Day: September 1, 2020

Isothiazole, cas is 288-16-4, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,288-16-4

Under nitrogen protection, compound 1 was added(20 g, 0.235 mol) was added to dry 100 ml of ether and stirred and dissolvedTemperature below 0 ,To this was added n-butyllithium (0.24 mol), and the mixture was kept at 0 C or less during the dropping,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)The reaction mixture was kept at 0 C or lower, and the mixture was slowly added to the room temperature after completion of the dropwise addition. After stirring for half an hour, the reaction was quenched by adding hydrochloric acid solution (2N, 500 ml) thereto.And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phase was combined and washed with sodium dithionite solution(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.

With the rapid development of chemical substances, we look forward to future research findings about 288-16-4

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890179; (2017); 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.288-16-4,Isothiazole,as a common compound, the synthetic route is as follows.

To a solution of isothiazole (5.0 g, 58.82 mmol) in AcOH (37 mL) was added Br2 (12.5 g, 78.12 mmol) dropwise at 95 oC over 20 min and the mixture was stirred for 6 h at 95 oC, then cooled to RT, and poured into ice water (100 mL). The resulting mixture was extracted with Et2O (200 mL x 2). The organic phases were washed with 6N NaOH to pH at 7~8, dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated in vacuo, and the resulting residue was purified by distillation to afford 4-bromoisothiazole as a white solid (1.5 g, 15%).

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; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GREENLEE, William, J.; GOOD, Andrew, C.; (309 pag.)WO2017/176961; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

3,4-Dichloroisothiazole-5-carboxylic acid, cas is 18480-53-0, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,18480-53-0

EXAMPLE 6 Synthesis of potassium 3,4-dichloroisothiazole-5-carboxylate (Compound No. 7) Potassium hydroxide (0.27 g) dissolved in 3 ml of water was added to a solution of 3,4-dichloroisothiazole-5-carboxylic acid (0.95 g) in 4 ml of ethanol. The solvent was distilled off under reduced pressure. The crystals thus obtained were washed with a small quantity of ethanol.

With the rapid development of chemical substances, we look forward to future research findings about 18480-53-0

Reference£º
Patent; Mitsui Toatsu Chemicals, Incorporated; US5240951; (1993); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

Isothiazole, cas is 288-16-4, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,288-16-4

Compound 1 (20 g, 0.235 mol) was added to dry 100 ml of diethyl ether under nitrogen atmosphere and stirred to dissolve,And then cooled to 0 C or lower, n-butyllithium (0.24 mol) was added dropwise thereto, and the temperature was kept below 0 C during the dropwise addition, and the reaction was carried out until the compound 1 was added.To the reaction solution was added bromine (0.5 mol), and the mixture was kept at 0 C or less during the dropping,After completion of the dropwise addition, the temperature was gradually raised to room temperature, and after stirring for half an hour, the hydrochloric acid solution was added thereto(2N, 500 ml).And the aqueous phase was extracted with ether (200 ml * 3) and discarded. The combined organic phase and sodium dithionite solution were washed(100 ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness to give compound 2 as a yellow oil.In this step, the ether can also be replaced with a solvent such as methyl ether, dimethyl ether, tetrahydrofuran, 1,4-dioxane and the like.

With the rapid development of chemical substances, we look forward to future research findings about 288-16-4

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890177; (2017); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

Isothiazole, cas is 288-16-4, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,288-16-4

EXAMPLE 26 N-[alpha-(5-isothiazolyl)benzyl]-4-pyridinamine The title compound is prepared in a similar manner to Examples 5, 6 and 7 by reacting 5-isothiazolyl lithium (formed from isothiazole and butyl lithium) with 4-benzylideneaminopyridine.

With the rapid development of chemical substances, we look forward to future research findings about 288-16-4

Reference£º
Patent; John Wyeth & Brother Limited; US4180670; (1979); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

4-Bromoisothiazole, cas is 24340-77-0, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,24340-77-0

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)+

With the rapid development of chemical substances, we look forward to future research findings about 24340-77-0

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

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

4. Preparation of ZPR in water containing 10% n-BuOH. In a three necked flask was charged BITP HCl (4. 9g), Na2C03 (6.91g), CEI (4.68g), water (25ml) and n-BuOH (2. 5ml), and the mixture was heated. After about 20 hours reflux, ziprasidone was 75.5% area from the reaction mixture, and after 35h reflux the conversion to ZPR was 88%. The solid was filtrated from the reaction mixture, washed with water and dried. The HPLC purity of the product was 93.6% area.

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

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

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, Ethyl chloroformate (136ml) was added dropwise to a chilled solution of 2,3-dihydro- 1,2-benzisothiazol-1 ,1 -dioxide (68.Og) in pyridine (340ml) over 1h, maintaining the temperature below 180C. The slurry was stirred for 10min at 2O0C, diluted dropwise with water (1000ml) over 75min and stirred for a further 30min. The mixture was chilled to 0-50C, aged for 1 h and isolated by filtration. The cake was washed with cold water (2x250ml), and dried in vacuo to give the title compound as a white solid (72.35g).400 MHz NMR in dimethyl sulphoxide-d6. Dimethyl sulphoxide-d5 as reference at 2.50 ppm. delta (ppm): 1.30 (3) t J=7.1Hz, 4.32 (2H) q J=7.1Hz, 5.01 (2H) s, 7.64-7.70 (2H) m, 7.81 (1 H) td J=7.6Hz J=1.0Hz, 7.98 (1 H) d J=8.0Hz

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

Reference£º
Patent; GLAXO GROUP LIMITED; WO2006/129100; (2006); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

3,4-Dichloroisothiazole-5-carboxylic acid, cas is 18480-53-0, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,18480-53-0

EXAMPLE 5 Synthesis of isopropyl 3,4-dicloroisothiazole-5-carboxylate (Compound No. 6) Thionyl chloride (20 g) was added to 1.5 g of 3,4-dichloroisothiazole-5-carboxylic acid and the resultant mixture was heated under reflux for 1 hour. After excess thionyl chloride was distilled off under reduced pressure, a small amount of benzene was added, and the solvent was again distilled off under reduced pressure to remove a trace amount of thionyl chloride. Dry diethyl ether (10 ml) was added to the residue, whereby an acid chloride solution was obtained. 2-Propanol (0.54 g) and triethylamine (0.92 g) were dissolved in dry diethyl ether, to which the above-prepared acid chloride solution was added dropwise under ice cooling. They were then reacted at 30¡ã C. for 30 minutes and, after insoluble matter was filtered off, the filtrate was concentrated and then purified by chromatography on a silica gel column (n-hexane:ethyl acetate=9:1) to obtain 1.02 g of the title compound.

With the rapid development of chemical substances, we look forward to future research findings about 18480-53-0

Reference£º
Patent; Mitsui Toatsu Chemicals, Incorporated; US5240951; (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.10271-85-9,Isothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of isothiazole-5-carboxylic acid (331 mg, 2.6 mmol) in DMF (21 ml) cooled to 0C was added HATU (1.0 g, 2.8 mmol) and after stirring for 30 minutes a solution ofIntermediate 7-d (1.0 g, 2.1 mmol) and DIPEA (1.1 ml, 6.4 mmol) in DMF (3 ml) was addeddropwise. The reaction was then stirred at room temperature for 1 day. A saturatedaqueous solution of ammonium chloride and ethyl acetate were then added, the organic layer was separated, washed with a saturated aqueous solution of NaHCO3 and brine, dried over anhydrous MgSO4, filtered and concentrated under reduced pressure. Purification by silica gel chromatography provided Intermediate 15-a as a beige solid.

10271-85-9, As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

Reference£º
Patent; PHARMASCIENCE INC.; LAURENT, Alain; ROSE, Yannick; MORRIS, Stephen J.; (181 pag.)WO2017/49401; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com