Tag: M.W:100-200

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of t-butyl 5-(2,2-dimethylbutyl)-2-{2-[4-(4,4,5,5-tetramethyl- 1,3,2- dioxaborolan-2-yl)phenyl]ethyl} lH-imidazole-l-carboxylate (intermediate 8, 3.59 g, 7.45 mmol), 4-bromoisothiazole (2.44 g, 14.90 mmol), l,r-bis(diphenylphosphino)ferrocene- palladium dichloride dichoromethane complex (1:1) (608 mg, 0.745 mmol), potassium carbonate (5.15 g, 37.25 mmol) and DME (35 mL) was degassed and filled with nitrogen. After stirring at 80C overnight, the mixture was cooled and partitioned between water (50 mL) and ethyl acetate (50 mL). The organic layer was separated and the aqueous layer was extracted with ethyl acetate (3x). The combined organic extracts were washed by water, brine, dried over MgSO4, filtered and concentrated. The residue was purified by silica gel chromatography (eluting with 5 to 20% ethyl acetate in hexanes) to afford t-butyl 5-(2,2-dimethylbutyl)-2-[2-(4-isothiazol-4- ylphenyl)ethyl]-lH-l-carboxylate. LCMS: found m/e 440 (M+eta)+.

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

Reference£º
Patent; MERCK & CO., INC.; WO2008/51405; (2008); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

Piperazine (508.8 g) and Tert. Butanol (200 ml) were placed in round bottom flask (RBF) and then the resulting solution heated up to 90 to 100 degree C. 3-chloro-1,2-benzisothiozole (40 g) was added to the solution 5 times with in time interval of 5 to 20 minutes at the same temperature. Temperature was raised up to 110 to 130 degree C. and maintained for 16 hours. After confirmation of the completion of the reaction by TLS (Thin Layer Chromatography), the resulting solution was cooled to 80 to 90 degree C. followed by addition of water (800 ml). The above mixture was cooled to 25 to 35 degree C. and was filtered to remove the solid particles. Water (100 ml) was added to the filtrate and then pH was raised to 12-14 with caustic lye (75 ml). Toluene (400 ml) was added to the alkaline solution the resulting bi-phasic mixture was stirred vigorously for 15 to 30 minutes at 25 to 35 degree C. Organic layer separated and the aqueous layer was multiply extracted with toluene followed by combing all organic layers. The combined organic layer was washed with water (200 ml). Active carbon (10 g) was added to the washed organic layer and then filtered out the carbon. The organic solvent was evaporated till the volume reaches to 150 to 200 ml. The resulting concentrated solution was cooled to 0 to 5 degree C. and maintained for about 2 hours. Separated solids were filtered and then washed with chilled toluene (20 ml). Finally, Isolated compound was dried under reduced pressure to get titled compound 130 to 135 g.

The synthetic route of 7716-66-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DR. REDDY’S LABORATORIES LIMITED; DR. REDDY’S LABORATORIES, INC.; US2005/49295; (2005); 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.7716-66-7,3-Chlorobenzo[d]isothiazole,as a common compound, the synthetic route is as follows.

7716-66-7, 3-Chloro-1 ,2-benzisothiazole (147 mg, 0.87 mmol) was added to a solution of the piperidine of preparation 60 (200 mg, 0.72 mmol) in acetonitrile (20 mi). 1 ,8-Diazabicyclo[5.4.0]undec-7-ene (111 mul, 0.72 mmol) was added, and the reaction mixture was then stirred at room temperature for 48 hours. It was then concentrated under reduced pressure and the crude product was purified by EPO column chromatography on silica gel using dichloromethane/methanol/aqueous ammonia as eluant (90:10:1 v/v/v) to yield the title compound (290 mg, 98percent) as a solid.1H NMR (400MHz, CD3OD): delta 1.80-1.85 (m, 2H), 2.00-2.10 (m, 2H), 2.23 (s, 3H), 2.57 (m, 1 H), 2.85-2.91 (m, 2H), 3.23-3.28 (m, 2H), 7.32 (t, 1 H), 7.43 (d, 2H), 7.61-7.68 (m, 4H), 7.74 (d, 1 H); LRMS APCI+ m/z 410 [MH]+.

The synthetic route of 7716-66-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER LIMITED; WO2006/114706; (2006); 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.936-16-3,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide,as a common compound, the synthetic route is as follows.,936-16-3

Example 89 2-[{1-(tert-Butyl)-5-(4-trifluoromethylphenyl)-1H-pyrazol-3-yl}methyl]-2,3-dihydro[d]isothiazole 1,1-dioxide (Compound 34) To a solution of 1,2-benzisothiazoline-1,1-dioxide (24.3 mg, 0.144 mmol) in N,N-dimethylformamide (1 mL) was added dropwise potassium carbonate (180 mg, 1.30 mmol) at room temperature, followed by stirring for 15 min. This solution was slowly added with drops of {1-(tert-butyl)-5-(4-trifluoromethylphenyl)-1H-pyrazol-3-yl}methyl bromide (51.6 mg, 0.143 mmol) in methylene chloride (4.5 mL), and stirred for a day at room temperature. When the reaction was completed as measured by TLC (Hexane:EtOAc=4:1), 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=4:1?2:1) to afford the title compound (25.4 mg, 39percent, white solid). M.P. 144.6-148.2¡ã C.; 1H NMR (300 MHz, CDCl3) delta 7.85 (d, J=7.7 Hz, 1H), 7.68-7.48 (m, 6H), 7.41 (d, J=7.4 Hz, 1H), 6.29 (s, 1H), 4.54 (s, 2H), 4.47 (s, 2H), 1.49 (s, 9H); 13C NMR (75 MHz, CDCl3) delta 143.9, 142.4, 137.9, 135.3, 134.2, 132.6, 130.9, 130.8, 130.5, 129.0, 125.7, 124.8, 124.7, 124.5, 122.1, 121.5, 109.4, 61.5, 50.1, 41.3, 31.3

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

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

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, General procedure for synthesis of 3-(piperazin-1-yl)benzo[d]isothiazole The compound 3-chloro-1, 2-benzisothiazole (1 mmol) was allowed to react with piperazine (1.2 mmol) in Ethanol at 80 ¡ãC for 36 h. Then reaction mixture was concentrate and RM was dissolved in ethyl acetate and washed with water. Ethylacetate layer dried with Na2SO4 and concentrate them and get 3-(piperazin-1-yl)benzo[d]isothiazole. White solid, 85percent yield, mp 215-217 ¡ãC, 1H NMR (400 MHz, CDCl3): delta = 7.42 (t, J = 7.2 Hz, 1H), 7.29 (m, 3H), 4.14 (t, J = 4.8 Hz, 4H), 3.15 (t, J = 4.8 Hz, 4H); 13C NMR (100 MHz, DMSO+CDCl3): 166.8, 156.2, 135.8, 128.5, 127.6, 125.2, 124.9, 119.8, 53.6, 49.2, 46.6, 45.1, 7.1. MS calcd for C19H20N4OS2: 219.31. Found: 220.33, (M+); Anal. Calcd for C19H20N4OS2: C, 60.24; H, 5.97; N, 19.16; S, 14.62; Found: C, 60.25; H, 5.99; N, 19.13; S, 14.61.

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

Reference£º
Article; Reddy, Kummetha Indrasena; Srihari, Konduri; Renuka, Janupally; Sree, Komanduri Shruthi; Chuppala, Aruna; Jeankumar, Variam Ullas; Sridevi, Jonnalagadda Padma; Babu, Kondra Sudhakar; Yogeeswari, Perumal; Sriram, Dharmarajan; Bioorganic and Medicinal Chemistry; vol. 22; 23; (2014); p. 6552 – 6563;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

936-16-3, Step 2. A mixture of 14 (200 mg, 0.70 mmol), 1 (143 mg, 0.84 mmol), Cs2CO3 (459 mg, 1.41 mmol), Cul (40 mg, 0.21 mmol) and 2-(dimethylamino)acetic acid hydrochloride (30 mg, 0.21 mmol) in dioxane (2 mL) was degassed and purged with N2 (3X). The mixture was stirred at 100¡ãC for 12 h under N2 atmosphere. The reaction mixture was diluted with ethyl acetate (50 mL), adjusted to pH=7 with 2N HC1, and separated. The aqueous layer was extracted with ethyl acetate (2 x 40 mL) and the combined organic layer was washed with saturated brine (80 mL), dried over anhydrous sodium sulfate, filtered and concentrated to give 15 (230 mg) as a light yellow solid.

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

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

2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, cas is 936-16-3, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,936-16-3

To a solution of {1-(tert-butyl)-5-(4-piperidin-1-yl-phenyl)-1H-pyrazol-3-yl}methanol (54.9 mg, 0.175 mmol) in methylene chloride (1.5 mL) were added PPh3 (93.1 mg, 0.355 mmol) and CBr4 (121 mg, 0.365 mmol) at 0¡ã C., followed by stirring at the same temperature for one hour to give {1-(tert-butyl)-5-(4-piperidin-1-yl-phenyl)-1H-pyrazol-3-yl}methyl bromide. When the reaction was completed as measured by TLC(Hexane:EtOAc=2:1), 1,2-benzisothiazoline-1,1-dioxide (27.3 mg, 0.161 mmol) in N,N-dimethylformamide (1.5 mL) was added dropwise. At the same temperature, potassium carbonate (228 mg, 1.65 mmol) was added, and the resulting solution was stirred for a day. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), water was added, after which extraction was carried out with ethyl acetate and brine. The organic layer thus formed was dried over anhydrous magnesium sulfate, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=4:1?1:1) to afford the title compound (15.2 mg, 20percent, white solid). (0324) M.P. 150.4-165.2¡ã C.; (0325) 1H NMR (300 MHz, CDCl3) delta 7.89 (d, J=7.9 Hz, 1H), 7.64-7.52 (m, 2H), 7.40 (d, J=7.1 Hz, 1H), 7.30-7.17 (m, 2H), 6.29 (d, J=8.7 Hz, 2H), 6.22 (s, 1H), 4.52 (s, 2H), 4.46 (s, 2H), 3.26-3.23 (brs, 4H), 1.79-1.74 (brs, 4H), 1.67-1.63 (brs, 2H), 1.49 (s, 9H); (0326) 13C NMR (75 MHz, CDCl3) delta 151.9, 144.4, 143.3, 135.4, 134.3, 132.5, 131.1, 128.9, 124.5, 123.7, 121.4, 114.9, 109.0, 61.0, 50.0, 41.4, 31.2, 25.7, 24.3

As the rapid development of chemical substances, we look forward to future research findings about 936-16-3

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

7716-66-7,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.

10.2 grams of piperidine,Mix 4.0 g of 3-chloro-1,2-benzothiazole and 10 ml of ethanol and mix at 80 ¡ã C under refluxAfter 18 hours, it was cooled, poured into water, separated with 100 ml of water and 200 ml of toluene, and the organic phase was washed with 100 ml of water. Dry, filter, concentrate to 20 ml, and refrigerate overnight (0-5 ¡ã C) in the refrigerator. Precipitation appeared, filtered to give a white solid, yield79.6percent.

The synthetic route of 7716-66-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Capital University of Medical Sciences; Jin Zengliang; Gao Nana; Zheng Yuanyuan; Xu Huanli; Li Xiaorong; Xiong Jie; (20 pag.)CN108440520; (2018); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a nitrogen atmosphere at 100 C,(2E) -3- (4- (tributylstannyl) pyridin-3-yl) ethyl acrylate (33 mg)4-bromoisothiazole (17.41 mg),Pd (Ph3P) 4 (8.18 mg),Cuprous iodide (I) (2.70 mg),A mixture of cesium fluoride (21.50 mg) and DMF (1.5 mL) was stirred at room temperature for 13 hours.Similarly, in a nitrogen atmosphere, 100 C,(2E) -3- (4- (tributylstannyl) pyridin-3-yl) acrylate (497 mg)4-bromoisothiazole (262 mg), Pd (Ph3P) 4 (123 mg),A mixture of cuprous iodide (I) (40.6 mg), cesium fluoride (324 mg) and DMF (10 mL) was stirred for 13 hours.The reaction mixture was combined and the insoluble material was filtered.The filtrate was diluted with ethyl acetate (20 mL), water (10 mL) and saturated aqueous sodium bicarbonate (10 mL), and the aqueous layer was extracted with ethyl acetate. The extract was washed with water and brine, dried over anhydrous sodium sulfate, and the solvent was removed by distillation under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane) to give the title compound (222 mg)., 24340-77-0

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

Reference£º
Patent; TAKEDA PHARMACEUTICAL COMPANYLIMITED; HIRAYAMA, TAKAHARU; FUJIMOTO, JUN; CARY, DOUGLAS ROBERT; OKANIWA, MASANORI; HIRATA, YASUHIRO; (289 pag.)TW2017/14883; (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.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

Step 4: 3-(6-Chloro-l-isothiazol-4-yl-2-methyl-lH-indol-3-ylsulfanyl)-benzoic acid ethyl ester[00503] 3-(6-Chloro-2-methyl-lH-indol-3-ylsulfanyl)-benzoic acid ethyl ester (0.250 g, 0.723 mmol) was combined with CuO (0.118 g, 1.48 mmol), potassium carbonate (0.130 g, 0.941 mmol) and 4- bromoisothiazole (0.250 g, 1.52 mmol) in pyridine (2 mL) and the reaction was heated to 145 C overnight. After cooling the reaction was partitioned between ?0 and DCM and the aqueous layer was extracted with DCM. The combined organics were dried over MgS04 and concentrated then submitted to silica gel chromatograp -20% EtOAc in hexanes) to yield the title compound.

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

Reference£º
Patent; AMIRA PHARMACEUTICALS, INC.; ROPPE, Jeffrey, Roger; PARR, Timothy, Andrew; STOCK, Nicholas, Simon; VOLKOTS, Deborah; HUTCHINSON, John, Howard; WO2012/24620; (2012); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com