Day: September 23, 2020

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

C. 1-{7-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-2,3,4,5- tetrahvdro-benzorblazepin-1-vll-ethanone methanesulfonate; A solution of the title compound from step B (602 mg, 2.39 mmol) in CH3CN (20 mL) was treated with 3-piperazin-1-yl-benzo [agisothiazole HCI (683 mg, 2.67 mmol), Nal (406 mg, 2.71 mmol), and K2CO3 (1.09 g, 7.86 mmol). The mixture was heated to reflux under N2 for 43 h, then allowed to cool. The mixture was diluted with H20 (100 mL) and extracted with CH2CI2 (3 x 100 mL). The combined organic layers were dried over Na2SO4, decanted, and the solvent was removed in vacuo. The residue was purified by flash column chromatography (silica gel, EtOAc) to give a white solid residue (430 mg, 0.99 mmol, 41%). The residue was dissolved in EtOAc (10 mL) and treated with a solution of CH3SO3H in Et20 (0.5 mL, 2M, 1 mmol). After stirring for 5 min, the resulting precipitate was isolated by filtration, washed with Et20 (3 x 10 mL), and dried in a vacuum oven at 50 C for 3 d to give the title compound (465 mg, 89%) as a white powder: mp 189-190 C (dec) ;’H NMR (300 MHz, CDCI3) 8 11.. 76 (s, 1 H), 7.85 (t, J = 7. 8 Hz, 2 H), 7.51-7. 56 (m, 1 H), 7.39-7. 45 (m, 1 H), 7.14-7. 18 (m, 2 H), 7.08 (d, J= 7.8 Hz, 1 H), 4.66-4. 70 (m, 1 H), 4.11-4. 20 (m, 2 H), 3.95-4. 03 (m, 2 H), 3.68 (d, J = 11.3 Hz, 2 H), 3.13-3. 34 (m, 6 H), 2.91 (s, 3 H), 2.68-2. 78 (m, 2 H), 2.51-2. 59 (m, 1 H), 1.74-2. 00 (m, 3 H), 1.83 (s, 3 H), 1.32-1. 40 (m, 1 H); ESI MS m/z 435 [C25H30N40S + H] + ; Rr 0. 35 (silica gel, 95: 5 EtOAc/MeOH); HPLC) >99% (AUC), tR = 12.68 min. Anal. Calc’d for C25H3oN40S’CH3SOsH : C, 58.84 ; H, 6.46 ; N, 10.56. Found: C, 58.56 ; H, 6.49 ; N, 10. 31.

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; WO2005/66165; (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

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

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, D. 1- (2-Acetvl-2, 3-dihvdro-1 H-isoindol-5-vl)-3- (4-benzordlisothiazol-3-vl- piperazin-1-vI)-propan-1-one; A mixture (suspension) of 1- (2-Acetyl-2, 3-dihydro-1 H-isoindol-5-yl)-3-chloro-propan- 1-one (2.14 g, 8.84 mmol), 3-piperazin-1-yl-benzo [d] isothiazole hydrochloride (2.49 g, 9.72 mmol), K2CO3 (3.63 g, 26.3 mmol), and Nal (1.40 g, 9.34 mmol) in anhydrous CH3CN (90 mL) under N2 was stirred at 25 OC for 20 h, then the solvent was removed in vacuo. The residue was suspended in H2O, then extracted twice with EtOAc, however a solid remained undissolved in the aqueous phase. The solid was collected by suction filtration, washing and triturating with H20, then dried in a vacuum oven at 50 C for 3 d to give the titled product (2.74 g, 71 %) as a light brown amorphous solid. ESI MS m/z 435 [M+1].

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

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

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

677304-75-5,677304-75-5, 6-Bromobenzo[d]isothiazole-3-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation 45; 6-(4-Hvdroxy-2-methyl-phenyl)-benzordlisothiazole-3-carboxylic acid; To a degassed solution of 6-Bromo-benzo[d]isothiazole-3-carboxylic acid (0.42g, 1.54mmol), 3-Methyl-4-(4,4,5,5-tetramethyl-[l,3,2]dioxaborolan-2-yl-phenol (0.54, 2.3 lmmol), 2-Dicyclohexylphosphino-2′,6′-dimethoxy- 1 , 1 ‘-biphenyl (0.064g, 0.154mmol), and potassium phosphate (0.7 Ig, 3. lmmol) in dioxane (8mL) and water (4mL) is added Pd(OAc)2 (6.5mg, 0.03mmol). The reaction is degassed again and heated to 80 degrees for 18 h. The reaction is cooled to room temperature and concentrated under reduced pressure. The material is diluted with EtOAc and IN HCl. The layers are separated and concentrated under reduced pressure. The crude material is diluted with 20 mL of MeOH and 2 mL H2SO4 and heated to reflux for 2 h. The reaction is concentrated onto silica and purified using a gradient of 20 to 50% EtOAc in Hexanes to yield the title compound (0.12g, 26% yield). ES/MS m/e 300.0 (M+l).

The synthetic route of 677304-75-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ELI LILLY AND COMPANY; WO2007/140174; (2007); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1,87691-88-1, 3-Piperazinobenzisothiazole hydrochloride is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 63 3-(4-(1-(1,2-Benzisothiazol-3-yl)-4-piperazinyl)butyl)-5-(2,2,2-trifluorethyl)-4-thiazolidinone hydrochloride A mixture of 3-(4-bromobutyl)-5-(2,2,2-trifluoroethyl)-4-thiazolidinone (3.20 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (2.81 g), K2 CO3 (4.83 g) and NaI (250 mg) in acetonitrile (280 ml) was heated at 70 C. for 15 hours and the product was processed in substantially the same manner as in Example 10 to afford 2.30 g of crystals, m.p. 188-200 C. ANALYSIS: Calculated for C20 H25 F3 N4 OS2 ¡¤HCl: 48.52% C; 5.29% H; 11.32% N; 7.16% Cl. Found: 48.51% C; 5.32% H; 11.20 % N; 7.28% Cl.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Inc.; US4933453; (1990); 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.87691-88-1,3-Piperazinobenzisothiazole hydrochloride,as a common compound, the synthetic route is as follows.,87691-88-1

EXAMPLE 6 The mixture of 2.1 g of 4-(1,2-benzisothiazol-3-yl)piperazine hydrochloride, 2.0 g of 3-(3-chloropropionyl)-2-methyl-4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepin-5-one, 2,2 g of potassium carbonate and 1.2 g of potassium iodide in 15 ml of N,N-dimethylformamide and 15 ml of toluene was stirred at 60 C. for 5 hours. After the mixture was cooled in a water bath, water was added thereto and the mixture was extracted with ethyl acetate. The organic layer was washed with saline solution, dried over magnesium sulfate and concentrated. The residue was purified by column chromatography on a silica gel, dissolved in isopropyl alcohol and crystallized from isopropyl alcohol-isopropyl ether. The resulting crystals were recrystallized from ethanol to give 1.30 g of 3-(3-(4-(1,2-benzisothiazol-3-yl)piperazin-1-yl)propionyl)-2-methyl-4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepin-5-one as white crystals, m.p. 146-147 C.

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

Reference£º
Patent; Yoshitomi Pharmaceutical Industries, Ltd.; US5532240; (1996); A;,
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: To the mixture of the precursor 10(2.26 g, 10.1 mmol, 1.5 equiv) and tert-butyl 1,2,5-thiadiazolidine-2-carboxylate 1,1-dioxide (1.50 g, 6.75 mmol, 1.0 equiv) in dry DMF(10 mL), was added Cs2CO3 (6.60 g, 20.25 mmol, 3.0 equiv). Themixture was stirred at room temperature overnight, and thenextracted with ethyl acetate. The organic phase was washed withsaturated NaHCO3 and brine, dried over anhydrous Na2SO4, filteredand concentrated. The resulting residue was purified via silica gelchromatography to give 11a as colorless oil (1.96 g, 79%).

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

Reference£º
Article; Chen, Shulun; Guo, Wei; Liu, Xiaohua; Sun, Pu; Wang, Yi; Ding, Chunyong; Meng, Linghua; Zhang, Ao; European Journal of Medicinal Chemistry; vol. 179; (2019); p. 38 – 55;,
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

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.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Incorporated; US5229388; (1993); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

76857-14-2, Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

76857-14-2, Into reactor cooling water was sequentially added purified water, intermediate II, start stirring. Drop 5% sodium bicarbonate solution, adjusting the pH value 5.7-6.0, stirring to make the solid completely dissolved. Then according to the feeding sequentially adding EDTA disodium, sodium bicarbonate. The reaction liquid pump CO2 gas, and drop trisodium salt aqueous solution, control reaction system pH value 7.5-8.5. Temperature 0-5 C. After dropping, control system pH value 7.9 – 8.1, reaction 8 hours.Then inject the CO2Gas, adjusting the pH value of the reaction solution of 7.5 – 7.8, HPLC monitoring isomerization, until the isomer ? 5.0%. The filtrate 9% hydrochloric acid aqueous solution to pH adjusting system 0.7 – 1.0, separating solid, centrifugal filtration, obtain cefotetan wet product.

The synthetic route of 76857-14-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Jichuan Pharmaceutical Group Co., Ltd.; Cao Longxiang; Dong Zibo; Niu Ben; Ding Xiaohua; Shao Jianguo; Zhu Jia; Li Ping; (15 pag.)CN106478670; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com