Category: isothiazole

2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, cas is 936-16-3, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,936-16-3

Example 27. 4-(1,1-Dioxido-1,2-benzisothiazol-2(3H)-yl)-2-piperazin-1-ylquinazoline. 2,4-Dichloroquinazoline (60 mg, 0.30 mmol), 2,3-dihydro-l,2-benzisothiazole 1,1-dioxide (50 mg, 0.30 mmol) and sodium hydride (11 mg, 0.45 mmol) were dissolved in anhydrous DMF (2 ml). The mixture was heated at 60¡ã C under nitrogen atmosphere for 10 min. Piperazine (52 mg, 0.60 mmol) was added and the heating was continued for 10 minutes. 5 The reaction mixture was diluted with water (0.5 ml), filtered and purified by preparative HPLC to give the acetate of the title compound as a solid (36 mg, 27 percent). 1H NMR (400 MHz, MeOD-d4) delta ppm 8.49 (1 H3 d) 7.58 – 7.87 (6 H, m) 730 – 7.38 (1 H, m) 5.58 (2 H, s) 4.03 – 4.16 (4 H3 m) 3.15 – 3.26 (4 H3 m); ESI-MS m/z M+H+ 382.

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Reference£º
Patent; ASTRAZENECA AB; WO2007/108743; (2007); A2;,
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Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide, cas is 27148-03-4, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,27148-03-4

General procedure: For 6: A solution of thiosaccharin (tsacH) (0.06 g, 0.307 mmol) in chloroform (8 cm3) was added to a solution of [PtCl2(kappa2-dppm)] (0.10 g, 0.154 mmol) in chloroform (10 cm3). A few drops of triethylamine were added and the resulting mixture was heated under reflex for 1 h. This produced a yellow solution was filtered off and reduced to half volume. Methanol (2 cm3) was added and the mixture was set a side to evaporate slowly at room temperature. The yellow crystalline solid thus formed was filtered off and dried in a vacuum oven (0.12 g, 91%).

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Reference£º
Article; Al-Jibori, Subhi A.; Al-Jibori, Mohamed H.S.; Hogarth, Graeme; Inorganica Chimica Acta; vol. 398; (2013); p. 117 – 123;,
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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

2,3-dihydro-1,1-dioxo-1,2-benzoisothiazole (150 mg, 0.887 mmol), N-Boc-bromoethylamine (238mg, 1.064mmol) And cesium carbonate (867mg, 2.66mmol) in 5ml DMF, It was then stirred overnight. On the following day, after the reaction was detected by TLC, water was added for extraction. It was washed with saturated brine and dried over anhydrous sodium sulfate. Suction filtration, the filtrate was concentrated under reduced pressure, the crude product was separated by column chromatography, 124 mg of a white solid were obtained with a yield of 45%.

As the paragraph descriping shows that 936-16-3 is playing an increasingly important role.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Zhang Ao; Meng Linghua; Ding Jian; Chen Shulun; Ding Chunyong; Guo Wei; (26 pag.)CN110143955; (2019); A;,
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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

The above intermediate IV (0.01 mol) and the hydrochloride salt of the piperazine compound (V) (0.01 mol)Dissolved in DMF (100 mL) and added K2CO3 (0.02 mol).According to the general operation three,Preparation of 3-(4-(4-(5-fluoro-1H-indol-3-yl)butyl)piperazin-1-yl)benzo[d]isothiazole (VI-3) hydrochloride ( White solid) 3.11 g, yield 70%.

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Reference£º
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Li Jianqi; Gu Zhengsong; Zhou Ainan; Xiao Ying; (26 pag.)CN109467554; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.,18480-53-0

730mg of 3,4-dichloroisothiazole-5-carboxylic acid (3.7 mmol) were dissolved in 10 ml of dichloromethane and a drop of dimethylformamide was added. 1.4 g of oxalyl chloride (11.1 mmol) were added dropwise at room temperature. After stirring for 1 h at room temperature, the solution was evaporated to dryness on a rotary evaporator. The residue was taken up in 3 ml ofdichloromethane and slowly added dropwise to a solution of 626 mg of 1- cyclohexylmethanamine (5.5 mmol) and 746 mg of triethylamine (7.4 mmol) in 10 ml of dichloromethane. The mixture was stirred at room temperature for 1 h. The reaction mixture was then added to water and extracted repeatedly with dichloromethane. The concentrated extracts were dried over MgSO4, concentrated and purified by column chromatography. Yield:1.05 g (97percent of theory).?H-NMR (400 MHz, CDC13 , ppm) 6.86 (br, 1H), 3.34 (tr, 2H), 1.77 (m, 4H), 1.66 (m, 1H), 1.58 (m, 1H), 1.3-1.15 (m, 3H), 1.0 (m, 2H).

18480-53-0 3,4-Dichloroisothiazole-5-carboxylic acid 49837, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; BERNIER, David; CRISTAU, Pierre; TSUCHIYA, Tomoki; RINOLFI, Philippe; DROeGE, Thomas; MAECHLING, Simon; SCHMIDT, Jan Peter; TELSER, Joachim; DOeLLER, Uwe; MOSRIN, Marc; REY, Jullien; TIEBES, Joerg; WACHENDORFF-NEUMANN, Ulrike; (467 pag.)WO2016/102435; (2016); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76857-14-2,Sodium 3-oxido-5-sulfidoisothiazole-4-carboxylate,as a common compound, the synthetic route is as follows.

76857-14-2, To the reaction solution B, 2000 ml of a saturated sodium hydrogencarbonate solution was added, and the mixture was stirred, and the phases were separated. The aqueous phase was taken and the temperature was lowered to 5 C or lower. To the solution was added 60 g / 400 ml of 4-carboxy-3-hydroxy-5-mercaptoisothiazolium trisodium (CHMT) aqueous solution. The pH of the reaction solution is controlled to be 6.0 to 9.0, the content of the cefotetan tautomer is less than or equal to 6.0%, the pH is adjusted to 6.5, 50g of active alumina is added, stirred for 1 hour, filtered, hydrochloric acid to adjust the pH of the filtrate is 1.5 to 2.5, filtration, in the original cefotetan acid.

As the paragraph descriping shows that 76857-14-2 is playing an increasingly important role.

Reference£º
Patent; Shenzhen Salubris Pharmaceuticals Co., Ltd.; Lei, Jiangang; Liang, Guilin; Yang, Siyuan; Zhao, Li; (11 pag.)CN103724359; (2016); B;,
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3-Chlorobenzo[d]isothiazole, cas is 7716-66-7, it is a common heterocyclic compound, the isothiazole compound, its synthesis 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.

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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;,
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2,3-Dihydrobenzo[d]isothiazole 1,1-dioxide, cas is 936-16-3, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,936-16-3

General procedure: Potassium carbonate was dissolved in DMF, and 1,2-bezeneisothiazolin-1,1-dioxide (8) (1 equiv.) in dichloromethanewas added to the reaction solution, and stirred for overnight. Then,the reaction mixture was filtered through Celite, and washed with1 N HCl and saturated sodium hydrogen carbonate solution. Residualsolution was dried over magnesium sulfate, and concentratedin vacuo, and purified by column chromatography to afford the titlecompound.

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Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
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3-Bromoisothiazole, cas is 55512-82-8, it is a common heterocyclic compound, the isothiazole compound, its synthesis route is as follows.,55512-82-8

In a 50-mL round-bottom flask purged and maintained with an inert atmosphere of nitrogen, was placed [4-[3-(benzyloxy)propyljquinolin-7-yljboronic acid (904 mg, 2.81 mmol, 1 equiv), Na2CO3 (596.6 mg, 5.63 mmol, 2 equiv), 3-bromo-1,2-thiazole (923.3 mg, 5.63 mmol, 2 equiv), and Pd(PPh3)4 (325.2 mg, 0.28 mmol, 0.1 equiv) in dioxane (20 mL) and H20 (5 mL). The resulting solution was stirred for 4 hours at 80 ¡ãC in an oil bath. The resulting mixture was cooled to room temperature and concentrated. Theresidue was applied onto a silica gel column with ethyl acetate/petroleum ether (1:1). This resulted in 500 mg (49.28percent) of 4- [3 -(benzyloxy)propylj -7-( 1 ,2-thiazol-3-yl)quinoline as a light brow solid. LC-MS: (ES, m/z): [M+Hj = 361.1.

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Reference£º
Patent; INNATE TUMOR IMMUNITY, INC.; O’MALLEY, Daniel; GAVAI, Ashvinikumar V.; GILL, Patrice; TARBY, Christine M.; WATTERSON, Scott Hunter; GONG, Hua; WILLIAMS, David K.; GHOSH, Shomir; ROUSH, William R.; (307 pag.)WO2019/14402; (2019); A1;,
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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, compound l (20 g, 0.235 mol)Add 100 ml of dry ether to dry,Then cool down to below 0 C,To this was added n-butyllithium (0.24mo 1)During the dropping process, it is 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, it is kept below 0 C,After the dropwise addition, slowly raise to room temperature,After stirring for half an hour, the reaction was quenched by the addition of hydrochloric acid solution (2N, 500 ml).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., 288-16-4

As the paragraph descriping shows that 288-16-4 is playing an increasingly important role.

Reference£º
Patent; Tianjin Jinyao Group Co., Ltd.; Li Jing; He Guangjie; Yang Xinyi; Wang Shuli; Chen Liying; Hu Xiaoyun; Sun Liang; (37 pag.)CN106890178; (2017); A;,
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