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

7 mg (0.03 mmol) of palladium(II) acetate and 18 mg (0.03 mmol) of Xantphos were stirred in 3.6 ml of dioxane under an argon atmosphere at 20 C. for 10 minutes. Then 150 mg (0.3 mmol) of the compound from Example 72A, 74 mg (0.06 mmol) of 1,3-propane sultam and 148 mg (0.46 mmol) of caesium carbonate were added and the mixture was stirred at 110 C. for 6 h. After cooling down to 23 C., the mixture was purified via preparative HPLC (eluent: acetonitrile/water gradient with 0.1% formic acid). This gave 95 mg (51% of theory) of the title compound. LC-MS (Method 1): Rt=1.15 min; m/z=579.2 [M+H]+. 1H-NMR (400 MHz, DMSO-d6) delta [ppm]: 1.156 (4.54), 1.174 (8.71), 1.192 (4.39), 1.987 (16.00), 2.297 (4.76), 2.314 (6.89), 2.331 (5.14), 3.577 (4.62), 3.590 (8.77), 3.606 (8.06), 3.634 (2.43), 4.020 (4.03), 4.037 (3.96), 4.815 (3.11), 4.827 (3.16), 4.845 (3.08), 4.859 (2.88), 7.325 (3.46), 7.334 (7.37), 7.356 (6.87), 7.380 (2.99), 7.399 (5.75), 7.420 (4.45), 7.526 (13.43), 7.546 (9.83), 7.555 (3.20), 7.811 (2.87), 7.826 (2.86), 8.595 (6.46), 8.617 (6.25), 8.754 (11.28), 10.157 (2.54), 10.171 (4.84).

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

Reference£º
Patent; Bayer Pharma Aktiengesellschaft; TELLER, Henrik; STRAUB, Alexander; BRECHMANN, Markus; MUeLLER, Thomas; MEININGHAUS, Mark; NOWAK-REPPEL, Katrin; TINEL, Hanna; MUeNTER, Klaus; FLIEGNER, Daniela; MONDRITZKI, Thomas; BOULTADAKIS ARAPINIS, Melissa; MARQUARDT, Tobias; VAKALOPOULOS, Alexandros; REBSTOCK, Anne-Sophie; WITTWER, Matthias Beat; (342 pag.)US2018/297994; (2018); 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.

To a solution of tert-butyl (3S)-3- [[4- [2- [(5 -iodo-2-methyl- 1 -naphthyl)oxy]-3 – pyridyl]pyrimidin-2-yl]amino]piperidine-1-carboxylate (110 mg, 0.17 mmol) in CH3CN (2 mL) was added 1,3-propanesultam (209.1 mg, 1.73 mmol), copper iodide (1.6 mg, 0.01 mmol), N,N?-dimethyl-1,2-ethanediamine (7.6 mg, 0.09 mmol) and potassium carbonate (47.8 mg, 0.34 mmol). The mixture was purged with N2 and stirred at 80 C for 88 h. After cooling down, the mixture was filtered, concentrated, dissolved in ethyl acetate (60 mL) and washed with H20 (50 mL x 2). The organic phase was dried over anhydrous sodium sulfate and concentrated and the residue was purified by Prep-TLC (50% ethyl acetate in petroleum ether,Rf= 0.1) to yield 55 mg (51%) of the title compound as a brown oil. LCMS (ESI) [M+H]=631.0.

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

Reference£º
Patent; GENENTECH, INC.; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; BRAUN, Marie-Gabrielle; GIBBONS, Paul; LEE, Wendy; LY, Cuong; RUDOLPH, Joachim; SCHWARZ, Jacob; ASHKENAZI, Avi; FU, Leo; LAI, Tommy; WANG, Fei; BEVERIDGE, Ramsay; ZHAO, Liang; (652 pag.)WO2018/166528; (2018); 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 mixture of Cs2C03(41 mg, 0.12 mmol), 5-(5-(4-bromophenyl)- l,2,4-oxadiazol-3-yl)-l-(3-(2-methoxyethoxy)benzyl)pyridin-2(lH)-one(synthesized with analogous method to Example 65, using 4-bromobenzoic acid instead of 4-(trifluoromethoxy)benzoic acid; 30 mg, 0.062 mmol), Pd2(dba)3 (0.6 mg, 0.62 muiotaetaomicron), and XPhos (1.1 mg, 2.5 muiotaetaomicron) in toluene (311 muEpsilon) previously degassed with N2, was added isothiazolidine 1,1 -dioxide (6.4 mu, 0.075 mmol). The mixture was heated to 80 C for 12 h, cooled to RT, filtered through a pad Celite and concentrated under reduced pressure. The residue was purified by prep-HPLC (Mobile phase: A = 0.1% TFA/H20, B = 0.1% TFA/ MeCN; Gradient: B = 30% – 70% in 12 min; Column: CI 8) to give the title compound; H NMR (600 MHz, Chloroform-if) delta 8.25 (d, J = 2.4 Hz, IH), 8.13 (d, J = 8.8 Hz, 2H), 8.04 (dd, J = 9.5, 2.4 Hz, IH), 7.35 (d, / = 8.8 Hz, 2H), 7.28 (m, IH), 6.95 (d, / = 8.0 Hz, IH), 6.93 (m, IH), 6.88 (dd, / = 8.1, 2.4 Hz, IH), 6.77 (d, / = 9.5 Hz, IH), 5.22 (s, 2H), 4.14 – 4.04 (m, 2H), 3.87 (t, / = 6.5 Hz, 2H), 3.79 – 3.68 (m, 2H), 3.46 – 3.43 (m, 2H), 3.43 (s, 3H), 2.67 – 2.56 (m, 2H); MS (ES+) C26H26N406S requires: 522, found: 523 [M+H]+

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

Reference£º
Patent; JONES, Philip; DIFRANCESCO, Maria, Emilia; PETROCCHI, Alessia; MARSZALEK, Joe; LIU, Gang; KANG, Zhijun; CARROLL, Christopher, L.; MCAFOOS, Timothy; CZAKO, Barbara; WO2014/31928; (2014); A2;,
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, 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).

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

Reference£º
Patent; MATRIX LABORATORIES LTD.; WO2007/113634; (2007); 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 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 paragraph descriping shows that 5908-62-3 is playing an increasingly important role.

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

A 40 mL scintillation vial was charged with 1 ,1-dloxo-isothiazolidine (115 mg, 0.949 mmol) and OMF (3 mL). The reaction mixture was cooled to 00C and sodium hydride (95 mg, 2.373 mmol) was added. The reaction was left to stir at room temperature for 20 min foliowed by the addition of 3-bromo~5-(chloromethyl)pyridine hydrochloride (277 mg, 1.139 mmol). The reaction was stirred at room temperature for 3 h, then quenched with water and extracted with ethyi acetate. The organic layer was washed with water twice, dried over sodium sulfate and concentrated in vacuo. The crude was purified by silica gei flash chromatography using heptane-ethyl acetate (6(MO, v/v) to afford 3-bromo-5-(1,1- dioxo-isothiazolidin-2?ylmethyl)?pyridine as a colorless oil. MS (ESI) m/z 292.9 <;M+H)+ As the paragraph descriping shows that 5908-62-3 is playing an increasingly important role. Reference£º
Patent; NOVARTIS AG; CHAMOIN, Sylvie; HU, Qi-Ying; PAPILLON, Julien; WO2010/130796; (2010); 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 15 6-[(1,1-Dioxido-1,2-thiazolidin-2-yl)methyl]-1-(2-methoxyethyl)-5-methyl-3-(2-phenylethyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione To a solution of 49 mul (0.668 mmol) of propane sultam in 1.5 ml of DMF were added 27 mg (0.668 mmol) of sodium hydride (60% suspension in mineral oil) and then the mixture was stirred at RT for 25 min (“Solution 1”). To a solution of 50 mg (0.134 mmol) of the compound from Ex. 138A in 1.3 ml of dichloromethane in another reaction vessel were added, at 0 C., 47 mul (0.267 mmol) of N,N-diisopropylethylamine and 10 mul (0.140 mmol) of thionyl chloride. After 20 min, one third of Solution 1 was added at 0 C. The reaction mixture was stirred at 0 C., with addition of a further third of Solution 1 after 20 min and after 40 min of reaction time. After the last addition, the cooling bath was removed and the reaction mixture was stirred at RT for about 18 h. All the volatile constituents were then removed on a rotary evaporator. The remaining residue was separated into its components by means of preparative HPLC (Method 8). After concentration of the product fractions and drying under high vacuum, 41 mg (64% of theory) of the title compound were obtained. 1H-NMR (400 MHz, CDCl3, delta/ppm): 7.41-7.16 (m, 5H, partially obscured by the CHCl3 signal), 4.30 (s, 2H), 4.25-4.17 (m, 2H), 4.11 (t, 2H), 3.70 (t, 2H), 3.35 (s, 3H), 3.26-3.15 (m, 4H), 2.99-2.88 (m, 2H), 2.50 (s, 3H), 2.44-2.28 (m, 2H). LC/MS (Method 1, ESIpos): Rt=1.03 min, m/z=478 [M+H]+.

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

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HAeRTER, Michael; KOSEMUND, Dirk; DELBECK, Martina; KALTHOF, Bernd; WASNAIRE, Pierre; SUessMEIER, Frank; LUSTIG, Klemens; (369 pag.)US2018/65981; (2018); 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

100 mg (0.231 mmol) of (¡À)-1-(4-bromophenyl)-7,8-dimethoxy-N,4-dimethyl-4,5-dihydro-3H-2,3-benzodiazepine-3-carboxamide (Example 49A), 33.6 mg (0.278 mmol) of 1,2-thiazolidine 1,1-dioxide (CAS [5908-62-3]), 64 mg (0.46 mmol) of potassium carbonate and 13 mg (0.023 mmol) of allylchloropalladium dimer (CAS [12012-95-2]) are charged in 3 ml of 2-methyltetrahydrofuran and the suspension is degassed with argon for 10 min. Then 39 mg (0.093 mmol) of di-tert-butyl(2?,4?,6?-triisopropylbiphenyl-2-yl)phosphane (CAS [564483-19-8]) are added, degassing with argon is carried out again, and the mixture is heated at 80 C. for 16 h. The crude mixture is filtered, and then the solvent is removed and the residue obtained is purified by preparative HPLC. This gave 32 mg (29% of theory) of the desired product as a solid. [2172] LCMS (Method 5): Rt=0.90 min; m/z=473 (M+H)+ [2173] 1H-NMR (300 MHz, CDCl3): delta=1.04 (d, 3H), 2.61 (pent, 2H), 2.83 (dd, 1H), 2.91 (d, 3H), 3.09 (dd, 1H), 3.46 (t, 2H), 3.70 (s, 3H), 3.87 (t, 2H), 3.96 (s, 3H), 5.37-5.50 (m, 1H), 6.42 (q, 1H), 6.62 (s, 1H), 6.75 (s, 1H), 7.30 (d, 2H), 7.55 (d, 2H).

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

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; Siegel, Stephan; Baeurle, Stefan; Cleve, Arwed; Haendler, Bernard; Fernandiez-Montalvan, Amaury Ernesto; Moenning, Ursula; Krause, Sabine; Lejeune, Pascale; Schmees, Norbert; Busemann, Matthias; Holton, Simon; Kuhnke, Joachim; US2015/203483; (2015); 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, Example 19 6-[(1,1-Dioxido-1,2-thiazolidin-2-yl)methyl]-3-ethyl-5-(trifluoromethyl)-1-(3,3,3-trifluoropropyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione 74 mg (0.612 mmol) of propane sultam were dissolved in 1.5 ml of DMF, 24 mg (0.612 mmol) of sodium hydride (60% suspension in mineral oil) were added and the mixture was stirred at RT for 25 min. This was followed by dilution with 0.25 ml of THF (“Mixture 1”). In another reaction vessel, 50 mg (0.122 mmol) of the compound from Example 182A were dissolved in 1 ml of DMF, and 350 mul of Mixture 1 were added dropwise at 0 C. After 2.5 h at 0 C., a further 350 mul of Mixture 1 were added. After a further 30 min at 0 C., the reaction mixture was separated directly into its components by means of preparative HPLC (Method 8). Concentration of the product fractions and drying under high vacuum gave 42 mg (69% of theory) of the title compound. 1H-NMR (400 MHz, CDCl3, delta/ppm): 4.57 (d, 2H), 4.23-4.14 (m, 2H), 4.08 (q, 2H), 3.40 (t, 2H), 3.31-3.19 (m, 2H), 2.74-2.57 (m, 2H), 2.53-2.38 (m, 2H), 1.26 (t, 3H). LC/MS (Method 1, ESIpos): Rt=0.98 min, m/z=494 [M+H]+.

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

Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; HAeRTER, Michael; KOSEMUND, Dirk; DELBECK, Martina; KALTHOF, Bernd; WASNAIRE, Pierre; SUessMEIER, Frank; LUSTIG, Klemens; (369 pag.)US2018/65981; (2018); 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, 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] +.

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2005/80382; (2005); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com