Heterocyclic Building Blocks-Isothiazole

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

To a solution of isothiazole (5.0 g, 58.82 mmol) in AcOH (37 mL) was added Br2 (12.5 g, 78.12 mmol) dropwise at 95 oC over 20 min and the mixture was stirred for 6 h at 95 oC, then cooled to RT, and poured into ice water (100 mL). The resulting mixture was extracted with Et2O (200 mL x 2). The organic phases were washed with 6N NaOH to pH at 7~8, dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated in vacuo, and the resulting residue was purified by distillation to afford 4-bromoisothiazole as a white solid (1.5 g, 15%)., 288-16-4

The synthetic route of 288-16-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GREENLEE, William, J.; GOOD, Andrew, C.; (309 pag.)WO2017/176961; (2017); A1;,
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87691-88-1, 3-Piperazinobenzisothiazole hydrochloride is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,87691-88-1

EXAMPLE 6 3-[3-{2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]ethyl}-5-(2-{[(4-chlorophenyl)sulphonyl]amino}ethyl)-1H-indol-1-yl]propanoic Acid The expected product is obtained according to the procedure described in Example 1, with the replacement of 4-(4-fluorobenzoyl)piperidinium tosylate with 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride in Step b.

The synthetic route of 87691-88-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Lavielle, Gilbert; Cimetiere, Bernard; Verbeuren, Tony; Simonet, Serge; Vayssettes-Courchay, Christine; US2003/109533; (2003); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27148-03-4,Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide,as a common compound, the synthetic route is as follows.

General procedure: For 6: A solution of thiosaccharin (tsacH) (0.06 g, 0.307 mmol) in chloroform (8 cm3) was added to a solution of [PtCl2(kappa2-dppm)] (0.10 g, 0.154 mmol) in chloroform (10 cm3). A few drops of triethylamine were added and the resulting mixture was heated under reflex for 1 h. This produced a yellow solution was filtered off and reduced to half volume. Methanol (2 cm3) was added and the mixture was set a side to evaporate slowly at room temperature. The yellow crystalline solid thus formed was filtered off and dried in a vacuum oven (0.12 g, 91%).

27148-03-4, As the paragraph descriping shows that 27148-03-4 is playing an increasingly important role.

Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4576-90-3,Isothiazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

To a slurry of isothiazole-3-carboxylic acid (5.0 g, 38.7 mmol) in tert-butanol (194 mL) was added triethylamine (4.3 g, 42.6 mmol) followed by diphenyl phosphoryl azide (11.9 g, 43.3 mmol). The reaction mixture was heated to reflux for 9 h. After cooling the ambient temperature, the reaction mixture was concentrated in vacuo and the residue dissolved in ethyl acetate (300 mL). The organic layer was washed with water (100 mL), 1 N sodium hydroxide solution (50 mL), water (100 mL), brine (50 mL), and dried over anhydrous magnesium sulfate. Filtration and concentration of the filtrate in vacuo afforded a residue. Purification of the residue by column chromatography, eluting with a gradient of 0 to 10% of ethyl acetate in heptane, provided the title compound as a colorless solid (6.16 g, 79% yield): 1H NMR (300 MHz, CDCl3) delta9.03-8.98 (m, 1H), 8.58 (d, J=4.9 Hz, 1H), 7.70 (d, J=4.9 Hz, 1H), 1.53 (d, J=0.7 Hz, 9H).

4576-90-3, The synthetic route of 4576-90-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Xenon Pharmaceuticals Inc.; Andrez, Jean-Christophe; Bogucki, David Earl; Burford, Kristen Nicole; Chowdhury, Sultan; Cohen, Charles Jay; Decker, Shannon Marie; Dehnhardt, Christoph Martin; Devita, Robert Joseph; Empfield, James Roy; Focken, Thilo; Grimwood, Michael Edward; Hasan, Syed Abid; Jia, Qi; Johnson, JR., James Philip; Wilson, Michael Scott; Zenova, Alla Yurevna; (287 pag.)US2018/162868; (2018); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4576-90-3,Isothiazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 500 mg (3.87 mmol) of isothiazol-3-carboxylic acid (Apollo Scientific), 415 mg (4.25 mmol) of N,O-dimethylhydroxylamine hydrochloride and 30 mg (0.196 mmol) of 1-hydroxybenzotriazole monohydrate in methylene chloride (20 ml) were added 2.7 mL (15.46 mmol) of diisopropylamine and 1.49 g (7.77 mmol) of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide under an argon atmosphere, and the mixture was stirred at room temperature for 21 hours. After completion of the reaction, to the reaction mixture was added water, and the mixture was extracted with ethyl acetate. The resulting organic layer was washed sequentially with water and saturated brine, subsequently dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The resulting residue was subjected to silica gel column chromatography (elution solvent; hexane:ethyl acetate = 90:10 to 60:40 (V/V)), and the fractions containing the desired compound were concentrated under reduced pressure to obtain 598 mg (3.47 mmol, yield 90%) of the title compound as a colorless oil Mass spectrum (EI, m/z): 172 [M]+. 1H-NMR spectrum (400 MHz, CDCl3) delta : 8.68 (1H, d, J = 4.6 Hz), 7.69 (1H, d, J = 4.0 Hz), 3.81 (3H, s), 3.47 (3H, brs).

4576-90-3, As the paragraph descriping shows that 4576-90-3 is playing an increasingly important role.

Reference£º
Patent; UBE Industries, Ltd.; IWASE, Noriaki; NISHIDA, Hiroshi; OKUDO, Makoto; ITO, Masaaki; KONO, Shigeyuki; MATOYAMA, Masaaki; USHIYAMA, Shigeru; OKANARI, Eiji; MATSUNAGA, Hirofumi; NISHIKAWA, Kenji; KIMURA, Tomio; EP2940013; (2015); A1;,
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24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 190Preparation of 1-Isothiazol-4-yl-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (190A) 1-(4-Methyl-pyridin-3-yl)-imidazolidin-2-one (I-14b: 150 mg, 0.847 mmol) was reacted with 4-bromo-isothiazole (166 mg, 1.016 mmol), 1,4-dioxane (15 mL), copper iodide (16.09 mg, 0.0847 mmol), trans-1,2-diamino cyclohexane (29 mg, 0.254 mmol) and potassium phosphate (540 mg, 2.541 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in CHCl3) afforded 120 mg of the product (54.54% yield).1H NMR (CDCl3, 300 MHz): delta 8.82 (s, 1H), 8.65-8.25 (m, 3H), 7.4-7.1 (m, 1H), 4.20-3.95 (m, 4H), 2.19 (s, 3H)LCMS purity: 97.95%, m/z=261.0 (M+1)HPLC: 96.08%

24340-77-0, 24340-77-0 4-Bromoisothiazole 5200358, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Novartis AG; US2010/331326; (2010); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

In a pressure-resistant Schlenk tube, copper fluoride (0.05 mmol) was charged,The system was evacuated and replaced with argon three times,Under gas protection,The isothiazole (. 5 mmol) was added sequentially with a micro-injector,Tert-butylperoxybenzoyl (2 mmol),And chlorobenzene (2 ml),The system was then sealed and heated at 130 C in an oil bath for 24 hours,After completion of the reaction, the solvent was distilled off under reduced pressure,The product N-methylisothiazolin-2-one (46 mg) was obtained by a simple column chromatography (eluent using a mixed solvent of petroleum ether (60 to 90 C) and ethyl acetate)The yield was 80%., 288-16-4

288-16-4 Isothiazole 67515, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; SUZHOU BOFEITE NEW MATERIALS TECHNOLOGY CO., LTD; Mao, jincheng; Wang, Ping; (7 pag.)CN103965136; (2016); B;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.87691-88-1,3-Piperazinobenzisothiazole hydrochloride,as a common compound, the synthetic route is as follows.

87691-88-1, EXAMPLE 75 3-[4-[1-(1,2-Benzisothiazol-3-yl)-4-piperazinyl]butyl]-1-thia-3-azaspiro[4.4]nonan-4-one A mixture of 3-(4-bromobutyl)-1-thia-3-azaspiro[4.4]-nonan-4-one (4.50 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (4.33 g), K2 CO3 (7.45 g) and NaI (560 mg), in acetonitrile (220 ml) was heated at 65 C. for 14.5 hours and the product was processed in substantially the same manner as in Example 10 to afford 2.25 g of crystals, m.p. 200-203 C. ANALYSIS: Calculated for C22 H30 N4 OS2 ¡¤HCl: 56.57%C; 6.69%H; 11.99%N; 7.59%Cl. Found: 56.15%C; 6.75%H; 12.11%N; 7.88%Cl.

87691-88-1 3-Piperazinobenzisothiazole hydrochloride 11521711, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Incorporated; US5229388; (1993); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.936-16-3,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide,as a common compound, the synthetic route is as follows.

936-16-3, General procedure: Potassium carbonate was dissolved in DMF, and 1,2-bezeneisothiazolin-1,1-dioxide (8) (1 equiv.) in dichloromethanewas added to the reaction solution, and stirred for overnight. Then,the reaction mixture was filtered through Celite, and washed with1 N HCl and saturated sodium hydrogen carbonate solution. Residualsolution was dried over magnesium sulfate, and concentratedin vacuo, and purified by column chromatography to afford the titlecompound.

As the paragraph descriping shows that 936-16-3 is playing an increasingly important role.

Reference£º
Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
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10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The target compounds were synthesized using the procedure given in literature by refluxing aryl/heteroaryl acids with carbohydrazide 4a or 4b in phosphorous oxychloride. The reaction was monitored with the help of TLC to check its completion. After completion of reaction, the mixture was poured over crushed ice and allowed to precipitate. The precipitate was vacuum filtered, dried and recrystallized from methanol. Column chromatography was done on using n-hexane: ethylacetate mixture (7:3). Solvent was evaporated invacuo using rotary evaporator to obtain pure product.

10271-85-9, 10271-85-9 Isothiazole-5-carboxylic acid 5200404, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Article; Rane, Rajesh A.; Bangalore, Pavankumar; Borhade, Sheetal D.; Khandare, Preeti K.; European Journal of Medicinal Chemistry; vol. 70; (2013); p. 49 – 58;,
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