Tag: 5908-62-3

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO38,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

A microwave vial was charged with 2-[(S)-{7-chloro-6-fluoro-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]-3- fluoropyridine (46 mg, 0.090 mmol), isothiazolidine 1,1-dioxide (16.3 mg, 0.135 mmol), tripotassium phosphate (26.7 mg, 0.126 mmol), Pd2(dba)3 (4.1 mg, 4.5 muetaiotaomicron), 2-di-tert- butylphosphino-3,4,5,6-tetramethyl-2′,4′,6′-triisopropyl-l, -biphenyl (4.3 mg, 9.0 muetaiotaomicron), and dry tert-butanol (0.85 mL). The reaction was heated at 84C ovemight. It was diluted with water and extracted with ethyl acetate. The organic layer was concentrated and purified by preparative HPLC (Column: XBridge C18, 19 x 200 mm, 5-muiotatauiota particles; Mobile Phase A: 5:95 acetonitrile: water with 0.1% trifluoroacetic acid; Mobile Phase B: 95:5 acetonitrile: water with 0.1% trifluoroacetic acid; Gradient: 22-62% B over 20 min, then a 5-min hold at 100% B; Flow: 20 mL/min) to give 12.3 mg (22%). LCMS (M+H) = 597.3, TR = 1.30 min (Column: Phenomenex LUNA C18, 30×2, 3u; Mobile Phase A: 90: 10 water: acetonitrile with 0.1% TFA; Mobile Phase B: 10:90 water: acetonitrile with 0.1% TFA; Temperature: 40 C; Gradient: 0-100% B over 2 min, hold 1 min; Flow rate: 1 mL/min).

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; 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

General procedure: To the mixture of the precursor 10(2.26 g, 10.1 mmol, 1.5 equiv) and tert-butyl 1,2,5-thiadiazolidine-2-carboxylate 1,1-dioxide (1.50 g, 6.75 mmol, 1.0 equiv) in dry DMF(10 mL), was added Cs2CO3 (6.60 g, 20.25 mmol, 3.0 equiv). Themixture was stirred at room temperature overnight, and thenextracted with ethyl acetate. The organic phase was washed withsaturated NaHCO3 and brine, dried over anhydrous Na2SO4, filteredand concentrated. The resulting residue was purified via silica gelchromatography to give 11a as colorless oil (1.96 g, 79%).

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

Reference£º
Article; Chen, Shulun; Guo, Wei; Liu, Xiaohua; Sun, Pu; Wang, Yi; Ding, Chunyong; Meng, Linghua; Zhang, Ao; European Journal of Medicinal Chemistry; vol. 179; (2019); p. 38 – 55;,
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, [0831] Preparation Example 231: Preparation of methyl 2-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)pyrimidine-5-carboxylate[0832][0833] Methyl 2-chloropyrimidine-5-carboxylate (173 mg) and isothiazolidine 1,1-dioxide (145 mg) were dissolved inN,N-dimethylformamide (1 mL), and sodium hydride (48mg, 60% in oil) was added under ice-cooling. After stirring atroom temperature for 6 hr, water was added, and the mixture was extracted with ethyl acetate. The solvent was evaporated,diisopropyl ether and ethyl acetate were added, and the precipitated solid was collected by filtration to give thetitle compound (185 mg).MS(ESI)m/z:258(M+H)+.

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

Reference£º
Patent; Mitsubishi Tanabe Pharma Corporation; MAEDA, Kazuhiro; ENDOH, Jun-ichi; TARAO, Akiko; TASHIRO, Kaoru; ISHIBUCHI, Seigo; HIKAWA, Hidemasa; EP2565182; (2013); 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, PREPARATION 19 STR75 (This is an alternative to the method of Preparation 2). A mixture of 4-vinylpyridine (324 g), isothiazolidine-1,1-dioxide (373 g), and “Triton B” solution (129 ml, 40% w/v in methanol) was heated in D.M.F. at 50-55 for 7 hours. The reaction mixture was then concentrated under vacuum, water (2.52 liters) was added, and the product was extracted into CH2 Cl2 (3*1.87 liters). The combined methylene chloride extracts were washed with water and then evaporated to dryness. The residue was dissolved in ethyl acetate (1.3 liters) at 35 and hexane (0.87 liters) was added over 10 minutes. The resulting crystalline product was granulated at -5 to 0 for 4 hours, filtered, washed with hexane (0.37 liters) and dried in vacuum at 25, to give 2-[2-(4-pyridyl)ethyl]isothiazolidine-1,1-dioxide (518 g). The material was confirmed by n.m.r., i.r. and m.p. to be identical in all respects to the product of Preparation 2.

With 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

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 the compound (58 mg) produced in Reference Example 7 in DMF (1 mL), cesium carbonate (51 mg) and 1,3-propanesultam (20 mg) were added, and the resulting mixture was stirred overnight at 50C. The reaction mixture was filtered, and then the filtrate was concentrated under reduced pressure, and the resulting residue was purified by Biotage SNAP KP-NH (hexane : ethyl acetate). The resulting purified product was dissolved in dimethoxyethane (1 mL) and methanol (1 mL), then an aqueous solution of sodium hydroxide (2 mol/L, 130 muL) was added, and the resulting mixture was stirred overnight at room temperature. The reaction mixture was neutralized with a hydrochloric acid aqueous solution, followed by concentration under reduced pressure. The resulting residue was washed with water in slurry, and washed with acetonitrile in slurry to obtain the compound (46 mg) of the present invention having the following physical property values. HPLC retention time (min): 2.90; MS (ESI, Pos.): 555.23 (M+H)+; 1H-NMR (CDCl3): delta 1.65-1.83, 2.24-2.61, 3.08, 3.13-3.25, 4.10-4.23, 5.78, 6.45, 7.03-7.13, 7.26, 7.51, 7.63, 8.19, 8.89, 9.41.

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

Reference£º
Patent; ONO Pharmaceutical Co., Ltd.; ASADA, Masaki; TANI, Kousuke; HIGUCHI, Satonori; EP3632898; (2020); 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, 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 %).

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

Reference£º
Patent; ANADYS PHARMACEUTICALS, INC.; WO2008/82725; (2008); 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.

Example 26: (lR.25.7R.85f)-5-r7-(l.l-Dioxo-llambda6-isothiazolidin-2 -yl)-l.1- dioxo-l,4-dihydro-llambda6-benzori,2,41thiadiazin-3-yll-3-(4-fluoro-benzyl)-6-hydroxy-3- aza-tricvclor6.2.1.02’7lundec-5-en-4-one[00353] A reaction flask was charged with copper (I) iodide (8 mg, 0.042 mmol), sarcosine (N-methyl glycine) (9 mg, 0.1 mmol), isothiazolidine 1,1 -dioxide (204 mg, 1.685 mmol), (lR,25′,7R,85r)-3-(4-fluoro-benzyl)-6-hydroxy-5-(7-iodo-l,l- dioxo-l,4-dihydro-llambda6-benzo[l,2,4]thiadiazin-3-yl)-3-aza-tricyclo[6.2.1.02’7]undec-5- en-4-one (prepared as described in Example 19, 100 mg, 0.168 mmol) and potassium phosphate (179 mg, 0.842 mmol). The flask was degassed and backfilled with nitrogen, and then anhydrous NN-dimethylformamide (3 mL) was added. The resulting suspension was vigorously stirred at 100 0C for 17 h, and then allowed to cool to 25 0C. The mixture was diluted with ethyl acetate (30 mL) and washed with 1.0 M aqueous hydrochloric acid solution (2 x 20 mL) and saturated aqueous brine solution (40 mL). The organic layer was dried over magnesium sulfate, filtered, and concentrated in vacuo. Purification by flash column chromatography (Teledyne Isco RediSep column; 1st column: 100% dichloromethane, 2n column: 5% hexanes in dichloromethane) to afford the desired product. The crude product was triturated with absolute ethanol (3 x) and dried in vacuo at 60 0C to afford the desired product, ( R,2S,1R, 8S>5 -[7-(1,I -dioxo- 1 lambda6-isothiazolidin-2-yl)- 1 , 1 -dioxo- 1 ,4-dihydro- 1 lambda6- benzo[l,2,4]thiadiazin-3-yl]-3-(4-fluoro-benzyl)-6-hydroxy-3-aza- tricyclo[6.2.1.02’7]undec-5-en-4-one (70 mg, 0.119 mmol, 71%), as a solid. 1H nuMR (400 MHz, DMSO-de) delta: 1.17 – 1.24 (2H, m), 1.40 – 1.61 (4H, m), 2.39 – 2.46 (2H, m), 2.51 – 2.54 (IH, m), 2.64 – 2.65 (IH, m), 3.03 – 3.05 (IH, m), 3.53 – 3.60 (3H, m), 3.83 (2H, t, J= 6.3 Hz), 4.43 (IH, d, J= 15.4 Hz), 4.97 (IH, d, J= 15.6 Hz), 7.15 (2H, t, J= 9.0 Hz), 7.32 – 7.35 (2H, m), 7.51 – 7.54 (2H, m), 7.62 (IH, d, J= 8.5 Hz). LC-MS (ESI) calcd for C27H27FN4O6S2 586.14, found 587.4 [M+H+].

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

Reference£º
Patent; ANADYS PHARMACEUTICALS, INC.; WO2008/124450; (2008); 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.

Example 60: 5-{5-[(3-{(1R,5S/1S,5R)-1-[4-(1,1-Dioxido-2-isothiazolidinyl)phenyl]-3- azabicyclo [3. 1.0] hex-3-yl} propyl) thio]-4-methyl-4H-1, 2, 4-triazol-3-yl}-2- methylquinoline hydrochloride; A Schlenk tube was charged with 5-[5-({3-[(1R,5S/1S,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 (0) (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 C for 12 h. The reaction mixture was allowed to cool to room temperature, diluted with dichloromethane (10 mL), filtered 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 Et20), the solvent evaporated in vacuo and the material thus obtained triturated with Et20 to give 52 mg of the title compound as a white solid. NMR (‘H, DMSO): 8 10.57 (bs, 1H), 8.27 (bd, 1H), 8.19 (d, 1H), 7.94 (t, 1H), 7.82 (d, 1H), 7.55 (d, 1H), 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, 1H), 1.66/1. 10 (t/m, 2H). MS (m/z) : 575 [MH] +.

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; WO2005/80382; (2005); 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

(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%).

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

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

EXAMPLE 24; 3,3-Difluoro-cyclobutanecarboxylic Acid ((S)-3-{5-[2-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-4,6-dimethyl-pyrimidine-5-carbonyl]-hexahydro-pyrrolo[3,4-c]pyrrol-2-yl}-1-phenyl-propyl)-amide (I-49); step 1-; A solution of isothiazolidine 1,1-dioxide (114, 40 mg, 0.33 mmol; CAS Reg No. 5908-62-3) in THF (0.4 mL) and DMF (0.4 mL) was treated with NaH (14 mg, 60% dispersion in mineral oil) and heated to 80 C. for 5 min before a solution of 84 (116 mg, 0.27 mmol) in DMF (1.6 mL) was added. The reaction mixture was stirred at 80 C. for 5 min, allowed to cool to RT, quenched by the addition of water, extracted with EtOAc, dried (Na2SO4) and concentrated in vacuo. The residue was purified by SiO2 column chromatography eluting with DCM:MeOH:NH4OH (60/10/1) to afford 115 mg (90%) of 115a.

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

Reference£º
Patent; Lemoine, Remy; Melville, Chris Richard; Rotstein, David Mark; Wanner, Jutta; US2007/191335; (2007); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com