Category: 87691-88-1

Name is 3-Piperazinobenzisothiazole hydrochloride, as a common heterocyclic compound, it belongs to isothiazole compound, and cas is 87691-88-1, its synthesis route is as follows.

3. Preparation of ZPR in water/Na3CO . Na2SO4. In a three necked flask was charged BITP HC1 (lOg), CEI (10.35g) Na2C03 (14.1 g, ), Na2SO4 (40g) and water (50. 7g) and the reaction mixture was heated at reflux for 9 hours. After 9 hours reflux, the ziprasidone peak is No.71% area from the reaction mixture.; 6. Preparation of ZPR in the presence of Na2SO4. In a 250g three necked flask was charged water (25ml), Na2C03 (6.91g), Na2S04 (19.72g), BITP HCl (4.9g) and CEI (4.68g). The mixture was stirred at-100C for 12 hours. The isolated solid weights after drying 7.77g (purity by HPLC 85.15%).

87691-88-1, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,87691-88-1 ,3-Piperazinobenzisothiazole hydrochloride, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/40160; (2005); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

Excess dried, -325 mesh potassium carbonate (257 mg, 1.86 MMOL) was diluted in 4 mL acetonitrile and 3-piperazin-1-yl-benzoisothiazole hydrochloride (395 mg, 1.55 MMOL), catalytic potassium iodide, and 1 (2- chloroethoxy)-4-nitrobenzene (250 mg, 1.20 MMOL) were added. This mixture was sealed in a Smith microwave vial and heated on the Smith Workstation at 150 C for 1.5 h. After cooling, the salts were filtered off and washed with ACETONITRILE and the filtrate was concentrated. The residue was taken up in methylene chloride and washed with water. The organic layer was dried over sodium sulfate, and concentrated to afford 530 mg of a yellow solid. Yield 89%; 92% HPLC purity at 214 nm; mp 115 C ; MS (APCI) : 385 [M+H] +.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 3-Piperazinobenzisothiazole hydrochloride, 87691-88-1

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

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

3) To 0.5 g of the product of step 2) were added 0.6 g of 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride, 2 g of anhydrous potassium carbonate, 0.2 g of potassium iodide and 25 ml of acetonitrile, and the mixture was heated under reflux for 20 hours, and then cooled to room temperature and filtrated. The solvent was distilled to give yellowish oil, which was passed through a column to give 0.52 g of white solid. Melting point: 110-112C, yield: 72.2%. 1H NMR(CDCl3) delta 1.75-1.90(m,4H), 2.38(s,3H), 2.51(t,2H,J=14.4Hz), 2.68-2.71(m,4H), 3.56-3.58 (m, 4H), 4.06 (t, 2H, J=12Hz), 6.11 (s, 1H), 6.80-6.86 (m, 2H), 7.29-7.36 (m, 1H), 7.43-7.48(m,2H), 7.79(d,1H,J=8Hz), 7.90 (d,1H,J=8.4Hz) MS(ESI)m/z 450.2 ([M+H]+)

The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Huazhong University of Science and Technology; NHWA Pharma. Corporation; ZHANG, Guisen; CHEN, Yin; XU, Xiangqing; LIU, Bifeng; LIU, Xin; ZHAO, Song; LIU, Shicheng; YU, Minquan; ZHANG, Heng; LIU, Xinghua; EP2698369; (2014); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

To a solution containing 3- (1-piperazinyl) -1,2_ benzisothiazole hydrochloride (100g) and potassium carbonate (136g) in acetonitrile(800ml) was added a solution of 1-chloro-4-bromo-butane (88g). Vigorous stirring mixture was refluxed for 10 hours, the solvent was distilled off pressure acetonitrile was added water (100ml) and toluene (300ml) to the reaction mixture was distilled net was effected under stirring to break up the product mixture, refluxing under stirring operation , the net after the water addition, cooling down, the suspension was filtered to give a white inorganic salts and organic salts of a mixture of the crude quaternary spiro ammonium base (267g).

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 3-Piperazinobenzisothiazole hydrochloride, 87691-88-1

Reference£º
Patent; Yantai Besten Pharmaceutical Co., Ltd.; Bi, Haidong; Zhang, Yifang; (8 pag.)CN105669665; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

88.7 g (0.837 mols, 3.21 molar equivalents) of sodium carbonate, 600 mL of acetonitrile and 66.7 g (0.261 mols, 1.0 molar equivalent) of 3- (1-piperazinyl) -1, 2- benzisothiazole hydrochloride are added into a beaker equipped with a magnetic stirrer. The resulting white suspension is stirred for 10 minutes. At this point 60.0 g (0.261 mols, 1.0 molar equivalent) of 5- (2- chloroethyl) -6-chloro-l, 3-dihydro-indole-2- (2H) -one and 0.3 g (0.002 mols, 0.008 molar equivalents) of NaI are added. The resulting brown suspension is charged into a 1 L reactor vessel, which is purged with nitrogen and heated to 120-125 C (internal pressure increases to 400- 500 kPa) for 25 hours. The reaction is cooled to room temperature, stirred for 30 minutes, filtered and the solid washed with acetonitrile. A wet mixture of zipradisone and inorganic salts is obtained, that is further washed with acetonitrile. The resulting wet mixture of ziprasidone and inorganic salts is stirred with 675 ml of water at reflux temperature for 1 h to remove inorganic salts. The suspension is cooled to room temperature, stirred for 30 minutes and filtered. The solid is washed with water, and 140 g of wet solid (corresponding to 87 g of dry material) are obtained. EPO The wet solid is stirred again with water at reflux temperature for 1 h to remove residual inorganic salts. The suspension is cooled to room temperature, stirred for 30 minutes and filtered. The solid is washed with water, and 170 g of wet solid (corresponding to 81 g of dry- material) are obtained. HPLC analysis reveals a purity of 97.8%.To remove starting materials present in the wet solid obtained in the previous step, it is stirred twice with400 ml of tetrahydrofuran at reflux temperature. The solution is cooled to room temperature, stirred for 30 minutes and filtered. The solid is washed twice with 40 ml of tetrahydrofuran, and 60 g of wet solid, corresponding to 54.8 g of dry material, are obtained.The solid obtained is ziprasidone base having a purity of 99.4% by HPLC and the global yield from the starting compounds is 51% (molar yield) . Potentiometric titration with HClO4: 100.03%

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 3-Piperazinobenzisothiazole hydrochloride, 87691-88-1

Reference£º
Patent; MEDICHEM, S.A.; WO2006/34965; (2006); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

EXAMPLE 4 The mixture of 1.0 g of 4-(1,2-benzisothiazol-3-yl)piperazine hydrochloride, 1.5 g of 7-(4-chlorobutyryl)-2,3-dihydrothieno[3,2-f][1,4]thiazepin-5(4H)-one, 2.5 g of potassium carbonate and 0.8 g of potassium iodide in 25 ml of N,N-dimethylformamide and 25 ml of toluene was stirred at 100 C. for 24 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 oxalic acid was added thereto to make oxalate. The resulting crystals were recrystallized from isopropyl alcohol to give 0.12 g of 7-(4-(4-(1,2-benzisothiazol-3-yl) piperazin-1-yl)butyryl)-2,3-dihydrothieno[3,2-f][1,4]thiazepin-5(4H)-one oxalate 1/2 hydrate as white crystals, m.p. 118-120 C.

The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Yoshitomi Pharmaceutical Industries, Ltd.; US5532240; (1996); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

10. Preparation of ziprasidone in toluene In a 250 ml three necked flask was charged BITP HCl (5g), Na2C03 (6. 5g), CEI (5g), NaI (1. 5g) and toluene (30ml) ; the mixture was heated at reflux for 22.5 hours. After cooling to the room temperature the reaction product was filtrated, washed with methanol and triturated in water. After drying the product weights 7.27g (yield 86%, purity by HPLC 98.3%).

The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/40160; (2005); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

It is a common heterocyclic compound, the isothiazole compound, 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1 its synthesis route is as follows.

3-Piperazin-1-yl-benzoisothiazole hydrochloride (1.31 g, 5.1 mmol) and (5-fluoro-2-nitro-phenyl)-acetic acid (800 mg, 4.3 mmol) were combined in 100 mL methylene chloride with triethylamine (1.20 mL, 8.6 mmol). This solution stirred for 15 min before bis-(2-oxo-3-oxazolidinyl) phosphinic chloride 1.09 g, 4.3 mmol) was added. After stirring overnight at room temperature (rt), the reaction was quenched with water and extracted into methylene chloride. The organic layer was washed with 0.5 N HCl, water, sodium bicarbonate then water before it was dried over sodium sulfate (Na2SO4) and concentrated. The organic layer was dried over sodium sulfate, concentrated, and purified by MPLC using a Biotage prepacked silica gel cartridge eluting with 3% methanol in methylene chloride (CH2Cl2) to afford 870 mg of an off-white foam. Yield 50%; mp 72 C.; MS (APCI): 401 [M+H]+.

87691-88-1, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,87691-88-1 ,3-Piperazinobenzisothiazole hydrochloride, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Davis, Jamie Marie; Gregory, Tracy Fay; Walters, Michael Anthony; US2004/67960; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

EXAMPLE 1; N-(5-r2-(4-BENZOrD1ISOTHIAZOL-3-YL-PIPERAZIN-1-YL)-ETHYU-15 INDAN-2-YU-2.2.2-TRIFLUORO-ACET AMIDE; N-[5-(2-Chloro-ethyl)-indan-2-yl]-2,2,2-trifluoro-acetamide (S.OOg, 10.28mmol), 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (5.26g, 20.57mmol) and sodium carbonate (2.18g, 20.57 mmol) in H2O (20mL) wassubjected to 175 C for 10 min. under microwave assistance using a GEM20 MARS-5 microwave. The reaction was diluted with H2O (50 mL) andEtOAc (100 ml). The layers were separated and the organics washedwith 4N HCI (2x 25 mL). The aqueous layer was made basic andextracted with CH2CI2 (3×50 mL). The organics were dried (MgSO4), andconcentrated to a solid residue. The residue was subjected to25 chromatography (3% MeOH/CH2CI2). N-{5-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-indan-2-yl}-2,2,2-trifluoro-acetamide (3.20g),wasisolated in 100% purity (at) 254 nm; LCMS (APCI): 475 [M+H]+. 1H NMR(400 MHz, CDCI3) 5 7.90 (d, J=8.2Hz, 1H), 7.80 (d, J= 8.2Hz, 1H), 7.46 (t,J = 7.4HZ, 1 H), 7.34 (t, J= 7.4Hz, 1 H), 7.17 (d, J= 7.4Hz, 1 H), 7.12 (s, 1 H),30 7.08 (d, J= 7.4Hz, 1 H), 6.46 (bs, 1 H), 4.82-4.71 (m, 1 H), 3.63-3.55 (m,4H), 3.40-3.29 (m, 2H), 2.90-2.80 (m, 4H), 2.79-2.72 (m, 4H), 2.71-2.65(m, 2H).

The chemical industry reduces the impact on the environment during synthesis,87691-88-1,3-Piperazinobenzisothiazole hydrochloride,I believe this compound will play a more active role in future production and life.

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

87691-88-1, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 3-Piperazinobenzisothiazole hydrochloride, cas is 87691-88-1,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

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.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 3-Piperazinobenzisothiazole hydrochloride, 87691-88-1

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