Analyzing the synthesis route of 87691-88-1

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

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 solution of 3- (1-piperazinyl) -1,2_ benzisothiazole hydrochloride (100g) and potassium carbonate (136g) in acetonitrile (800ml) added the suspension 1,4_ butanediol dimethyl sulfonate (lllg). Under vigorous stirring for 10 hours the resulting mixture was refluxed. After the solvent was distilled off under reduced pressure to acetonitrile was added, the reaction mixture was evaporated to clean water (100ml) and toluene (300ml), with stirring to break up the product mixture, refluxing under stirring operation, in addition to the net after the water, cool down, the suspension was filtered to give a white inorganic salts and organic salts of a mixture of the crude quaternary spiro ammonium base (272g).

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

Reference£º
Patent; Yantai Besten Pharmaceutical Co., Ltd.; Bi, Haidong; Zhang, Yifang; (8 pag.)CN105669665; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Downstream synthetic route of 87691-88-1

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

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

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]+.

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

Reference£º
Patent; Davis, Jamie Marie; Gregory, Tracy Fay; Walters, Michael Anthony; US2004/67960; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Application of 1,2,3,4-Tetrahydroisoquinoline

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The isothiazole compound, cas is 87691-88-1 name is 3-Piperazinobenzisothiazole hydrochloride, mainly used in chemical industry, its synthesis route is as follows.,87691-88-1

To a solution of 6-(2-chloro-ethyl)-4,4,8-trimethyl-3,4-dihydro-1H-quinolin-2-one (1.5eq) in dioxane/H2O (0.03M 1:1) was added sodium carbonate (2.2 eq), sodium iodide (catalytic), and added 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (1.0eq). The reaction mixture was heated to reflux for 24-72 hours. The reaction mixture was then concentrated and partitioned between H2O and CH2CI2. The organic layer was dried (MgSO4), concentrated and purified by chromatography (4:1 EA/Hex) to yield the title compound in 15-48% yield. LC/MS column: Phenomenex Develosil Combi-RP-3 3Μ 50×4.6mm, length 150×4.6

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/26864; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Application of D-Phenylalanine

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The isothiazole compound, cas is 87691-88-1 name is 3-Piperazinobenzisothiazole hydrochloride, mainly used in chemical industry, its synthesis 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] +.

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

 

Introduction of a new synthetic route about 87691-88-1

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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

A mixture of the product from step C of Example 24 (2.2896 g, 8.488mmol), 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (2.4295 g, 8.489 mmol), potassium carbonate (2.3472 g, 16.983 mmol) and potassium iodine (0.1406 g, 0.847 mmol) were reacted in acetonitrile (14.0 mL) in a CEM MARS5 microwave reactor for 20 min at 175 C. The reaction was cooled to room temperature, diluted with H2O and the resulting solid was filtered and washed with H2O and hexanes. The solid was >98% pure by LC-MS. The while solid was dried in a vacuum over at 50 C to give 3.2518 g (7.185 mmol, 85%) of the titled compound as a white solid. >98 % pure by LC-MS. MS( APCI): (M+1)+ = 453.2.

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

Reference£º
Patent; WARNER-LAMBERT COMPANY LLC; WO2004/26864; (2004); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Introduction of a new synthetic route about 3-Piperazinobenzisothiazole hydrochloride

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

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

EXAMPLE 61 3-(4-(1-[1,2-Benzisothiazol-3-yl]-4-piperazinyl)butyl)-5-methyl-4-thiazolidinone A mixture of 3-(4-bromobutyl)-5-methyl-4-thiazolidinone (4.00 g), 1-(1,2-benzisothiazol-3-yl)piperazine hydrochloride (4.46 g), K2 CO3 (8.00 g) and NaI (300 mg) in acetonitrile (210 ml) was heated at 40-45 C. for 64 hours and the product was processed in substantially the same manner as in Example 10 to afford 3.64 g of crystals, m.p. 113-115 C. ANALYSIS: Calculated for C19 H26 N4 OS2: 58.43%C; 6.71%H; 14.34%N. Found: 58.32%C; 6.69%H; 14.29%N.

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

Reference£º
Patent; Hoechst-Roussel Pharmaceuticals Incorporated; US5229388; (1993); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Simple exploration of 87691-88-1

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

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, (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.

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

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

 

New learning discoveries about 87691-88-1

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

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.

Examples 1. Preparation of ZPR in n-BuOH with 0.9 mol NaI. In a three necked flask was charged n-BuOH (50 ml) and 1, 2-Benzisothiazole-3- piperazinyl hydrochloride (BITP HC1) (5.6g, 0.022 mol), and the obtained slurry was heated at 100C. To the slurry, Na2CO3 (11.6 g), NaI (3g) and 5- (2-chloroethyl)-6- chloro-1, 3-dihydro-indole-2 (2H)-one (CEI) (7. 5g, 0.032 mol) were added at 110C. The heating was maintained for 8. 5h. After cooling the reaction product was filtrated, washed with hexane and water, and dried at 60 C. The dried product weights 8.12g and has an HPLC purity 92.7%.

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

 

New learning discoveries about 87691-88-1

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

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, 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.

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

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

 

Simple exploration of 87691-88-1

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

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

A 2 L reaction flask was charged with 88.5 g (lR, 2R) -1,2-cyclohexanedimethanol dimethanesulfonate, 71.8 g3- (1-piperazinyl) -1,2-benzisothiazole hydrochloride, 77.5 g of potassium carbonate and 1 L of acetonitrile were added and the mixture was heated under reflux with stirring. After the reaction is complete, hotFiltration, filter cake rinse with acetonitrile, the filtrate concentrated to dry under vacuum, in an off-white solid 104. 6g, 88% yield, HPLC purity is greater than99%, m.p. 228-230 C.

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

Reference£º
Patent; Suzhou Er Ye Pharmaceutical Co., Ltd; Liu, Zhi; Wu, Yongfeng; Fan, Shengya; (5 pag.)CN105732644; (2016); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com