Tag: M.W:200-300

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

The following procedure was used to prepare benzisothiazole fer/-butyl esters:Di-ferz’-butyldicarbonate (128 mmol) was added to a suspension of 6-bromo-l,2- benzisothiazole-3-carboxyIic acid (46.5 mmol) and 4-dimethylaminopyridine (4.26 mmol) in tert-buty alcohol (40.0 mL) and tetrahydrofuran (40.0 mL) and the reaction mixture was heated at 65 0C for 16 hours. There was vigorous carbon dioxide evolution which gradually subsided as the mixture become homogeneous. The reaction mixture was concentrated and the residue was dissolved in dichloromethane. The dichloromethane solution was filtered through silica gel (ca. 5Og) and the eluent was concentrated to provide the ester product in 99% yield.The following ester was prepared using this method:tert-Butyl S-brorno-l^-benzisothiazole-S-carboxylate. tert-Butyl -bromo-l^-benzisothiazole-S-carboxylate.

677304-75-5 6-Bromobenzo[d]isothiazole-3-carboxylic acid 53401192, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; WO2007/56582; (2007); 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, 119 ml (90.1 g, 0.698 mols, 3.21 molar equivalents) of N,N-diisopropylethylamine, 500 ml of acetonitrile and 55.8 g (0.218 mols, 1.0 molar equivalents) of 3-(l- piperazinyl) -1, 2-benzisothiazole hydrochloride (addition salt of compound of formula (III) and hydrochloric acid) are added into a beaker equipped with a magnetic stirrer. The resulting suspension is stirred for 10 minutes. At this point 50 g (0.217 mols, 1.0 molar equivalent) of 5- (2-chloroethyl) -6-chloro-l, 3-dihydro-indole-2- (2H) -one (Compound of formula (II) wherein X is chlorine) and 0.26 g (1.174 mmols, 0.008 molar equivalents) of NaI are added. The resulting brown suspension is charged into a 1 L reactor vessel, which is heated to 121-122 C (internal pressure increases to 200 kPa) for 25 hours. The reaction is cooled to room temperature and filtered. The solid is washed with acetonitrile, and 56 g of a wet solid are obtained. –> The resulting wet solid is stirred with 4 volumes of water at reflux temperature for 1 h to remove inorganic salts. The suspension is cooled to room temperature and filtered. The solid is washed with water. Ziprasidone base is obtained in 56% molar yield and the purity is 97.8% by HPLC.

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

Reference£º
Patent; MEDICHEM, S.A.; WO2006/34964; (2006); A1;,
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

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

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

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

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, 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

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

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, N-[4-(2-BROMO-ETHYL)-2-FLUORO-PHENYL]-ACETAMIDE (0.2609 g, 1.00 mmol), 3-piperazin-1-yl-benzo [AGISOTHIAZOLE HYDROCHLORIDE (0.3887 g, 1.52 mmol), potassium carbonate (0.2109 g, 1.53 mmol), potassium iodide (0.1662 g, 1.00 MMOL) and acetonitrile (5.0 mL) were added to a Smith microwave reaction tube containing a magnetic stir bar and then crimped shut. The reaction was run on a Smith Personal Chemistry microwave at 140 C for 0.5 h. After removing the crimped septum, the contents were transferred to a separatory funnel with water (10 mL) and extracted with methylene chloride (2 x 40 mL). The combined organic extracts were dried over anhydrous sodium sulfate, filtered and concentrated to give an oily residue. Purification by MPLC on a 40M silica gel cartridge using a linear gradient over 1 h of 0-3% methanol in methylene chloride provided 0.1230 g (0.309 MMOL) of the product as an off-white solid after drying in vacuo. Several fractions containing product and a by-product (0.1487 g total) were discarded. Yield : 31% ; MS (APCI) : 399.2 [M+H] + ; Anal. Calcd. For C2IH23FN40S’0. 25 H20 : C, 62.59 ; H, 5.88 ; N, 13.90. Found: C, 62.72 ; H, 5.53 ; N, 13.53.

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/41793; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com