 1H).

With the complex challenges of chemical substances, we look forward to future research findings about 5908-62-3,belong thiazolidine compound

Reference£º
Patent; NOVARTIS AG; BONAZZI, Simone; CONNOLLY, Michael; GLASS, David Jonathan; MIHALIC, Manuel; PATTERSON, Andrew William; ROGGO, Silvio; SHAVLAKADZE, Tea; (68 pag.)US2019/92788; (2019); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO419,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

To a solution of 6-(6-fluoro-4-iodo-2-pyridyl)-5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H- pyrido[4,3-d]pyrimidine (the product of step 1 in Example 96, 100 mg, 223 muiotaetaomicron) in dioxane ( 3mL) was added isothiazolidine-1,1-dioxide (54.1 mg, 446 muiotaetaomicron), cesium carbonate (145 mg, 446 muetaiotaomicron), Xantphos (25.8 mg, 44.6 muetaiotaomicron) and Pd(OAc)2(5.01 mg, 22.3 muetaiotaomicron). After being heated at 100 C with stirring for 20 hrs under argon, the resulting reaction mixture was then filtered and the filtrate was concentrated in vacuo. The residue was purified by prep-HPLC to give 2-[2-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-4- pyridyl]-1,2-thiazolidine-1,1-dioxide (8 mg) as a light yellow solid. 1H NMR (400MHz, DMSO- d6) delta ppm: 8.99 (d, 2H), 8.95 (s, 1H), 7.64 (t, 1H), 6.32 (s, 1H), 6.15 (s, 1H), 5.69-5.64 (m, 1H), 4.47-4.36 (m, 1H), 3.89 – 3.79 (m, 2H), 3.68-3.59(m, 2H), 3.54 – 3.43 (m, 1H), 3.14 – 2.98 (m, 2H), 2.42-2.37 (m, 2H), 1.52 (d, 3H). MS obsd (ESI) [(M+H)+]: 442.

With the synthetic route has been constantly updated, we look forward to future research findings about 1,1-Dioxo-isothiazolidine,belong thiazolidine compound

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Yongguang; YANG, Song; (211 pag.)WO2018/1952; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

1,1-Dioxo-isothiazolidine, cas is 5908-62-3, it is a common heterocyclic compound, the thiazolidine compound, its synthesis route is as follows.,5908-62-3

108371 To a solution of isothiazolidine 1,1-dioxide (500 mg, 4.13 mmol) in acetonitrile (10 mL) was added potassium carbonate (1.14 g, 8.25 mmol), 4-methoxybenzyl chloride (646 mg, 4.13 mmol). The mixture was heated to 80 C for 12 h under nitrogen atmosphere. The mixture was poured into H20 (50 mL) and extracted with ethyl acetate (50 mL). The organic layer was washed with H20 (50 mL x 2) and saturated brine solution (50 mL). The organic layers was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The residue was purified via flash silica chromatography (solvent gradient: 0-40% ethyl acetate in petroleum ether) to yield 1.0 g (99% yield) of the title compound as a white solid. ?H NMR (400 MHz, CDC13) oe 7.28 (d, J= 8.4 Hz, 2H), 9.89 (d, J= 8.8 Hz, 2H), 4.13 (s, 2H), 3.82 (s, 3H), 3.23 – 3.18 (t,J= 8.8 Hz, 2H), 3.12-3.07 (m, 2H), 2.34-2.25 (m, 2H).

5908-62-3 is used more and more widely, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

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Patent; GENENTECH, INC.; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; BRAUN, Marie-Gabrielle; GIBBONS, Paul; LEE, Wendy; LY, Cuong; RUDOLPH, Joachim; SCHWARZ, Jacob; ASHKENAZI, Avi; FU, Leo; LAI, Tommy; WANG, Fei; BEVERIDGE, Ramsay; ZHAO, Liang; (652 pag.)WO2018/166528; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

1,1-Dioxo-isothiazolidine, cas is 5908-62-3, it is a common heterocyclic compound, the thiazolidine compound, its synthesis route is as follows.,5908-62-3

Example 98 Preparation of Intermediate 100 [0785] [0786] To an oven dried 50 mL round-bottom flask, methyl 2-bromo-5-methylbenzoate (352 mg, 1.54 mmol), sultam (236 mg, 1.95 mmol), cesium carbonate (732 mg, 2.25 mmol), palladium acetate (40.4 mg, 0.18 mmol), and Xanphos (136 mg, 0.235 mmol) were added and flask was placed under argon. The reagents were suspended in 8 mL of anhydrous dioxane and mixture was heated at 100 C. overnight. After cooling to room temperature, the reaction mixture was filtered, washing with ethyl acetate. The combined filtrate was concentrated under reduced pressure and resulting film was purified by silica gel column chromatography (25-100% ethyl Acetate in hexanes) to yield intermediate 100 (322 mg, 78%) as a yellow off-white solid. [0787] 1H-NMR (DMSO, 400 MHz): delta 7.75 (d, 1H), 7.44 (m, 1H), 7.35 (m, 1H), 3.89 (s, 3H), 3.81 (t, 2H), 3.28 (t, 2H), 2.55 (m, 2H), 2.39 (s, 3H). [0788] LCMS m/z [M+H]+ C12H15NO4S requires: 270.07. Found 270.12.

5908-62-3 is used more and more widely, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

Reference£º
Patent; Siegel, Dustin; Sperandio, David; Yang, Hai; Sangi, Michael; Parrish, Jay P.; Hui, Hon Chung; US2013/273037; (2013); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

Name is 1,1-Dioxo-isothiazolidine, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

To a solution of 3-iodo-N-(3,4,5-trifluorophenyl)-4,5,6,7-tetrahydropyrazolo[l,5- a]pyridine-5-carboxamide (compound lh, 20 mg, 0.048 mmol) in DMSO (1.0 mL) was added Cul (2 mg, 0.0095 mmol), K2C03 (7 mg, 0.095 mmol), N,N’-dimethyl-l,2-cyclohexanediamine (2 mg, 0.0095 mmol), and 1,2-thiazolidine 1,1-dioxide (compound 5a, 5 mg, 0.057 mmol). The reaction mixture was stirred at 110 C for 18 hours and then purified by flash chromatography and prep-HPLC to give 3-(l,l-dioxo-l,2-thiazolidin-2-yl)-N-(3,4,5-trifluorophenyl)-4,5,6,7- tetrahydropyrazolo[l,5-a]pyridine-5-carboxamide (Example 5, 11.5 mg) as a white solid. 1H NMR (400MHz, CDC13) delta 8.21 (s, 1H), 7.56 (s, 1H), 7.41 – 7.26 (m, 2H), 4.27 – 4.14 (m, 1H), 4.07 (m, 1H), 3.73 – 3.54 (m, 2H), 3.36 (t, 2H), 3.25 – 3.08 (m, 2H), 2.84 – 2.72 (m, 1H), 2.60 – 2.39 (m, 3H), 2.34 – 2.21 (m, 1H). MS obsd. (ESI+) [(M+H)+]: 415

With the complex challenges of chemical substances, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

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Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HU, Taishan; SHEN, Hong; HAN, Xingchun; (45 pag.)WO2018/11100; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

Name is 1,1-Dioxo-isothiazolidine, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

1,2-thiazolidine 1,1-dioxide (0.031 g, 0.259 mmol) in dimethylformamide (1 mL) was treated with 60% sodium hydride (0.012g, 0.518 mmol, 0.021 g of a 60%> in oil dispersion). The reaction mixture was stirred for 5 min. To this solution was added Example 41b (0.05 g, 0.086 mmol). The reaction mixture was stirred at room temperature for 2 hours. 2 N NaOH (1 mL) was added and the reaction mixture was heated at 65 C for 2 hours. After cooling to room temperature, the reaction mixture was partitioned between water and ethyl acetate. The aqueous layer was extracted with additional ethyl acetate twice. The combined organic layers were washed with brine, dried over MgSC^, filtered, and concentrated. The residue was purified by preparative HPLC (CI 8, 10-80% acetonitrile in 0.1% TFA water) to afford 0.025 g (64%) of the title compound. 1H NMR (500 MHz, DMSO-d6) delta 2.21-2.25 (m, 2H), 3.15 (t, J=6.97 Hz, 2H), 3.23-3.27 (m, 2H), 3.50 (s, 3H), 4.13 (s, 2H), 6.25-6.26 (m, 1H), 6.88 (d, J=7.63 Hz, 2H), 7.00 (d, J=8.54 Hz, 1H), 7.03-7.05 (m, 1H), 7.25-7.30 (m, 4H), 7.34 (dd, J=8.39, 2.29, 1H), 7.48 (d, J=2.44 Hz, 1H), 12.00 (s, 1 H). MS (ESI+) m/z 450.2 (M+H)+.

With the complex challenges of chemical substances, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

Reference£º
Patent; ABBVIE INC.; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; WANG, Le; PRATT, John K.; MCDANIEL, Keith F.; DAI, Yujia; FIDANZE, Steven D.; HASVOLD, Lisa; HOLMS, James H.; KATI, Warren M.; LIU, Dachun; MANTEI, Robert A.; MCCLELLAN, William J; SHEPPARD, George S.; WADA, Carol K.; WO2013/97601; (2013); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

Name is 1,1-Dioxo-isothiazolidine, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 5908-62-3, its synthesis route is as follows.,5908-62-3

Example 9 Preparation of Intermediate 11 [0449] [0450] To an oven dried 50 mL round-bottom flask, methyl 2-bromo-5-methylbenzoate (352 mg, 1.54 mmol), sultam (236 mg, 1.95 mmol), cesium carbonate (732 mg, 2.25 mmol), palladium acetate (40.4 mg, 0.18 mmol), and Xanphos (136 mg, 0.235 mmol) were added and flask was placed under argon. Reagents were suspended in 8 mL of anhydrous dioxane and mixture was heated at 100 C. overnight. After cooling to room temperature, reaction mixture was filtered, washing with ethyl acetate. Combined filtrate was concentrated under reduced pressure and resulting film was purified by silica gel column chromatography (25-100% Ethyl Acetate in Hexanes) to yield intermediate 11. [0451] 1H-NMR (DMSO, 400 MHz): delta 7.75 (d, 1H), 7.44 (m, 1H), 7.35 (m, 1H), 3.89 (s, 3H), 3.81 (t, 2H), 3.28 (t, 2H), 2.55 (m, 2H), 2.39 (s, 3H). [0452] LCMS m/z [M+H]+C12H15NO4S requires: 270.07. Found 270.12.

With the complex challenges of chemical substances, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

Reference£º
Patent; GILEAD SCIENCES, INC.; Boojamra, Constantine G.; Hui, Hon Chung; Jansa, Petr; Mackman, Richard L.; Parrish, Jay P.; Sangi, Michael; Siegel, Dustin; Sperandio, David; Yang, Hai; US2013/164280; (2013); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com