Category: 5908-62-3

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

To a solution of compound from example 308 (50 mg, 0.10 mmol) in DMF (0.5 mL), 1,1-Dioxoisothiazolidine (18.3 mg, 0.15 mmol) was added followed by K2C03 (14 mg, 0.1 mmol) and stirred at 50 C. o/n. The crude waspurified on prep-HPLC (C-18, Acetonitrile/water) to give the title compound (16 mg, 26%) as a white solid. ESI-MS rnlz=617.25, 619.25 [M-Hr.

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

Reference£º
Patent; ENANTA PHARMACEUTICALS, INC.; Qiu, Yao-Ling; Gao, Xuri; Kass, Jorden; Cao, Hui; Li, Wei; Peng, Xiaowen; Suh, Byung-Chul; Or, Yat Sun; US2019/60258; (2019); 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

A mixture of 2-(4-bromophenyl)-6-cyclobutyl-5,6,7,8-tetrahydro-4H-[1 ,3]thiazolo[4,5- ofjazepine (may be prepared as described in Example 2) (57.0mg, 0.16mmol), isothiazolidine 1 ,1 -dioxide (38.0mg, 0.31 mmol), cesium carbonate (78.0mg, 0.24mmol), tris(dibenzylideneacetone)dipalladium(0) (7.00mg, 0.00deltammol), and 4,5- bis(diphenylphosphino)-9,9-dimethyl-xanthene (Xantphos) (14.0mg, 0.024mmol) in 1 ,4- dioxane (3ml) was heated under argon at 1060C for 3 hours. The reaction was then cooled to room temperature, diluted with methanol and passed down an ion exchange cartridge (SCX) and washed with methanol and then a 2M ammonia in methanol solution. The basic fractions were then reduced and purified using silica gel chromatography, eluting with a mixture of 2M ammonia in methanol and dichloromethane (1-2.5%) to afford the product (E99); MS (ES+) m/e 404 [M+H]+.

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2006/97691; (2006); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

A common heterocyclic compound, 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, PREPARATION 1 STR61 A mixture of 4-isopropenyl pyridine (1.79 g) and isothiazolidine-1,1-dioxide (1.81 g) was heated at 130 C. during the addition of “Triton B” (Trade Mark, trimethylbenzylammonium hydroxide) (0.25 g added every hour for four hours; 40% solution in water). After stirring for 16 hours at 130 the mixture was cooled and taken in chloroform (50 cm3) and water (50 cm3). The aqueous phase was extracted with chloroform (3*20 cm3) and the dried (MgSO4) extracts were evaporated to given an oil. Chromatography on silica (“Merck 60. 9385”) eluding with ethyl acetate gave 2-[2-(4-pyridyl)prop-1-yl]isothiazolidine-1,1-dioxide which crystallized from ethyl acetate-hexane as needles, m.p. 90-92 (1.01 g). Analysis %: Found: C,55.0; H,6.8; N,12.0. Calculated for C11 H16 N2 O2 S: C,55.0; H,6.7; N,11.7.

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

Reference£º
Patent; Pfizer Inc.; US4489075; (1984); A;,
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 stirred solution of 5-{9-fluoro-5-[(S)-(4-fluorophenyl)(oxan-4-yl)methyl]-6- methanesulfonyl-5H-pyrido[3,2-b]indol-3-yl}-4-(2H3)methyl-l-methyl-lH-l,2,3-triazole (24.0 mg, 0.0400 mmol) and isothiazolidine-l,l-dione (26.2 mg, 0.220 mmol) in NMP (0.25 mL) was added t-BuOK (19.4 mg, 0.170 mmol). This mixture was heated at 65 C for 2 h and cooled to room temperature. The mixture was then diluted with MeOH and purified via preparative LC/MS with the following conditions: Column: Waters XBridge Phenyl, 19 x 200 mm, 5-muiotaeta particles; Mobile Phase A: 5:95 ACN: water with 10 mM NH4OAc; Mobile Phase B: 95:5 ACN: water with 10 mM NH4OAc; Gradient: 15-70% B over 20 min, then a 5-min hold at 100% B; Flow: 20 mL/min. Fractions containing the desired product were combined and dried via centrifugal evaporation to give 2-{5-[(S)-(4- fluorophenyl)(oxan-4-yl)methyl]-6-methanesulfonyl-3-[4-(2H3)methyl-l -methyl-lH- l,2,3-triazol-5-yl]-5H-pyrido[3,2-b]indol-9-yl} -l 6,2-thiazolidine-l,l-dione (11.6 mg, 40%). NMR (500MHz, DMSO-de) delta 8.73 (s, IH), 8.37 (d, J=8.5 Hz, IH), 7.90 (s, IH), 7.71-7.65 (m, 2H), 7.61 (d, J=8.4 Hz, IH), 7.16 (br t, J=8.7 Hz, 2H), 6.78 (br d, J=10.2 Hz, IH), 4.10 (br t, J=6.8 Hz, 2H), 3.88 (br d, J=10.7 Hz, IH), 3.83 (s, 3H), 3.64 (br d, J=8.7 Hz, IH), 3.57 (br t, J=7.5 Hz, IH), 3.47 (br s, 2H), 3.39 (br s, IH), 3.17 (br t, J=11.4 Hz, IH), 2.66-2.57 (m, 2H), 2.54 (s, 3H), 1.90 (br d, J=12.6 Hz, IH), 1.64 (br t, J=12.1 Hz, 2H), 0.42 (br d, J= 1.8 Hz, IH). LCMS: RT = 1.670 min; (ES): m/z (M+H)+ = 656.15. LCMS: Column: Waters Acquity UPLC BEH C18, 2.1 x 50 mm, 1.7-muetaiota particles; Mobile Phase A: 5:95 ACN:water with 10 mM NH4OAC; Mobile Phase B: 95:5 ACN:water with 10 mM NH4OAc; Temperature: 50 C; Gradient: 0-100% B over 3 min, then a 0.75-min hold at 100% B; Flow: 1.11 mL/min. HPLC Purity at 220 nm: 98 %

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

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; HAN, Wen-Ching; DEGNAN, Andrew P.; DESKUS, Jeffrey A.; GAVAI, Ashvinikumar V.; GILL, Patrice; SCHMITZ, William D.; STARRETT, John E., Jr.; (193 pag.)WO2016/183115; (2016); 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, 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.

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

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

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 the mixture of 4-(5-bromo-6-nitropyridin-3-yl)morpholine (1.00 g, 3.47 mmol) in toluene (20 ml), isothiazolidine 1,1-dioxide (0.63 g, 5.21 mmol), Cul (0.17 g, 0.87 mmol), DMEDA (0.15 g, 1.74 mmol) and K2C03 (0.96 g, 6.94 mmol) were added successively. The mixture was heated at 80C for 5 h under nitrogen atmosphere. After cooling down to room temperature, the mixture was filtrated and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography (DCM/MeOH= 100/1 ) to give the desired product (0.49 g, 43.1 %). NMR (300 MHz, -DMSO) delta 8.16 (d, J = 2.7 Hz, 1H), 7.51 (d, J = 2.7 Hz, 1H), 3.79-3.72 (m, 6H), 3.43-3.34 (m, 6H), 2.43 (m, 2H ).MS (ESI+) m/z 329 (M+l)

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

Reference£º
Patent; AVEXA LIMITED; SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY (SIOC); RHODES, David, Ian; DEADMAN, John, Joseph; LE, Giang, Thanh; VAN DE GRAFF, Nicholas, Andrew; LONG, Lu; XINMING, Li; XIAO, Feng; CHANGJIANG, Yu; WO2012/6680; (2012); 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, 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.

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

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

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, A mixture of 3-(5-amino-2-(2-(chloromethy l)-6-fluorobenzyl)-8-(pyrimidm-4-yl)- [l,2,4]triazolo[l,5-c]pyrimidin-7-yl)benzonitrile (10 mg, 0.021 mmol), (3RAR)-4- fluoropyrrolidm-3-ol hydrochloride (4.51 mg, 0.032 mmol) and CS2CO3 (20.7 mg, 0.064 mmol) in DMF (1 mL) was stirred at 100 C for 10 min. The reaction mixture was then cooled to r.t., diluted with methanol (4 mL), and purified by preparative LC-MS (pH 2, acetonitrile/water with TFA) to afford the product as a TFA salt. LCMS calculated for C2.8H24F2N9O ( M i l ) : 540.2; found 540.2.

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

Reference£º
Patent; INCYTE CORPORATION; WANG, Xiaozhao; GAN, Pei; HAN, Heeoon; HUANG, Taisheng; MCCAMMANT, Matthew S.; QI, Chao; QIAN, Ding-Quan; WU, Liangxing; YAO, Wenqing; YU, Zhiyong; ZHANG, Fenglei; (284 pag.)WO2019/168847; (2019); 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

Preparation 64 2-(2-Methylbut-3-yn-2-yl)-isothiazolidine-1,1-dioxide To a stirred solution of 1,3-propanesultam (2.000 g, 16.5 mmol) in anhydrous N,N-dimethylformamide (30 mL) at 0 C. was added 60% sodium hydride in mineral oil (1.981 g, 49.5 mmol) and the mixture was stirred at 0 C. for 1 hr. 3-Chloro-3-methyl-1-butyne (2.300 g, 22.4 mmol) was added and the reaction mixture was stirred at 0 C. for 1 hr and then slowly warmed to room temperature and stirred for 16 hrs. The reaction was carefully quenched with water and extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium chloride, dried (anhydrous sodium sulfate), and concentrated in vacuo. The residue was purified by silica gel chromatography (0-70% ethyl acetate/hexanes) to afford the desired product as a yellow oil (1.35 g, 44%). 1H NMR (300 MHz, CDCl3) delta 3.52 (t, 2H, J=6.6 Hz), 3.23 (t, 2H, J=7.5 Hz), 2.46 (s, 1H), 2.42-2.28 (m, 2H), 1.74 (s, 6H).

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

Reference£º
Patent; Bersot, Ross; Humphries, Paul; US2013/303524; (2013); 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

Compound 20: N-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)isothiazolidine 1,1-dioxide To a stirred solution of 1,3-propanesultam (0.80 g, 6.6 mmol) in anhydrous N,N-dimethylformaide (20 mL) was added sodium hydride (60% in mineral oil, 0.053 g, 1.3 mmol) and the mixture was stirred at room temperature for 1 hour. 9-(Oxiran-2-ylmethyl)-9H-carbazole (1.622 g, 7.3 mmol) was added and the mixture was stirred at 70 C. overnight. After cooling, the reaction was diluted with water and extracted three times with ethyl acetate. The combined organic layers were washed with saturated aqueous sodium chloride, dried (anhydrous sodium sulfate), filtered, and concentrated. The residue was purified by silica gel column chromatography (0-70% ethyl acetate in hexanes) and then recrystallized from ethyl acetate/hexanes to give the pure compound as a white solid (1.6 g, 70%). 1H NMR (300 MHz, CDCl3) delta 8.10 (d, 2H, J=7.5 Hz), 7.48 (d, 4H, J=3.9 Hz), 7.30-7.22 (m, 2H), 4.55-4.35 (m, 3H), 3.42-3.12 (m, 6H), 2.59 (d, 1H, J=3.0 Hz), 2.37 (m, 2H). ESI (m/z): 344.9 (M+H). HPLC analysis: (C18, 10-90% acetonitrile in water+0.1% trifluoroacetic acid over 10 min: retention time, % area at 254 nm): 11.8 min, >98%.

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

Reference£º
Patent; Bersot, Ross; Humphries, Paul; US2013/303524; (2013); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com