Tag: M.W:200-300

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 flask equipped with mechanical stirrer, thermometer, condenser and nitrogen inlet was added 6-cUoro-5-(2-cHoroethyl)-l,3-dihydro-2H-indol-2- one (9.0 g, 39.1 mrnol), 3-(l-pirhoerazinyl)-l,2-benzoisothiazole hydrochloride (10.0 g, 39.1 mmol), sodium carbonate (9.96 g, 117.5 mmol) and poly(ethylene glycol) methyl ether (Mn= 350, 40 mL) and the suspension was heated to 120- 1250C under nitrogen for about 48 hrs. The suspension was cooled and poured into water. The suspension was cooled to 20-250C, the product was collected by filtration on a Buchner funnel and the filter cake was rinsed with water at 20-250C. The damp product was transferred to a flask equipped with mechanical stirrer, 100 mL of water were added and the suspension stirred at ambient temperature for 1 h. The suspension was filtered, washed with water and transferred to a drying oven and dried in vacuo. This afforded 14.2 g (88% yield) of crude ziprasidone.

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

Reference£º
Patent; APOTEX PHARMACHEM INC.; WO2006/47893; (2006); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

Name is Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate, as a common heterocyclic compound, it belongs to isothiazole compound, and cas is 76857-14-2, its synthesis route is as follows.,76857-14-2

The second intermediate obtained in step (4) is added in portions to the aqueous solution of 4-carboxy-3-hydroxy-5-mercaptoisothiazole trisodium in acetone at a low temperature of 2 to 8C.Then, the pH of the mixed solution was adjusted with sodium bicarbonate to be 7.5 to 9, and allowed to react at 15 to 30 C. and a stirring rate of 30 to 80 r/min for 3 to 8 hours.After filtering, the filter cake is washed with a small amount of deionized water to neutrality, and then dried under reduced pressure to obtain crude cefotetan acid; The cefotetan acid crude product obtained in step (5) is configured as an aqueous acetone suspension, and the excess sodium bicarbonate is stirred and dissolved in batch at room temperature.Then use activated carbon to stir for more than 1h, filter, -5 ~ 5 C,Stir and add 5 ~ 8mol/L hydrochloric acid solution to adjust the pH to less than 3, stir, filter and dry to obtain purified cefotetanic acid; The method for adding sodium bicarbonate is as follows: first, sodium bicarbonate is added in an amount of 30 to 50 g per batch, and after each batch is added,After stirring for 1-3 hours to dissolve, add the next batch, and so on, until the added sodium bicarbonate does not dissolve; At a low temperature of -5 to 10C, cefotetan obtained in step (6) is dissolved in purified water, and then sodium bicarbonate is added in portions.Stir and dissolve and adjust the pH of the solution to below 6, then add the activated carbon to stir for more than 1h, filter,The filtrate is first filtered through a 0.25 mum nylon filter and then filtered through a 0.2-0.3 mum filter.Finally, it is filtered through a nanofiltration membrane of 10 to 50 nm, then sterilized in a sterilization chamber, and freeze-dried at -40 C. to -15 C. for more than 12 hours to obtain the disodium cefotetan.

With the complex challenges of chemical substances, we look forward to future research findings about Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate

Reference£º
Patent; Jiangsu Han Sitong Pharmaceutical Co., Ltd.; Wang Duoping; Wei Genghu; Shi Jiagui; Lu Lihuan; (9 pag.)CN107540694; (2018); A;,
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, The above intermediate IV (0.01 mol) and the hydrochloride salt of the piperazine compound (V) (0.01 mol) were dissolved in DMF (100 mL).In the middle, K2CO3 (0.02 mol) was added. 3-(4-(3-(5-methyl-1H-indol-3-yl)propyl)piperazine-1-yl)benzo[d]isothiazole (VI-8) hydrochloride (white solid) 3.20 g, yield 75%.

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

Reference£º
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Li Jianqi; Gu Zhengsong; Zhou Ainan; Xiao Ying; (26 pag.)CN109467554; (2019); A;,
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.,87691-88-1

PREPARATION 7 6-r2- (4-Benzordlisothiazol-3-vl-piperazin-1-vl)-ethvll-2a, 3, 4, 5-tetrahydro-1 H- benzoRcdlindol-2-one; A 20 mL reaction vial was charged with 0.47 g (2 mmol, 1 eq) 6- (2-chloro- ethyl)-2a, 3,4, 5-tetrahydro-1 H-benzo [cd] indol-2-one, 0.51 g 3-piperazin-1-yl-benzo [d] – iso-thiazole hydrochloride, and 5 mL of 1 M aqueous sodium carbonate (Na2CO3) and heated to 100C for 60 h. The solid was filtered, washed with water and dried in vacuo overnight. The resulting solid was purified by medium pressure liquid chromatography (MPLC) (ethyl acetate (EtOAc) eluent) to give 0.36 g (43 % yield) of the desired material as a white solid. 1H NMR (400 MHz, CDCl3) 8 ppm 1.3 (qd, J=12. 3,3. 5 Hz, 1 H) 1.9 (m, 1 H) 2.2 (m, 1 H) 2.4 (dt, J=12. 2,4. 4 Hz, 1 H) 2.6 (m, 3 H) 2.8 (m, 6 H) 3.3 (dd, J=11. 8,5. 0 Hz, 1 H) 3.6 (s, 4 H) 6.6 (d, J=7. 6 Hz, 1 H) 7.0 (d, J=7. 8 Hz, 1 H) 7.3 (m, 1 H) 7.5 (m, 1 H) 7.8 (d, J=8. 1 Hz, 1 H) 7.9 (d, J=8.1 Hz, 1 H) 8.2 (s, 1 H). MS (APCI), (M+1) + = 292,419.

With the complex challenges of chemical substances, we look forward to future research findings about 3-Piperazinobenzisothiazole hydrochloride

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2005/66165; (2005); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

The above intermediate IV (0.01 mol) and the hydrochloride salt of the piperazine compound (V) (0.01 mol) were dissolved in DMF (100 mL).In the middle, K2CO3 (0.02 mol) was added. 3-(3-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl) was prepared according to the general procedurePropyl)-1H-indole-5-cyano (VI-7) hydrochloride (white solid) 3.15 g, yield 72%.

With the synthetic route has been constantly updated, we look forward to future research findings about 3-Piperazinobenzisothiazole hydrochloride,belong isothiazole compound

Reference£º
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Li Jianqi; Gu Zhengsong; Zhou Ainan; Xiao Ying; (26 pag.)CN109467554; (2019); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belong isothiazole compound,(3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide,94594-90-8,Molecular formula: C10H17NO2S,mainly used in chemical industry, its synthesis route is as follows.,94594-90-8

To a stirred solution of 4-methyl itaconate (1) (864 mg, 6.0 mmol) in dry CH2Cl2 (23 ml) were added 4-(dimethylamino)pyridine (161 mg, 1.3 mmol) and (S)-(?)-2,10-camphorsultam (15) (431 mg, 2.0 mmol). The mixture was cooled to 0 ¡ãC and N,N?-dicyclohexylcarbodiimide (1.36 g, 6.6 mmol) was added. The mixture was stirred at 0 ¡ãC for 1 h under N2 atmosphere. The solution was warmed to room temperature and further stirred overnight. The resulting precipitates of N,N?-dicyclohexylurea were filtered off and the filtrate was washed successively with 5percent aqueous NaHCO3, water, 1 N HCl, water and brine. The organic layer was dried over anhydrous Na2SO4 and evaporated in vacuo. The residue was purified by column chromatography on silica gel [ SiO2 51 g; hexane?EtOAc (5:1 then 3:1 v/v)] to afford amide 2 (612 mg, 90percent) as a colourless solid. Mp 86.2 ¡ãC (from diethyl ether); [alpha]D22 ?82.9 (c 1.95, CHCl3); IR (KBr) 3119, 1738, 1674, 1633, 1436, 1328, 1175, 1132, 1114, 1063, 979, 764 cm?1; 1H NMR (600 MHz) delta 6.05 (1H, d, J=1.0 Hz, =CHH), 5.88 (1H, d, J=1.0 Hz, =CHH), 4.06 (1H, dd, J=7.5, 4.9 Hz, NCH), 3.69 (3H, s, OMe), 3.52 (1H, d, J=13.7 Hz, CHHSO2), 3.47 (1H, d, J=16.1 Hz, CHHCO2Me), 3.45 (1H, d, J=13.7 Hz, CHHSO2), 3.25 (1H, d, J=16.1 Hz, CHHCO2Me), 2.05?2.00 (2H, m, CH2), 2.00?1.85 (3H, m, CH, CH2), 1.49?1.29 (2H, m, CH2), 1.22 (3H, s, Me), 1.00 (3H, s, Me); 13C NMR (100 MHz) delta 169.9, 169.0, 135.6, 127.7, 65.4, 53.2, 51.8, 47.8, 47.5, 44.9, 38.0, 32.9, 26.2, 20.9, 19.7; MS (EI+) (m/z) 341 (M+, 1percent), 310 (15), 277 (16), 218 (19), 127 (100), 99 (72), 69 (32), 59 (25); HRMS calcd for C16H24NO5S (MH+) 342.1375, found 342.1396.

With the synthetic route has been constantly updated, we look forward to future research findings about (3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide,belong isothiazole compound

Reference£º
Article; Kumazaki, Eri; Nagano, Hajime; Tetrahedron; vol. 69; 16; (2013); p. 3486 – 3494;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

100.0 g of 6-Chloro-5-(2-chloroethyl) oxindole, 133.39 g of 3-(l-Piperazinyle)- 1,2-benzisothiazole hydrochloride, 105.94 g of sodium carbonate and 1500 mL of water were taken in round bottom flask and heated to 1000C to HO0C for 24-26 hours. The reaction mixture was cooled and maintained for 30 min. The solid was filtered and washed with water. The wet solid was further slurried with water followed by adjusting the pH of the reaction mass with dilute acetic acid to 6.0 to 7.5 and maintain the reaction mass for 1-2 hours. The solid was filtered and washed with water. The wet solid was treated with isopropanol 1100 mL in round bottom flask and heated at 750C to 850C for 2 hours. The reaction mixture was cooled, the obtained solid was filtered and washed with isopropanol. The wet solid was dried at 6O0C to 650C for 8-10 hours to obtain crude Ziprasidone base.

With the complex challenges of chemical substances, we look forward to future research findings about 87691-88-1,belong isothiazole compound

Reference£º
Patent; CADILA HEALTHCARE LIMITED; SHAH, Niraj, Shyamlal; DWIVEDI, Shriprakash, Dhar; WO2010/73255; (2010); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

3-Piperazin-1-yl-benzoisothiazole hydrochloride (5. 29 G, 20.7 MMOL) and 4, 5-dimethoxy-2-nitrophenylacetic acid (5 g, 20.7 MMOL) were combined in 200 mL methylene chloride with triethylamine (5.77 mL, 41.4 MMOL). This solution stirred for 15 min before BIS- (2-OXO-3-OXAZOLIDINYL) phosphinic chloride (5.26 g, 20.7 MMOL) was added. After stirring overnight at rt, the reaction was quenched with water and extracted into methylene chloride. The organic layer was washed with 0.5 N HCI, water, sodium bicarbonate then water before it was dried over NA2SO4 and concentrated. The residue was taken up in methylene chloride and washed with water. The organic layer was dried over sodium sulfate, and concentrated then purified by MPLC using a Biotage prepacked silica gel cartridge eluting with 3% methanol in methylene chloride to afford 6.5 g of a tan solid. Yield 71% ; 100% purity at 214 nm; LCMS (APCI) : 443 [M+H] + ; MP 170C.

87691-88-1 is used more and more widely, we look forward to future research findings about 3-Piperazinobenzisothiazole hydrochloride

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

As a common heterocyclic compound, it belongs to isothiazole compound, name is Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate, and cas is 76857-14-2, its synthesis route is as follows.,76857-14-2

4-carboxy-5-mercapto-3-hydroxy-isothiazolium trisodium (5) (24.31 g, 0.10 mol) was added to a solution of(About 65ml) hydrochloric acid stirring, the pH to 2-3, by adding 297mgDMAPStirring was continued for 20 minutes,Followed by addition of 50 ml of tert-butanol,6 ml of pyridine, Boc2O (21.83 g, 0.10 mol),In a dry environmentThe reaction was stirred at room temperature for 18 h. The reaction was complete by HPLC and the solvent was removed by rotary evaporation to give an oil which was chromatographed on ethyl acetate, The organic layer was dried over anhydrous magnesium sulfate, concentrated, and recrystallized from ethanol to give Intermediate 6 (24.11 g) in a molar yield87%, HPLC purity 99.2%.

With the complex challenges of chemical substances, we look forward to future research findings about 76857-14-2,belong isothiazole compound

Reference£º
Patent; Shandong Luoxin Pharmaceutical Group Co Ltd; Sun, Song; Xu, Qinyan; Chang, Zhicheng; (7 pag.)CN105646544; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

The above intermediate IV (0.01 mol) and the hydrochloride salt of the piperazine compound (V) (0.01 mol)Dissolved in DMF (100 mL) and added K2CO3 (0.02 mol).According to the general operation three,Preparation of 3-(4-(3-(5-fluoro-1H-indol-3-yl)propyl)piperazin-1-yl)benzo[d]isothiazole (VI-2)The hydrochloride (white solid) was 3.44 g, yield 80%.

87691-88-1 is used more and more widely, we look forward to future research findings about 3-Piperazinobenzisothiazole hydrochloride

Reference£º
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Li Jianqi; Gu Zhengsong; Zhou Ainan; Xiao Ying; (26 pag.)CN109467554; (2019); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com