Day: September 21, 2020

822-82-2,822-82-2, Isothiazole-4-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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)

The synthetic route of 822-82-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER LIMITED; US2008/103130; (2008); 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

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¡ãC for 3 hrs to give ethyl 3-aminobenzo[b]thiophene-2-carboxylate (19.9 g, 76percent yield).

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

Reference£º
Patent; Universal Display Corporation; Xia, Chuanjun; Joseph, Scott; EP2826781; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

To a solution of isothiazole (5 g, 0.06 mol) in anhydrous THF (50 mL) was added n- BuLi (28.2 mL, 0.07 mol) dropwise at -70 oC over 1 h. After stirring at -70 oC for 1 h, Br2 (6 mL, 0.12 mol) was added dropwise over 30 min and the resulting mixture was allowed to warm to RT and poured into an excess of cold 2N HCl solution. The organic layer was separated and the aqueous layer was extracted with Et2O (200 mL x 3). The combined organic extracts were washed with saturated sodium dithionite solution (200 mL x 2), dried over anhydrous Na2SO4, and filtered. The filtrate was concentrated in vacuo, and the resulting residue was distilled to afford 5-bromoisothiazole (2 g, 21%) as yellow oil.1H NMR (400 MHz, CDCl3) delta 8.33 (d, J = 1.6 Hz, 1H), 7.28 (d, J = 1.6 Hz, 1H)., 288-16-4

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

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
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

(3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, cas is 94594-90-8, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,94594-90-8

In a round-bottomed flask, 80 g of (1S)-(-)-2,10-camphorsultam, 236.4 g of methyl tert-butyl ether, 2.27 g of 4-(dimethylamino)-pyridine and 41.36 g of triethylamine were placed, and to this, 63.46 g of capryloyl chloride was added dropwise at room temperature. After stirring for 1 hour, the reaction solution was added to a mixed solution of 7.75 g of 35percent hydrochloric acid and 200 g of water, and the organic layer was separated. The organic layer was washed with 25percent aqueous sodium hydroxide solution and subsequently with water, and concentrated under reduced pressure. Thus, 125.34 g of the titled compound was obtained (quality: 99.7percent measured by GC).Gas chromatography analysis was carried out using Shimadzu GC-14A (Column: 5percent Silicone OV-17 manufactured by GL Science, Detector: FID).

With the rapid development of chemical substances, we look forward to future research findings about 94594-90-8

Reference£º
Patent; Yamazaki, Shigeya; Hosoya, Takeshi; US2009/118542; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1,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.

EXAMPLE 121; 3-f4-[2-(3′, 4′-DIHYDRO-1’H-SPI RO [91, 31DIOXOLANE-2. 2′- NAPHTHALEN1-6′-YL)-ETHYL1-PI PERAZI N-1-YLi- BENZOrDlISOTHIAZOLE; A mixture of 3- (piperazin-1-yl) benzo [d] isothiazole hydrochloride (349 mg, 1.36 mmol) and the title compound from Preparation 36 (530 mg, 1.36 mmol) with anhydrous K2CO3 (376 mg, 2.72 mmol) in acetonitrile (20 ml) was heated at reflux for 24 hours. The reaction mixture was filtered and the filtrate was concentrated. The crude product was purified by elution through a flash column (silica gel 60,230-400 mesh, 1: 1 hexanes: EtOAc) to give a clear oil which crystallized on standing, 497 mg (84%). MS (APCI) : (M + 1) + = 436.’H-NMR (CDCI3, a) : 7.89 (d, 1 H, J = 7.8 Hz), 7.80 (d, 1 H, J = 8. 1 Hz), 7.46 (t, 1 H, J = 7. 3,7. 3 Hz), 7.34 (t, 1 H, J = 7. 3, 7.3 Hz), 6.98 (s, 3H), 4.01 (s, 4H), 3.58 (br s, 4H), 2.95-2. 65 (m, 12H), 1.93 (t, 2H, J = 6.8, 6.8 Hz). CHN, calc’d for C25H29N302S : C, 68.94% ; H, 6. 71% ; N, 9.65% ; found: C, 68.75% ; H, 6.70% ; N, 9.54%.

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (2005); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

(3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, cas is 94594-90-8, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,94594-90-8

Example 3Step 1. Synthesis of (3aS,6R,7aR)-1 -methaciotayloyl-8,8-dimethylhexahydro-3a,6-methano-2,1- benzisothiazole 2,2-dioxide.(1 S)-(-)-2,10-camphorsultamProcedure: To a solution of the (1S)-(-)-2,10-camphorsultam (5.00Og, 23.22 mmoles) in anhydrous THF (50ml) at -20¡ã C was added lithium chloride (1.08g, 25.5 mmoles, – small balls), triethylamine (4.21 ml, 30.2 mmoles, 1.30 equivalents.) and then the mixture was allowed to stir for 10 minutes. The lithium chloride did not go into solution. 2-methylacrylic anhydride (4.15 ml, 27.9 mmoles, 1.20 equivalents.) in THF (15ml) was then added. The internal temperature varied between -20¡ã C and -10¡ã C during addition which took about 5 minutes. The thick white mixture was stirred within the cooling bath and allowed to reach room temperature. After stirring overnight the white heterogeneous reaction mixture was added to 350ml of water with stirring. The white crystalline solid (3aS,6R,7aR)-1 -methacryloyl-8,8- dimethylhexahydro-3a,6-methano-2,1-benzisothiazole 2,2-dioxide (6.302g, 96percent yield) was collected and dried under vacuum.-Analytical HPLC run with a Vydac 218TP54 C18 reverse phase column run with solvents A: 0.1percent trifluoroacetic acid in H2O and B: 0.1percent trifluoroacetic acid in acetonitrile. Gradient (0 to 100percentB) over 22 minutes. Retention time 18.166 min (100percent).Optical rotation = 0.02Og in 2ml; c=0.01g/ml (C= 1 (CHCI3)}; measurement -0.226; optical rotation = – 0.226×4000/10 = – 90.4.Combustion Anal sis:Steps 2 through 5 were performed as in Example 2.

With the rapid development of chemical substances, we look forward to future research findings about 94594-90-8

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/65503; (2008); 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

PREPARATION 23; 6-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-7-chloro-4,8-trimethyl- 3s4-dihydro-1 H-quinolin-2-one; A mixture of 7-chloro-6- (2-chloro-ethyl)-4, 4, 8-trimethyl-3, 4-dihydro-1 H- quinolin-2-one (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 microwave reactor for 1 h at 200 C. The reaction was cooled to rt, diluted with H2O and filtered. The solid was washed with H20 and hexanes. The resulting solid was eluted through a flash column (silica gel 60,230-400 mesh, 0-3% MeOH in CH2CI2 gradient over 1 h) to give an off-white solid. Yield: 5.6591 g (12.065 mmol, 69%). Anal. : calculated for C25H29CIN40S’0. 02CH2CI2 : C, 63.84 ; H, 6.22 ; N, 11.90. Found: C, 63.49, H, 6.13 ; N, 11.72. LC-MS (APCI) : (M+1) + = 471. 0. H NMR (400 MHz, CDCI3) 8 7.90 (d, J=8. 2 Hz, 1 H), 7.80 (d, J=8.0 Hz, 1 H), 7.58 (s, 1 H), 7.45 (ddd, J=8. 0,7. 1,1. 0 Hz, 1 H), 7.34 (ddd, J=8. 2,7. 1,1. 0 Hz, 1 H), 7.08 (s, 1 H), 3.61 (m, 4 H), 2.98 (m, 2 H), 2.80 (s, 4 H), 2.68 (m, 2 H), 2.44 (s, 2 H), 2.31 (s, 3H), 1.30 (s, 6H).

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2005/66165; (2005); A1;,
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

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