Category: 288-16-4

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;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

Isothiazole, cas is 288-16-4, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,288-16-4

Under nitrogen protection, compound 1 was added(20 g, 0.235 mol) was added to dry 100 ml of ether and stirred and dissolvedTemperature below 0 ,To this was added n-butyllithium (0.24 mol), and the mixture was kept at 0 C or less during the dropping,After the dropwise addition, the incubation reaction was carried out until no compound 1 was added.To the reaction solution was added bromine (0.5 mol)The reaction mixture was kept at 0 C or lower, and the mixture was slowly added to the room temperature after completion of the dropwise addition. After stirring for half an hour, the reaction was quenched by adding hydrochloric acid solution (2N, 500 ml) thereto.And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phase was combined and washed with sodium dithionite solution(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.

With the rapid development of chemical substances, we look forward to future research findings about 288-16-4

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890179; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, Isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 20 tert-Butyl N-allyl-N-(2-isothiazol-5-yl-2-oxo-ethyl)carbamate To a -78 C. solution of diisopropylamine (9.01 mL, 64.01 mmol) in tetrahydrofuran (80 mL) is added n-butyl lithium (30.78 mL, 49.24 mmol, 1.6 M in hexanes) drop wise under nitrogen. The resulting solution is stirred at -78 C. for 20 minutes and then a solution of isothiazole (4.19 g, 49.24 mmol) in tetrahydrofuran (10 mL) is added drop wise. The resultant white slurry is stirred for 30 minutes at -78 C. A solution of tert-butyl N-allyl-N-[2-(methoxy(methyl)amino)-2-oxo-ethyl]carbamate (6.36 g, 24.62 mmol) in tetrahydrofuran (50 mL) is then added to the slurry over a 15 minutes period. The reaction is then stirred for 30 minutes at -78 C., warmed to ambient temperature and is stirred for 30 minutes. Saturated ammonium chloride (200 mL) is then added. The resulting solution is extracted three times with ethyl acetate. The combined organic layers are dried over sodium sulfate, filtered, and concentrated under vacuum. The crude product is purified over silica gel with a 35 minute, 5% to 100% ethyl acetate in hexanes gradient, to give the title compound (6.00 g, 21.25 mmol, 86%). ES/MS (m/e): 283.0 (M+H).

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; Eli Lilly and Company; BECK, James Peter; GREEN, Steven James; LOPEZ, Jose Eduardo; MATHES, Brian Michael; MERGOTT, Dustin James; PORTER, Warren Jaye; RANKOVIC, Zoran; SHI, Yuan; WATSON, Brian Morgan; WINNEROSKI, JR, Leonard Larry; US2013/261111; (2013); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

EXAMPLE 12 6-Chloro-1-hydroxy-1-(5-isothiazolyl)-1,2,3,4-tetrahydronaphthalene Analogously to Example 1, the title compound is obtained starting from 225 mg of isothiazole, 0.51 ml of diisopropylamine, 1.87 ml of 1.6M n-butyllithium in hexane and 540 mg of 6-chloro-1-tetralone in 36 ml of THF. The crude product is purified by column chromatography (SiO2, 0.2 bar, hexane/ethyl acetate 9:1). 1 H-NMR (CDCl3): delta(ppm)=1.9-2.31 (m,4H), 2.17 (s,1H), 2.9 (t,2H), 6.83 (d,1H), 7.17 (m,3H), 8.34 (d,1H)., 288-16-4

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

Reference£º
Patent; Ciba-Geigy Corporation; US5246952; (1993); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, Isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 1 alpha,alpha-Bis(4-chlorophenyl)-5-isothiazolemethanol To a solution of 1.0 g of isothiazole in 20 ml of tetrahydrofuran were added 8.1 ml of a 1.52M solution of n-butyllithium in hexane at -78 C. The mixture was allowed to stir for 15 minutes at which time 3.2 g of 4,4′-dichlorobenzophenone were added as a solution in 25 ml of tetrahydrofuran. The reaction was allowed to warm to room temperature and was stirred for 2 hours. Twenty-five milliliters of a saturated ammonium chloride solution were added and the tetrahydrofuran was removed by evaporation. The resulting mixture was extracted three times with ethyl acetate. The combined organic extracts were washed with a saturated ammonium chloride solution, water, and a saturated sodium chloride solution, dried over magnesium sulfate and evaporated. The resulting oil was chromatographed over silica gel. The appropriate fractions were combined and evaporated resulting in an oil. Cyclohexane was added and 1.21 g of the desired title product were recovered by filtration as white crystals, m.p. 118-119.5 C. Analysis for C16 H11 Cl2 NOS: Calc.: C, 57.15; H, 3.30; N, 4.17; Found: C, 57.17; H, 3.07; N, 4.17.

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

Reference£º
Patent; Eli Lilly and Company; US4560695; (1985); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, Isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 1 (20 g, 0.235 mol) was added under stirring with nitrogen to dry 100 ml of ether and stirred and dissolvedThe temperature is 0 C or lower, n-butyllithium (0.24 mol) is added dropwise thereto, and the mixture is kept at 0 C or lower during the dropwise addition.Temperature reaction until no compound 1.To the reaction solution was added dropwise bromine (0.5 mol), and the mixture was kept below 0 C during the dropwise addition, and the mixture was gradually raised toAfter stirring for half an hour, the reaction was quenched by adding hydrochloric acid solution (2N, 500 ml) thereto.And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phase was combined and washed with sodium dithionite solution(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.

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

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (38 pag.)CN106890180; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

288-16-4, Isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 1 (20 g, 0.235 mol 1) was added to dry 100 ml of diethyl ether under stirring under nitrogen and then cooled to below 0 C, n-butyllithium (0.24 mol 1) was added dropwise thereto, 0 C or less, dropwise after completion of the incubation until no compound 1 is added.To the reaction solution was added dropwise bromine (0.5 mol), and the mixture was kept below 0 C during the dropwise addition. After the completion of the dropwise addition, the temperature was gradually raised to room temperature. After stirring for half an hour, the hydrochloric acid solution (2N, 500 ml) TheAnd the aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phase was combined and washed with sodium dithionite solution(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.In this step, the ether can also be replaced with a solvent such as methyl ether, dimethyl ether, tetrahydrofuran, 1,4-dioxane and the like.

As the paragraph descriping shows that 288-16-4 is playing an increasingly important role.

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Ge Yu; Li Yanfeng; (39 pag.)CN106892913; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

a) 5-Isothiazolecarboxylic acid was prepared from isothiazole, n-BuLi and dry ice according to the method of step a of Example 258.

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

Reference£º
Patent; Monsanto Company; US5498630; (1996); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

a) 5-Isothiazolecarboxylic acid was prepared from isothiazole, n-BuLi and dry ice according to the method of step a of Example 258.

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

Reference£º
Patent; Monsanto Company; US5498630; (1996); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com