Category: 5908-62-3

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.

Example 10.Lambdar-[(2,6-Dimethylphenyl)methyl]-6-(l,l-dioxido-2-isothiazolidinyl)-2,3- dimethylimidazo[l,2-alpha]pyridin-8-amine hydrochlorideA mixture of 6-bromo-N-[(2,6-dimethylphenyl)methyl]-2,3-dimethylimidazo[ 1 ,2- alpha]pyridin-8-amine (100 mg, 0.28 mmol; WO 98/37080), isothiazolidine 1,1 -dioxide (67 mg, 0.56 mmol; WO 04/050619), copper(I) iodide (16 mg, 0.083 mmol), potassium carbonate (138 mg, 1.0 mmol) and N,N’-dimethylethylenediamine (7.4 mg, 0.083mmol) in dioxane (2 mL) was heated in an Initiator Microwave Synthesizer at 14O0C for 12 hours. The cooled mixture was applied to an Isolute SCX cartridge. Elution with methanol, followed by water, then methanol then IM NH3 in methanol gave, after evaporation, the product which was further purified by chromatography on EPO silica gel. Elution with dichloromethane/methanol (0 to 10%) gave a pale yellow solid which was dissolved in dichloromethane (2 mL), Ethereal HCl (IM; LOmL) was added and the solvent evaporated. The residue was triturated under ether (1 mL) and filtered to give the title compound as a colourless solid; MS (ES+ve): [M+H]+ at m/z 399 (C2IH26N4O2S requires [M+H]+ at m/z 399).

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2007/3386; (2007); 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

Intermediate 4 (0.146 g, 0.150 mmol) and isothiazolidine 1,1-dioxide (0.181 g, 1.496 mmol) were dissolved into anhydrous acetonitrile (1.5 mE). para-Toluenesulfonic acid monohydrate (2.84 mg, 0.015 mmol) was added in one portion. The reaction mixture was stirred at room temperature for two hours.10479] Aqueous saturated NaHCO3 was added. The mixture was extracted several times with ethyl acetate. The organic extracts were combined, dried over Na2SO, decanted and concentrated to give a colorless tar crude product.10480] The crude product was dissolved in MeOH (2.5 mE) and was purified in one injection via preparative-scale reverse phase chromatography (40-90% acetonitrile-water plus 0.1% TFA modifier on 100 g C18 ISCO column).10481] The first eluting peak fractions were pooled and reduced to about volume on a rotary evaporatot The remaining solution was made basic with saturated aqueous NaHCO4 and was extracted several times with EtOAc. The organic extracts were combined, dried over Na SO4, decanted and concentrated to give Example 14 (0.05 g, 0.044 mmol, 29.3% yield) as a white solid.Example 1410482] ESIMS [M+NH4] 1082.8, [M-H] 1063.7.10483] HRMS: calculated for C55H89N2O14PSNa as sodium adduct-1087.5670. Found-1087.5725.10484] ?H NMR (400 MHz, Chloroform-d) oe 6.45 (dd, J=14.4, 10.9 Hz, 1H), 6.22 (dd, J=14.5, 10.6 Hz, 1H), 6.13 (dd, J=14.6, 10.5 Hz, 1H), 5.8 (d, J=10.8 Hz, 1H), 515 (dd, i=14.7, 9.8 Hz, 1H), 5.23-5.17 (m, 1H), 5.10 (d, J=9.8 Hz, 1H), 4.67 (m, 2H), 4.47 (d, J=1.8 Hz, 1H), 4.18-4.04 (m, 2H), 4.03-3.91 (m, 1H), 3.72 (d, J=6.5 Hz, 1H), 3.68-3.48 (m, 2H), 3.38 (m, 4H), 3.28 (s, 3H), 3.26-3.12 (m, 2H), .12-2.91 (m, 4H), 2.74 (m, HI), 2.48-2.26 (m, 3F1), 2.26- 2.12 (m, 3H), 2.12-2.04 (m, 2H), 1.87 (s, 3H), 1.85-1.72 (m, 4H), 1.72-1.54 (m, 12H), 1.54-1.43 (m, 6H), 1.43-1.33 (m, 3H), 1.33-1.21 (m, 2H), 1.21-1.09 (m, 2H), 1.03 (m, 7H),1.00-0.78 (m, 9H), 0.72 (q, J=11.9 Hz, 1H).10485] The second eluting peak fractions were pooled and reduced to about volume on the rotary evaporatot The remaining solution was made basic with saturated aqueous NaHCO3. The mixture was extracted several times with ethyl acetate. The organic extracts were combined, dried over Na2504, decanted and concentrated to give Example 15 (0.010 g, 7.51 tmol, 5.02% yield) as a white solid.Example 1510486] ESIMS [M+NH4] 1082.8 [M-H] 1063.8.10487] ?H NMR (400 MHz, Chloroform-d) oe 6.36 (dd,J=19.2, 10.3 Hz, 1H), 6.13 (m, 1H), 6.04-5.84 (m, 1H), 5.65(m, 1H), 5.32 (m, 1FI), 6.21 (m, 1FI), 5.11 (m, 1?H), 4.1 (dd,i=13.7, 7.5 Hz, 1H), 4.21-4.03 (m, IH), 3.83 (dd, J=15.2, 5.1Hz, 2H), 3.74 (d, J?=13.2 Hz, 1H), 3.59 (dq, J=10.9, 6.8, 5.6Hz, 2H), 3.52 (d, J=7.1 Hz, 1H), 3.46-3.33 (m, 7H), 3.30 (m,3H), 3.18 (m, 3H), 3.10-2.82 (m, 3H), 2.39 (t, J=4.1 Hz, 1112.28(m,311),2.14(m,3H), 1.90-1.77(m,4H), 1.74(m,4H

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

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

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, To a mixture of Intermediate 1 (1 equiv.) and isothiazo lidine 1,1-dioxide (1.2 equiv.) in 1 ,4-dioxane was added cesium carbonate (1.5 equiv.). The reaction was heated to 100 C for 16 h, after which the reaction was diluted with water, and extracted with ethyl acetate. The combined organic layers were dried over sodium sulfate, filtered, and concentrated in vacuo. The crude material was purified via silica gel chromatography utilizing a 3-10% methanol in dichloromethane gradient to deliver the desired compound, Compound 1-503 (71.3 mg, 73% yield) as an off- white solid.1H-NMR (500 MHz, CDC13) oe 8.57 (d, 1 H), 8.47 (d, 1 H), 7.36 (s, 1 H), 7.20-7.25 (m, 1 H),7.03-7.07 (m, 1 H), 6.96-7.01 (m, 1 H), 6.84-6.88 (m, 1 H), 6.61 (m, 1 H), 5.99 (s, 2 H), 4.27 (t, 2 H), 3.44 (t, 2 H), 2.66 (t, 2 H).

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

Reference£º
Patent; NAKAI, Takashi; MOORE, Joel; PERL, Nicholas Robert; IYENGAR, Rajesh R.; MERMERIAN, Ara; IM, G-Yoon Jamie; LEE, Thomas Wai-Ho; HUDSON, Colleen; RENNIE, Glen Robert; JIA, James; RENHOWE, Paul Allen; BARDEN, Timothy Claude; YU, Xiang Y; SHEPPECK, James Edward; IYER, Karthik; JUNG, Joon; WO2014/144100; (2014); A2;,
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.

To a stirred solution of KHMDS in THF (1 M, 0.410 ml_, 0.410 mmol) and THF (1 mL) at 0 C was added a solution of 1 , 1-dioxo-isothiazolidine (0.044 g, 0.35 mmol) in THF (0.5ml_). The reaction mixture was stirred for 30 minutes at 0 C and then 3-[4-(bromomethyl)-3-chloro-phenyl]-5- (trifluoromethyl)-1 ,2,4-oxadiazole (0.100 g, 0.293 mmol), prepared according to procedures described in example 1 using 3-chloro-4-methyl-benzonitrile as starting material, was added. The reaction mixture was stirred at 0C for 2 h. The reaction mixture was then quenched with water and warmed to RT. The mixture was extracted with ethyl acetate and the combined organic layers washed with brine, dried over MgSC , filtered and concentrated under reduce pressure. LC/MS (Method A) retention time = 1.07 minutes, 398 (M+OH)”. The mass observed only in the negative ionization and corresponded to that of a hydrated species.

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

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

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+].

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

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.,5908-62-3

Into a 4 mL vial was added isothiazolidine 1,1-dioxide (9.04 mg, 0.075 mmol) and (S)-6-chloro-3-(1-(4-chloropyrimidin-2-ylamino)ethyl)quinolin-2(1H)-one IV-1 (25 mg, 0.075 mmol) in DMF (250 muL). To this solution was added Cs2CO3 (48.6 mg, 0.149 mmol) and DIEA (26.1 muL, 0.149 mmol) and the reaction mixture was stirred at 110 C. for 1.5 hours. The mixture was then diluted with EtOAc and washed with brine (*2). The organic extract was dried over Na2SO4, filtered, and concentrated under reduced pressure to provide the crude product. This crude material was purified by column chromatography on a Biotage chromatography system (eluted with 0-100% EtOAc in hexanes) to afford the title compound (5.2 mg, 17% yield). 1H NMR (300 MHz, CDCl3): delta ppm 8.03 (br s, 1H), 7.93 (br s, 1H), 7.61 (br s, 1H), 7.41 (br d, J=8.50 Hz, 2H), 6.70 (br s, 1H), 5.42 (br s, 1H), 4.03 (br s, 1H), 3.83 (br s, 1H), 3.46 (m, 2H), 3.38 (m, 2H), 1.55-1.71 (m, 3H). LCMS (Method 1): Rt 2.02 min, m/z 419.89[M+H]+.

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

Reference£º
Patent; Forma Therapeutics, Inc.; Lin, Jian; Ericsson, Anna; Campbell, Ann-Marie; Gustafson, Gary; Wang, Zhongguo; Diebold, R Bruce; Ashwell, Susan; Lancia, JR., David R.; Caravella, Justin Andrew; Lu, Wei; (171 pag.)US2016/83365; (2016); 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, 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.

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

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

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.

1, 3-propanesultam (72 mg, 0.60 MMOL) in anhydrous DMF (3 mL) was added under N2 to 60 % NaH in mineral oil (36 mg, 0.90 MMOL). The mixture was stirred for 20 min, then the compound prepared in Preparative Example 196 (200 mg, 0.46 MMOL) was added. The mixture was stirred at 100 C for 30 min, the solvent was evaporated and the residue was purified by flash chromatography using EtOAc as eluent to yield colorless solid (150 mg, 63%). LCMS : M+=523.

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

Reference£º
Patent; SCHERING CORPORATION; PHARMACOPEIA, INC.; WO2004/22561; (2004); 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 microwave vial was charged with (5-{7-chloro-6-fluoro-5-[(S)-oxan-4- yl(phenyl)methyl]-5H-pyrido[3,2-b]indol-3-yl}-4-(2H3)methyl-l-methyl-lH-l,2,3- triazole (30 mg, 0.061 mmol), isothiazolidine 1,1-dioxide (11.1 mg, 0.091 mmol), tripotassium phosphate (18.1 mg, 0.085 mmol), Pd2(dba)3 (2.8 mg, 3.0 muiotatauiotaomicron), 2-di-tert- butylphosphino-3,4,5,6-tetramethyl-2′,4′,6′-triisopropyl-l, -biphenyl (2.9 mg, 6.1 mumol), and dry tert-butanol (0.5 mL). The reaction was heated at 84C overnight. It was diluted with water and extracted with ethyl acetate. The organic layer was concentrated and purified by preparative HPLC (Column: XBridge CI 8, 19 x 200 mm, 5-muiotatauiota particles; Mobile Phase A: 5:95 acetonitrile: water with 10-mM ammonium acetate; Mobile Phase B: 95:5 acetonitrile: water with 10-mM ammonium acetate; Gradient: 15-55% B over 15 min, then a 5-min hold at 100% B; Flow: 20 mL/min) to give 2.1 mg (6%). NMR (500 MHz, DMSO) delta 8.61 (s, 1H), 8.11 (m, 1H), 7.96 (s, 1H), 7.64 (m, 2H), 7.45 (m, 1H), 7.35 (m, 2H), 7.28 (m, 1H), 5.91 (m, 1H), 3.9 (m, 5H), 3.77 (m, 1H), 3.52 (m, 3H), 3.29 (m, 1H), 2.55 9m, 2H), 1.78 (m, 1H), 1.35 (m, 2H), 1.1 (m, 1H); LCMS (M+H) = 578.35

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

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, 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.

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

Reference£º
Patent; Pfizer Inc.; US4489075; (1984); A;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com