Category: 5908-62-3

5908-62-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.

A flask was charged under nitrogen with 3-bromo-5-iodo-benzoic acid tert-butyl ester D8b (1 g, 2.6 mmol, 1 equiv), Cs2CO3 (1.26 g, 3.9 mmol, 1.5 equiv), tris (DIBENZYLIDENEACETONE) DIPALLADIUM (0) (12 mg, 0.013 mmol, 0.005 equiv), Xantphos (22 mg, 0.038 mmol, 0.015 equiv) and toluene (20 ML). ISOTHIAZOLIDINE 1,1-dioxide (D22a) (350 mg, 2.9 mmol, 1.1 equiv) was then added and the resulting mixture was stirred at 100C for 16 h then cooled to room temperature and diluted with AcOEt. The organic phase was washed with saturated aqueous NAHC03 solution, dried over MGS04 and concentrated in vacuo. The residue was triturated with Et20 to give 3-BROMO-5-(1, 1-DIOXO-116-ISOTHIAZOLIDIN-2-YL)-BENZOIC acid tert-butyl ester (D17) (350 mg 38%) as a white solid.

As the paragraph descriping shows that 5908-62-3 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/50619; (2004); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

5908-62-3, 1,1-Dioxo-isothiazolidine is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5908-62-3

A 50 ml flask was charged under nitrogen with 3-bromo-5-nitro-benzoic acid methyl ester (D11) (1 g, 3.8 mmol, 1 equiv), Cs2CO3 (536 mg, 4.4 mmol, 1.2 equiv) tris (DIBENZYLIDENEACETONE) DIPALLADIUM (0) (5 mg, 0.0055 mmol, 0.0154 equiv), Xantphos (10 mg, 0.014 mmol, 0.04 equiv) and toluene (15 ML). Isothiazolidine 1,1-dioxide (D22a) (536 mg, 4.4 mmol, 1.1 equiv) was then added and the resulting mixture was stirred at 90C for 16 hours then cooled to room temperature and diluted with H20 and AcOEt. The layers were separated, the aqueous phase diluted with a saturated aqueous NAHC03 solution and extracted with AcOEt. The combined organic phases were dried over MGS04 and concentrated in vacuo to give 3- (1, 1-DIOXO-116-ISOTHIAZOLIDIN-2-YL)-5-NITRO-BENZOIC acid methyl ester (D15) (187 mg, 16%) as a yellow solid. [M+H+NH3] + = 318.0, RT = 2. 81 min

The synthetic route of 5908-62-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/50619; (2004); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

5908-62-3, 1,1-Dioxo-isothiazolidine is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5908-62-3

suspension 01 lsothiazolidme 1,1-dioxide (1.2 equiv.), cesium carbonaie equiv.j, and l-(3-(4-chloro-5-fluoropyrimidin-2-yl)-l-(2-fluorobenzyl)-lH-pyrazol-5-yl)ethanone (Intermediate-IB, 1 equiv) in DMF was stirred at 130 C for 2 h. The solution was diluted with ethyl acetate, and washed with water and brine. The organics were combined, dried over magnesium sulfate, filtered, and the solvent was removed in vacuo. The crude residue was purified via reverse phase HPLC to deliver the desired compound (11 mg, 42.0 % yield) as a white solid. NMR (500 MHz, DMSO-i e) delta ppm 8.80 (d, 1 H), 7.78 (s, 1 H), 7.31 – 7.37 (m, 1 H), 7.20 – 7.26 (m, 1 H), 7.11 (t, 1 H), 6.84 (t, 1 H), 5.85 (s, 2 H), 4.15 (t, 2 H), 3.64 (t, 2 H), 2.59 (s, 3 H), 2.50 (t, 2H).

As the paragraph descriping shows that 5908-62-3 is playing an increasingly important role.

Reference£º
Patent; IRONWOOD PHARMACEUTICALS, INC.; BARDEN, Timothy Claude; SHEPPECK, James Edward; RENNIE, Glen Robert; RENHOWE, Paul Allan; PERL, Nicholas; NAKAI, Takashi; MERMERIAN, Ara; LEE, Thomas Wai-Ho; JUNG, Joon; JIA, James; IYER, Karthik; IYENGAR, Rajesh R.; IM, G-Yoon Jamie; (293 pag.)WO2016/44447; (2016); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.,5908-62-3

To a solution of tert-butyl (3S)-3- [[4- [2- [(5 -iodo-2-methyl- 1 -naphthyl)oxy]-3 – pyridyl]pyrimidin-2-yl]amino]piperidine-1-carboxylate (110 mg, 0.17 mmol) in CH3CN (2 mL) was added 1,3-propanesultam (209.1 mg, 1.73 mmol), copper iodide (1.6 mg, 0.01 mmol), N,N?-dimethyl-1,2-ethanediamine (7.6 mg, 0.09 mmol) and potassium carbonate (47.8 mg, 0.34 mmol). The mixture was purged with N2 and stirred at 80 C for 88 h. After cooling down, the mixture was filtered, concentrated, dissolved in ethyl acetate (60 mL) and washed with H20 (50 mL x 2). The organic phase was dried over anhydrous sodium sulfate and concentrated and the residue was purified by Prep-TLC (50% ethyl acetate in petroleum ether,Rf= 0.1) to yield 55 mg (51%) of the title compound as a brown oil. LCMS (ESI) [M+H]=631.0.

5908-62-3 1,1-Dioxo-isothiazolidine 642157, athiazolidine compound, is more and more widely used in various fields.

Reference£º
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

5908-62-3,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.

Scheme 13d5-Hydroxy-4-(7-iodo- 1 , 1 -dioxo- 1 ,4-dihydro- 1 lambda6-benzo[ 1 ,2,4]thiadiazin-3-yl)-2-(3- methyl-butyl)-6-1hiophen-2-yl-2H-pyridazin-3-one (3a); (0.25 g, 0.438 mmol), potassium triphosphate (0.465 g, 2.19 mmol), sarcosine (0.023 g, 0.263 mmol), and copper (I) iodide (0.021 g, 0.110 mmol) were combined. Anhydrous N1N- dimethylformamide (3 mL) was added followed by isothiazolidine 1,1-dioxide (0.531 g, 4.38 mmol, prepared according to the procedure from Org. Lett; 5; 22; 2003; 4175- 4178). The solution was degassed while stirring under vacuum and the flask charged with nitrogen. The mixture stirred at 1000C for 16 h. LC-MS indicated the major product to be the amino acid intermediate. Additional isothiazolidine 1,1-dioxide (0.531 g, 4.38 mmol) was added. The solution was degassed while stirring under vacuum and the flask charged with nitrogen. The mixture stirred at 1000C for 16 h. LC-MS indicated complete reaction at this point.Upon cooling, the mixture was diluted with ethyl acetate (80 mL), washed with IM aqueous hydrochloric acid (2 x 10 mL), saturated aqueous ammonium chloride (10 mL), dried over magnesium sulfate filtered. Methyl alcohol (100 mL) was added and the desired product crystallized over a period of 2 h. Collection by filtration followed by rinsing with methyl alcohol (2 x 10 mL) followed by drying in vacuo for 3 h afforded the desired product, 4-[7-(l,l-dioxo-llambda6-isothiazolidm-2-yi)-l,l-dioxo-l,4- dihydro-llambda6-benzo[l,2,4]miadiazin-3-yl]-5-hydroxy-2-(3-methyl-butyl)-6-thiophen- 2-yl-2H-pyridazin-3-one (66a) (0.0693, 0.123 mmol, 28 % yield), as an orange powder. 1H NMR (400 MHz, DMSO-d6) delta: 0.96 (6H, d, J= 6.2 Hz), 1.59 – 1.71 (3H, m), 2.44 (2H, quintet, J= 7.1 Hz), 3.59 (2H, t, J= 6.9 Hz), 3.85 (2H, t, J= 6.7 Hz), 4.17 (2H, t, J= 6.7 Hz), 7.17 (IH, dd, J1 = 5.6 Hz, J2 = 3.9 Hz), 7.54 – 7.58 (2H, m), 7.68 – 7.71 (2H, m), 7.91 (IH, d, J= 4.0 Hz), 13.94 (IH, s). LC-MS (ESI): (exact mass: 563.10): m/e = 564.66 [M+H]+ (100 %).

As the paragraph descriping shows that 5908-62-3 is playing an increasingly important role.

Reference£º
Patent; ANADYS PHARMACEUTICALS, INC.; WO2008/82725; (2008); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

The thiazolidine compound, name is 1,1-Dioxo-isothiazolidine,cas is 5908-62-3, mainly used in chemical industry, its synthesis route is as follows.

5908-62-3, A flask was charged under nitrogen with 3-bromo-5-iodo-benzoic acid tert-butyl ester D8b (1 g, 2.6 mmol, 1 equiv), Cs2CO3 (1.26 g, 3.9 mmol, 1.5 equiv), tris (DIBENZYLIDENEACETONE) DIPALLADIUM (0) (12 mg, 0.013 mmol, 0.005 equiv), Xantphos (22 mg, 0.038 mmol, 0.015 equiv) and toluene (20 ML). ISOTHIAZOLIDINE 1,1-dioxide (D22a) (350 mg, 2.9 mmol, 1.1 equiv) was then added and the resulting mixture was stirred at 100C for 16 h then cooled to room temperature and diluted with AcOEt. The organic phase was washed with saturated aqueous NAHC03 solution, dried over MGS04 and concentrated in vacuo. The residue was triturated with Et20 to give 3-BROMO-5-(1, 1-DIOXO-116-ISOTHIAZOLIDIN-2-YL)-BENZOIC acid tert-butyl ester (D17) (350 mg 38%) as a white solid.

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2004/50619; (2004); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

The thiazolidine compound, name is 1,1-Dioxo-isothiazolidine,cas is 5908-62-3, mainly used in chemical industry, its synthesis route is as follows.

5908-62-3, To 2-choro-5-nitro-3-trifluoromethypyridine (056 g, 2.48 mmo) and isothiazoHdine 1,1- dioxide (060 g, 496 mmo) in 1,4-dioxane (12 m) were added Cs2003 (0.81 g, 2.48 mmo) and argon was bubbed though the mixture for 10 mm. Then Xantphos (287 mg, 0,50 mrnoD and Pd2(dba)3 (114 mg, 0.124 mmoD were added. The reaction mixture was stirred for 40 mm at 140C in a microwave oven. The mixture was fi?tered through a pad of C&ite and the sovent was evaporated. The crude product was purified by flash co?umn chromatography on sihca ge (cyciohexane/AcOEt 100/0 to 50/50) to afford 2-(5- nitro-3-(trifluoromethy)pyridmn-2-y)isothiazoidine 1,1-dioxide. M/z = 312 [M+H]+, Rt = 0.87 mm (U PLC Method 32).

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

Reference£º
Patent; NOVARTIS AG; PISSOT SOLDERMANN, Carole; QUANCARD, Jean; SCHLAPBACH, Achim; SIMIC, Oliver; TINTELNOT-BLOMLEY, Marina; ZOLLER, Thomas; (161 pag.)WO2015/181747; (2015); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

5908-62-3, 1,1-Dioxo-isothiazolidine is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5908-62-3

General procedure: Example 2 3-Ethyl-5-methyl-6-[(2-oxoazetidin-1-yl)methyl]-1-(3,3,3-trifluoropropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione To a solution of 85 mg (1.19 mmol) of 2-azetidinone in 1.6 ml of THF were added 48 mg (1.19 mmol) of sodium hydride (60% suspension in mineral oil), then the mixture was heated to 60 C. for 60 min and subsequently cooled back down to RT (“Solution 1”). To a solution of 80 mg (0.238 mmol) of the compound from Ex. 140A in 1.6 ml of dichloromethane in another reaction vessel were added, at 0 C., 83 mul (0.476 mmol) of N,N-diisopropylethylamine and 18 mul (0.250 mmol) of thionyl chloride. After 20 min at 0 C., Solution 1 was added and the cooling bath was removed. The reaction mixture was stirred at RT for about 18 h. All the volatile constituents were then removed on a rotary evaporator. The remaining residue was separated into its components by means of preparative HPLC (Method 10). After concentration of the product fractions and drying under high vacuum, 5 mg (5% of theory, 92% purity) of the title compound were obtained. 1H-NMR (400 MHz, DMSO-d6, delta/ppm): 4.26 (s, 2H), 4.12 (t, 2H), 3.90 (q, 2H), 3.29-3.21 (m, 2H), 3.17 (t, 2H), 2.86-2.69 (m, 2H), 2.41 (s, 3H), 2.29-2.16 (m, 2H), 1.12 (t, 3H). LC/MS (Method 1, ESIpos): Rt=0.96 min, m/z=440 [M+H]+.

5908-62-3 1,1-Dioxo-isothiazolidine 642157, athiazolidine compound, is more and more widely used in various fields.

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HAeRTER, Michael; KOSEMUND, Dirk; DELBECK, Martina; KALTHOF, Bernd; WASNAIRE, Pierre; SUessMEIER, Frank; LUSTIG, Klemens; (369 pag.)US2018/65981; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

5908-62-3, 1,1-Dioxo-isothiazolidine is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5908-62-3

A sealed tube was charged with 4-iodobenzonitrile (0.50 g, 2.2 mmol), 1 ,2-thiazolidine 1 , 1- dioxide (1.2 equiv.; 0.32 g, 2.6 mmol), dimethylethylenediamine (0.1 equiv., 0.23 mL, 0.22 mmol), cesium fluoride (2.5 equiv., 0.83 g, 5.47 mmol), copper iodide (0.05 equiv., 0.02 g, 0.10 mmol), tetrahydrofuran (4.7 mL) and the reaction contents were stirred at room temperature for 24 hours. The reaction contents were diluted with ethyl acetate and a saturated aqueous ammonium chloride solution. The layers were separated and the organic fraction was washed with water, dried over sodium sulfate, and concentrated under reduced pressure. The corresponding crude yellow oil (449 mg) was taken up in the next step without additional purification or characterization. (0600) NMR (400 MHz, CDCIs) delta ppm: 7.85 (d, 2H), 7.30 (d, 2H), 3.82 (t, 2H), 3.28 (t, 2H), 3.30 (m, 2H).

The synthetic route of 5908-62-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SYNGENTA PARTICIPATIONS AG; HOFFMAN, Thomas, James; STIERLI, Daniel; POULIOT, Martin; BEAUDEGNIES, Renaud; (96 pag.)WO2017/93348; (2017); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.,5908-62-3

Step 2-1-(1,1-dioxo-isothiazolidin-2-ylmethyl)-3-benzyl-5-bromo-benzene (8B) A mixture of 8A (5 g, 14.7 mmol), 1,3-propanesultam (3.6 g, 29.7 mmol) and potassium carbonate (4.1 g, 29.7 mmol) in acetonitrile (60 mL) was refluxed overnight. The solvent was removed under reduced pressure. The residue was partitioned between ethyl acetate and brine. The organic phase was dried over sodium sulfate, filtered and concentrated under reduced pressure. The residue was purified by flash chromatograph (ethyl acetate/hexanes) to give 8B as a white solid.

The synthetic route of 5908-62-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Zhuang, Linghang; Wai, John S.; Payne, Linda S.; Young, Steven D.; Fisher, Thorsten E.; Embrey, Mark W.; Guare, James P..; US2005/10048; (2005); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com