Heterocyclic Building Blocks-Isothiazole

7716-66-7, 3-Chlorobenzo[d]isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,7716-66-7

A dry 2-neck 500 mL round-bottom flask (RBF) was charged with sodium ethanolate (46.2 mL, 124 mmol), diluted with 151 mL absolute EtOH, cooled in an ice bath and treated dropwise with diethyl malonate (17.98 mL, 118 mmol) under an atmosphere of nitrogen. After stirring for 20 minutes, the ice bath was removed and 3-chlorobenzo[d]isothiazole (20.0 g, 118 mmol) was added in one portion and stirred for 24 hours. The reaction solution was quenched with water, extracted with ether and treated with excess 4 M HCl/dioxane. A pinkish-white precipitate was filtered off, suspended in water, basified with Na2CO3, extracted with ether, washed with water and brine, dried over sodium sulfate, filtered and concentrated to yellow solids (20 g) which were recrystallized from ethanol/water and dried in a vacuum oven at 60¡ã C. for 3 hrs to give ethyl 3-aminobenzo[b]thiophene-2-carboxylate (19.9 g, 76percent yield).

7716-66-7 3-Chlorobenzo[d]isothiazole 598190, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; Universal Display Corporation; Joseph, Scott; Kwang, Raymond; Lee, Chi Hang; Shia, Chuan Jun; Ram, SiV Cheung; (131 pag.)KR2015/9461; (2015); A;,
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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.

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.

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.)CN106890181; (2017); A;,
Isothiazole – Wikipedia
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677304-75-5, 6-Bromobenzo[d]isothiazole-3-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

677304-75-5, The following acids were prepared using this method: -Bromobenzisothiazole-S-carboxylic acid. 5-Bromobenzisothiazole-3-carboxy lie acid. 6-Methoxybenzisothiazole-3-carboxylic acid.The following esters were prepared from the acid using ethanol and sulfuric acid:Ethyl 6-bromobenzisothiazole-3-carboxylate. Ethyl 5-bromobenzisothiazole-3-carboxylate. Ethyl 6-methoxybenzisothiazole-3-carboxylate.

As the paragraph descriping shows that 677304-75-5 is playing an increasingly important role.

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; WO2007/56582; (2007); A1;,
Isothiazole – Wikipedia
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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

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).

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

Reference£º
Patent; Yantai Besten Pharmaceutical Co., Ltd.; Bi, Haidong; Zhang, Yifang; (8 pag.)CN105669665; (2016); A;,
Isothiazole – Wikipedia
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The isothiazole compound, name is 3,4-Dichloroisothiazole-5-carboxylic acid,cas is 18480-53-0, mainly used in chemical industry, its synthesis route is as follows.,18480-53-0

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).

As the rapid development of chemical substances, we look forward to future research findings about 18480-53-0

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

A mixture of the product from step C above (5.0016 g, 17.476 mmol), 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (4.4811 g, 17.520 mmol), potassium carbonate (4.8299 g, 34.946 mmol) and potassium iodine (0.2903 g, 1.749 mmol) were reacted in acetonitrile (29.0 mL) in a CEM MARS5 microwave reactor for 1 h at 200 C. The reaction was cooled to room temperature, diluted with H2O and filtered. The solid was washed with H2O and hexanes. The resulting solid was purified by MPLC [silica gel, 100 % methylene chloride (CH2CI2) to 3 % MeOH/CH2CI2 over 1 h, then hold at 3 % MeOH/CH2CI2] to give 5.6591 g, (12.065 mmol, 69 %) of the titled compound as an off-white crystalline solid. LC-MS (APCI): (M-1)+ = 469.1, (M+1)+ = 471.0

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/26864; (2004); 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

3-Piperazin-1-yl-benzoisothiazole hydrochloride (1.31 g, 5.1 mmol) and (5-fluoro-2-nitro-phenyl)-acetic acid (800 mg, 4.3 mmol) were combined in 100 mL methylene chloride with triethylamine (1.20 mL, 8.6 mmol). This solution stirred for 15 min before bis-(2-oxo-3-oxazolidinyl) phosphinic chloride 1.09 g, 4.3 mmol) was added. After stirring overnight at room temperature (rt), the reaction was quenched with water and extracted into methylene chloride. The organic layer was washed with 0.5 N HCl, water, sodium bicarbonate then water before it was dried over sodium sulfate (Na2SO4) and concentrated. The organic layer was dried over sodium sulfate, concentrated, and purified by MPLC using a Biotage prepacked silica gel cartridge eluting with 3% methanol in methylene chloride (CH2Cl2) to afford 870 mg of an off-white foam. Yield 50%; mp 72 C.; MS (APCI): 401 [M+H]+.

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

Reference£º
Patent; Davis, Jamie Marie; Gregory, Tracy Fay; Walters, Michael Anthony; US2004/67960; (2004); A1;,
Isothiazole – Wikipedia
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The isothiazole compound, cas is 288-16-4 name is Isothiazole, mainly used in chemical industry, its synthesis route is as follows.,288-16-4

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%).

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

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

To a solution of l-[(5R)-4-[methyl(tetrahydropyran-4-yl)amino]-5-oxido-6,7- dihydrothieno[3,2-d]pyrimidin-5-iunn-2-yl]azetidin-3-ol (2.5 g, 7.4 mmol) in DCM (50 mL) was added 4-isothiazolecarboxylic acid ( 1.2 g, 9.6 mmol), DMAP (90 mg, 0.74 mmol) and EDAC ( 1.8 g, 9.6 mmol). The mixture was stirred at room temperature overnight before it was concentrated in vacuo. The residue was purified by column chromatography (DCM/MeOH gradient 20 : 1 to 10 : l(Rf= 0.47 (MeOH/DCM 1 : 10))) and subsequently crystallized twice from n-butyl acetate. The title compound was obtained as colorless crystalline material. 1H NMR (DMSO-d6) delta: 9.81 (s, 1H), 8.99 (s, 1H), 5.59 – 5.38 (m, 1H), 4.94 – 4.75 (m, 1H), 4.47 (dd, J = 10.4, 6.6 Hz, 2H), 4.21 – 4.05 (m, 2H), 4.04 – 3.88 (m, 2H), 3.56 – 3.33 (m, 3H), 3.27 – 3.13 (m, 4H), 3.10 – 2.93 (m, 2H), 1.95 – 1.75 (m, 2H), 1.71 – 1.48 (m, 2H). HPLC-Retention time (XE Metode 7 CM) : 1.89 minutes. Detected “M + l”-mass: 450.12.

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

Reference£º
Patent; LEO PHARMA A/S; LARSEN, Jens; (110 pag.)WO2019/57806; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

936-16-3,936-16-3, 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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.

The synthetic route of 936-16-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
Isothiazole – Wikipedia
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