Tag: 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

Intermediate 5 (0.109 g, 0.114 mmol) was combined with isothiazolidine 1,1-dioxide (0.139 g, 1.145 mmol) in anhydrous acetonitrile (1.1 mE). para-Toluenesulfonic acid monohydrate (0.0022 g, 0.011 mmol) was added. The reaction was stirred at room temperature for two hours. 10503] The reaction was diluted with saturated aqueous NaHCO3. The mixture was extracted several times with EtOAc. The organic extracts were combined, dried over Na2SO, decanted and concentrated to give a yellow tar crude product.10504] The crude product was purified by silica gel flash column chromatography (0-40% acetone-heptane, gradient elution, 24 g silica column, TEC in 40% acetone-heptane, visualize under UV) to give Example 17 (0.053 g, 0.046 mmol, 40.0% yield) as a white solid.Example 1710505] ESIMS [M+H] 1041.8, [M-H] 1039.8.10506] HRMS: calculated for C54H84N6012SNa-1063.5765. Found-1063.5759.10507] ?H NMR (600 MHz, Chloroform-d) oe 8.86 (s, 1H),6.39 (dd, J=14.7, 11.0 Hz, 1H), 6.22 (dd, J=14.7, 10.7 Hz,1H), 6.11 (dd, J=15.0, 10.5 Hz, 1H), 5.99 (d, J=10.9 Hz, 1H),5.34 (dd, J=14.9, 9.8 Hz, 1H), 5.18 (d, J=5.7 Hz, 1H), 5.10(d, J=9.8 Hz, 1H), 4.87 (m, 1H), 4.67 (m, 1H), 4.63 (d,J=12.2 Hz, 1H), 4.50 (s, 1H), 4.13 (d, J=6.1 Hz, 1H), 3.97(t, J=11.4 Hz, 1H), 3.78 (d, J=6.2 Hz, 1H), 3.69-3.62 (m,1H), 3.55 (dt, J=11.2, 4.0 Hz, 1H), 3.50-3.39 (m, 1H), 3.39(s, 3H), 3.38-3.30 (m, 1H), 3.27 (s, 3H), 3.25-3.13 (m, 1H),3.07 (td, J=8.4, 3.8 Hz, 1H), 3.01 (m, 1H), 2.96 (q, J=7.9 Hz,1H), 2.70-2.63 (m, 2H), 2.39 (m, 1H), 2.35-2.21 (m, 3H),2.18 (d, J=13.7 Hz, 1H), 2.16-2.09 (m, 1H), 1.95-1.81 (m,3H), 1.82 (s, 3H), 1.75 (m, 3H), 1.65 (s, 3H), 1.60 (m, 6H),1.58-1.50 (m, 1H), 1.53-1.34 (m, 2H), 1.32 (m, 1H), 1.29(m, 1H), 1.25 (m, 6H), 1.12 (m, 1H), 1.05 (d, J=6.6 Hz, 3H),1.05-0.78 (m, 12H).

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

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

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

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).

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

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

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.

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

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

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

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

2, 4-Dichloro-5,7-difluoro-3-methylquinoline (800 mg, 3.20 mmol), crude isothiazolidine 1,1-dioxide (390 mg, 3.20 mmol), Pd2(dba)3 (150 mg, 0.16 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (XantPhos) (280 mg, 0.48 mmol) and cesium carbonate (1.50 g, 4.50 mmol) were slurried in 10.0 mL of dry dioxane along with ~1.0 gram of activated 3 A molecular sieves. The reaction was heated in a microwave reactor at 100 C for 2 h. The reaction was then cooled to rt, diluted with EtOAc and DCM and filtered. The filtrate was concentrated and the residue was purifiied by medium pressure chromatography (silica, 0 to 25% EtOAc : hexanes followed by 0 to 20% EtOAc : DCM) to give 2- (4-chloro-5,7-difluoro-3-methylquinolin-2-yl)isothiazolidine 1,1-dioxide. Mass Spectrum (ESI) m/e = 333.1.

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

Reference£º
Patent; AMGEN INC.; DRANSFIELD, Paul, John; GONZALEZ LOPEZ DE TURISO, Felix; KOHN, Todd, J.; PATTAROPONG, Vatee; SIMARD, Jillian, L.; WO2012/3283; (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

Intermediate 96To 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 96 (322 mg, 78%) as a yellow off-white solid.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).LCMS m/z [M+H]+ Ci2H15N04S requires: 270.07. Found 270.12.

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

Reference£º
Patent; GILEAD SCIENCES, INC.; BABAOGLU, Kerim; BOOJAMRA, Constantine, G.; EISENBERG, Eugene, J.; HUI, Hon Chung; MACKMAN, Richard, L.; PARRISH, Jay, P.; SANGI, Michael; SAUNDERS, Oliver, L.; SIEGEL, Dustin; SPERANDIO, David; YANG, Hai; WO2011/163518; (2011); 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

To a stirring solution of Intermediate 1 (2.0 g,2.222 mmol) and isothiazolidine 1,1-dioxide (4.04 g, 33.3 mmol, 15 equivalents) in anhydrous dichloromethane (5.6 mE) was added p-toluenesulphonic acid*H20 (0.042 g, 0.222 mmol, 0.1 equivalent) in one portion. The reaction was stirred at ambient temperature under a nitrogen atmosphere for 34 minutes. The entire reaction mixture was directly chromatographed by over silica (gradient elution from 100% heptane to 40% acetone-heptane) to give a product mixture of both diastereomers in a ratio of about 3:1 by UV absorbance at 279 nm on EC/MS analysis.10415] The diastereomeric mixture was separated by normal phase chromatography on silica (gradient elution from 100% dichloromethane to 40% acetonitrile-dichloromethane).10416] The first eluting diastereomer (Rf 0.23 on silica TEC developed in 30% acetonitrile-dichloromethane) affords Example 1 (5)-diastereomer as a white solid.Example 110417] ESIMS [M+NH4] 1006.7, ESIMS [M-H] 987.8.10418] ?H NMR (600 MHz, Chloroform-d) oe 6.43 (dd,J=14.9, 10.4 Hz, 1H), 6.35 (dd, J=14.9, 10.7 Hz, 1H), 6.16(dd, J=15.1, 10.2 Hz, 1H), 6.06-6.01 (m, 1H), 5.67 (dd,J=15.2, 8.6 Hz, 1H), 5.35 (dd, J=6.4, 1.8 Hz, 1H), 5.26 (d,J=9.6 Hz, 1H), 4.83 (td, J=6.6, 4.7 Hz, 1H), 4.12 (d, J=7.4Hz, 1H), 3.88 (dd, J=11.1, 5.1 Hz, 1H), 3.84-3.77 (m, 1H),3.63-3.60 (m, 2H), 3.51 (d, J=7.5 Hz, 1H), 3.46 (s, 3H),3.45-3.42 (m, 3H), 3.35 (s, 3H), 3.29-3.14 (m, 3H), 3.06-2.96 (m, 2H), 2.93 (ddd, J=10.4, 6.4, 1.5 Hz, 1H), 2.44 (U,J=8.6, 6.2 Hz, 1H), 2.37-2.23 (m, 4H), 2.22-2.14 (m, 2H),2.03 (dt, J12.3, 3.8 Hz, 1H), 1.96 (pd, J6.4, 5.7, 3.5 Hz,2H), 1.92-1.82 (m, 3H), 1.80-1.76 (m, 2H), 1.75 (d, J=1.2Hz, 4H), 1.72 (d, J=3.1 Hz, 1H), 1.68 (d, J=1.3 Hz, 3H),1.65-1.53 (m, 4H), 1.48-1.17 (m, 9H), 1.07 (d, J=6.5 Hz,1H), 1.06 (s, 3H), 1.04 (d, J=7.3 Hz, 3H), 1.01 (d, J=6.6 Hz,3H), 0.99 (dd, J=6.7, 2.3 Hz, 3H), 0.95 (d, J=6.8 Hz, 3H),0.74 (q, J=11.9 Hz, 1H).10419] The second eluting diastereomer (Rf 0. 16 onsilica TEC developed in 30% acetonitrile-dichloromethane)affords Example 2 (R)-diastereomer as a white solidExample 210420] ESIMS [M+NH4] 1006.9, ESIMS [M-H] 988.1.10421] ?H NMR (Chloroform-d) oe 6.48 (dd, J14.7, 10.9Hz, 1H), 6.24 (dd, J=14.6, 10.6 Hz, 1H), 6.16 (dd, J14.9,10.6 Hz, 1H), 6.01 (d, J=11.0 Hz, 1H), 5.38 (dd, J=14.9, 9.8Hz, 1H), 5.23 (dd, J=6.2, 2.0 Hz, 1H), 5.12 (d, J9.9 Hz,1H), 4.73 (dd, J=12.1, 2.9 Hz, 1H), 4.65 (dt, J8.3, 3.9 Hz,1H), 4.14 (d, J=6.7 Hz, 1H), 3.97 (m, 1H), 3.74 (d, J=6.7 Hz,1H), 3.62 (qd, J=13.9, 12.7, 5.5 Hz, 2H), 3.42 (s, 3H), 3.39(m, 1H), 3.31 (s, 3H), 3.24 (ddd, J=12.2, 7.5, 4.6 Hz, 1H),3.10 (td, J=8.2, 3.8 Hz, 1H), 3.08 (s, 1H), 3.02-2.97 (m, 1H),2.97-2.92 (m, 1H), 2.83-2.71 (m, 1H), 2.42 (ddt, J=13.1, 9.5,6.4 Hz, 1H), 2.34 (d, J=4.3 Hz, 1H), 2.31 (s, 1H), 2.28-2.23(m, 1H), 2.22-2.19 (m, 1H), 2.19 (s, 2H), 2.12-2.08 (m, 2H),2.03-1.99 (m, 1H), 1.90 (s, 3H), 1.88 (s, 1H), 1.79 (s, 1H),1.77 (s, 1H), 1.76 (s, 1H), 1.72-1.68 (m, 1H), 1.48 (s, 1H),1.46 (s, 1H), 1.40 (d, J=3.0 Hz, 1H), 1.38 (s, 1H), 1.66 (d, J=3.0 Hz, 2H), 1.64 (d, J=2.9 Hz, 1H), 1.62 (s, 2H), 1.62 (s, 2H), 1.58-1.53 (m, 1H), 1.37 (s, 1H), 1.36 (d, J=2.3 Hz, 1H),1.33 (d, J=2.9 Hz, 1H), 1.30 (dd, J=6.7, 1.8 Hz, 1H), 1.28 (s, 2H), 1.28 (s, 2H), 1.24 (s, 1H), 1.09 (s, 1H), 1.07 (d, J=6.6 Hz, 3H), 1.05 (d, J=6.6 Hz, 3H), 1.01 (d, J=3.2 Hz, 1H), 0.95 (d, J=6.8 Hz, 3H), 0.92 (s, 1H), 0.92-0.90 (m, 3H), 0.88 (d, J=6.8 Hz, 2H), 0.66 (q, J=12.0 Hz, 1H)

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

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

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 47 5-tert-Butyl-3-(2-chloro-benzyl)-7-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine A mixture of 5-tert-butyl-7-chloro-3-(2-chlorobenzyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine (15.9 mg, 47.2 mumol), 1,1-dioxo-isothiazolidine (11.4 mg, 94.4 mumol) and DBU (14.2 muL, 94.4 mumol) in DMF (250 muL) was stirred at the room temperature overnight. The reaction mixture was directly purified by preparative HPLC (column: Gemini Sum C18 110A 75*30 mm. mobile phase: water (0.05% Et3N): acetonitrile 75:25% to 5:95%. WL: 230 nm Flow: 30 mL/min.) to afford the title compound as white solid (3.10 mg, 16%). MS (m/e): 387.3 (MH+).

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

Reference£º
Patent; Hoffmann-La Roche Inc.; Adam, Jean-Michel; Bissantz, Caterina; Grether, Uwe; Kimbara, Atsushi; Nettekoven, Matthias; Roever, Stephan; Rogers-Evans, Mark; US2013/116236; (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

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.

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

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.

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).

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; WO2007/3386; (2007); 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

[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)+.

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

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