Category: 87691-88-1

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 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.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Incorporated; US5229388; (1993); 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.,87691-88-1

EXAMPLE 6 The mixture of 2.1 g of 4-(1,2-benzisothiazol-3-yl)piperazine hydrochloride, 2.0 g of 3-(3-chloropropionyl)-2-methyl-4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepin-5-one, 2,2 g of potassium carbonate and 1.2 g of potassium iodide in 15 ml of N,N-dimethylformamide and 15 ml of toluene was stirred at 60 C. for 5 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 crystallized from isopropyl alcohol-isopropyl ether. The resulting crystals were recrystallized from ethanol to give 1.30 g of 3-(3-(4-(1,2-benzisothiazol-3-yl)piperazin-1-yl)propionyl)-2-methyl-4,6,7,8-tetrahydro-5H-thieno[3,2-b]azepin-5-one as white crystals, m.p. 146-147 C.

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

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

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 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.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Inc.; US4933453; (1990); 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, D. 1- (2-Acetvl-2, 3-dihvdro-1 H-isoindol-5-vl)-3- (4-benzordlisothiazol-3-vl- piperazin-1-vI)-propan-1-one; A mixture (suspension) of 1- (2-Acetyl-2, 3-dihydro-1 H-isoindol-5-yl)-3-chloro-propan- 1-one (2.14 g, 8.84 mmol), 3-piperazin-1-yl-benzo [d] isothiazole hydrochloride (2.49 g, 9.72 mmol), K2CO3 (3.63 g, 26.3 mmol), and Nal (1.40 g, 9.34 mmol) in anhydrous CH3CN (90 mL) under N2 was stirred at 25 OC 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 H20, then dried in a vacuum oven at 50 C for 3 d to give the titled product (2.74 g, 71 %) as a light brown amorphous solid. ESI MS m/z 435 [M+1].

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

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

C. 1-{7-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-2,3,4,5- tetrahvdro-benzorblazepin-1-vll-ethanone methanesulfonate; A solution of the title compound from step B (602 mg, 2.39 mmol) in CH3CN (20 mL) was treated with 3-piperazin-1-yl-benzo [agisothiazole HCI (683 mg, 2.67 mmol), Nal (406 mg, 2.71 mmol), and K2CO3 (1.09 g, 7.86 mmol). The mixture was heated to reflux under N2 for 43 h, then allowed to cool. The mixture was diluted with H20 (100 mL) and extracted with CH2CI2 (3 x 100 mL). The combined organic layers were dried over Na2SO4, decanted, and the solvent was removed in vacuo. The residue was purified by flash column chromatography (silica gel, EtOAc) to give a white solid residue (430 mg, 0.99 mmol, 41%). The residue was dissolved in EtOAc (10 mL) and treated with a solution of CH3SO3H in Et20 (0.5 mL, 2M, 1 mmol). After stirring for 5 min, the resulting precipitate was isolated by filtration, washed with Et20 (3 x 10 mL), and dried in a vacuum oven at 50 C for 3 d to give the title compound (465 mg, 89%) as a white powder: mp 189-190 C (dec) ;’H NMR (300 MHz, CDCI3) 8 11.. 76 (s, 1 H), 7.85 (t, J = 7. 8 Hz, 2 H), 7.51-7. 56 (m, 1 H), 7.39-7. 45 (m, 1 H), 7.14-7. 18 (m, 2 H), 7.08 (d, J= 7.8 Hz, 1 H), 4.66-4. 70 (m, 1 H), 4.11-4. 20 (m, 2 H), 3.95-4. 03 (m, 2 H), 3.68 (d, J = 11.3 Hz, 2 H), 3.13-3. 34 (m, 6 H), 2.91 (s, 3 H), 2.68-2. 78 (m, 2 H), 2.51-2. 59 (m, 1 H), 1.74-2. 00 (m, 3 H), 1.83 (s, 3 H), 1.32-1. 40 (m, 1 H); ESI MS m/z 435 [C25H30N40S + H] + ; Rr 0. 35 (silica gel, 95: 5 EtOAc/MeOH); HPLC) >99% (AUC), tR = 12.68 min. Anal. Calc’d for C25H3oN40S’CH3SOsH : C, 58.84 ; H, 6.46 ; N, 10.56. Found: C, 58.56 ; H, 6.49 ; N, 10. 31.

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; WO2005/66165; (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.

87691-88-1, N-[4-(2-BROMO-ETHYL)-2-FLUORO-PHENYL]-ACETAMIDE (0.2609 g, 1.00 mmol), 3-piperazin-1-yl-benzo [AGISOTHIAZOLE HYDROCHLORIDE (0.3887 g, 1.52 mmol), potassium carbonate (0.2109 g, 1.53 mmol), potassium iodide (0.1662 g, 1.00 MMOL) and acetonitrile (5.0 mL) were added to a Smith microwave reaction tube containing a magnetic stir bar and then crimped shut. The reaction was run on a Smith Personal Chemistry microwave at 140 C for 0.5 h. After removing the crimped septum, the contents were transferred to a separatory funnel with water (10 mL) and extracted with methylene chloride (2 x 40 mL). The combined organic extracts were dried over anhydrous sodium sulfate, filtered and concentrated to give an oily residue. Purification by MPLC on a 40M silica gel cartridge using a linear gradient over 1 h of 0-3% methanol in methylene chloride provided 0.1230 g (0.309 MMOL) of the product as an off-white solid after drying in vacuo. Several fractions containing product and a by-product (0.1487 g total) were discarded. Yield : 31% ; MS (APCI) : 399.2 [M+H] + ; Anal. Calcd. For C2IH23FN40S’0. 25 H20 : C, 62.59 ; H, 5.88 ; N, 13.90. Found: C, 62.72 ; H, 5.53 ; N, 13.53.

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; WO2004/41793; (2004); 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,87691-88-1

EXAMPLE 75 3-[4-[1-(1,2-Benzisothiazol-3-yl)-4-piperazinyl]-butyl]-1-thia-3-azaspiro[4.4]nonan-4-one A mixture of 3-(4-bromobutyl)-1-thia-3-azaspiro[4.4]-nonan-4-one (4.50 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (4.33 g), K2 CO3 (7.45 g) and NaI (560 mg), in acetonitrile (220 ml) was heated at 65 C. for 14.5 hours and the product was processed in substantially the same manner as in Example 10 to afford 2.25 g of crystals, m.p. 200-203 C. ANALYSIS: Calculated for C22 H30 N4 OS2 *HCl: 56.57%C; 6.69%H; 11.99%N; 7.59%Cl. Found: 56.15%C; 6.75%H; 12.11%N; 7.88%Cl.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Inc.; US4933453; (1990); 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.,87691-88-1

8. Preparation of ZPR in glycerol by Na C03 portion-wise addition To a three necked flask was charged BITP HC1 (15g), CEI (16. 2g), glycerol (60ml) and Na2C03 (3. 11 g, 0. 5mol). The reaction mixture was heated at 115 C and after 15′ a new portion of 0.12 mol Na2C03 was added. The heating was continued by addition of 0.12 mol base each hour. After 5 hours the base addition was completed and the reaction mixture was heated for an additional hour. After cooling to room temperature, the mixture was diluted with water (120ml) and after 1 hour stirring the product crude was filtrated, washed with water and dried at 50C to afford 25.7g dried product (yield 82. 4%) (purity by HPLC 94%).

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

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

N-[4-(2-BROMO-ETHYL)-2-FLUORO-PHENYL]-ACETAMIDE (0.2609 g, 1.00 mmol), 3-piperazin-1-yl-benzo [AGISOTHIAZOLE HYDROCHLORIDE (0.3887 g, 1.52 mmol), potassium carbonate (0.2109 g, 1.53 mmol), potassium iodide (0.1662 g, 1.00 MMOL) and acetonitrile (5.0 mL) were added to a Smith microwave reaction tube containing a magnetic stir bar and then crimped shut. The reaction was run on a Smith Personal Chemistry microwave at 140 C for 0.5 h. After removing the crimped septum, the contents were transferred to a separatory funnel with water (10 mL) and extracted with methylene chloride (2 x 40 mL). The combined organic extracts were dried over anhydrous sodium sulfate, filtered and concentrated to give an oily residue. Purification by MPLC on a 40M silica gel cartridge using a linear gradient over 1 h of 0-3% methanol in methylene chloride provided 0.1230 g (0.309 MMOL) of the product as an off-white solid after drying in vacuo. Several fractions containing product and a by-product (0.1487 g total) were discarded. Yield : 31% ; MS (APCI) : 399.2 [M+H] + ; Anal. Calcd. For C2IH23FN40S’0. 25 H20 : C, 62.59 ; H, 5.88 ; N, 13.90. Found: C, 62.72 ; H, 5.53 ; N, 13.53.

As the rapid development of chemical substances, we look forward to future research findings about 87691-88-1

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.,87691-88-1

PREPARATION 23; 6-[2-(4-Benzo[d]isothiazol-3-yl-piperazin-1-yl)-ethyl]-7-chloro-4,8-trimethyl- 3s4-dihydro-1 H-quinolin-2-one; A mixture of 7-chloro-6- (2-chloro-ethyl)-4, 4, 8-trimethyl-3, 4-dihydro-1 H- quinolin-2-one (5.0016 g, 17.476 mmol), 3-piperazin-1-yl-benzo [d] isothiazole hydrochloride (4.4811 g, 17.520 mmol), potassium carbonate (4.8299 g, 34.946 mmol) and potassium iodine (0.2903 g, 1.749 mmol) were reacted in acetonitrile (29.0 mL) in a microwave reactor for 1 h at 200 C. The reaction was cooled to rt, diluted with H2O and filtered. The solid was washed with H20 and hexanes. The resulting solid was eluted through a flash column (silica gel 60,230-400 mesh, 0-3% MeOH in CH2CI2 gradient over 1 h) to give an off-white solid. Yield: 5.6591 g (12.065 mmol, 69%). Anal. : calculated for C25H29CIN40S’0. 02CH2CI2 : C, 63.84 ; H, 6.22 ; N, 11.90. Found: C, 63.49, H, 6.13 ; N, 11.72. LC-MS (APCI) : (M+1) + = 471. 0. H NMR (400 MHz, CDCI3) 8 7.90 (d, J=8. 2 Hz, 1 H), 7.80 (d, J=8.0 Hz, 1 H), 7.58 (s, 1 H), 7.45 (ddd, J=8. 0,7. 1,1. 0 Hz, 1 H), 7.34 (ddd, J=8. 2,7. 1,1. 0 Hz, 1 H), 7.08 (s, 1 H), 3.61 (m, 4 H), 2.98 (m, 2 H), 2.80 (s, 4 H), 2.68 (m, 2 H), 2.44 (s, 2 H), 2.31 (s, 3H), 1.30 (s, 6H).

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