Tag: M.W:100-200

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO419,mainly used in chemical industry, its synthesis route is as follows.,5908-62-3

To a solution of 6-(6-fluoro-4-iodo-2-pyridyl)-5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H- pyrido[4,3-d]pyrimidine (the product of step 1 in Example 96, 100 mg, 223 muiotaetaomicron) in dioxane ( 3mL) was added isothiazolidine-1,1-dioxide (54.1 mg, 446 muiotaetaomicron), cesium carbonate (145 mg, 446 muetaiotaomicron), Xantphos (25.8 mg, 44.6 muetaiotaomicron) and Pd(OAc)2(5.01 mg, 22.3 muetaiotaomicron). After being heated at 100 C with stirring for 20 hrs under argon, the resulting reaction mixture was then filtered and the filtrate was concentrated in vacuo. The residue was purified by prep-HPLC to give 2-[2-fluoro-6-(5-methyl-2-pyrimidin-2-yl-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl)-4- pyridyl]-1,2-thiazolidine-1,1-dioxide (8 mg) as a light yellow solid. 1H NMR (400MHz, DMSO- d6) delta ppm: 8.99 (d, 2H), 8.95 (s, 1H), 7.64 (t, 1H), 6.32 (s, 1H), 6.15 (s, 1H), 5.69-5.64 (m, 1H), 4.47-4.36 (m, 1H), 3.89 – 3.79 (m, 2H), 3.68-3.59(m, 2H), 3.54 – 3.43 (m, 1H), 3.14 – 2.98 (m, 2H), 2.42-2.37 (m, 2H), 1.52 (d, 3H). MS obsd (ESI) [(M+H)+]: 442.

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; HOFFMANN-LA ROCHE INC.; CHENG, Zhanling; HAN, Xingchun; JIANG, Min; WANG, Jianhua; WANG, Yongguang; YANG, Song; (211 pag.)WO2018/1952; (2018); A1;,
Thiazolidine – Wikipedia
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As a common heterocyclic compound, it belongs to thiazolidine compound, name is (R)-2-Oxothiazolidine-4-carboxylic acid, and cas is 19771-63-2, its synthesis route is as follows.,19771-63-2

EXAMPLE 17 (4R)-N-[1-(Nitrooxymethyl)ethyl]-2-oxothiazolidine-4-carboxamide (Compound No. 1-30) A procedure similar to that described in Example 1 was repeated, but using 1.5 g of (4R)-2-oxothiazolidine-4-carboxylic acid and 2.3 g of 1-(nitrooxymethyl)ethylamine nitrate, to obtain 0.35 g of the title compound as colorless crystals, melting at 112-114 C. (after recrystallization from ethanol). Nuclear Magnetic Resonance Spectrum (CDCl3 +hexadeuterated dimethyl sulfoxide) delta ppm: 1.27 (3H, doublet, J=7 Hz); 3.68 (2H, doublet, J=7 Hz);

With the rapid development of chemical substances, we look forward to future research findings about (R)-2-Oxothiazolidine-4-carboxylic acid

Reference£º
Patent; Sankyo Company, Limited; US5298516; (1994); A;,
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: C8H14ClNO227,mainly used in chemical industry, its synthesis route is as follows.,1438-16-0

General procedure: O-phenylenediamines (0.065 mol) was heated with N-aminorhodanine (0.065 mol) in xylene (50 ml) for 5 hours. The obtained residue was filtered and was crystallized from aqueous alcohol (charcoal). The obtained solid was recrystallized in ethanol. 2-mercaptobenzimidazole 3a Yield = 87 %; mp>250 C.1HNMR (DMSO-d6): 7.10 (m, 2Har); 7.27 (m, 2Har); 12.42 (s,NH).13CNMR (DMSO-d6): 119.43 (CH); 126.36 (CH); 138.82 (C); 167.12 (C=S). HRMS, m/z: 150(M), calcd for C7H6N2S: 150.02517, found: 150.0251.

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

Reference£º
Article; El Kihel; Ait Sir; Jebbari; Ahbala; Guesmi; Bauchat; Oriental Journal of Chemistry; vol. 32; 4; (2016); p. 1765 – 1768;,
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: A mixture of aminorhodanine (1 mmol), isatin (1 mmol) and 5 muL of acetic acid in 2mL of distilled ethanol was placed in a cylindrical quartz reactor (Phi = 4 cm). The reactor was introducedinto a monomode microwave (Anton Paar) apparatus, for 5 min at100 C and 50 Watts. The crude reaction mixture was allowed tocool down at room temperature and ethanol (10 mL) or mixture of H2O/EtOH (10 mL) was directly added in the cylindrical quartzreactor. The resulting precipitated product was filtered off and waspurified by recrystallization from ethanol if necessary.

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

Reference£º
Article; Khaldoun, Khadidja; Safer, Abdelmounaim; Boukabcha, Nourdine; Dege, Necmi; Ruchaud, Sandrine; Souab, Mohamed; Bach, Stephane; Chouaih, Abdelkader; Saidi-Besbes, Salima; Journal of Molecular Structure; vol. 1192; (2019); p. 82 – 90;,
Thiazolidine – Wikipedia
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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

108371 To a solution of isothiazolidine 1,1-dioxide (500 mg, 4.13 mmol) in acetonitrile (10 mL) was added potassium carbonate (1.14 g, 8.25 mmol), 4-methoxybenzyl chloride (646 mg, 4.13 mmol). The mixture was heated to 80 C for 12 h under nitrogen atmosphere. The mixture was poured into H20 (50 mL) and extracted with ethyl acetate (50 mL). The organic layer was washed with H20 (50 mL x 2) and saturated brine solution (50 mL). The organic layers was dried over anhydrous sodium sulfate, filtered and concentrated in vacuo. The residue was purified via flash silica chromatography (solvent gradient: 0-40% ethyl acetate in petroleum ether) to yield 1.0 g (99% yield) of the title compound as a white solid. ?H NMR (400 MHz, CDC13) oe 7.28 (d, J= 8.4 Hz, 2H), 9.89 (d, J= 8.8 Hz, 2H), 4.13 (s, 2H), 3.82 (s, 3H), 3.23 – 3.18 (t,J= 8.8 Hz, 2H), 3.12-3.07 (m, 2H), 2.34-2.25 (m, 2H).

5908-62-3 is used more and more widely, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

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

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

A solution of 3,5-dibromo-2-hydroxybenzaldehyde (104 mg, 0.371 mmol) in methanol (1 ML) was added to a solution of 3-aminorhodanine (50 mg, 0.337 mmol) in methanol (5 ML) and the mixture allowed to stand at room temperature.. After 1 h, the precipitate was filtered, washed (methanol, ether) and dried to give the title compound (93 mg, 67%) as a pale yellow solid. LCMS m/e 409, 411, 413 [M+H]+.

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

Reference£º
Patent; SmithKline Beecham Corporation; US6720345; (2004); B1;,
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

Example 98 Preparation of Intermediate 100 [0785] [0786] To 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. The reagents were suspended in 8 mL of anhydrous dioxane and mixture was heated at 100 C. overnight. After cooling to room temperature, the reaction mixture was filtered, washing with ethyl acetate. The 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 100 (322 mg, 78%) as a yellow off-white solid. [0787] 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). [0788] LCMS m/z [M+H]+ C12H15NO4S requires: 270.07. Found 270.12.

5908-62-3 is used more and more widely, we look forward to future research findings about 1,1-Dioxo-isothiazolidine

Reference£º
Patent; Siegel, Dustin; Sperandio, David; Yang, Hai; Sangi, Michael; Parrish, Jay P.; Hui, Hon Chung; US2013/273037; (2013); A1;,
Thiazolidine – Wikipedia
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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 solution of 3-iodo-N-(3,4,5-trifluorophenyl)-4,5,6,7-tetrahydropyrazolo[l,5- a]pyridine-5-carboxamide (compound lh, 20 mg, 0.048 mmol) in DMSO (1.0 mL) was added Cul (2 mg, 0.0095 mmol), K2C03 (7 mg, 0.095 mmol), N,N’-dimethyl-l,2-cyclohexanediamine (2 mg, 0.0095 mmol), and 1,2-thiazolidine 1,1-dioxide (compound 5a, 5 mg, 0.057 mmol). The reaction mixture was stirred at 110 C for 18 hours and then purified by flash chromatography and prep-HPLC to give 3-(l,l-dioxo-l,2-thiazolidin-2-yl)-N-(3,4,5-trifluorophenyl)-4,5,6,7- tetrahydropyrazolo[l,5-a]pyridine-5-carboxamide (Example 5, 11.5 mg) as a white solid. 1H NMR (400MHz, CDC13) delta 8.21 (s, 1H), 7.56 (s, 1H), 7.41 – 7.26 (m, 2H), 4.27 – 4.14 (m, 1H), 4.07 (m, 1H), 3.73 – 3.54 (m, 2H), 3.36 (t, 2H), 3.25 – 3.08 (m, 2H), 2.84 – 2.72 (m, 1H), 2.60 – 2.39 (m, 3H), 2.34 – 2.21 (m, 1H). MS obsd. (ESI+) [(M+H)+]: 415

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

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HU, Taishan; SHEN, Hong; HAN, Xingchun; (45 pag.)WO2018/11100; (2018); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com

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

General procedure: O-phenylenediamines (0.065 mol) was heated with N-aminorhodanine (0.065 mol) in xylene (50 ml) for 5 hours. The obtained residue was filtered and was crystallized from aqueous alcohol (charcoal). The obtained solid was recrystallized in ethanol.

With the complex challenges of chemical substances, we look forward to future research findings about 1438-16-0,belong thiazolidine compound

Reference£º
Article; El Kihel; Ait Sir; Jebbari; Ahbala; Guesmi; Bauchat; Oriental Journal of Chemistry; vol. 32; 4; (2016); p. 1765 – 1768;,
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

1,2-thiazolidine 1,1-dioxide (0.031 g, 0.259 mmol) in dimethylformamide (1 mL) was treated with 60% sodium hydride (0.012g, 0.518 mmol, 0.021 g of a 60%> in oil dispersion). The reaction mixture was stirred for 5 min. To this solution was added Example 41b (0.05 g, 0.086 mmol). The reaction mixture was stirred at room temperature for 2 hours. 2 N NaOH (1 mL) was added and the reaction mixture was heated at 65 C for 2 hours. After cooling to room temperature, the reaction mixture was partitioned between water and ethyl acetate. The aqueous layer was extracted with additional ethyl acetate twice. The combined organic layers were washed with brine, dried over MgSC^, filtered, and concentrated. The residue was purified by preparative HPLC (CI 8, 10-80% acetonitrile in 0.1% TFA water) to afford 0.025 g (64%) of the title compound. 1H NMR (500 MHz, DMSO-d6) delta 2.21-2.25 (m, 2H), 3.15 (t, J=6.97 Hz, 2H), 3.23-3.27 (m, 2H), 3.50 (s, 3H), 4.13 (s, 2H), 6.25-6.26 (m, 1H), 6.88 (d, J=7.63 Hz, 2H), 7.00 (d, J=8.54 Hz, 1H), 7.03-7.05 (m, 1H), 7.25-7.30 (m, 4H), 7.34 (dd, J=8.39, 2.29, 1H), 7.48 (d, J=2.44 Hz, 1H), 12.00 (s, 1 H). MS (ESI+) m/z 450.2 (M+H)+.

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

Reference£º
Patent; ABBVIE INC.; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; WANG, Le; PRATT, John K.; MCDANIEL, Keith F.; DAI, Yujia; FIDANZE, Steven D.; HASVOLD, Lisa; HOLMS, James H.; KATI, Warren M.; LIU, Dachun; MANTEI, Robert A.; MCCLELLAN, William J; SHEPPARD, George S.; WADA, Carol K.; WO2013/97601; (2013); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com