Downstream synthetic route of 24340-77-0

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The above oily liquid was dissolved in 10 mL of DME and 2 mL of water, and 4-bromoisothiazole (275 mg, 1.68 mmol), Pd(PPh3)4 (48 mg, 0.042 mmol) and Na2CO3 (296 mg, 2.80 mmol), and the reaction was stirred at 100 C for 2 hours under nitrogen atmosphere. After cooling to room temperature, the reaction solution was poured into 60 mL of water and extracted three times with 20 mL of ethyl acetate. The combined ethyl acetate was washed with brine and dried over anhydrous sodium sulfate. Filtered, and concentrated by column chromatography (petroleum ether / ethyl acetate 1/1) to give 72mg as a white solid powder.

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Zhao Jiuyang; (35 pag.)CN109651359; (2019); A;,
Isothiazole – Wikipedia
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Analyzing the synthesis route of 7716-66-7

The synthetic route of 7716-66-7 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.7716-66-7,3-Chlorobenzo[d]isothiazole,as a common compound, the synthetic route is as follows.,7716-66-7

An eggplant type flask was charged with 3-chloro(1,2-benzisothiazole) (14 g, 200 mmol) and piperazine anhydride (6.8 g, 40 mmol) and heated at 125 ¡ã C. for 24 hours. After completion of the reaction, 52 ml of ice- In addition, quench, add 3.2 g of 50percent NaOH solution, stir for 5 min, extract with CH 2 Cl 2 50 ml * 3, wash the organic layer with 50 ml each of ice water * 2, 50 ml * 2 of saturated brine * 2 and anhydrous MgSO4 To give 4- (1,2-benzisothiazol-3-yl)piperazine.

The synthetic route of 7716-66-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JIANGSU HENGYI PHARMACEUTICAL COMPANY LIMITED; SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY; Li, JIANQI; PENG, SHAOPING; CAI, WANGPING; GAO, KAI; (39 pag.)JP5714152; (2015); B2;,
Isothiazole – Wikipedia
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Analyzing the synthesis route of 288-16-4

288-16-4, The synthetic route of 288-16-4 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.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

Under nitrogen protection, compound 1 was added(20 g, 0.235 mol) was added to dry 100 ml of ether and stirred to dissolve,And then cooled to below 0 ,To this was added n-butyllithium (0.24 mol)During the dropping process, the temperature was kept below 0 C,After the dropwise addition, the incubation reaction was carried out until no compound 1 was added.To the reaction solution was added bromine (0.5 mol)During the dropping process, the temperature was kept below 0 C,After completion of the dropwise addition, the temperature was gradually raised to room temperature, and after stirring for half an hour, the reaction was quenched by adding thereto a hydrochloric acid solution (2N, 500 ml). (100ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness. After drying, the aqueous phase was washed with diethyl ether (200ml * 3) and extracted.To give the yellow oily compound 2.

288-16-4, The synthetic route of 288-16-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890175; (2017); A;,
Isothiazole – Wikipedia
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Some tips on 7716-66-7

7716-66-7 3-Chlorobenzo[d]isothiazole 598190, aisothiazole compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7716-66-7,3-Chlorobenzo[d]isothiazole,as a common compound, the synthetic route is as follows.

7716-66-7, A mixture of 508.2 g of piperazine, 200 ml of tertiary butanol and 200 g of 3-chloro-1,2-benzisithiazole was refluxed for 15 hours. The reaction mass was quenched with 800 ml of water and filtered through a Hyflow (flux calcined diatomaceous earth) bed to make it particle-free. The pH of the reaction mass was adjusted to 13 with 50percent aqueous NaOH and then the reaction mass was extracted three times with 1200 ml volumes of toluene. The combined organic layers were washed with 200 ml of water, treated with 10 g of carbon, and the carbon was removed by filtration. The solvent was distilled until about 1000 ml remained, under reduced pressure at a temperature below 65¡ã C. The reaction mass was cooled to 0-5¡ã C. and stirred for 80 minutes. The formed solid was filtered and washed with 20 ml of toluene to yield 148.3 g of the title compound.

7716-66-7 3-Chlorobenzo[d]isothiazole 598190, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Venkataraman, Sundaram; Rao, Uppala Venkata Bhaskara; Muvva, Venkateswarlu; Chitta, Vijayawardhan; US2006/89502; (2006); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Downstream synthetic route of 24340-77-0

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7 (497 mg, 1.07 mmol) in DMF (10 mL) were added 4-bromoisothiazole (262 mg, 1.60 mmol), CsF (324 mg, 2.13 mmol), Pd(PPh3)4 (123 mg, 0.11 mmol) and copper(I) iodide (40.6 mg, 0.21 mmol) at rt. The mixture was stirred at 100 C for 13 h. After removal of insoluble materials by filtration, the filtrate was diluted with EtOAc (20 mL), water (10 mL), and sat. aq. NaHCO3 (10 mL). The aqueous layer was extracted with EtOAc (15 mL ¡Á 3). The organic layers were combined, washed with water and brine, dried over Na2SO4, and concentrated under vacuum. The residue was purified by column chromatography (silica gel, eluted with 5-60% EtOAc/hexane) to yield 8a (208 mg, 75%) as a pale yellow solid. 1H NMR (300 MHz, DMSO-d6) delta 1.24 (3H, t, J = 7.1 Hz), 4.19 (2H, q, J = 7.1 Hz), 6.76 (1H, d, J = 16.1 Hz), 7.53-7.62 (2H, m), 8.66 (1H, d, J = 5.1 Hz), 8.77 (1H, s), 9.06 (1H, s), 9.28 (1H, s). MS (API): m/z 260.9 (M + H)+

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

Reference£º
Article; Fujimoto, Jun; Hirayama, Takaharu; Hirata, Yasuhiro; Hikichi, Yukiko; Murai, Saomi; Hasegawa, Maki; Hasegawa, Yuka; Yonemori, Kazuko; Hata, Akito; Aoyama, Kazunobu; Cary, Douglas R.; Bioorganic and Medicinal Chemistry; vol. 25; 12; (2017); p. 3018 – 3033;,
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

 

Simple exploration of 4576-90-3

The synthetic route of 4576-90-3 has been constantly updated, and we look forward to future research findings.

4576-90-3,4576-90-3, Isothiazole-3-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[00163] To a solution of isothiazole-3-carboxylic acid (20 mg, 0.15 mmol), EDC (32.4 mg, 0.17 mmol), HOBt (23. mg, 0.17 mmol) in DMF (0.3 mL) was added 3- amino-N-cyclopropyl-4-methyl-benzamide hydrochloride (35 mg, 0.15 mmol) followed by DIPEA (0.03 mL, 0.17 mmol). The reaction was heated at 500C for 1 h. Water (0.6 mL) was added dropwise and the reaction removed from heating. The solids were stirred overnight at room temp, filtered, and washed with water to give (42.1 mg, 91% yield). HPLC tR= 2.63 min, 99.80 % purity; LCMS 302.1 (M + H).

The synthetic route of 4576-90-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; WO2008/57775; (2008); 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

 

Some tips on 936-16-3

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.936-16-3,2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide,as a common compound, the synthetic route is as follows.,936-16-3

General procedure: [1-(tert-Butyl)-5-{4-(piperidin-1-yl)phenyl}-1H-pyrazol-3-yl]methanol (54.9 mg, 0.18 mmol) was reacted with tripheny phosphine(93.1 mg, 0.36 mmol) and carbontetrabromide (121 mg,0.37 mmol) for 1 h. at 0 C. Without purification, the reaction mixturewas added to compound 8 (27.3 mg, 0.16 mmol) in DMF, andstirred for overnight. Then the reaction mixture was extracted withethyl acetate. The organic layer was dried over magnesium sulfate,filtered, concentrated in reduced pressure, and purified by columnchromatography (Hex: EtOAc = 4: 1 then 1: 1) to give title compound(15.2 mg, 20percent). 1H NMR (300 MHz, CDCl3) d 7.89 (d, J = 7.9 Hz, 1H), 7.64?7.52(m, 2H), 7.40 (d, J = 7.1 Hz, 1H), 7.30?7.17 (m, 2H), 6.29 (d,J = 8.7 Hz, 2H), 6.22 (s, 1H), 4.52 (s, 2H), 4.46 (s, 2H), 3.26?3.23(m, 4H), 1.79?1.74 (m, 4H), 1.67?1.63 (m, 2H), 1.49 (s, 9H).; 13CNMR (75 MHz, CDCl3) d 151.9, 144.4, 143.3, 135.4, 134.3, 132.5, 131.1, 128.9, 124.5, 123.7, 121.4, 114.9, 109.0, 61.0, 50.0, 41.4,31.2, 25.7, 24.3.

936-16-3 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide 13638, aisothiazole compound, is more and more widely used in various.

Reference£º
Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
Isothiazole – Wikipedia
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Brief introduction of 936-16-3

The synthetic route of 936-16-3 has been constantly updated, and we look forward to future research findings.

936-16-3, 2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,936-16-3

2-Chloro-4-(4-Boc-piperazin-l-yl)quinazoline (140 mg, 0.40 mmol), 253-dihydro-l,2- benzisothiazole l5l-dioxide (85 mg, 0.50 mmol) and potassium carbonate (110 mg, 0.80 mmol) in DMSO (2 ml) were heated at 90¡ã for 16 h and then at 110¡ã for 5 h. The reaction mixture was diluted with brine and extracted with dichloromethane (x3). The combined o organic phases were dried (MgSO4) and evaporated to dryness. The residue was dissolved in dichloromethane (2 ml) and TFA (0.5 ml) was added. The reaction mixture was stirred at ambient temperature for 16 h. The solvent was evaporated and the crude was purified by preparative HPLC to give the acetate of the title compound (71 mg, 40percent). 1H NMR (400 MHz, DMSO-J6) d ppm 7.90 – 8.02 (2 H, m) 7.61 – 7.84 (5 H, m) 7.33 – 7.41 (1 H3 m) 5.19 (2 H, s) 3.79 – 3.88 (4 H, m) 2.87 – 2.95 (4 H, m); ESI-MS m/z M+H+ 382.

The synthetic route of 936-16-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; WO2007/108744; (2007); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com