Category: thiazolidine

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, Intermediate 7 (0.088 g, 0.087 mmol) was combined with isothiazolidine 1,1-dioxide (0.105 g, 0.866 mmol) in anhydrous dichloromethane (0.87 mE). paraToluenesulfonic acid monohydrate (1.647 mg, 8.66 tmol) was added. The reaction was stirred at room temperature for 30 minutes.10517] The entire reaction mixture was purified by normal phase flash column chromatography (0-60% acetonitriledichloromethane, gradient elution, 12 g silica column, TEC in 30% acetonitrile-dichloromethane) to give Example 19 (0.020 g, 0.017 mmol, 19.9% yield) as a white solid.Example 1910518] ESIMS [M+NH4] 1123.0, [M-H] 1104.0.10519] HRMS: Calculated for ammonium adductC58H92N20165NH4-1122.6511; found 1122.652.10520] ?H NMR (600 MHz, Chloroform-d) oe 6.45 (dd,J=14.7, 10.9 Hz, 1H), 6.22 (dd, J=14.7, 10.7 Hz, 1H), 6.13(dd, J=14.9, 10.6 Hz, 1H), 5.99 (d, J=10.9 Hz, 1H), 5.35 (dd,J=14.9, 9.8 Hz, 1H), 5.21 (d, J=5.8 Hz, 1H), 5.10 (d, J=9.9Hz, 1H), 4.73 (ddd, J=11.0, 9.2, 4.7 Hz, 1H), 4.69 (d, J=12.4Hz, 1H), 4.64 (m, 1H), 4.49 (s, 1H), 4.13 (d, J=6.5 Hz, 1H),3.97 (t, J=11.3 Hz, 1H), 3.84 (dd, J=18.5, 11.4 Hz, 2H),3.78-3.69 (m, 2H), 3.64 (m, 2H), 3.56 (td, J=13.5, 3.0 Hz,1H), 3.43-3.31 (m, 4H), 3.28 (m, 3H), 3.26-3.17 (m, 2H),3.12-2.92 (m, 3H), 2.76-2.68 (m, 1H), 2.45-2.34 (m, 1H),2.31-2.21 (m, 3H), 2.20-2.10 (m, 3H), 2.06 (m, 1H), 1.87(m, 4H), 1.75 (m, 3H), 1.71-1.59 (m, 3H), 1.60 (s, 3H),1.60-1.50 (m, 1H), 1.48-1.39 (m, 1H), 1.42-1.31 (m, 2H),1.33-1.20 (m, 8H), 1.11 (s, 3H), 1.11-1.05 (m, 2H), 1.03 (dd,J=18.2, 6.6 Hz, 6H), 0.99-0.82 (m, 1OH), 0.79 (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
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As a common heterocyclic compound, it belong thiazolidine compound,2-Cyanoimino-1,3-thiazolidine,26364-65-8,Molecular formula: C4H5N3S,mainly used in chemical industry, its synthesis route is as follows.,26364-65-8

3.42g (0.01mol) of intermediate IIc was addedIn a 250 mL reaction flask,Then add 30g acetonitrile,Add 1.2g of triethylamine,10 g of acetonitrile and 1.27 g (0.01 mol) were added dropwise with stirring.a mixture of 2-cyanoimido-1,3-thiazolidine,After the completion of the dropwise addition, the reaction was heated to reflux for 2 h.TLC tracking intermediate IIc reaction is complete,After adding 150 g of water and stirring, a solid precipitated.Filtered, dried, A pale yellow solid was obtained in 4.14 g, yield 96%.

With the synthetic route has been constantly updated, we look forward to future research findings about 2-Cyanoimino-1,3-thiazolidine,belong thiazolidine compound

Reference£º
Patent; Qingdao University of Science and Technology; Wang Minghui; Xu Liangzhong; Peng Zhuang; Cui Huanqi; Sun Jianxin; (7 pag.)CN109336882; (2019); A;,
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7025-19-6, 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,7025-19-6

General procedure: To a mixture of aldehyde (1.0 mmol), 3-(4-oxo-2-thioxothiazolidin-3-yl)propanoic acid (205 mg,1.0 mmol) or 3-(2-(1H-tetrazol-5-yl)ethyl)-2-thioxothiazolidin-4-one (229 mg, 1.0 mmol) and NaOAc (820 mg, 10.0 mmol) was added acetic acid (5.0 mL). The reaction was allowed to stir at 105 C for 0.5h – 12h, then cooled to room temperature. To the reaction was added water (15mL). The resulting mixture was sonicated to give yellow-orange slurry. After filtration, the solid was washed with water (75 mL) and dried under high vacuum to yield the corresponding product as a red fine powder.

As the paragraph descriping shows that 7025-19-6 is playing an increasingly important role.

Reference£º
Article; Liang, Dongdong; Robinson, Elizabeth; Hom, Kellie; Yu, Wenbo; Nguyen, Nam; Li, Yue; Zong, Qianshou; Wilks, Angela; Xue, Fengtian; Bioorganic and Medicinal Chemistry Letters; vol. 28; 6; (2018); p. 1024 – 1029;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belong thiazolidine compound,2-Cyanoimino-1,3-thiazolidine,26364-65-8,Molecular formula: C4H5N3S,mainly used in chemical industry, its synthesis route is as follows.,26364-65-8

General procedure: Thiazolidin-2-ylidene-cyanamide (0.317 g, 2.50 mmol) inacetonitrile (20 mL) was dropwise added to a stirred solutionof substituted benzyl bromide (2.5 mmol) and 14 mL NaOHaqueous solution (1 M). The mixture is stirred at room temperaturefor 8-10 h. The soild was collected by filtration,washed with n-hexane and dried in vacuo.

With the synthetic route has been constantly updated, we look forward to future research findings about 2-Cyanoimino-1,3-thiazolidine,belong thiazolidine compound

Reference£º
Article; Jia, Ai-Quan; Ma, Sen; Wang, Jun-Ling; Zhang, Qian-Feng; Journal of Chemical Crystallography; (2020);,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belong thiazolidine compound,2-Cyanoimino-1,3-thiazolidine,26364-65-8,Molecular formula: C4H5N3S,mainly used in chemical industry, its synthesis route is as follows.,26364-65-8

General procedure: Thiazolidin-2-ylidene-cyanamide (0.317 g, 2.50 mmol) inacetonitrile (20 mL) was dropwise added to a stirred solutionof substituted benzyl bromide (2.5 mmol) and 14 mL NaOHaqueous solution (1 M). The mixture is stirred at room temperaturefor 8-10 h. The soild was collected by filtration,washed with n-hexane and dried in vacuo.

With the synthetic route has been constantly updated, we look forward to future research findings about 2-Cyanoimino-1,3-thiazolidine,belong thiazolidine compound

Reference£º
Article; Jia, Ai-Quan; Ma, Sen; Wang, Jun-Ling; Zhang, Qian-Feng; Journal of Chemical Crystallography; (2020);,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.179087-93-5,2-(4-((2,4-Dioxothiazolidin-5-yl)methyl)phenoxy)acetic acid,as a common compound, the synthetic route is as follows.,179087-93-5

(Example 2) tert-Butyl N-{2-{4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetylamino}-5-methoxyphenyl}-N-methylcarbamate Thionyl chloride (27.66 g, 232.5 mmol) and dimethylformamide (12 ml) were poured into a suspension of 4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetic acid (60.0 g, 213.3 mmol) in dichloromethane (390 ml), and the mixture was heated to reflux (39C). After completion of dissolution, the solution was stirred for 30 minutes and cooled to 0 to 5C. A solution of tert-butyl N-(2-amino-5-methoxyphenyl)-N-methylcarbamate (53.84 g, 213.4 mmol) and triethylamine (25.92 g, 256.2 mmol) in dichloromethane (624 ml) was added dropwise while maintaining the internal temperature at 5C or less. The reaction solution was stirred at 5C for one hour. Then, dichloromethane (300 ml) was poured in, followed by addition of a solution prepared from sodium bicarbonate (24 g) and water (480 ml). The mixture was stirred at 20C for 20 minutes, allowed to stand, and then separated, and the aqueous layer was discarded. Water (480 ml) was added to the organic layer, the mixture was stirred at 20C for 20 minutes, allowed to stand, and then separated, and the aqueous layer was discarded. A solution of 38% hydrochloric acid (19.8 ml) and water (480 ml) was poured into the organic layer. The mixture was stirred at 20C for 20 minutes, and then the aqueous layer was discarded. Activated carbon (1.8 g) and dichloromethane (18 ml) were further added to the organic layer, and the mixture was stirred for 30 minutes. Thereafter, activated carbon was filtered off. The residue was washed with dichloromethane (90 ml) and the filtrate and the washing liquid were combined and concentrated under reduced pressure at an internal temperature of 25C to a fluid volume of 300 ml. After stirring at normal pressure for 10 minutes, methanol (300 ml) was added and the mixture was concentrated under reduced pressure at an internal temperature of 25C to a fluid volume of 300 ml. Methanol (300 ml) was further added and the mixture was concentrated under reduced pressure at an internal temperature of 30C to a fluid volume of 300 ml. Methanol (198 ml) was added thereto and the mixture was cooled to 0 to 5C and further stirred for one hour. The resulting crystals were separated by filtration, washed with cold methanol (240 ml), and then dried under reduced pressure at 50C to obtain tert-butyl N-{2-{4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetylamino}-5-methoxyphenyl}-N-methylcarbamate (97.09 g, 188.3 mmol) (yield: 89%).(Example 5) {5-4-[(6-Methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzyl}thiazolidine-2,4-dione hydrochloride (5-1) Thionyl chloride (28.15 kg, 236.6 mol) and dimethylformamide (6.1 L) were poured into a suspension of 4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetic acid (61.0 kg, 216.9 mol) in dichloromethane (398 L), and the mixture was refluxed for six hours. After cooling the resulting solution to 0 to 5C, a solution of tert-butyl N-(2-amino-5-methoxyphenyl)-N-methylcarbamate (54.72 kg, 216.9 mol) and triethylamine (26.35 kg, 260.4 mol) in dichloromethane (562 L) was added dropwise over one hour while maintaining the internal temperature at 5C or less, and the mixture was stirred at 0 to 5C for 15 minutes. Water (488 L) was poured in with stirring and sodium bicarbonate (24.4 kg) was added (the internal temperature was raised to about 20C). Then, dichloromethane (305 L) was poured in and the mixture was stirred for 20 minutes while cooling to 0 to 3C. Water (488 L) was poured in, the mixture was stirred at 10 to 20C for five minutes and allowed to stand for 30 minutes, and the aqueous layer was discarded. Water (488 L) and then 38% hydrochloric acid (23.8 kg) were poured in, the mixture was stirred for five minutes and then allowed to stand for 10 minutes, and the aqueous layer was discarded. Water (488 L) was poured in, the mixture was stirred for five minutes and then allowed to stand for 12 hours, and the aqueous layer was discarded. A suspension of activated carbon (1.83 kg) in dichloromethane (18 L) was added thereto. After stirring for 30 minutes, activated carbon was separated by filtration. Activated carbon was washed with dichloromethane (92 L) and the filtrate and the washing liquid were combined and concentrated under reduced pressure at an internal temperature of 20 to 30C to about 300 L. Methanol (305 L) was poured in and the mixture was concentrated under reduced pressure at an internal temperature of 20 to 30C to about 300 L. Methanol (305 L) was further poured in and the mixture was concentrated under reduced pressure at an internal temperature of 20 to 30C to about 300 L. Methanol (201 L) was poured in and the mixture was stirred at 5C for one hour. Then, the resulting crystals were separated by filtration, washed with methanol (244 L), and then dried under reduced pressure at 50C to obtain tert-butyl N-{2-{4-[(2,4-dioxothiazolidin-5-yl)methyl]phenoxyacetylamino}-5-methoxyphenyl}-N-methylcarbamate (103.9 kg, …

As the paragraph descriping shows that 179087-93-5 is playing an increasingly important role.

Reference£º
Patent; Daiichi Sankyo Company, Limited; EP1894929; (2008); A1;,
Thiazolidine – Wikipedia
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2682-49-7, Thiazolidin-2-one is a thiazolidine compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,2682-49-7

[0050] To a solution of 2-thiazolidinone (4.15 g, 40.18 mmol) in acetonitrile (60 ml) were added potassium carbonate (13.3 g 96.2 mmol), N,N-dimethyl-3-aminopropyl chloride hydrochloride (7.63 g, 48.3 mmol), and 18-crown-6 (catalytic amount). The mixture was refluxed for 18 hours, solvent removed in vacuo, then redissolved in dichloromethane and 1 M potassium chloride (40 ml each). The aqueous phase was isolated and extracted twice with 30 ml portions of dichloromethane. The combined organic fraction was washed with saturated sodium chloride (50 ml), dried over sodium sulfate, filtered, and dried in vacuo. The crude product was purified via silica gel chromatography, using a 10:1 ratio of silica gel A, 200-425 mesh, and eluting with 5% methanol in chloroform, yielding 1.15 g (15%) pure product.

The synthetic route of 2682-49-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Roberts, Jeannette C.; Wilmore, Britta H.; Cassidy, Pamela B.; Dominick, Pamela K.; Short, Megan D.; US2003/225255; (2003); A1;,
Thiazolidine – Wikipedia
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As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO43,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

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)

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; 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

EXAMPLE 9 STR38 Sodium hydride (1.25 g of a 50% dispersion in oil) was added at room temperature to a stirred solution of isothiazolidine-1,1-dioxide (2.42 g) in DMF (15 cm3). After stirring for 0.5 hours 2-methyl-2-[1-(6,7-dimethoxyquinazolin-4-yl)piperid-4-yl]oxirane (5.0 g) was added and the mixture was stirred for 4 hours at 100. Volatile material was removed in vacuo, the residue was partitioned between chloroform (100 cm3) and water (50 cm3) and the chloroform layer was dried (MgSO4) and evaporated. The residue was chromatographed on silica (“Merck” 60.9385) eluding with methanol:ethyl acetate, 1:4, to give a solid which was recrystallized from ethyl acetate-methanol to give 2-{2-hydroxy-2-[1-(6,7-dimethoxyquinazolin-4-yl)piperid-4-yl]prop-1-yl}isothiazolidine-1,1-dioxide, m.p. 173-174 (4.15 g). Analysis %: Found: C,55.6; H,6.8; N,12.4; Calculated for C21 H30 N4 O5 S: C,56.0; H,6.7; N,12.4.

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

Reference£º
Patent; Pfizer Inc.; US4542132; (1985); A;,
Thiazolidine – Wikipedia
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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
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