Category: 18480-53-0

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(3,4-dichloroisothiazol-5-yl)methanolA solution of 3,4-dichloroisothiazole-5-carboxylic acid (2.0 g), N1N- dimethylformamide (few drops) and thionyl chloride (20 mL) in toluene (60 mL) was heated at 1000C for 16 hours. The reaction mixture was cooled to room temperature and concentrated under reduced pressure. The residue was dissolved in tetrahydrofuran (20 mL), cooled to -200C under a nitrogen atmosphere and treated dropwise with a 1.0 M sodium borohydride solution in N, N- dimethylformamide (8.5 ml.) over 1 hour. The mixture was stirred for 5 minutes after the end of addition and quenched with 1.0 M aqueous hydrochloric acid solution. The mixture was concentrated to low bulk under reduced pressure and extracted with ethyl acetate. The combined organic layer was washed with brine, dried over magnesium sulfate and concentrated under reduced pressure. The residue was purified by column chromatography on silica gel, eluting with a mixture of cyclohexane and dichloromethane (1 :0 to 0:1 by volume), to afford the title compound as a pale yellow solid (1.1 g).1H NMR (300 MHz, CDCI3): delta 2.60 (s, 1H); 4.96 (s, 2H).

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

Reference£º
Patent; PULMAGEN THERAPEUTICS (ASTHMA) LIMITED; HYND, George; MONTANA, John Gary; FINCH, Harry; ARIENZO, Rosa; AHMED, Shahadat; WO2010/142934; (2010); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of the starting material: At room temperature, 146 g (1.23 mol) of thionyl chloride are added dropwise with stirring over a period of 5 minutes to 8.92 g (0.045 mol) of 3,4-dichloro-isothiazole-5-carboxylic acid. 4 drops of dimethylformamide are then added, and the reaction mixture is heated at reflux for one hour. The reaction mixture is subsequently cooled to room temperature and concentrated under reduced pressure. This gives 12.19 g of 3,4-dichloro-isothiazole-5-carbonyl chloride in the form of an orange oil. The compounds of the formula (I) listed in the table below are also prepared by the method given above.

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Bayer Aktiengesellschaft; US6191155; (2001); B1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

3,4-Dichloroisothiazol-5-carboxylic acid (0.235 g, 1.2 mmol), dichloromethane (6 ml), N,N-dimethylformamide (2 drops) were added dropwise to the reaction flask. Add oxalyl chloride (1 g, 8 mmol),The reaction solution was stirred at room temperature for 4 hours.The solvent was then evaporated to give 3,4-dichloroisothiazol-5-carbonyl chloride, which was dissolved in dichloromethane (2 mL).Then 4-fluoro-2-(2-pentyloxy)aniline (0.197 g, 1 mmol) was added to the reaction flask and triethylamine (0.13 mL) was added.Further, a 3,4-dichloroisothiazol-5-formyl chloride solution was added dropwise to the reaction flask, and the mixture was stirred at room temperature for 16 hours.Then after monitoring the reaction by thin layer chromatography,Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate.The organic layer was washed with saturated brine.After drying over anhydrous sodium sulfate, it was concentrated under reduced pressure.The residue was purified by column chromatography (eluent: petroleum ether: ethyl acetate = 20:1).Obtained a fresh yellow solid of 0.236 g.The yield was 62.76percent.

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

Reference£º
Patent; Shanghai Taihe International Trade Co., Ltd.; Ma Wenjing; Lv Liang; Li Hongwei; Hou Shuang; Du Yonglei; Liu Jiyong; (31 pag.)CN108383791; (2018); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a suspension of 3,4-dichloroisothiazole-5-carboxylic acid (0.15 g, 0.76 mmol) in oxalyl chloride (2 mL) was added a catalytic amount of dimethylformamide (2 drops) and the mixture was heated to 80¡ã C. and stirred for 2 h. The excess oxalyl chloride was removed on the rotary evaporator. Meanwhile, 5-fluoro-2-(4-fluorobenzyloxy)-pyrimidin-4-ylamine (0.17 g, 0.68 mmol) was dissolved in THF (1 mL), treated with LiHMDS (1M in THF, 0.76 mL, 0.76 mmol) and stirred for 10 min. The freshly prepared 3,4-dichlorothiazole-5-carbonyl chloride*, dissolved in THF (1 mL), was added and the reaction was capped and stirred for 12 h. The reaction was diluted with water and the target compound was extracted with CH2Cl2 (3.x.5 mL). The combined extracts were dried over MgSO4 and then evaporated under reduced pressure. The mixture was eluted with CH2Cl2 through an anionic-exchange solid phase extraction column and then further purified by reverse-phase chromatography to give 3,4-dichloroisothiazole-5-carboxylic acid [5-fluoro-2-(4-fluorobenzyloxy)pyrimidin-4-yl]amide (0.035 g, 12percent) as a tan solid: mp 87-90¡ã C.; 1H NMR (400 MHz, DMSO-d6) delta 11.78 (s, 1H), 8.67 (s, 1H), 7.51-7.48 (m, 2H), 7.24-7.19 (m, 2H), 5.25 (s, 2H); MS (ESI) m/z 417 (M+H)+, 415 (M-H)-. *Nagata, T.; Kogure, A.; Yonekura, N.; Hanai, R.; Kaneko, I.; Nakano, Y. JP 2007211002 A

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; DOW AGROSCIENCES LLC; US2009/203647; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

2.1. Synthesis of ethyl 3,4-dichloroisothiazole-5-carboxylate: 15 g of 3,4-dichloroisothiazole-5-carboxylic acid (75.7 mmol) were dissolved in 300 ml of ethanol and 8.4 ml of concentrated sulphuric acid were added. The mixture was stirred under reflux for 20 h. The reaction mixture was then concentrated to half the original volume, neutralized with saturated NaHC03, added to water and extracted with dichloromethane. The dichloromethane phases were dried and carefully concentrated on a rotary evaporator. Yield: 15.2 g (89percent of theory).’H-NMR (400 MHz, CDC13delta, ppm) 4.44 (q,2H), 1.42 (tr,3H).

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

Reference£º
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; TIEBES, Joerg; MOSRIN, Marc; REY, Jullien; DOeLLER, Uwe; DROeGE, Thomas; MAECHLING, Simon; SCHMIDT, Jan Peter; TELSER, Joachim; SCHMUTZLER, Dirk; DIETRICH, Hansjoerg; GATZWEILER, Elmar; ROSINGER, Christopher Hugh; BERNIER, David; CRISTAU, Pierre; TSUCHIYA, Tomoki; (180 pag.)WO2016/102420; (2016); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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.

Preparation of the Starting Material At room temperature, 146 g (1.23 mol) of thionyl chloride are added dropwise with stirring over a period of 5 minutes to 8.92 g (0.045 mol) of 3,4-dichloro-isothiazole-5-carboxylic acid. Four drops of dimethylformamide are then added and the reaction mixture is heated under reflux for one hour. The reaction mixture is subsequently cooled to room temperature and concentrated under reduced pressure. In this manner, 12.19 g of 3,4-dichloro-isothiazole-5-carbonyl chloride are obtained in the form of an orange oil.

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

Reference£º
Patent; Bayer Aktiengesellschaft; US6277791; (2001); B1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

18480-53-0, 3,4-Dichloroisothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1.1. Synthesis of 3,4-dichloro-N-(cyclohexylmethyl)isothiazole-5-carboxamide: 730 mg 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 of dichloromethane 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 MgS04, concentrated and purified by column chromatography. Yield: 1.05 g (97percent of theory).’H-NMR (400 MHz, CDC13delta, ppm) 6.86 (br,lH), 3.34 (tr,2H), 1.77 (m,4H), 1.66 (m,lH), 1.58 (m,lH), 1.3-1.15 (m,3H), 1.0 (m,2H).

The synthetic route of 18480-53-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER CROPSCIENCE AKTIENGESELLSCHAFT; TIEBES, Joerg; MOSRIN, Marc; REY, Jullien; DOeLLER, Uwe; DROeGE, Thomas; MAECHLING, Simon; SCHMIDT, Jan Peter; TELSER, Joachim; SCHMUTZLER, Dirk; DIETRICH, Hansjoerg; GATZWEILER, Elmar; ROSINGER, Christopher Hugh; BERNIER, David; CRISTAU, Pierre; TSUCHIYA, Tomoki; (180 pag.)WO2016/102420; (2016); A2;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com