Heterocyclic Building Blocks-Isothiazole

A common heterocyclic compound, the isothiazole compound, name is Isothiazole,cas is 288-16-4, mainly used in chemical industry, its synthesis route is as follows.,288-16-4

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

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.

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., 288-16-4

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

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

A common heterocyclic compound, the isothiazole compound, name is Isothiazole-4-carboxylic acid,cas is 822-82-2, mainly used in chemical industry, its synthesis route is as follows.,822-82-2

To a solution of 1,2-thiazole-4-carboxylic acid (10.0 g, 77.4 mmol) in methanol (200 mL) was added drop-wise thionyl chloride (8 mL) and the mixture was stirred at reflux for 2h. The mixture was cooled to RT and the solvent was evaporated to give product as brown solid (11.0 g, 99%).

As the rapid development of chemical substances, we look forward to future research findings about 822-82-2

Reference£º
Patent; VERNALIS (R&D) LIMITED; BROUGH, Paul Andrew; MACIAS, Alba; ROUGHLEY, Stephen David; WANG, Yikang; PARSONS, Rachel Jane; NORTHFIELD, Christopher John; WO2015/40425; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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, To a solution containing 3- (1-piperazinyl) -1,2_ benzisothiazole hydrochloride (100g) and potassium carbonate (136g) in acetonitrile(800ml) was added a solution of 1-chloro-4-bromo-butane (88g). Vigorous stirring mixture was refluxed for 10 hours, the solvent was distilled off pressure acetonitrile was added water (100ml) and toluene (300ml) to the reaction mixture was distilled net was effected under stirring to break up the product mixture, refluxing under stirring operation , the net after the water addition, cooling down, the suspension was filtered to give a white inorganic salts and organic salts of a mixture of the crude quaternary spiro ammonium base (267g).

As the paragraph descriping shows that 87691-88-1 is playing an increasingly important role.

Reference£º
Patent; Yantai Besten Pharmaceutical Co., Ltd.; Bi, Haidong; Zhang, Yifang; (8 pag.)CN105669665; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

A common heterocyclic compound, the isothiazole compound, name is 3-Chlorobenzo[d]isothiazole,cas is 7716-66-7, mainly used in chemical industry, its synthesis route is as follows.,7716-66-7

(a) 3-(1-PIPERAZINYL)-1,2-BENZOISOTHIAZOLE STR50 A mixture of 3-chloro-1,2-benzisothiazole (37.8 g., 0.235 mole) and piperazine (304.2 g., 3.53 mole) is heated under an argon atmosphere for a period of 20 hr. at 120 C. in a closed reactor. The reaction mixture is dissolved in 2 liters of water and the aqueous solution repeatedly extracted with methylene chloride. Extracts are combined, dried over magnesium sulfate and concentrated in vacuo. Residual material is taken up in ether, filtered and concentrated in vacuo to afford 24.4 g. (47%) of 3-(1-piperazinyl)-1,2-benzisothiazole free base as a viscous oil. A sample of the free base converted to the hydrochloride salt in ether with ethanolic hydrogen chloride and crystallized from methanol-ethanol affords analytically pure 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride, m.p. 280 C. (dec.). Anal. Calcd. for C11 H13 N3 S.HCl: C, 51.66; H, 5.52; N, 16.43. Found: C, 51.34; H, 5.46; N, 16.16.

As the rapid development of chemical substances, we look forward to future research findings about 7716-66-7

Reference£º
Patent; Mead Johnson & Company; US4487773; (1984); 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.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

Step 1: Synthesis of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isothiazole To a stirred solution of 4-bromoisothiazole (0.2 g, 1.21 mmol) and Bis(pinacolato)diboron (0.464 g, 1.81 mmol) in Dioxane (10 mL) was added AcOK (0.358 g, 3.61 mmol) along with TPP (0.032 g, 0.12 mmol) and reaction mass was purged with nitrogen for 30 min. Then, Pd2(dba)3 (0.056 g, 0.061 mmol) was added to it and stirred at 100 C. for 16 h. Reaction was monitored by TLC. On completion reaction mass was concentrated under reduced pressure and extracted with ethyl acetate. The organic layer was washed with water, brine, dried over sodium sulphate, concentrated under reduced pressure obtained crude which was purified column chromatography; eluent 3% EtOAc/Hexane to afford 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isothiazole (0.07 g, 27%) as yellow solid. MS: 212.1[M++1]

24340-77-0, The synthetic route of 24340-77-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Mankind Pharma Ltd.; Patil, Rakesh Ishwar; Verma, Jeevan; Shah, Dharmesh; Ali, Sazid; Bapuram, Srinivasa Reddy; Rai, Santosh Kumar; Kumar, Anil; (146 pag.)US2017/291910; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 3,4-dichloroisothiazole-5-carboxylic acid (2.0 g) and toluene (20 mL) was treated with thionyl chloride (5.0 ml_) and lambda/,lambda/-dimethylformamide (0.5 mL), and the resulting mixture was heated at 1000C for 16 hours. The mixture was concentrated under reduced pressure and the residue was dissolved in tetrahydrofuran (5.0 mL). The mixture was cooled to -780C and treated dropwise over a period of 1 hour with a 2.0 M solution of sodium borohydride in lambda/,lambda/-dimethylformamide (8.5 mL). The mixture was stirred at – 780C for 5 minutes, diluted with 1.0 M aqueous hydrochloric acid solution and extracted with ethyl acetate. The combined organic extract was washed with saturated aqueous sodium chloride solution, dried over sodium sulfate and concentrated under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with a mixture of cyclohexane and dichloromethane (1:0 to 0:1 by volume) to afford the title compound as a pale yellow solid (1.1 g).1H NMR (CDCI3): delta 4.96 (s, 2H).

18480-53-0, As the paragraph descriping shows that 18480-53-0 is playing an increasingly important role.

Reference£º
Patent; ARGENTA DISCOVERY LIMITED; WO2009/77728; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

A common heterocyclic compound, the isothiazole compound, name is Isothiazole-3-carboxylic acid,cas is 4576-90-3, mainly used in chemical industry, its synthesis route is as follows.,4576-90-3

To a stirred suspension of isothiazole-3-carboxylic acid (10.02 g, 77.6 mmol) in anhydrous te/f-butanol (80 ml_) and anhydrous toluene (120 ml_) was slowly added triethylamine (13.0 ml_, 93.12 mmol). The mixture was stirred at ambient temperature for 5 minutes and then diphenyl phosphoryl azide (18.42 ml_, 85.36 mmol) was added dropwise to it. The reaction mixture was stirred at ambient temperature for 1 h, gradually warmed to 85 C over 1 h, and then heated at 85 C with stirring for 7 h. After cooling to ambient temperature, the reaction mixture was diluted with ethyl acetate (150 ml_) and saturated aqueous sodium bicarbonate (150 ml_). The layers were separated and the aqueous layer was extracted with ethyl acetate (2 c 100 ml_). The combined organic layers were washed with water (150 ml_), brine (150 ml_), dried over magnesium sulfate, and filtered. Concentration of the filtrate in vacuo provided a residue, which was purified by column chromatography, eluting with a gradient of 0 to 10% of ethyl acetate in heptane. Further purification by column chromatography, eluting with a gradient of 0 to 10% of ethyl acetate in dichloromethane, afforded the title compound as a colorless solid (10.33 g, 66% yield): 1H NMR (400 MHz, CDCI3) d 8.56 (dd, J = 4.9, 0.6 Hz, 1 H), 8.11 (s, 1 H), 7.66 (d, J = 4.9 Hz, 1 H), 1.53 (s, 9H); MS (ES+) m/z 201.1 (M + 1).

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Reference£º
Patent; XENON PHARMACEUTICALS INC.; FOCKEN, Thilo; BURFORD, Kristen Nicole; LOFSTRAND, Verner Alexander; WILSON, Michael Scott; ZENOVA, Alla Yurevna; (121 pag.)WO2019/241533; (2019); 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.87691-88-1,3-Piperazinobenzisothiazole hydrochloride,as a common compound, the synthetic route is as follows.

87691-88-1, The above intermediate IV (0.01 mol) and the hydrochloride salt of the piperazine compound (V) (0.01 mol) were dissolved in DMF (100 mL), and K2CO3 (0.02 mol) was added.According to the general operation three,Preparation of 3-(4-(3-(6-fluoro-1H-indol-3-yl)propyl)piperazin-1-yl)benzo[d]isothiazole(VI-11) hydrochloride (white solid) 3.44 g, yield 80%.

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

Reference£º
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Li Jianqi; Gu Zhengsong; Zhou Ainan; Xiao Ying; (26 pag.)CN109467554; (2019); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

A common heterocyclic compound, the isothiazole compound, name is 3-Piperazinobenzisothiazole hydrochloride,cas is 87691-88-1, mainly used in chemical industry, its synthesis route is as follows.,87691-88-1

To a solution of 3- (1-piperazinyl) -1,2_ benzisothiazole hydrochloride (100g) and potassium carbonate (136g) in acetonitrile (800ml) added the suspension 1,4_ butanediol dimethyl sulfonate (lllg). Under vigorous stirring for 10 hours the resulting mixture was refluxed. After the solvent was distilled off under reduced pressure to acetonitrile was added, the reaction mixture was evaporated to clean water (100ml) and toluene (300ml), with stirring to break up the product mixture, refluxing under stirring operation, in addition to the net after the water, cool down, the suspension was filtered to give a white inorganic salts and organic salts of a mixture of the crude quaternary spiro ammonium base (272g).

As the rapid development of chemical substances, we look forward to future research findings about 87691-88-1

Reference£º
Patent; Yantai Besten Pharmaceutical Co., Ltd.; Bi, Haidong; Zhang, Yifang; (8 pag.)CN105669665; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com