Day: September 29, 2020

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 6-(2-chloro-ethyl)-4,4,8-trimethyl-3,4-dihydro-1H-quinolin-2-one (1.5eq) in dioxane/H2O (0.03M 1:1) was added sodium carbonate (2.2 eq), sodium iodide (catalytic), and added 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (1.0eq). The reaction mixture was heated to reflux for 24-72 hours. The reaction mixture was then concentrated and partitioned between H2O and CH2CI2. The organic layer was dried (MgSO4), concentrated and purified by chromatography (4:1 EA/Hex) to yield the title compound in 15-48% yield. LC/MS column: Phenomenex Develosil Combi-RP-3 3Μ 50×4.6mm, length 150×4.6

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; WO2004/26864; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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
Isothiazole – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.94594-90-8,(3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide,as a common compound, the synthetic route is as follows.

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., 94594-90-8

As the paragraph descriping shows that 94594-90-8 is playing an increasingly important role.

Reference£º
Patent; PFIZER PRODUCTS INC.; WO2008/65503; (2008); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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
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.

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

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

Step 5; Sulfuryl dichloride (86.7 mg, 728 mumol) is added to a solution of6-bromobenzo[d]-isothiazole-3-carboxylic acid (188 mg, 728 mumol). The reaction mixture is stirred for 30 min before removing the volatiles by rotovap. The residue is taken up in CH2Cl2 (0.587 ml) and a solution of 2-prorhoylamine (62.5 muL, 728 mumol) and triethylamine (101 mul, 728 mumol) in CHjCl2 (1.2 ml) is added. The reaction mixture is stirred at room temperature until LC/MS analysis indicates complete conversion to the desired product. The reaction mixture is diluted with distilled water and ethyl acetate. The layers are separated and the aqueous is extracted with ethyl acetate. The combined organics are washed with brine and dried over Na2SO4, filtered and concentrated to give 6-bromo-N-isopropylbenzo[d]isothiazole- 3-carboxamide.

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

Reference£º
Patent; AMGEN INC.; MEMORY PHARMACEUTICALS CORPORATION; WO2007/100880; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

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
Isothiazole – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

15 g of 3,4-dichloroisothiazole-5-carboxylic acid (75.7 mmol) were dissolved in 300 ml of ethanol and 8.4 ml of concentrated sulphuric acid were added. The mixture was stirred under reflux for 20 h. The reaction mixture was then concentrated to half the original volume, neutralized with saturated NaHCO3, added to water and extracted with dichloromethane. The dichloromethane phases were dried and carefully concentrated on a rotary evaporator. Yield:15.2 g (89percent of theory).?H-NMR (400 MHz, CDC13 3, ppm) 4.44 (q, 2H), 1.42 (tr, 3H)., 18480-53-0

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; BERNIER, David; CRISTAU, Pierre; TSUCHIYA, Tomoki; RINOLFI, Philippe; DROeGE, Thomas; MAECHLING, Simon; SCHMIDT, Jan Peter; TELSER, Joachim; DOeLLER, Uwe; MOSRIN, Marc; REY, Jullien; TIEBES, Joerg; WACHENDORFF-NEUMANN, Ulrike; (467 pag.)WO2016/102435; (2016); A2;,
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, EXAMPLE 80 3-(4-(1-[1,2-Benzisothiazol-3-yl]-4-piperazinyl)butyl)-1-thia-3-azaspiro[4.5]decan-4-one A mixture of 3-(4-bromobutyl)-1-thia-3-azaspiro[4.4]nonan-4-one (4.00 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (3.67 g), K2 CO3 (7.00 g) and NaI (300 mg) in acetonitrile (220 ml) was heated at 70 C. for 20 hours and the product was processed in substantially the same manner as in Example 10 to afford 3.01 g of crystalline solid, m.p. 209 C. ANALYSIS: Calculated for C23 H32 N4 OS2 *HCl: 57.42%C; 6.91%H; 11.64%N; 7.37%Cl. Found: 57.51%C; 6.82%H; 11.75%N; 7.30%Cl.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Inc.; US4933453; (1990); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com