Heterocyclic Building Blocks-Isothiazole

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

SYNTHESIS EXAMPLE 2 Process (a): After thionyl chloride (10 ml) had been added to 3,4-dichloro-5-isothiazole-carboxylic acid (1.28 g), the mixture was refluxed by heating for 2 hours. The excess of thionylchloride was then distilled off under reduced pressure, and 3,4-dichloro-5-isothiazolecarboxylic acid chloride was obtained.

As the paragraph descriping shows that 18480-53-0 is playing an increasingly important role.

Reference£º
Patent; Assmann, Lutz; Kitagawa, Yoshinori; Ishikawa, Koichi; Yamazaki, Daiei; Sawada, Haruko; Araki, Yasuo; Sakuma, Haruhiko; Kinbara, Taro; Imanishi, Kinya; US2003/13750; (2003); A1;,
Isothiazole – Wikipedia
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7716-66-7,7716-66-7, 3-Chlorobenzo[d]isothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 1 3-(1-Piperazinyl)-1,2-benzisothiazole STR26 A mixture of 3-chloro-1,2-benzisothiazole (37.8 g., 0.235 mole) and piperazine (304.2 g., 3.53 mole) is heated under an argon atmosphere for a period of 20 hr. at 120¡ã C. in a closed reactor. The reaction mixture is dissolved in 2 liters of water and the aqueous solution repeatedly extracted with methylene chloride. Extracts are combined, dried over magnesium sulfate and concentrated in vacuo. Residual material is taken up in ether, filtered and concentrated in vacuo to afford 24.4 g. (47percent) of 3-(1-piperazinyl)-1,2-benzisothiazole free base as a viscous oil. A sample of the free base converted to the hydrochloride salt in ether with ethanolic hydrogen chloride and crytallized from methanol-ethanol affords analytically pure 3-(1-piperazinyl)-1,2-benzisothiazole hydrochloride, m.p. 280¡ã C. (dec.). Anal. Calcd. for C11 H13 N3 S.HCl: C, 51.66; H, 5.52; N, 16.43. Found: C, 51.34; H, 5.46; N, 16.16.

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

Reference£º
Patent; Mead Johnson & Company; US4411901; (1983); A;,
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

To a solution of (1-isobutyl-5-phenyl-1H-pyrazol-3-yl)methanol (52.1 mg, 0.226 mmol) in methylene chloride (1 mL) were added PPh3 (146 mg, 0.557 mmol), CBr4 (185 mg, 0.557 mmol) at 0¡ã C., followed by stirring at the same temperature for 30 min to give (1-isobutyl-5-phenyl-1H-pyrazol-3-yl)methyl bromide. When the reaction was completed as measured by TLC (Hexane:EtOAc=4:1), a solution of 1,2-benzisothiazoline-1,1-dioxide (57.1 mg, 0.388 mmol) in N,N-dimethylformamide (1.5 mL) was added dropwise. (0333) Then, drops of potassium carbonate (313 mg, 2.26 mmol) were added at the same temperature to the solution that was then stirred for 3 days. When the reaction was completed as measured by TLC (Hexane:EtOAc=2:1), water was dropped to the reaction mixture. After extraction with ethyl acetate and brine, the organic layer was dried over anhydrous magnesium sulfate, filtered, and concentrated in vacuo. The concentrate was purified by column chromatography (Hexane:EtOAc=2:1) to afford the title compound (37.8 mg, 44percent percent, white solid). (0334) M.P 129.7-137.3¡ã C.; (0335) 1H NMR (300 MHz, CDCl3) delta 7.86-7.63 (m, 1H), 7.63-7.51 (m, 2H), 7.49-7.37 (m, 6H), 6.42 (s, 1H), 4.56 (s, 2H), 4.41 (s, 2H), 3.96 (d, J=7.5 Hz, 2H), 2.24-2.15 (m, 1H), 0.79 (d, J=6.7 Hz, 6H); (0336) 13C NMR (75 MHz, CDCl3) delta 145.9, 145.6, 136.8, 135.2, 134.0, 133.0, 132.6, 130.8, 129.0, 128.7, 124.6, 121.4, 106.1, 56.8, 49.9, 41.3, 29.6, 19.8

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

Reference£º
Patent; KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY; NAM, Ghil Soo; CHOI, Kyung Il; KIM, Jung Hyun; PAE, Ae Nim; HONG, Jin Ri; LEE, Jae Kyun; (30 pag.)US2015/329533; (2015); A1;,
Isothiazole – Wikipedia
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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.

Compound 1 (20 g, 0.235 mol) was added under stirring with nitrogen to dry 100 ml of ether and stirred to dissolve,And then cooled to 0 C or lower, to which n-butyllithium (0.24 mol)During the dropwise addition, the temperature was kept below 0 C, 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 (2N, 500 ml)Quenching reaction.The aqueous phase was extracted with ether (200 ml * 3) and discarded. The organic phases were combined,Sodium dithionite solution (100ml * 2), dried over anhydrous sodium sulfate, filtered and concentrated to dryness,A yellow oily compound was prepared.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.

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.; Ge Yu; Li Yanfeng; (33 pag.)CN106892912; (2017); A;,
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27148-03-4, Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Room temperature: To a benzene solution (20mL) containing [Os3(CO)10(NCMe)2] (0.13g, 0.14mmol) was added tsacH (56g, 0.28mmol), after which the solution was allowed to stir at room temperature for 2h. TLC examination of the reaction revealed the presence of two new products in a 3:1 ratio representing 1 and 2, respectively. The products were isolated by chromatography using an eluent composed of cyclohexane/ CH2Cl2 (1:1, v/v) that afforded two bands corresponding to [HOs3(CO)10(mu-N,S-1,3-tsac)] (2) (32mg, 22%) and [HOs3(CO)10(mu-S-tsac)] (1) (0.10g, 68%) in order of elution. Each product was obtained as orange crystals after recrystallization from n-hexane/CH2Cl2 at 4C. Data for 1: Anal. Calc. for C17H5NO12Os3S2: C, 19.44; H, 0.48, N, 1.33. Found: C, 19.92; H, 0.54, N, 1.36%. IR (nuCO, CH2Cl2): 211m, 2076vs, 2066s, 2028s, 2019s, 1992m cm-1. 1H NMR (CDCl3): delta 8.00 (m, 1H), 7.90 (m, 1H), 7.86 (m, 2H),-17.10 (s, 1H). Data for 2: Anal. Calc. for C17H5NO12Os3S2: C, 19.44; H, 0.48, N, 1.33. Found: C, 19.98; H, 0.52; N, 1.37%. IR (nuCO, CH2Cl2): 2113m, 2076s, 2065s, 2029s, 2018s, 1994w, 1982w cm-1. 1H NMR (CDCl3): delta 7.94 (d, J 7.2Hz, 1H), 7.84 (d, J 7.2Hz, 1H), 7.72 (m, 2H),-13.96 (s, 1H)., 27148-03-4

As the paragraph descriping shows that 27148-03-4 is playing an increasingly important role.

Reference£º
Article; Pinky, Tamanna; Rahman, Md Matiar; Ghosh, Shishir; Azam, Kazi A.; Mia, Md. Jadu; Alam, Md. Mahbub; Tocher, Derek A.; Richmond, Michael G.; Kabir, Shariff E.; Journal of Organometallic Chemistry; vol. 880; (2019); p. 223 – 231;,
Isothiazole – Wikipedia
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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

EXAMPLE B4 A mixture of 3,4-dihydro-7-methoxybenzofuro[2,3-c]pyridine-2(1H)-butanamine (0.0055 mol), 3-chloro-1,2-benzisothiazole (0.0089 mol) and NaHCO3 (0.01 mol) was stirred for 1.5 hour at 120¡ã C. (melt). 1-Butanol (0.5 ml) was added. The reaction mixture was cooled, then dissolved in CH2Cl2 and purified by column chromatography over silica gel (eluent: CH2Cl2/(CH3OH/NH3) 98/2). The desired fractions were collected and the solvent was evaporated. The residue was dissolved in 2-propanone and converted into the hydrochloric acid salt (1:2) with HCl/2-propanol. The mixture was stirred at room temperature. The precipitate was filtered off and dried, yielding 1.60 g of N-(1,2-benzisothiazol-3-yl)-3,4-dihydro-7-methoxybenzofuro[2,3-c]pyridine-2(1H)-butanamine monohydrochloride monohydrate (61percent) (compound 55).

As the paragraph descriping shows that 7716-66-7 is playing an increasingly important role.

Reference£º
Patent; Janssen Pharmaceutica N.V.; US6495555; (2002); B1;,
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, 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.

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

Reference£º
Article in Press; Hong, Jin Ri; Choi, Young Jin; Keum, Gyochang; Nam, Ghilsoo; Bioorganic and Medicinal Chemistry; (2017);,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.27148-03-4,Benzo[d]isothiazole-3(2H)-thione 1,1-dioxide,as a common compound, the synthetic route is as follows.

A solution of Htsac (0.035 g, 0.18 mmol) in MeOH was added toa solution of 1 (0.10 g, 0.18 mmol) in CHCl3 (10 cm3). The mixturewas stirred for 2 h and the resulting pale brown solid was collectedand dried in vacuum. Yield 0.116 g, 90%. Anal. Calc. for C25H28ClN3-O2Pd2S2: C, 42.0, H, 4.0, N, 5.9. Found: C, 42.2, H, 4.0, N, 5.7. Molarconductivity (DMSO): 0.30 (X-1 mol1 cm1). IR: 3083w, 2916w,1558 m, 1453vs, 1317 s, 1168 s, 1020 s, 815 s, 449w, 362 s cm1.1H NMR (DMSO d6): d 8.12-8.10 (dd, J 7.2, 1.2 2H, Ph), 7.97-7.95(m, 1H, Ph), 7.84-7.82 (m, 2H, Ph), 7.60 (d, J 7.2, 1H, Ph), 7.47 (d, J 7.2, 1H, Ph), 7.05-6.91 (m, 5H, Ph), 6.82 (d, J 7.2, 1H, Ph), 4.02(s, 4H, CH2), 2.72 (s, 12H, 4CH3). Mp: 202-204 C., 27148-03-4

The synthetic route of 27148-03-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Al-Jibori, Subhi A.; Hameed, Wisam J.; Al-Janabi, Ahmed S.; Basak-Modi, Sucharita; Wagner, Christoph; Hogarth, Graeme; Inorganica Chimica Acta; vol. 479; (2018); p. 197 – 202;,
Isothiazole – Wikipedia
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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 mixture of 6-(2-chloro-ethyi)-7-fluoro-4,4,8-trimethyl-3,4-dihydro-1H-quinolin-2-one (0.7499 g, 2.780 mmol), 3-piperazin-1-yl-benzo[d]isothiazole hydrochloride (0.7834 g, 3.063 mmol), potassium carbonate (0.8456 g, 6.118 mmol) and potassium iodine (0.0495 g, 0.298 mmol) were reacted in acetonitrile (7.0 mL) in a CEM MARS5 microwave reactor for 1 h at 150 C. The reaction was cooled to room temperature, diluted with H2O (70 mL) and extracted with dichloromethane (2 x 75 mL). The organic extracts were combined, dried over anhydrous sodium sulfate, filtered and the solvent removed under reduced pressure. The resulting solid was purified by MPLC (The solid was washed with H2O and hexanes. The resulting solid was purified by MPLC (silica gel, 100% CH2CI2 to 3% MeOH/CH2CI2 over 1 h then hold at 3% MeOH/CH2CI2) to give a mixture of the titled compound and the product of step C. This mixture was dissolved in dichloromethane and 4 M hydrogen chloride in dioxane was slowly added until the product precipitated. The titled compound (0.3137 g, 0.660 mmol, 53% over two steps) was isolated as a white solid. MS (APCI): (M+1, free base)+= 439.2. 1H NMR (400 MHz, CDCl3) delta 1.29 (s, 6 H), 2.12 (d, J=1.6 Hz, 3 H), 2.44 (s, 2 H), 3.19 (s, 4 H), 3.32 (s, 2 H), 3.59 (s, 2 H), 4.17 (m, 4 H), 7.12 (d, J=7.6 Hz, 1H), 7.38-7.45 (m, 2 H), 7.49-7.54 (m, 1H), 7.84 (t, J=8.8 Hz, 2 H), 13.2 (br s, 1H). Anal, calcd. for C24H27FN4OS*HCl*0.75 H2O*0.10 CH2CI2: 58.24; H, 6.02; N, 11.27; H2O, 2.72. Found: 57.84; H, 6.17; N, 10.98; H2O, 2.57.

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; WO2004/26864; (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.677304-78-8,5-Bromobenzo[d]isothiazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.,677304-78-8

The following acids were prepared using this method: -Bromobenzisothiazole-S-carboxylic acid. 5-Bromobenzisothiazole-3-carboxy lie acid. 6-Methoxybenzisothiazole-3-carboxylic acid.The following esters were prepared from the acid using ethanol and sulfuric acid:Ethyl 6-bromobenzisothiazole-3-carboxylate. Ethyl 5-bromobenzisothiazole-3-carboxylate. Ethyl 6-methoxybenzisothiazole-3-carboxylate.

The synthetic route of 677304-78-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; WO2007/56582; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com