Tag: M.W:200-300

As a common heterocyclic compound, it belongs to isothiazole compound, name is 6-Bromobenzo[d]isothiazole-3-carboxylic acid, and cas is 677304-75-5, its synthesis route is as follows.

Step 5[00200] Sulfuryl dichloride (86.7 mg, 728 mumol) was added to a solution of 6- bromobenzo[d]-isothiazole-3-carboxylic acid (188 mg, 728 mumol). The reaction mixture was stirred for 30 min before removing the volatiles by rotovap. The residue was taken up in CH2Cl2 (0.587 ml) and a solution of 2-propylamine (62.5 muL, 728 mumol) and triethylamine (101 mul, 728 mumol) in CH2Cl2 (1.2 ml) was added. The reaction mixture was stirred at room temperature until LCMS analysis indicated complete conversion to the desired product. The reaction mixture was diluted with distilled water and ethyl acetate. The layers were separated and the aqueous was extracted with ethyl acetate. The combined organics were washed with brine and dried over Na2SO4, filtered and concentrated to give 6-bromo-N- isopropylbenzo[d]isothiazole-3-carboxamide.

677304-75-5, 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.,677304-75-5 ,6-Bromobenzo[d]isothiazole-3-carboxylic acid, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; AMGEN INC.; MEMORY PHARMACEUTICALS CORPORTION; WO2007/98169; (2007); A1;,
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.

Excess dried, -325 mesh potassium carbonate (20 g) was diluted in 500 mL acetone and 3-piperazin-1-yl-benzoisothiazole hydrochloride (13.37 g, 52.4 mmol was added. The mixture was stirred for 15 min before 2-nitrophenethyl tosylate (15.3 g, 47.7 mmol) and catalytic 18-crown-6 (0.5 g, 1.9 mmol) was added. The mixture was stirred at reflux for 42 h. After cooling, the salts were filtered off and washed with acetone 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. The residue was triturated with ethyl acetate and the collected solid was washed with ethyl ether and dried in vacuo to afford 13.08 g of a viscous, brown liquid. Yield 75%; MS (APCI): 369 [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.

(iii) Preparation of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one : Charge 1.0 litre demin water, 100 gm of step (ii) product, 122.4 gm 3-(1-piperazinyl)-1,2-benzisothiazole HCl] and 138.2 gm of sodium carbonate into a 3 litre three neck flask at 25 to 30C. Stir for 15 mins and heat to reflux temperature 95 to 100C. Maintain at reflux temperature for 15 hrs. Cool the reaction mixture to 45-50C. Add 1.0 lt of demin water into the reaction mixture and stir for 30 mins. Filter at 45 to 50C and wash with demin water. Suck dry for 30 mins to yield crude product. Charge 2 lt of demin water and above crude product and heat the mixture gradually to 45 to 50C and stir for 30 mins. Filter the product at 45 to 50C and wash with demin water. Suck dry the product for 30 mins. Charge 2.0 lt of demin water and 300 gm of crude product into a 1.0 litre three neck flask at 25 to 30C and heat the mixture gradually to 45 to 50C. Stir for 30 mins. Filter the product at 45 to 50C and wash with demin water till about neutral pH (6.5 to 7.0). Suck dry the product for 30 mins to get wet crude base [5-[2- [4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one. Add 300 gms of wet crude base and 1.0 lt of isopropanol at 25 to 30C. Warm the reaction mixture to 50 to [55C] and stir for 1.0 hr. Cool the reaction mixture gradually to 10 to 15C and stir for 30 mins. Filter the product and wash with chilled isopropanol. Suck dry for 30 mins. Charge 300 gm of wet crude base and 6 lt of tetrahydrofuran (THF). Heat the reaction mixture gradually to reflux temperature 65- 70C. Reflux till clear solution. Cool to 50 to 55C and add charcoal and stir for 30 min at 50 to 55C. Filter the charcoal and wash with hot THF. Distill out THF at 50 to 55C under vacuum till residual volume is 1 lt and cool the reaction mixture gradually to 5 to 10C and stir for 1 hr. Filter the product and wash with chilled THF. Suck dry the product for 30 mins. Dry the product at 60 to 65C.

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; SUN PHARMACEUTICAL INDUSTRIES LIMITED; WO2003/99198; (2003); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 6-Bromobenzo[d]isothiazole-3-carboxylic acid, and cas is 677304-75-5, its synthesis route is as follows.

Step 3: DIEA (11.7 mL, 67.4 mmol) and HBTU (7.03 g, 18.5 mmol) were added to a solution of 6-bromobenzo[d]isothiazole-3-carboxylic acid (4.35 g, 16.9 mmol) and N,O-dimethylhydroxylamine hydrochloride (2.14 g, 21.9 mmol) in DMF (100 mL). The reaction was stirred at room temperature for 2 hours. The mixture was partitioned between water and EtOAc. The organic layer was washed with aqueous NaHCO3 solution and brine, dried and concentrated. The residue was purified by column chromatography (hexane:EtOAc, 3:1) to give 6-bromo-N-methoxy-N-methylbenzo[d]isothiazole-3- carboxamide (4.60 g, 91%) as a solid. 1H NMR (CDCl3, 400 MHz) delta 8.12 (m, 2H), 8.59 (d, J = 8.8 Hz, IH), 3.83 (s, 3H), 3.49 (s, 3H).

677304-75-5, 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.,677304-75-5 ,6-Bromobenzo[d]isothiazole-3-carboxylic acid, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; WO2009/89462; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

677304-75-5, 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. 6-Bromobenzo[d]isothiazole-3-carboxylic acid, cas is 677304-75-5,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

The following esters were prepared from the acid using ethanol and sulfuric acid: Ethyl 6-bromobenzisothiazole-3-carboxylate. Ethyl 6-methoxybenzisothiazole-3-carboxylate. tert-Butyl 5-bromo-1,2-benzisothiazole-3-carboxylate.

The chemical industry reduces the impact on the environment during synthesis,677304-75-5,6-Bromobenzo[d]isothiazole-3-carboxylic acid,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Schumacher, Richard; Danca, Mihaela Diana; Ma, Jianguo; Herbert, Brian; Nguyen, True Minh; Xie, Wenge; Tehim, Ashok; US2007/78147; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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