Simple exploration of 7716-66-7

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

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 solution of the product from step b) (200 mg) and 3-chloro-1, 2-benzisothiazole (171mg) in NMP (2ml) and 4M hydogen chloride in dioxan (0.2 ml) was stirred at [140¡ãC] overnight and then at [150 ¡ãC] for 1 hour. and evaporated. The residue was taken up in ethyl acetate, washed with brine (3X), dried [(MGSO4)] and evaporated. The residue was purified by silica chromatography using 20percent acetone in isohexane as eluent to give the title compound (219 mg). MS: APCI (-ve): 331 [[M+H] +] [APOS;H] NMR (DMSO-d6) [8] 8.33 [(1H,] s), 8.01 [(1H,] d), 7.66 [(1H,] d), 7.56 [(1H,] t), 7.39 [(1H,] t), 6.99 [(1H,] d), 2.34 (3H, s), 1.79 (3H, d).

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

Reference£º
Patent; ASTRAZENECA AB; WO2003/101981; (2003); A1;,
Isothiazole – Wikipedia
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Simple exploration of 936-16-3

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various fields.

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,936-16-3

Step 2. A mixture of 12 (100 mg, 0.40 mmol), 1 (67 mg, 0.40 mmol), potassium carbonate (55 mg, 0.40 mmol), Cul (3.8 mg, 0.019 mmol), and L-proline (2.3 mg, 0.019 mmol) in dioxane (4 mL) was stirred at 110¡ãC for 16 hours under an inert atmosphere. Upon completion, water (40 mL) was added and the reaction mixture was extracted with EtOAc (90 mL). The organic phase was washed with brine (50 mL) and concentrated under reduced pressure. Purification with prep-HPLC (0.075percent TFA/CH3CN/H20 system) resulted in Compound 121 (40 mg, 29percent) as yellow solid and TFA salt. 1H NMR (DMSO-d6, 400MHz) delta 8.69-8.68 (d, 1H), 8.53-8.52 (d, 1H), 7.99-7.94 (m, 3H), 7.77 (m, 1H), 7.67-7.62 (m, 3H), 7.07-7.05 (d, 1H), 6.83-6.81 (d, 1H), 4.95 (s, 2H); LCMS (ESI): m/z 340.1 (M+H).

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; NUMERATE, INC.; RAIMUNDO, Brian; KOLTUN, Elena S.; GRIFFIN, John; STANGELAND, Eric; (93 pag.)WO2018/49324; (2018); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Some tips on 24340-77-0

24340-77-0, 24340-77-0 4-Bromoisothiazole 5200358, 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.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

A solution of 5,7-dimethyl-N-(4-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2- yl)phenyl)pyrazolo[l,5-a]pyrimidine-3-carboxamide 6 (286 mg, 0.73 mmol) in DMF (5 mL) was charged with 4-bromoisothiazole (100 mg, 0.60 mmol), potassium acetate (179 mg, 1.8 mmol) and Pd(dppf)Cl2DCM adduct (49 mg, 0.06 mmol) under argon at room temperature. The reaction mixture was heated to 100C for 16 h. The reaction mixture was quenched with water (5 mL), extracted with ethyl acetate (3 X 10 mL) and concentrated under vacuum to obtain crude compound. The crude compound was purified by FCC (eluent, 3-5% methanol in DCM) to afford the title compound as an off-white solid (50 mg, 23%).XH NMR (400 MHz, CDCI3) delta 10.24 (s, 1H), 8.79 (s, 1H), 8.71 (s, 1H), 8.68 (s, 1H), 7.84 (d, J=8.57 Hz, 2H), 7.61 (d, J=8.57 Hz, 2H), 6.78 (s, 1H), 2.83 (s, 3H), 2.74 (s, 3H). ES-MS m/z 350.20 (M+H)+. HPLC purity 99.1%.

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

Reference£º
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; LANSBURY, Peter, T.; GOOD, Andrew, C.; BOURQUE, Elyse, Marie Josee; (139 pag.)WO2016/73895; (2016); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Brief introduction of 936-16-3

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

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

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.

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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Simple exploration of 27148-03-4

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

27148-03-4, Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of thiosaccharin (tsacH) (0.04 g, 0.24 mmol) in methanol (8 cm3) was added to a solution of K2[PtCl4] (0.05 g, 0.12 mmol) in water (3 cm3). The orange mixture was heated at reflux on a steam bath for 2 h. After cooling to room temperature the brown solid formed was filtered off, washed with water and dried in a vacuum oven to give 1 (0.049 g, 70%). 1H NMR (d6-dmso): delta 8.50 (d, J 7.0 Hz, 2H), 8.86 (d, J 6.8 Hz, 2H), 7.76 (m, 4H); IR v/cm-1; IR(KBr) 3085w, 1419s, 1340vs, 1100vs, 1012s, 804vs, 366m cm-1; Elemental Anal. Calc. for PtS4N2O4C14H8¡¤H2O. Found: C, 27.58 (27.63); H, 1.64 (1.49); N, 4.60 (4.59)%., 27148-03-4

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
Isothiazole – Wikipedia
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New learning discoveries about 936-16-3

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

936-16-3,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.

Intermediate 30Ethyl 1 -[4-(1 ,1 -dioxido-1 ,2-benzisothiazol-2(3H)-yl)phenyl]-3-[[(frapis-4- methylcyclohexyl)carbonyl](1-methylethyl)amino]-1H-pyrazole-4-carboxylateA solution of Intermediate 5 (108 mg), 2,3-dihydro-1 ,2-benzisothiazole 1 ,1 -dioxide (35 mg), copper (I) iodide (4 mg), potassium carbonate (58 mg) and (IR^RJ-lambda/./V-dimethyl-i ^- cyclohexanediamine (12 mg) in DMF (4 mL) was heated in a microwave at 100¡ã C, 300 W for 1 h and then evaporated to dryness. The residue was dissolved in ethyl acetate and washed sequentially with aqueous sodium bicarbonate solution, water and 2M HCI, dried using a EPO hydrophobic frit and evaporated to dryness. The crude product was then purified by MDAP HPLC to give the title compound. MS calcd for (C30H36N4O5 + H)+: 565 MS found (electrospray): (M+H)+ = 565

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

Reference£º
Patent; SMITHKLINE BEECHAM CORPORATION; WO2007/39146; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

New learning discoveries about 7716-66-7

As the paragraph descriping shows that 7716-66-7 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.7716-66-7,3-Chlorobenzo[d]isothiazole,as a common compound, the synthetic route is as follows.,7716-66-7

EXAMPLE 3 3-(1-Piperazinyl)-1,2-benzisothiazoleodsold;hydrochloride Anhydrous piperazine (49.4 g, 0.57 mol) and t-butanol (10 mL) were added to a dry, 300 mL round bottom flask equipped with a mechanical stirrer, thermometer, condenser topped with a nitrogen inlet, and pressure-equalizing dropping funnel. After the flask was purged with nitrogen, it was heated to 100¡ã C. in an oil bath. A solution of 3-chloro-1,2-benzisothiazole (19.45 g, 0.11 mol) in t-butanol (10 mL) was added to the addition, funnel, and then slowly added to the reaction flask over 20 minutes to moderate an exothermic reaction (112-118¡ã C.). Once addition was complete the yellow solution was heated to reflux (121¡ã C.) and then maintained at reflux for 24 hours. Thin-layer chromatography showed that the reaction was complete. The reaction mixture was cooled to 85¡ã C. and 120 mL of water was added. The hazy solution was filtered and the filter cake rinsed with 60 mL of t-butanol/water (1:1) solution. The pH of the combined filtrate and wash was adjusted to 12.2 with 50percent aqueous caustic. The aqueous solution was extracted with toluene (200 mL), the layers were separated, and the aqueous layer was extracted with fresh toluene (100 mL). The combined toluene layers were washed with water (75 mL), and then the toluene solution was concentrated in vacuo at 48¡ã C. to 90 mL. Isopropanl (210 mL) was added to the concentrate and then the pH was slowly adjusted to 3.8 with 7.6 mL of concentrated hydrochloric acid. The resulting slurry was cooled to 0¡ã C., granulated for 45 min, and then filtered. The filter cake was washed with cold isopropanol (50 mL) and then dried in vacuo at 40¡ã C. to afford 23.59 g (80percent yield) of 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride as an off white solid.

As the paragraph descriping shows that 7716-66-7 is playing an increasingly important role.

Reference£º
Patent; Pfizer, Inc.; US6111105; (2000); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Some tips on 936-16-3

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various fields.

936-16-3,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.

Example 88 2-[{1-(tert-Butyl)-5-(4-fluorophenyl)-1H-pyrazol-3-yl}methyl]-2,3-dihydro[d]isothiazole 1,1-dioxide (Compound 33) To a solution of 1,2-benzisothiazoline-1,1-dioxide (10.3 mg, 0.061 mmol) in N,N-dimethylformamide (0.9 mL) was added potassium carbonate (88.5 mg, 0.640 mmol) at room temperature, followed by stirring for 10 min. The solution was slowly added with drops of {1-(tert-butyl)-5-(4-fluorophenyl)-1H-pyrazol-3-yl}methyl bromide (20.9 mg, 0.067 mmol) in methylene chloride (3 mL), and stirred at room temperature for a day. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), the reaction mixture was filtered through celite. The filtrate was neutralized with 1M HCl and an aqueous saturate sodium hydrogen carbonate solution. After extraction with ethyl acetate and water, the organic layer thus formed was dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=6:1?1:1) to afford the title compound (10.2 mg, 42percent, white solid). M.P. 163.5-167.5¡ã C.; 1H NMR (300 MHz, CDCl3) delta 7.86 (d, J=7.6 Hz, 1H), 7.65-7.53 (m, 2H), 7.41 (d, J=7.5 Hz, 1H), 7.35-7.29 (m, 2H), 7.13-7.06 (m, 2H), 6.27 (s, 1H), 4.53 (s, 2H), 4.46 (s, 2H), 1.48 (s, 9H); 13C NMR (75 MHz, CDCl3) delta 164.4, 162.3, 161.1, 143.6, 142.9, 135.3, 134.2, 132.6, 132.2, 132.1, 129.9, 129.0, 124.5, 121.5, 115.0, 114.7, 109.3, 61.3, 50.0, 41.3, 31.2

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; NAM, Ghil Soo; CHOI, Kyung Il; KIM, Jung Hyun; PAE, Ae Nim; HONG, Jin Ri; LEE, Jae Kyun; (30 pag.)US2015/329533; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Analyzing the synthesis route of 27148-03-4

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

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

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Share a compound : Isothiazole-4-carboxylic acid

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

Isothiazole-4-carboxylic acid, cas is 822-82-2, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,822-82-2

To a solution of the compound of Preparation 141 (1.4 g, 11.0 mmol) in tetrahydrofuran (6 ml), at -5 C., was added dropwise borane (1M in tetrahydrofuran, 16.5 ml). The reaction mixture was allowed to warm to room temperature and stirred for 18 h. The mixture was quenched by addition of water: acetic acid (1:1, 4 ml) and the mixture was concentrated in vacuo. The residue was added to saturated aqueous sodium hydrogen carbonate solution (5.5 ml) at 0 C. and the two layers were separated. The aqueous layer was extracted with ethyl acetate (750 ml) and the combined extracts were concentrated in vacuo to give the title compound (700 mg). 1H-NMR (CDCl3): 4.80-4.84 (2H), 8.69-8.71 (1H), 8.76-8.78 (1H)

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

Reference£º
Patent; PFIZER LIMITED; US2008/103130; (2008); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com