New learning discoveries about 288-16-4

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

To a solution of isothiazole (A.157) (3.0 g, 35.3 mmol) in 50 mL THF at -78 0C under argon was added n-butyllithium (1.6 M in hexane, 22.1 mL, 35.3 mmol) dropwise over 10 minutes. The mixture stirred at -780C for 1.5 hours. A solution of 2-fluoro-5-iodobenzaldehyde (A.156)(7.35 g, 29.4 mmol) in 30 mL THF was added dropwise over 15 minutes, and the reaction stirred an additional 2 hours at -78 0C. Water was added to quench the reaction, and the mixture warmed to 0 0C. The solution was neutralized with 2 N HCl to pH 7, partitioned between water and dichloromethane, and the aqueous layer further extracted with dichloromethane. The combined organic extracts were washed with brine, dried over MgSO4 and condensed. Purification by flash chromatography (0-15-100% ethyl acetate in hexane) gave 7.19 g (2- fluoro-5-iodophenyl)(isothiazol-5-yl)methanol A.158. IH NMR (500 MHz, CHLOROFORM- d) delta ppm 8.30 (1 H, s), 7.76 (1 H, dd, J=6.8, 2.2 Hz), 7.56 (1 H, ddd, J=8.6, 5.0, 2.3 Hz), 6.97 (1 H, s), 6.79 (1 H, dd, J=9.8, 8.8 Hz), 6.37 (1 H, s)

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

Reference£º
Patent; AMGEN INC.; WO2009/158011; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

The important role of 288-16-4

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

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

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).

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

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

 

Downstream synthetic route of Isothiazole

With the synthetic route has been constantly updated, we look forward to future research findings about Isothiazole,belong isothiazole compound

As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO460,mainly used in chemical industry, its synthesis route is as follows.,288-16-4

Under nitrogen, compound l (20 g, 0.235 mol)Add 100 ml of dry ether to dry,Then cool down to below 0 C,To this was added n-butyllithium (0.24mo 1)During the dropping process, it is kept below 0 C,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)During the dropping process, it is kept below 0 C,After the dropwise addition, slowly raise to room temperature,After stirring for half an hour, the reaction was quenched by the addition of hydrochloric acid solution (2N, 500 ml).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 synthetic route has been constantly updated, we look forward to future research findings about Isothiazole,belong isothiazole compound

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890178; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

New learning discoveries about 288-16-4

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

EXAMPLE 15 6-Cyano-1-hydroxy-1-(5-isothiazolyl)-1,2,3,4-tetrahydronaphthalene Analogously to Example 12, the crude title compound is obtained starting from 353 mg of isothiazole, 0.632 ml of diisopropylamine, 3 ml of 1.6M n-butyllithium in hexane and 546 mg of 6-cyano-1-tetralone in 38 ml of THF. It is purified by column chromatography (SiO2, hexane/ethyl acetate 4:1) and crystallisation from hexane; m.p. 182-184; 1 H-NMR (d6 -DMSO): delta(ppm)=1.76 and 1.97 (2m,4H), 2.9 (t,2H), 6.65 (s,1H), 6.93 (d,1H), 7.37 (dd,1H), 7.59 (dd,1H), 7.7 (d,1H), 8.39 (d,1H).

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

 

Share a compound : 288-16-4

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

Compound l (20 g, 0.235 mol) was added under stirring with nitrogen to dry 100 ml of ether and stirred to dissolve,Then cooled to below 0 C, to which n-butyllithium (0.24mo 1) was added dropwise,During the dropwise addition, the reaction was kept below 0 C and the incubation was completed until the compound 1 was added.To the reaction solution was added bromine (0.5 mol)Dropping the process to maintain the following 0 C, drop out after the completion of slowly rose to room temperature,After stirring for half an hour, the reaction was quenched by the addition of hydrochloric acid solution (2N, 500 ml).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.[0188] 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.

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890181; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Brief introduction of 288-16-4

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

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

288-16-4, Compound 1 (20 g, 0.235 mol) was added under stirring with nitrogen to dry 100 ml of ether and stirred to dissolve,And then cooled to below 0 ,To this was added n-butyllithium (0.24 mol)During the dropping process, the temperature was kept below 0 C,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)During the dropping process, the temperature was kept below 0 C,After the dropwise addition, slowly raise to room temperature,After stirring for half an hour, the reaction was quenched by the addition of hydrochloric acid solution (2N, 500 ml).The aqueous phase was extracted with ether (200 ml * 3) and discarded.The combined organic phase, sodium dithionite solution (100 ml * 2)Dried over anhydrous sodium sulfate, filtered and concentrated to dryness,A yellow oily compound was prepared.

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

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Ge Yu; Li Yanfeng; (38 pag.)CN106892911; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Brief introduction of 288-16-4

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

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

Under a nitrogen atmosphere, compound 1 (20 g, 0.235 mol)Add 100 ml of dry ether to dry,And then cooled to below 0 ,To this was added n-butyllithium (0.24 mol)During the dropping process, the temperature was kept below 0 C,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)During the dropping process, the temperature was kept below 0 C,After the dropwise addition, slowly raise to room temperature,After stirring for half an hour, the reaction was quenched by the addition of hydrochloric acid solution (2N, 500 ml).Layered,The aqueous phase was extracted with ether (200 ml * 3) and discarded.Combined organic phase,Sodium dithionite solution(100 ml * 2),Dried over anhydrous sodium sulfate,Filtered and concentrated to dry,A yellow oily compound was prepared.In this step, the ether can also be treated with methyl ether, dimethyl ether, tetrahydrofuran,1,4-dioxane and other solvents instead.

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; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (33 pag.)CN106890139; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

New learning discoveries about 288-16-4

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

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).

With the rapid development of chemical substances, we look forward to future research findings about Isothiazole

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

 

New learning discoveries about 288-16-4

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

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 (A.157) (3.0 g, 35.3 mmol) in 50 mL THF at -78 0C under argon was added n-butyllithium (1.6 M in hexane, 22.1 mL, 35.3 mmol) dropwise over 10 minutes. The mixture stirred at -780C for 1.5 hours. A solution of 2-fluoro-5-iodobenzaldehyde (A.156)(7.35 g, 29.4 mmol) in 30 mL THF was added dropwise over 15 minutes, and the reaction stirred an additional 2 hours at -78 0C. Water was added to quench the reaction, and the mixture warmed to 0 0C. The solution was neutralized with 2 N HCl to pH 7, partitioned between water and dichloromethane, and the aqueous layer further extracted with dichloromethane. The combined organic extracts were washed with brine, dried over MgSO4 and condensed. Purification by flash chromatography (0-15-100% ethyl acetate in hexane) gave 7.19 g (2- fluoro-5-iodophenyl)(isothiazol-5-yl)methanol A.158. IH NMR (500 MHz, CHLOROFORM- d) delta ppm 8.30 (1 H, s), 7.76 (1 H, dd, J=6.8, 2.2 Hz), 7.56 (1 H, ddd, J=8.6, 5.0, 2.3 Hz), 6.97 (1 H, s), 6.79 (1 H, dd, J=9.8, 8.8 Hz), 6.37 (1 H, s)

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

Reference£º
Patent; AMGEN INC.; WO2009/158011; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Some tips on 288-16-4

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

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.

Compound 1 (20 g, 0.235 mol) was added to dry 100 ml of diethyl ether under nitrogen atmosphere and stirred to dissolve,And then cooled to 0 C or lower, n-butyllithium (0.24 mol) was added dropwise thereto, and the temperature was kept below 0 C during the dropwise addition, and the reaction was carried out until the compound 1 was added.To the reaction solution was added bromine (0.5 mol), and the mixture was kept at 0 C or less during the dropping,After completion of the dropwise addition, the temperature was gradually raised to room temperature, and after stirring for half an hour, the hydrochloric acid solution was added thereto(2N, 500 ml).And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The combined organic phase and sodium dithionite solution were washed(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., 288-16-4

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

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890177; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com