Month: October 2020

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO121,mainly used in chemical industry, its synthesis route is as follows.,26364-65-8

11.8 g (0.05 mL) of Compound X, 150 mL of DMF, 8.28 g (0.05 mL) of K2CO3 and 6.35 g of thiazolidine were added to a 150 mL three-necked flask, and reacted at 80 C for 4 h.Compound X disappeared by TLC. Filter by suction, take the filtrate, add 300mL after coolingWater, a large amount of solids are precipitated, stirred for a while, and then filtered.The filter cake is the product compound I. After drying, 14.15 g of a white solid was obtained, yield 86%.

With the complex challenges of chemical substances, 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; Xu Liangzhong; Zhang Mingming; Sun Jianxin; Wang Minghui; (6 pag.)CN108440519; (2018); A;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

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

To a stirred solution of 5-{9-fluoro-5-[(S)-(2-fluorophenyl)(oxan-4-yl)methyl]-6- methanesulfonyl-5H-pyrido[3,2-b]indol-3-yl}-4-(2H3)methyl-l-methyl-lH-l,2,3-triazole (7.8 mg, 0.0140 mmol) and isothiazolidine-l,l-dione (8.5 mg, 0.0560 mmol) in NMP (0.15 mL) was added t-BuOK (6.3 mg, 0.0560 mmol). This mixture was heated at 65 C for 100 min and cooled to room temperature. The mixture was then diluted with MeOH and purified via preparative LC/MS with the following conditions: Column: Waters XBridge Phenyl, 19 x 200 mm, 5-muiotatauiota particles; Mobile Phase A: 5:95 ACN: water with 10 mM NH4OAc; Mobile Phase B: 95:5 ACN: water with 10 mM NH4OAc; Gradient: 15-70% B over 20 min, then a 5-min hold at 100% B; Flow: 20 mL/min. Fractions containing the desired product were combined and dried via centrifugal evaporation to give 2-{5-[(S)-(2-fluorophenyl)(oxan-4-yl)methyl]-6-methanesulfonyl-3-[4-(2H3)methyl- l-methyl-lH-l,2,3-triazol-5-yl]-5H-pyrido[3,2-b]indol-9-yl}- 6,2-thiazolidine-l,l-dione (6.1 mg, 64%). NuMuRhonu (500MHz, DMSO-de) delta 8.69 (s, 1H), 8.42 (d, J=8.5 Hz, 1H), 8.15-8.06 (m, 1H), 7.99 (s, 1H), 7.63 (d, J=8.5 Hz, 1H), 7.31 (br d, J=4.2 Hz, 2H), 7.06- 6.95 (m, 2H), 4.18-4.09 (m, 1H), 4.06-3.99 (m, 1H), 3.93-3.84 (m, 1H), 3.76 (s, 3H), 3.72 (br d, J=8.3 Hz, 1H), 3.60 (s, 1H), 3.53 (br s, 3H), 3.27 (br t, J=11.3 Hz, 1H), 2.66-2.58 (m, 3H), 2.54 (s, 2H), 1.96-1.84 (m, 1H), 1.79 (br s, 2H), 0.71 (br d, J=12.3 Hz, 1H). LCMS: RT = 1.610 min; (ES): m/z (M+H)+= 656.10, LCMS: Column: Waters Acquity UPLC BEH C18, 2.1 x 50 mm, 1.7-mutaueta particles; Mobile Phase A: 5:95 ACN:water with 10 mM NH4OAc; Mobile Phase B: 95:5 ACN:water with 10 mM NH4OAc; Temperature: 50 C; Gradient: 0-100% B over 3 min, then a 0.75-min hold at 100% B; Flow: 1.11 mL/min. HPLC Purity at 220 nm: 97 %

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

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

2-Cyanoimino-1,3-thiazolidine, cas is 26364-65-8, it is a common heterocyclic compound, the thiazolidine compound, 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.

26364-65-8 is used more and more widely, we look forward to future research findings about 2-Cyanoimino-1,3-thiazolidine

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

Name is 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 7025-19-6, its synthesis route is as follows.,7025-19-6

General procedure: A solution of 0.002 mol of rhodanine in 5 mL of ethanol and 0.05 mL of 2-aminoethanol were added to a solution of 0.002 mol of aldehyde 1 in 5 mL of ethanol. The mixture was refluxed for 2-3 h and cooled. The precipitate was filtered off and recrystallized.

With the complex challenges of chemical substances, we look forward to future research findings about 3-(4-Oxo-2-thioxothiazolidin-3-yl)propanoic acid

Reference£º
Article; Sinenko; Slivchuk; Pil?o; Raenko; Brovarets; Russian Journal of General Chemistry; vol. 86; 7; (2016); p. 1597 – 1603; Zh. Obshch. Khim.; vol. 86; 7; (2016); p. 1119 – 1125,7;,
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

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]+.

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

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

Name is 3-Aminorhodanine, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 1438-16-0, its synthesis route is as follows.,1438-16-0

General procedure: General procedure for synthesis of N-substituted-rhodanine derivatives RhAs: To a solution of aldehydes (3a-3h, 1.0 equiv.) in ethanol (10 mL) was added slowly to the solution of 3-amino-2-thioxothiazolidin-4-one (2, 1.0 equiv.) in EtOH. The reaction mixture was stirred at room temperature without a catalyst for between 4 h and 12 h, and was monitored by TLC. After, the mixture product was recrystallized from EtOH. After recrystallization, N-substituted-rhodanine derivatives (RhAs) were obtained as follows.

With the complex challenges of chemical substances, we look forward to future research findings about 3-Aminorhodanine

Reference£º
Article; Bayindir; Caglayan, Cuneyt; Karaman, Muhammet; Guelcin, ?lhami; Bioorganic Chemistry; vol. 90; (2019);,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

2-Cyanoimino-1,3-thiazolidine, cas is 26364-65-8, it is a common heterocyclic compound, the thiazolidine compound, its synthesis route is as follows.

General procedure: In a 100 ml three-necked flask equipped with a thermometer and an electromagnetic stir bar were added 0.01 mol of anhydrous K2CO3 powder, 0.01 mol of 2-nitroaniline,30 ml of acetone,A solution prepared by dissolving 0.01 mol of 1,3-dimethyl-4-pyrazolecarboxylic acid chloride in 20 ml of acetone was gradually added dropwise at low temperature (0 to 5 C), and the reaction was continued at room temperature for 10 hours. The reaction mixture was filtered under reduced pressure, and the resulting filtrate was decompressed to yield a crude product of compound Q110907. The crude product of compound Q110907 was recrystallized from acetonitrile to give the compound (Q110907) in a yield of 42.9%. Using Thiazoline-2-imino-cyanamide instead of 2-nitroaniline; Acetonitrile was used as the reaction solvent; reaction temperature was 45 ¡À 5 C; reaction time was 8 hours; toluene recrystallization, 26364-65-8

With the rapid development of chemical substances, we look forward to future research findings about 2-Cyanoimino-1,3-thiazolidine

Reference£º
Patent; Qingdao Agricultural University; sun, Jia Long; (11 pag.)CN103524417; (2016); B;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO331,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

A sealed tube was charged with 4-iodobenzonitrile (0.50 g, 2.2 mmol), 1 ,2-thiazolidine 1 , 1- dioxide (1.2 equiv.; 0.32 g, 2.6 mmol), dimethylethylenediamine (0.1 equiv., 0.23 mL, 0.22 mmol), cesium fluoride (2.5 equiv., 0.83 g, 5.47 mmol), copper iodide (0.05 equiv., 0.02 g, 0.10 mmol), tetrahydrofuran (4.7 mL) and the reaction contents were stirred at room temperature for 24 hours. The reaction contents were diluted with ethyl acetate and a saturated aqueous ammonium chloride solution. The layers were separated and the organic fraction was washed with water, dried over sodium sulfate, and concentrated under reduced pressure. The corresponding crude yellow oil (449 mg) was taken up in the next step without additional purification or characterization. (0600) NMR (400 MHz, CDCIs) delta ppm: 7.85 (d, 2H), 7.30 (d, 2H), 3.82 (t, 2H), 3.28 (t, 2H), 3.30 (m, 2H).

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; SYNGENTA PARTICIPATIONS AG; HOFFMAN, Thomas, James; STIERLI, Daniel; POULIOT, Martin; BEAUDEGNIES, Renaud; (96 pag.)WO2017/93348; (2017); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

Name is Thiazolidine hydrochloride, as a common heterocyclic compound, it belongs to thiazolidine compound, and cas is 14446-47-0, its synthesis route is as follows.,14446-47-0

N-t-Butyloxycarbonylglutamine (2.0 g, 8.12 mmol) was dissolved in THF (5 mL) and cooled TO-15C. CAIBE (ISOBUTYLCHLOROFORMATE) (1.06 mL, 8.12 mmol) and 4- METHYLMORPHOLINE (0.895 mL, 8.12 mmol) were added and the solution stirred for 15 min, The formation of the mixed anhydride was checked by TLC (eluent: CHCL3/MEOH : 9/1). After warming to-10C another equivalent of 4-methylmorpholine (0.895 mL, 8.12 mmol) and THIAZOLIDINEHYDROCHLORIDE (1.02 g, 8. 12 mmol) was added. The mixture was brought to room temperature and stirred overnight. The sediment FORMED was filtered off and the solvent was evaporated. The resulting oil was taken up in chloroform (20 ml) and washed with a saturated solution of sodium hydrogensulfate followed by a saturated solution of sodium bicarbonate, water and brine. The organic layer was separated, dried and evaporated. The resulting product was checked for purity by TLC (eluent: CHC13/MEOH : 9/1). Yield: 1.64 g. A portion of this product (640 mg) was dissolved in 3.1 mL ice cold HCl in dioxane (12.98 M, 20 equivalents) and left on ice. The progress of the reaction was monitored by TLC (eluent: CHCL3/MEOH : 9/1). After completion of the reaction the solvent was removed and the resulting residue was taken up in methanol and evaporated again. The resulting oil was dried over phosphorous-V-oxide and triturated twice with diethylether to give the title compound (0.265 g). The purity was checked by HPLC. The identity of the reaction product was checked by NMR analysis.

With the complex challenges of chemical substances, we look forward to future research findings about Thiazolidine hydrochloride

Reference£º
Patent; PROSIDION LTD.; WO2005/20983; (2005); A2;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO343,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

Under a nitrogen atmosphere, a solution of 5-bromo-6-chloro- pyridine-2-carboxylic acid methyl ester (Example 9 c, lg, 4 mmol), isothiazolidine 1 , 1 -dioxide (730 mg, 06 mmol), copper(I) iodide (150 mg, 0.8 mmol), l ,3-di(pyridin-2-yl)propane-l ,3-dione (CAN 10198- 89-7, 180 mg, 0.8 mmol) and potassium carbonate (1.1 g, 8 mmol) in DMF (20 mL) was reacted for 24 h at 1 10C. The reaction mixture was poured into water, and extracted with ethyl acetate (3 x 50 mL). The combined organic extracts were washed with water and brine, dried over anhydrous sodium sulfate and evaporated. The residue was purified by column chromatography (silica gel, 4 g, 10% ethyl acetate in petroleum ether) to yield the title compound (0.048 g, 1.6 mmol, 41.4 %) as yellow solid; MS (EI): m/e = 291.0[M+Hf.

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; F. HOFFMANN-LA ROCHE AG; BISSANTZ, Caterina; GRETHER, Uwe; HEBEISEN, Paul; KIMBARA, Atsushi; LIU, Qingping; NETTEKOVEN, Matthias; PRUNOTTO, Marco; ROEVER, Stephan; ROGERS-EVANS, Mark; SCHULZ-GASCH, Tanja; ULLMER, Christoph; WANG, Zhiwei; YANG, Wulun; WO2012/168350; (2012); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com