Tag: M.W:200-300

94594-90-8, 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. (3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, cas is 94594-90-8,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

In a round-bottomed flask, 80 g of (1S)-(-)-2,10-camphorsultam, 236.4 g of methyl tert-butyl ether, 2.27 g of 4-(dimethylamino)-pyridine and 41.36 g of triethylamine were placed, and to this, 63.46 g of capryloyl chloride was added dropwise at room temperature. After stirring for 1 hour, the reaction solution was added to a mixed solution of 7.75 g of 35percent hydrochloric acid and 200 g of water, and the organic layer was separated. The organic layer was washed with 25percent aqueous sodium hydroxide solution and subsequently with water, and concentrated under reduced pressure. Thus, 125.34 g of the titled compound was obtained (quality: 99.7percent measured by GC).Gas chromatography analysis was carried out using Shimadzu GC-14A (Column: 5percent Silicone OV-17 manufactured by GL Science, Detector: FID).

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 (3aS,6S,7aS)-8,8-Dimethylhexahydro-1H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, 94594-90-8

Reference£º
Patent; Yamazaki, Shigeya; Hosoya, Takeshi; US2009/118542; (2009); 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 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.

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 Inc.; US4933453; (1990); 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.

EXAMPLES 115-116 A-C N-{5-[2-(4-BENZO[D]ISOTHIAZOL-3-YL-PIPERAZIN-1-YL)-ETHYL]-1, 1- DIMETHYL-INDAN-2-YLl-ACETAMIDE AND N-{6-[2-(4- BENZOrDllSOTHIAZOL-3-YL-PI PERAZIN-1-YL)-ETHYL1-1, 1- DIMETHYL-INDAN-2-YLl-ACETAMIDE (RACEMATES AND (+) AND (-) ENANTIOMERS) A suspension of piperazinylbenzisothiazole hydrochloride (16.50 g, 75.3 mmol), amidoindane as a mixture of regioisomers (10.00 g, 37.63 mmol) and Na2CO3 (5.98 g, 56.4 mmol) in water (180 ml) split evenly into 6 microwave reactor vessels, were heated to 175C for 30 min under microwave assistance. Upon cooling, MS indicated only desired product with no starting chloroethyl amidoindane. The reactions were diluted with ethyl acetate and water then combined. The layers were separated and the organics washed with water (100 ml), dried (MgS04) and concentrated to a viscous residue. The regioisomers were separated by chomatography (30% ethyl acetate/Hex) and identified by NMR 2D-NOE, then each stereoisomer was separated using chiral HPLC from a portion of each racemate and finally isolated as its HCI salt. Total reaction conversion was 95% based on recovered desired products. ; EXAMPLE 115 A; 11f5-f2- (4-BENZOf D11SOTHIAZOL-3-YL-PIPERAZIN-1-YL)-ETHYL1-1, 1- DIMETHYL-INDAN-2-YLl-ACETAMIDE 1H NMR (400 MHz, DMSO-D6) 8 ppm 0.94 (s, 3 H) 1.16 (s, 3 H) 1.84 (s, 3 H) 2.56 (m, 2 H) 2.68 (q, J=13. 35 Hz, 7 H) 2.95 (dd, J=15. 63,7. 62 Hz, 1 H) 3.43 (s, 4 H) 4.24 (q, J=8.60 Hz, 1 H) 7.02 (s, 3 H) 7.40 (t, J=7. 62 Hz, 1 H) 7.52 (t, J=7.52 Hz, 1 H) 7.95 (d, J=8.99 Hz, 1 H) 8.01 (dd, J=8. 21,3. 52 Hz, 2 H) chiral HPLC: two enantiomers, retention time (r. t. ) 9.78 and 19.73min., ChiralCel OJ (250×4.6mm), 80: 20 Hexane/EtOH; LCMS: Phenomenex Develosil Combi RP3 50×4.6mm column, 45C, 90-2% H20/MeCN w/0. 1 % HC02H over 3.5min, hold 0.5min, total run time 4. 0min. Results: 100% purity 254nM, M+= 449, r. t. = 2. 68min; EXAMPLE 116A; ll-f6-r2- (4-BENZOf D11SOTHIAZOL-3-YL-PI PERAZIN-1-YL)-ETHYL1-1, 1- DIMETHYL-INDAN-2-YLT-ACETAMIDE 1H NMR (400 MHz, DMSO-D6) 8 ppm 0.95 (s, 3 H) 1.17 (s, 3 H) 1.84 (s, 3 H) 2.56 (m, 2 H) 2.69 (m, 7 H) 2.94 (dd, J=15. 43,8. 01 Hz, 1 H) 3.42 (s, 4 H) 4.25 (q, J=8.66 Hz, 1 H) 6.98 (d, J=7.46Hz, 1 H) 7.00 (s, 1 H, NOE with 1. 17ppm, s, 3H) 7.05 (d, J=7.43Hz, 1 H, NOE with 2.69ppm, m, 7H) 7.40 (t, J=7. 72 Hz, 1 H) 7.52 (m, 1 H) 7.93 (d, J=9. 18 Hz, 1 H) 8.01 (d, J=8.21 Hz, 2 H) chiral HPLC: two enantiomers r. t. 7.28 and 15. 51 min., Chiralcel OJ (250×4.6mm), 80: 20 Hex/EtOH ; LCMS: Phenomenex Develosil Combi RP3 50×4.6mm column, 45C, 90-2% H20/MeCN w/0. 1 % HC02H over 3.5min, hold 0.5min, total run time 4. 0min. Results: 100% purity 254nM, M+= 449, r. t. = 2.64min.

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; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (2005); 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.

A mixture of 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (1.62 g, 6.34 mmol), product from Example 88B (1.90 g, 7.61 mmol), anhydrous potassium carbonate (1.93 g, 13.9 mmol), and potassium iodide (200 mg) in acetonitrile (80 ml) was refluxed for 48 hours. The reaction mixture was concentrated and the residue was partitioned between methylene chloride and water. The organic layer was dried over magnesium sulfate, filtered, and concentrated. The crude product was eluted through a flash column (silica gel 60, 230-400 mesh, EtOAc) to give a clear, viscous oil which crystallized on standing. Yield = 1.16 g (42%); MS(APCI), (M + 1)+ = 433. 1H-NMR (DMSO-d6, delta) 8.03 (d, 2H, J = 9.0 Hz), 7.53 (t, 1H, J =8.1, 7.8 Hz), 7.40 (t, 1H, J = 8.1, 7.3 Hz), 6.87 (d, 2H, J = 7.3 Hz), 3.69 (t, 2H, J = 5.9, 5.9 Hz), 3.26-3.43 (m, 6H), 2.46-2.78 (m, 12H), 1.78 (m, 2H). CHN: calculated for C25H28N4OS; C, 69.41%, H, 6.52%, N, 12.95%; found C, 69.28%, H, 6.60%, N, 12.65%.

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; WARNER-LAMBERT COMPANY LLC; WO2004/26864; (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.

9. Preparation of ZPR in sulfolane In a three necked flask was charged: BITP HC1 (5.14g, 20mmol), Na2C03 (2.33g, 22mmol), NaI (3g, 20mmol) and sulfolane (20ml). The mixture was heated at 90oC and than CEI (5.29g, 23mmol) was added with more sulfolane (10ml) ; the reaction mixture was maintained at 90C for 4. 5h. The mixture was cooled to the room temperature and THF was added (150ml) ; the solid was filtrated and washed with THF. From the mother liquors a second crop was obtained by precipitation with water. The yield of the two crops is 70% (purity by HPLC 98.4%).

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.

A mixture of 10 mmol of compound (IVa) as hydrochloride and 10 mmol of compound (IVb), 30 mmol of potassium carbonate, small crystal of potassium iodide and 20 ml of Nu,Nu-dimethylformamide was stirred at room temperature until disappearance of starting materials (TLC monitoring). Usually, the reaction was carried out for 2 days. The reaction mixture was subsequently poured into 50 ml of water, and precipitate thus formed was isolated by filtration. For purification, crude product was suspended in 20 ml of methanol, then the solid was filtered off and dried to constant weight. Alternatively (for 111-8), the reaction was carried out in acetonitrile, after completion of the reaction the solvent was evaporated and product was purified by column chromatography on silica gel using chloroform/methanol 95:5 as eluent.Structures of products were confirmed by mass spectrometry.According to the above procedure the following compounds were prepared:2-(4-(4-(1 ,2-benzothiazol-3-yl)piperazin-1 -yl)butyl)-1 H-isoindole-1 ,3(2H)-dione (111- 1 ), reaction in Nu,Nu-dimethylformamide, MS: 421 [M+H+], yield: 87%;

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; ADAMED SP. Z O.O.; KO?ACZKOWSKI, Marcin; KOWALSKI, Piotr; JA?KOWSKA, Jolanta; MARCINKOWSKA, Monika; MITKA, Katarzyna; BUCKI, Adam; WESO?OWSKA, Anna; PAW?OWSKI, Maciej; WO2012/35123; (2012); 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.

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.

76857-14-2, 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.,76857-14-2 ,Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate, other downstream synthetic routes, hurry up and to see

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

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.

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-(2-(5-fluoro-1H-indol-3-yl)ethyl)piperazin-1-yl)benzo[d]isothiazole (VI-1)Hydrochloride (white solid) 2.5 g, yield 60%.

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; 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

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.

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

Reference£º
Patent; MEDICHEM, S.A.; WO2006/34964; (2006); 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, EXAMPLE 67; 1-(2-Acetyl-2, 3-dihvdro-1 H-isoindol-5-vl)-2-(4-benzordlisothiazol-3-ylpiperazin- 1-vl) ethanone; A mixture (suspension) of the title compound of Preparation 38 (2.10 g, 8.84 mmol), 3-piperazin-1-yl-benzo [cisothiazole hydrochloride (2.49 g, 9.72 mmol), K2CO3 (3.63 g, 26.3 mmol), and Nal (1.40 g, 9.34 mmol) in anhyd CH3CN (90 mL) under N2 was stirred at 25 C 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 H2O, then dried in a vacuum oven at 50C for 3 d to give the title compound (2.68 g, 72%) as a light brown amorphous solid. Both TLC and ‘H NMR analyses indicated that the product was of high purity :’H NMR (300 MHz, CDCl3) # 8. 02 (d, J= 8.1 Hz, 1 H), 7.98 (br s, 1 H), 7.90 (d, J = 8. 2 Hz, 1 H), 7.82 (d, J= 8.0 Hz, 1 H), 7.48 (t, J= 7.5 Hz, 1 H), 7.32-7. 43 (m, 2 H), 4.87 (br s, 2 H), 4.85 (br s, 2 H), 3.91 (s, 1 H), 3.90 (s, 1 H), 3.59-3. 67 (m, 4 H), 2.81-2. 89 (m, 4 H), 2.20 (s, 1.5 H), 2.19 (s, 1.5 H); ESI MS milz421 [C23H24N402S + H] +.

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; WO2005/66165; (2005); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com