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

To 4.0 g (20.3 mmol) of 3,4-dichloroisothiazole-5-carboxylic acid were added 8 ml of oxalyl chloride and a catalytic amount of DMF, followed by stirring at 50¡ãC for 30 minutes to give rise to a reaction. The reaction mixture was concentrated under vacuum to obtain 3,4-dichloroisothiazole-5-carbonyl chloride. 1.9 g (50.5 mmol) of sodium borohydride was suspended in 40 ml of water. To the resulting suspension was dropwise added, at 10 to 15¡ãC, a solution of the 3,4-dichloroisothiazole-5-carbonyl chloride dissolved in THF (4 ml). Stirring was conducted at 15¡ãC for 30 minutes. Then, an aqueous citric acid solution was added to make the mixture weakly acidic and extraction with ethyl acetate was conducted. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and concentrated. The resulting crystals were washed with hexane to obtain 3.0 g (yield: 81percent) of (3,4-dichloroisothiazol-5-yl)methanol as colorless crystals (melting point: 94 to 95¡ãC). 1H-NMR (CDCl3) delta: 2.28 (1H, bs), 4.96 (2H, s) ppm In 6 ml of acetonitrile were dissolved 0.62 g (3.10 mmol) of 3-chloro-1,2-benzoisothiazole 1,1-dioxide and 0.57 g (3.10 mmol) of the (3,4-dichloroisothiazol-5-yl)methanol. To the resulting solution was dropwise added 0.34 g (3.4 mmol) of triethylamine, followed by stirring at room temperature for 5 hours to give rise to a reaction. After the completion of the reaction, 12 ml of water was added. The resulting crystals were obtained by filtration. The crystals were washed with water and isopropyl alcohol to obtain 0.89 g (yield: 82percent) of 3-(3,4-dichloroisothiazol-5-ylmethoxy)-1,2-benzoisothiazole 1,1-dioxide as a colorless powder (melting point: 165 to 167¡ãC). 1H-NMR (CDCl3) delta: 5.79 (2H, s), 7.73-7.94 (4H, m) ppm.

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

Reference£º
Patent; KUMIAI CHEMICAL INDUSTRY CO., LTD.; IHARA CHEMICAL INDUSTRY CO., LTD.; EP2017268; (2009); 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

3,4-Dichloroisothiazole-5-carboxylic acid (CAS 18480-53-0, 34.8 mg, 0.18 mmol) was dissolved in DMF (200 iL). HBTU (83 mg, 0.22 mmol) and TEA (61.1 iL, 0.44 mmol) were added. The solution was stirred for 6 mm and then 4-(2-amino-3-methylbutanoyl)benzonitrile hydrochloride (Example 49b, 35 mg, 0.15 mmol) in DMF (400 iL) and TEA (61.1 iL, 0.44 mmol) was added. The reaction mixture was stirred at rt for 1 h and then purified by preparative HPLC to give 3,4-dichloro-N-(1-(4-cyanophenyl)-3-methyl-1-oxobutan-2-yl)isothiazole-5-carboxamid (15 mg, 28percent).1H NMR (500 MHz, CDCI3) 5 ppm 0.87 (d, 3 H) 1.12 (d, 3 H) 2.26 – 2.36 (m, 1 H) 5.75 (dd, 1 H)7.74 (d, 1 H) 7.86 (d, 2 H) 8.12 (d, 2 H).MS (ESI) m/z 379.7 [M-H]

With the rapid development of chemical substances, we look forward to future research findings about 3,4-Dichloroisothiazole-5-carboxylic acid

Reference£º
Patent; ACTURUM LIFE SCIENCE AB; LINDE, Christian Erik; PAULSEN, Kim; SOHN, Daniel; SVENSSON, Mats A; VALLIN, Karl S A; WEIGELT, Dirk; MINIDIS, Alexander; WO2014/184235; (2014); 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

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.

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

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.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

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 NaHCO3, 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, CDC13 3, ppm) 4.44 (q, 2H), 1.42 (tr, 3H)., 18480-53-0

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; 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;,
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-ylcarboxylic acid (400 mg, 2.02 mmol) was dissolved in abs. dichloromethane (20 ml), and triethylamine (0.85 ml, 6.06 mmol) was added. After stirring at room temperature for 5 minutes, pyrrolidine-i-amine (209 mg, 2.42 mmol) and 2,4,6-tripropyl-1,3, 5,2,4,6-trioxatriphosphorinane 2,4,6-trioxide (1.80 ml, 3.03 mmol, 50percent solution in tetrahydrofuran) were added. The resulting reaction mixture was stirred at room temperature for a further 30 minutes, and then water, sat. sodium hydrogencarbonate solution and dichloromethane were added. The aqueous phase was repeatedly extracted vigorously with dichloromethane, and the combined organic phases were then dried over magnesium sulfate, filtered and concentrated. Final purification of the resulting crude product by colunm chromatography gave 3,4-dichloro-N-(pyr- rolidin-i-yl)-i,2-thiazole-5-carboxamide in the form of a colorless solid (520 mg, 92percent of theory). ?H-NMR (400 MHz, CDC13 oe, ppm) 3.38-3.28 (m, 2H), 2.73-2.64 (m, 2H), 2.03-1.98 (m, 4H). 3,4-Dichloro-N-(pyrrolidin- 1 -yl)-i ,2- thiazole-5-carboxamide (120 mg, 0.45 mmol) was dissolved in abs. tetrahydroffiran (5 ml) under argon, and sodium hydride (40 mg, 1.99 mmol, 60percent purity) was added at room temperature. Stirring at room temperature for 30 minutes was followed by the addition of picolyl chloride (HC1 salt, 74 mg, 0.45 mmol), and the resulting reaction mixture was stirred under reflux conditions for approx. 3 hours. After cooling to room temperature, sat. sodium hydrogencarbonate solution, water and dichloromethane were added. The aqueous phase was repeatedly extracted vigorously with dichloromethane, and the combined organic phases were then dried over magnesium sulfate, filtered and concentrated. Final purification of the resulting crude product by colunm chromatography gave 3,4-dichloro-N-(pyridin-2-yl- methyl)-N-(pyrrolidin- 1 -yl)-i ,2-thiazole-5-carboxamide in the form of a colorless solid (112 mg, 69percent of theory). ?H-NMR (400 MHz, CDC13 oe, ppm) 8.62 (m, 1H), 7.71-7.67 (m, 1H), 7.53 (m, 1H), 7.33 (m, 1H), 5.15 (s, 2H), 4.18-4.13 (m, 2H), 3.71-3.66 (m, 2H), 2.30-2.24 (m, 2H), 2.13-2.08 (m, 2H).

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

Reference£º
Patent; Bayer CropScience Aktiengesellschaft; FRACKENPOHL, Jens; BOJACK, Guido; BRUENJES, Marco; HELMKE, Hendrik; LEHR, Stefan; BRUECHNER, Peter; TIEBES, Joerg; MOSRIN, Marc; DITTGEN, Jan; SCHMUTZLER, Dirk; DESBORDES, Philippe; (92 pag.)US2018/206498; (2018); 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.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;,
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

A mixture of 3,4-dichloroisothiazole-5-carboxylic acid (2.0 g) and toluene (20 mL) was treated with thionyl chloride (5.0 ml_) and lambda/,lambda/-dimethylformamide (0.5 mL), and the resulting mixture was heated at 1000C for 16 hours. The mixture was concentrated under reduced pressure and the residue was dissolved in tetrahydrofuran (5.0 mL). The mixture was cooled to -780C and treated dropwise over a period of 1 hour with a 2.0 M solution of sodium borohydride in lambda/,lambda/-dimethylformamide (8.5 mL). The mixture was stirred at – 780C for 5 minutes, diluted with 1.0 M aqueous hydrochloric acid solution and extracted with ethyl acetate. The combined organic extract was washed with saturated aqueous sodium chloride solution, dried over sodium 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 (CDCI3): delta 4.96 (s, 2H).

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

Reference£º
Patent; ARGENTA DISCOVERY LIMITED; WO2009/77728; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

A common heterocyclic compound, the isothiazole compound, name is 3,4-Dichloroisothiazole-5-carboxylic acid,cas is 18480-53-0, mainly used in chemical industry, its synthesis route is as follows.,18480-53-0

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.

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

Reference£º
Patent; Bayer Aktiengesellschaft; US6277791; (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-Dichloroisothiazole-5-carboxylic acid (CAS 18480-53-0, 34.8 mg, 0.18 mmol) was dissolved in DMF (200 iL). HBTU (83 mg, 0.22 mmol) and TEA (61.1 iL, 0.44 mmol) were added. The solution was stirred for 6 mm and then 4-(2-amino-3-methylbutanoyl)benzonitrile hydrochloride (Example 49b, 35 mg, 0.15 mmol) in DMF (400 iL) and TEA (61.1 iL, 0.44 mmol) was added. The reaction mixture was stirred at rt for 1 h and then purified by preparative HPLC to give 3,4-dichloro-N-(1-(4-cyanophenyl)-3-methyl-1-oxobutan-2-yl)isothiazole-5-carboxamid (15 mg, 28percent).1H NMR (500 MHz, CDCI3) 5 ppm 0.87 (d, 3 H) 1.12 (d, 3 H) 2.26 – 2.36 (m, 1 H) 5.75 (dd, 1 H)7.74 (d, 1 H) 7.86 (d, 2 H) 8.12 (d, 2 H).MS (ESI) m/z 379.7 [M-H], 18480-53-0

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

Reference£º
Patent; ACTURUM LIFE SCIENCE AB; LINDE, Christian Erik; PAULSEN, Kim; SOHN, Daniel; SVENSSON, Mats A; VALLIN, Karl S A; WEIGELT, Dirk; MINIDIS, Alexander; WO2014/184235; (2014); 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.18480-53-0,3,4-Dichloroisothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.,18480-53-0

To a solution of S^-dichloroisothiazole-delta-carboxylic acid (4.0Og, 20.1 mmol) in dichloromethane (75 ml_), cooled with an ice-brine bath, was added N,N-dimethylformamide (78 mul_, 1 mmol) followed dropwise by oxalyl chloride (1.94 ml_, 22.2 mmol). After stirring at room temperature for 2h, meanwhile gas evolution had completely stopped, all volatiles were removed in vacuo to affor the crude acid chloride (4.30 g).

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 SA; WO2009/130193; (2009); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com