Category: 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.,5908-62-3

1,2-thiazolidine 1,1-dioxide (0.03 I 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 mm. 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 layerswere washed with brine, dried over MgSO4, filtered, and concentrated. The residue was purified by preparative HPLC (C18, 10-80% acetonitrile in 0.1% TFA water) to afford 0.025 g (64%) of the title compound. 1H NMR (500 MHz, DMSO-d6) 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, IH), 6.88 (d, J=7.63 Hz, 2H), 7.00 (d, J8.54 Hz, 1H), 7.03-7.05 (m, IH), 7.25-7.30 (m, 4H), 7.34 (dd,J=8.39, 2.29, ZH), 7.48 (d, J=2.44 Hz, 1H), 12.00 (s, 1 H). MS (ESI+) m/z 450.2 (M+H).

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

Reference£º
Patent; ABBOTT LABORATORIES; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; WANG, Le; PRATT, John, K.; MCDANIEL, Keith, F.; WO2013/97052; (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, Example 86; N- (3-Cyclobutyl-2, 3, 4,5-tetrahydro-1 H-3-benzazepin-7-yl)-4- (1, 1-dioxido-2- isothiazolidinyl) benzamide (E86); A mixture of N- (3-cyclobutyl-2, 3,4, 5-tetrahydro-1 H-3-benzazepin-7-yl)-4-iodobenzamide (E11) (150mg, 0.34 mmol), potassium carbonate (169 mg, 1.22 mmol), copper (1) iodide (19 mg, 0.1 mmol), N,N’-dimethyl-1, 2-ethanediamine (0.01 ml, 0.1 mmol) and isothiazolidine 1,1-dioxide (123 mg, 1.0 mmol) in dioxan (3 ml) was heated in a microwave reactor at 140 C for 20 minutes. The mixture was diluted with methanol and purified on an SCX ion exchange cartridge eluting with methanol and then a 2M methanolic ammonia solution. The basic fractions were concentrated in vacuo and the residue purified by column chromatography eluting with a mixture of 2M methanolic ammonia solution and dichloromethane (3-97) to afford the title compound (E86) MS (ES+), m/e 440 [M+H] +.

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2005/58837; (2005); 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 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

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.; HU, Taishan; SHEN, Hong; HAN, Xingchun; (45 pag.)WO2018/11100; (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

Preparation 71 2-(2,4-Dimethoxybenzyl)-isothiazolidine-1,1-dioxide A solution of 1,1-(azodicarbonyl)dipiperidine (1.874 g, 7.4 mmol) in anhydrous tetrahydrofuran (10 mL) was added dropwise to a 0 C. solution of 1,3-propanesultam (0.6 g, 4.95 mmol), triphenylphosphine (1.95 g, 7.4 mmol), and 2,4-dimethoxybenzyl alcohol (1.0 g, 6.2 mmol) in anhydrous tetrahydrofuran (20 mL). The resultant solution was stirred at 0 C. for 3 hrs, warmed to room temperature and stirred for a further 16 hrs. The solution was concentrated under reduced pressure and suspended in ethyl acetate/hexanes to precipitate a white solid. The solid was removed by filtration and the filtrate purified by silica gel chromatography (25-70% ethyl acetate/hexanes) to give a pale yellow oil (0.505 g). 1H NMR (CDCl3, 300 MHz) delta 7.31-7.28 (dd, 1H, J=0.6, 7.8 Hz), 6.49-6.44 (m, 2H), 4.17 (s, 2H), 3.81 (s, 3H), 3.80 (s, 3H), 3.19-3.13 (m, 4H), 2.32-2.23 (m, 2H).

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

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

To a stirred solution of racemic 3-fluoro-2-({9-fluoro-6-methanesulfonyl-3-[4- (2H3)methyl-l-methyl-lH-l,2,3-triazol-5-yl]-5H-pyrido[3,2-b]indol-5-yl}(oxan-4- yl)methyl)pyridine (80.0 mg, 0.140 mmol) and isothiazolidine- 1,1 -dione (69.8 mg, 0.580 mmol) in NMP (0.70 mL) was added t-BuOK (56.5 mg, 0.500 mmol). The mixture was heated at 65 C for 70 min and cooled to room temperature. The mixture was diluted with water and extracted with EtOAc. Combined EtOAc extracts were dried (MgSCn), filtered, and concentrated. The crude product was purified by silica gel column chromatography (Teledyne ISCO CombiFlash 0% to 100% solvent A/B= DCM/10% MeOH/DCM, RediSep Si02 12 g, detecting at 254 nM, and monitoring at 220 nM). Concentration of appropriate fractions provided racemic 2-{5-[(3-fluoropyridin-2- yl)(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 (110 mg). This racemic mixture was separated by chiral prep SFC (Berger SFC MGII, ColummChiral IB 25 X 2.1 cm ID, 5muiotaeta Flow rate: 50.0 mL/min. Mobile Phase: 80/20 CC /MeOH Detector Wavelength: 220 nm) to give Enantiomers A (13.3 mg, 13%) and B (10.5 mg, 11%). Enantiomer A: NMR (400MHz, CDCb) delta 8.57 (d, J=1.8 Hz, 1H), 8.46 (dt, J=4.4, 1.5 Hz, 1H), 8.40 (d, J=8.6 Hz, 1H), 8.15 (d, J=2.0 Hz, 1H), 7.77 (d, J=8.6 Hz, 1H), 7.41- 7.28 (m, 3H), 4.34-4.24 (m, 1H), 4.21-4.11 (m, 1H), 4.01 (br dd, J=12.0, 2.7 Hz, 1H), 3.95 (s, 3H), 3.82 (br dd, J=11.6, 3.1 Hz, 1H), 3.61-3.53 (m, 2H), 3.46 (br d, J=2.3 Hz, 1H), 3.43 (s, 3H), 3.34 (br d, J=11.7 Hz, 1H), 3.20 (td, J=l 1.9, 1.9 Hz, 1H), 2.84-2.71 (m, 2H), 1.89-1.74 (m, 3H), 0.54 (br d, J=13.0 Hz, 1H); SFC RT = 10.07 min (Column: Chiralcel IB 250 x 4.6 mm, 5 muiotaeta; Mobile Phase: 80/20 CCh/MeOH; Flow: 2 mL/min); Enantiomer B: NMR (400MHz, CDCb) delta 8.56 (d, J=1.8 Hz, 1H), 8.45 (dt, J=4.3, 1.4 Hz, 1H), 8.40 (d, J=8.6 Hz, 1H), 8.15 (d, J=1.8 Hz, 1H), 7.76 (d, J=8.6 Hz, 1H), 7.42- 7.28 (m, 3H), 4.34-4.24 (m, 1H), 4.22-4.12 (m, 1H), 4.01 (br dd, J=11.7, 2.8 Hz, 1H), 3.95 (s, 3H), 3.82 (br dd, J=l 1.3, 3.2 Hz, 1H), 3.56 (dt, J=7.7, 3.9 Hz, 2H), 3.46 (br d, J=2.4 Hz, 1H), 3.43 (s, 3H), 3.37-3.28 (m, 1H), 3.23-3.15 (m, 1H), 2.84-2.69 (m, 2H), 1.79 (br dd, J=12.8, 4.2 Hz, 3H), 0.54 (br d, J=12.8 Hz, 1H) LCMS (M+H) = 556.2; SFC RT = 12.21 min (Column: Chiralcel IB 250 x 4.6 mm, 5 muiotaeta; Mobile Phase: 80/20 CCh/MeOH; Flow: 2 mL/min).

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

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

Under a nitrogen atmosphere, a solution of 5-bromo-6-chloro- pyridine-2-carboxylic acid methyl ester (Example 9 c, lg, 4 mmol), isothiazolidine 1 , 1 -dioxide (730 mg, 06 mmol), copper(I) iodide (150 mg, 0.8 mmol), l ,3-di(pyridin-2-yl)propane-l ,3-dione (CAN 10198- 89-7, 180 mg, 0.8 mmol) and potassium carbonate (1.1 g, 8 mmol) in DMF (20 mL) was reacted for 24 h at 1 10C. The reaction mixture was poured into water, and extracted with ethyl acetate (3 x 50 mL). The combined organic extracts were washed with water and brine, dried over anhydrous sodium sulfate and evaporated. The residue was purified by column chromatography (silica gel, 4 g, 10% ethyl acetate in petroleum ether) to yield the title compound (0.048 g, 1.6 mmol, 41.4 %) as yellow solid; MS (EI): m/e = 291.0[M+Hf.

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

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; BISSANTZ, Caterina; GRETHER, Uwe; HEBEISEN, Paul; KIMBARA, Atsushi; LIU, Qingping; NETTEKOVEN, Matthias; PRUNOTTO, Marco; ROEVER, Stephan; ROGERS-EVANS, Mark; SCHULZ-GASCH, Tanja; ULLMER, Christoph; WANG, Zhiwei; YANG, Wulun; WO2012/168350; (2012); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belong thiazolidine compound,1,1-Dioxo-isothiazolidine,5908-62-3,Molecular formula: C3H7NO2S,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

Procedure E; [00215] To a sealed tube containing CuI (8mg, 0.039mmol), K2CO3 (0.2 Ig, 1.54 mmol) and (IS, 25)-cyclohexane-l,2-diamine (9mg, 0.077 mmol) under a N2 atmosphere was added a solution of 5-bromo-2-(naphthalene-2-yl)benzo[d]oxazole (0.25g, 0.77 mmol) in anhydrous toluene (2.5 mL), followed by a solution of isothiazolide-l,2-dioxide (0.12g, 0.96 mmol) in anhydrous toluene (2.5 mL). The resulting reaction mixture was heated to HO0C for 12h, cooled to room temperature, filtered over celite and concentrated under reduced pressure. The residue was purified by column chromatography eluting with petroleum ether/EtOAc (1/0 to 0/1, v/v), followed by a crystallisation from industrial methylated spirits to give 30mg (11%) of 5-(isothiazolidin-dioxide-2-yl)-2-(naphthalene-2-yl)benzo[d]oxazole. LCMS RT = 2.24 min, M+H+ 364.8. 1H NMR (D6-DMSO): 8.84 (IH, br s), 8.26 (IH, dd, J 1.6 &; 8.6), 8.20- 8.13 (2H, m), 8.06-8.03 (IH, m), 7.85 (IH, d, J 8.8), 7.70-7.63 (3H, m), 7.38 (IH, dd, J2.3 &; 8.9), 3.84 (2H, t, J6.5), 3.55 (2H, t, J7.3), 2.45 (2H, m).

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; BioMarin IGA, Ltd.; WREN, Stephen, Paul; WYNNE, Graham, Michael; WILSON, Francis, Xavier; POIGNANT, Severine, Danielle; WO2010/112093; (2010); 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 stirred solution of 3-bromo-9-fluoro-6-methanesulfonyl-5H-pyrido[3,2- bjindole (200 mg, 0.583 mmol) and isothiazolidine-l,l-dione (278 mg, 2.30 mmol) in NMP (2.40 mL) was added t-BuOK (203 mg, 1.81 mmol). This mixture was heated at 115 C for 11 h and cooled to room temperature. The mixture was diluted with EtOAc (20 mL) and 10% aq. LiCl solution (20 mL). Some insoluble solid was filtered to give the desired product, 2-(3-bromo-6-(methylsulfonyl)-5H-pyrido[3,2-b]indol-9- yl)isothiazolidine-l,l-dione (115 mg, 44%). NMR (400MHz, DMSO-de) delta 11.94 (br s, 1H), 8.72 (br s, 1H), 8.32 (br s, 1H), 8.04 (br d, J=7.6 Hz, 1H), 7.55 (br s, 1H), 4.22 (br s, 2H), 3.59 (br s, 2H), 3.39 (br s, 3H), 2.61 (br s, 2H). HPLC: RT=2.055 min (Chromolith ODS 4.6 x 50 mm (4 min grad) eluting with 10-90% aqueous MeOH over 4 min containing 0.1 % TFA, 4 mL/min, monitoring at 220 nm); MS (ES): m/z= 444,1 ; 445.9 (Br pattern) [M+H]+.

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,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.

The product of example 67 (460 mg, 8.6 mmol), sulfonamide (210 mg, 1.73 mmol), K2CO3 (240 mg, 1.73 mmol), CuI (30 mg, 0.17 mmol) and DMEDA (30 mg, 0.34 mmol) were mixed in toluene (10 ml) and heated at 90 0C for 3 hours. After being cooled to room temperature, the mixture was filtered, washed with DCM. The filtrate was concentrated into dryness, and the residue was purified by column chromatography using DCM/EA (5/2) as eluent to give the title compound (129 mg, 26.0 % yield).1H NMR (300 MHz, DMSO-/) delta 1.12 (q, J= 6.2 Hz, 6H), 2.34 (dd, J= 10.5, 12.4 Hz, IH), 2.41-2.50 (m, 2H?), 2.78 (dd, J= 10.6, 13.0 Hz, IH), 3.41-3.53 (m, 3H), 3.55-3.67 (m, IH), 3.77 (s, 3H), 3.78 -3.91 (m, 3H), 4.14 (d, J= 12.9 Hz, IH), 4.95 (d, J= 17.2 Hz, IH), 5.02 (s, 2H), 5.19 (d, J= 16.8 Hz, IH), 7.29-7.44 (m, 5H), 7.70 (s, IH).MS (ESI+) m/z 51 A (M+l)

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

Reference£º
Patent; AVEXA LIMITED; DEADMAN, John, Joseph; JONES, Eric, Dale; LE, Giang, Thanh; RHODES, David, Ian; THIENTHONG, Neeranat; VAN DE GRAFF, Nicholas, Andrew; WINFIELD, Lisa, Jane; WO2010/31; (2010); 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 stirred mixture of [3-(2-Methyl-l,3-dioxolan-2-yl)tricyclo[3.3.1.03’7]non-l-yl] methyl methanesulfonate as obtained in preparation 2 (1.0 g, 2.9 mmol), K2CO3 (1.16 g, 8.7 mmol) and isothiazolidine- 1,1 -dioxide (0.53 g, 4.35 mmol) in DMF (12.0 mL) was heated to 110C for 16 h. The reaction mixture was cooled to room temperature, diluted with water and extracted with EtOAc. The combined organic layer was washed with brine, dried over Na2SO4 and the solvent was removed under reduced pressure. The crude product was purified by column chromatography to obtain 2-{[3-(2-methyl-l,3-dioxolan-2- yl)tricyclo[3.3.1.03’7]non-l-yl] methyljisothiazolidine 1,1-dioxide as a viscous liquid (0.69 g) in 70% yield, m/z (M+l) 342; 1H NMR (CDCl3) 300 MHz delta 4.04-3.92 (m, 4H), 3.30 (t, J= 6.8 Hz, 2H), 3.10 (t, J= 7.4 Hz, 2H), 2.94 (d, J= 14.6 Hz, IH), 2.87 (d, J= 14.6 Hz, IH), 2.40-2.27 (m, 4H), 1.88-1.72 (m, 2H), 1.72-1.55 (m, 4H), 1.55-1.38 (m, 4H), 1.27 (s, 3H).

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

Reference£º
Patent; MATRIX LABORATORIES LTD.; WO2007/113634; (2007); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com