Tag: 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 59; (R)(-)-N-{5-[2-(4-BENZO[D]ISOTHIAZOL-3-YL-PIPERAZIN-1-YL)- ETHYL1-INDAN-2-YLl-ACETAMIDE; A slurry of (R)-N- [5- (2-Chloro-ethyl)-indan-2-yl]-acetamide (2. 00g, 8. 41mmole), Na2CO3(1. 5eq) and 3-Piperazin-1-yl-benzo [d] isothiazole hydrochloride (2. 0eq) in H20 (20moi) was reacted under microwave assistance using a CEM MARS-5 microwave reactor to 175C for 10min. Upon cooling, the reaction was diluted with EtOAc (250moi), H20 (100mol) and the layers separated. The aqueous layer was extracted with EtOAc (2x 50ml). The organics were dried (MgSO4), concentrated, and the residue purified by chromatography (EtOAc) to give (R) (-)-N- {5- [2- (4- Benzo [d] isothiazol-3-yl-piperazin-1-yl)-ethyl]-indan-2-yl}-acetamide (2. 92g, 6. 94mmole) in 100% purity 254 nm; LCMS (APCI) 474 [M+H] +. [a] D25- 3. 6 (c 5.5, CHCl3). 1 H NMR (400 MHz, CHLOROFORM-D) 8 ppm 1.94 (s, 3 H) 2.65-2. 71 (m, 2 H) 2.73-2. 80 (m, 6 H) 2.81-2. 87 (m, 2 H) 3.28 (ddd, J=16. 04,6. 10,5. 92 Hz, 2 H) 3.57-3. 62 (m, 4 H) 4.69-4. 76 (m, 1 H) 5.70 (d, J=7.08 Hz, 1 H) 7.06 (d, J=7.81 Hz, 1 H) 7.11 (s, 1 H) 7.16 (d, J=7.56 Hz, 1 H) 7.35 (ddd, J=8.17, 7.08, 1.10 Hz, 1 H) 7.46 (ddd, J=8.11, 7.02, 1.22 Hz, 1 H) 7.81 (dt, J=8.05, 0.85 Hz, 1 H) 7.91 (dt, J=8.30, 0.98 Hz, 1 H).

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (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.

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

Reference£º
Patent; Yoshitomi Pharmaceutical Industries, Ltd.; US5532240; (1996); 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

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%).

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

Reference£º
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/40160; (2005); 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

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).

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC?; WO2005/56540; (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.

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%.

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

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

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.

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]+)

As the paragraph descriping shows that 87691-88-1 is playing an increasingly important role.

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, 3-Piperazinobenzisothiazole hydrochloride is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Excess dried, -325 mesh potassium carbonate (20 G) was diluted in 500 mL acetone and 3-PIPERAZIN-1-YL-BENZOISOTHIAZOLE hydrochloride (13.05 G, 51.2 mmol) was added. The mixture was stirred for 15 min before 4-nitrophenethyl tosylat (14.93 G, 46. 5 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 14.86 g of a bright yellow solid. Yield 84%; mp 99 C ; MS (APCI) : 369 [M+H] +.

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/41793; (2004); 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.

N- [4- (2-CHLORO-ETHYL)-2-METHYL-PHENYL]-N-METHYL-ACETAMIDE (0.300 g, 1. 153 mmol), 3-PIPERAZIN-1-YL-BENZO [d] isothiazole hydrochloride (0.442 g, 1.729 MMOL), potassium carbonate (0.237 g, 1.729 MMOL), and potassium iodide (0.173 g, 1.153 MMOL) in ACETONITRILE (3.5 mL) was subjected to 150 C for 30 min. under microwave assistance using a Smith Personal Chemistry microwave. The reaction was diluted with H20 (50 mL) and CH2CI2 (100 mL). The layers were separated and the organics washed with 1 N HCI (2x 25 mL). The aqueous layer was made basic and extracted with CH2CI2 (3X50 mL). The organics were dried (MGS04), and concentrated to a solid residue. The residue was subjected to chromatography (MEOH : CH2CI2 1 : 19) and collected as an amorphous residue and taken up in 1,4-dioxane and subjected to HCI gas for 10 min. The resulting solid was collected by filtration and dried at 50 C under high vacuum overnight (0.770 g). 100% purity at 254nm; LCMS (APCI) : 409.2 [M+H] +.

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; WO2004/41793; (2004); 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.

A mixture of 8 (700 mg, 2.2 mmol), 9 (817 mg, 3.2 mmol), Nal (651 mg, 4.3 mmol), and triethylamine (1.5 mL, 10.9 mmol) in acetonitrile (50.0 mL), was heated to reflux for 48 h, and allowed to cool. The mixture was concentrated to dryness in vacuo. The residue was suspended in water (50 mL) and sonicated for 5 min, and then filtered through a sintered glass frit. The solid was rinsed with additional water, dried under vacuum, and purified by chromatography (silica gel, gradient 3 – 5 % MeOH in CH2CI2) to provide compound 10 (630 mg, 63 %) as a white solid. 1H NMR (400 MHz, CDCl3): delta 10.75 (br s, 1H), 7.93 (d, 1H), 7.80 (d, 1H), 7.50-7.43 (m, 1H), 7.40-7.35 (m, 1H), 7.29-7.22 (m, 1H), 7.10 (d, 1H), 6.98 (s, 1H), 4.10 (t, 2H), 3.61-3.52 (m, 4H), 3.15 (t, 2H), 3.00 (t, 2H), 2.80-2.72 (m, 4H), 2.70 (t, 2H), 2.29-2.20 (m, 2H), 2.10-2.02 (m, 2H), MS m/z 460.97 [C26H28N4O2S + H]+

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/26864; (2004); 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.

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.

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