Category: 24340-77-0

24340-77-0, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 4-Bromoisothiazole, cas is 24340-77-0,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

(B) (2E)-Ethyl 3-(4-(isothiazol-4-yl)pyridin-3-yl)acrylate A mixture of (2E)-ethyl 3-(4-(tributylstannyl)pyridin-3-yl)acrylate (33 mg), 4-bromoisothiazole (17.41 mg), Pd(Ph3P)4 (8.18 mg), copper(I) iodide (2.70 mg), cesium fluoride (21.50 mg) and DMF (1.5 mL) was stirred under nitrogen atmosphere at 100 C. for 13 hours. Likewise, a mixture of (2E)-ethyl 3-(4-(tributylstannyl)pyridin-3-yl)acrylate (497 mg), 4-bromoisothiazole (262 mg), Pd(Ph3P)4 (123 mg), copper(I) iodide (40.6 mg), cesium fluoride (324 mg) and DMF (10 mL) was stirred under nitrogen atmosphere at 100 C. for 13 hours. The reaction mixtures were combined, and the insoluble matter was then filtered. The filtrate was diluted with ethyl acetate (20 mL), water (10 mL) and saturated aqueous sodium bicarbonate solution (10 mL), and the aqueous layer was extracted with ethyl acetate. The extract was washed with water and brine and then dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate/hexane) to obtain the title compound (222 mg). MS: [M+H]+ 260.9.

The chemical industry reduces the impact on the environment during synthesis,24340-77-0,4-Bromoisothiazole,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Takeda Pharmaceutical Company Limited; HIRAYAMA, Takaharu; FUJIMOTO, Jun; CARY, Douglas Robert; OKANIWA, Masanori; HIRATA, Yasuhiro; (147 pag.)US2017/44132; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 4-Bromoisothiazole, and cas is 24340-77-0, its synthesis route is as follows.

10456] 0.150 g (0.67 mmol) of 2-[6-(1H-pyrazol-4-yl)py- ridin-2-yl]pyrimidine (cf. Step 3) were initially charged, and 0.350 g (1.07 mmol) of caesium carbonate, 4.81 mg (0.03 mmol) of copper(I) oxide, 18.4mg (0.13 mmol) of salicylaldoxime, 0.165 g (1.0 mmol) of 4-bromoisothiazole and 1 ml of N,N-dimethylformamide were added successively under argon. The reaction mixture was heated at 110 C. for 24 hours. After cooling, the solvent was removed on a rotary evaporator under reduced pressure and the residue was purified by medium pressure column chromatography (MPLC) with cyclohexane/acetone (100:0 to 0:100). This gave 4.7mg (2% of theory) of2-{6-[1 -(isothiazol-4-yl)-1 H-pyrazol-4-yl] pyridin-2-yl}pyrimidine.10457] HPLC-MS: log P (HCOOH)=1.65, log P (neutral)=1.64.

24340-77-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,24340-77-0 ,4-Bromoisothiazole, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; BAYER CROPSCIENCE AG; Koehler, Adeline; Bretschneider, Thomas; Muehlthau, Friedrich August; Fuesslein, Martin; Jeschke, Peter; Fischer, Reiner; Voerste, Arnd; Malsam, Olga; Ilg, Kerstin; US2015/284380; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 4-Bromoisothiazole, cas is 24340-77-0,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

To a reaction flask were added compound 41 (100 mg, 0.19 mmol), 4-bromoisothiazole (50 mg, 0.27 mmol), Pd(dppf)Cl2 (5 mg, 0.006 mmol) and sodium carbonate (60 mg, 0.558 mmol), 5 mL glycol dimethyl ether and 0.9 mL water were added, bubbled with nitrogen gas for 10 minutes, and the reaction was heated to 100 C in microwave and reacted for half an hours. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 58 mg of a product, yield: 63%. LC-MS(APCI): m/z = 485.3 (M+1)+. 1H NMR (400 MHz, CDCl3) delta 10.23 (s, 1H), 9.09 (s, 1H), 8.77 (d, J = 2.0 Hz, 1H), 8.72 (s, 1H), 8.10 (d, J = 2.0 Hz, 1H), 7.87 (d, J = 9.0 Hz, 2H), 7.34 (d, J = 8.7 Hz, 2H), 5.47 (d, J = 3.5 Hz, 1H), 4.94 (d, J = 51.5 Hz, 1H), 4.18 (s, 1H), 3.64 (ddd, J = 41.8, 13.5, 3.1 Hz, 1H), 3.43 – 3.38 (m, 1H), 3.02 (d, J = 11.9 Hz, 1H).

The chemical industry reduces the impact on the environment during synthesis,24340-77-0,4-Bromoisothiazole,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; Shenzhen Targetrx, Inc.; WANG, Yihan; ZHAO, Jiuyang; AL, Yixin; (51 pag.)EP3553057; (2019); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 4-Bromoisothiazole, cas is 24340-77-0,the isothiazole compound, it is a common compound, a new synthetic route is introduced below.

Step 1: Synthesis of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isothiazole To a stirred solution of 4-bromoisothiazole (0.2 g, 1.21 mmol) and Bis(pinacolato)diboron (0.464 g, 1.81 mmol) in Dioxane (10 mL) was added AcOK (0.358 g, 3.61 mmol) along with TPP (0.032 g, 0.12 mmol) and reaction mass was purged with nitrogen for 30 min. Then, Pd2(dba)3 (0.056 g, 0.061 mmol) was added to it and stirred at 100 C. for 16 h. Reaction was monitored by TLC. On completion reaction mass was concentrated under reduced pressure and extracted with ethyl acetate. The organic layer was washed with water, brine, dried over sodium sulphate, concentrated under reduced pressure obtained crude which was purified column chromatography; eluent 3% EtOAc/Hexane to afford 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isothiazole (0.07 g, 27%) as yellow solid. MS: 212.1[M++1]

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 4-Bromoisothiazole, 24340-77-0

Reference£º
Patent; Mankind Pharma Ltd.; Patil, Rakesh Ishwar; Verma, Jeevan; Shah, Dharmesh; Ali, Sazid; Bapuram, Srinivasa Reddy; Rai, Santosh Kumar; Kumar, Anil; (146 pag.)US2017/291910; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

The above oily liquid was dissolved in 10 mL of ethylene glycol dimethyl ether and 2 mL of water, and 4-bromoisothiazole (163 mg, 0.99 mmol), Pd(PPh3)4 (29 mg, 0.025 mmol) and Na2CO3 (263 mg, 2.48 mmol), the reaction was stirred at 100 C for 2 hours under nitrogen atmosphere. After cooling to room temperature, the reaction solution was poured into 60 mL of water and extracted three times with 20 mL of ethyl acetate. The combined ethyl acetate was washed with brine and dried over anhydrous sodium sulfate. Filtered, and concentrated by column chromatography (petroleum ether / ethyl acetate 1/1) to give 43mg as a white solid powder.

24340-77-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,24340-77-0 ,4-Bromoisothiazole, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Zhao Jiuyang; (35 pag.)CN109651359; (2019); A;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

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

To a reaction flask were added compound 5 (200 mg, 0.392 mmol), 4-bromoisothiazole (96 mg, 0.588 mmol), Pd(dppf)Cl2 (32 mg, 0.02 mmol) and sodium carbonate (126 mg, 1.18 mmol), 2 mL glycol dimethyl ether and 0.4 mL water were added, bubbled with nitrogen gas for 10 minutes, and the reaction was heated to 120 C in microwace for half an hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 58 mg of a product, yield: 31.7%. LC-MS(APCI): m/z = 467.3(M+1)+; 1H NMR (400 MHz, DMSO) delta 10.17 (s, 1H), 9.04 (s, 1H), 8.76 (d, J = 2.3 Hz, 1H), 8.70 (s, 1H), 8.05 (d, J = 2.3 Hz, 1H), 7.86 (d, J = 9.1 Hz, 2H), 7.33 (d, J = 8.8 Hz, 2H), 4.86 (d, J = 3.4 Hz, 1H), 4.21 (s, 1H), 3.41 (dd, J = 17.0, 9.3 Hz, 1H), 3.29 – 3.18 (m, 2H), 2.90 (d, J = 11.1 Hz, 1H), 1.89 – 1.80 (m, 1H), 1.75 (s, 1H).

24340-77-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,24340-77-0 ,4-Bromoisothiazole, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Shenzhen Targetrx, Inc.; WANG, Yihan; ZHAO, Jiuyang; AL, Yixin; (51 pag.)EP3553057; (2019); A1;,
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.

Example 190Preparation of 1-Isothiazol-4-yl-3-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (190A) 1-(4-Methyl-pyridin-3-yl)-imidazolidin-2-one (I-14b: 150 mg, 0.847 mmol) was reacted with 4-bromo-isothiazole (166 mg, 1.016 mmol), 1,4-dioxane (15 mL), copper iodide (16.09 mg, 0.0847 mmol), trans-1,2-diamino cyclohexane (29 mg, 0.254 mmol) and potassium phosphate (540 mg, 2.541 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in CHCl3) afforded 120 mg of the product (54.54% yield).1H NMR (CDCl3, 300 MHz): delta 8.82 (s, 1H), 8.65-8.25 (m, 3H), 7.4-7.1 (m, 1H), 4.20-3.95 (m, 4H), 2.19 (s, 3H)LCMS purity: 97.95%, m/z=261.0 (M+1)HPLC: 96.08%

24340-77-0, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,24340-77-0 ,4-Bromoisothiazole, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; Novartis AG; US2010/331326; (2010); A1;,
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

A mixture of 4-bromo-isothiazole (4.7 g, 28.66 mmol), tert-butyl acrylate (13 mL, 96.96 mmol), Pd(OAc)2 (700 mg, 3.13 mmol), tris-(o-tolyl)phosphine (2.1 g, 6.91 mmol), and TEA (10 g, 99.01 mmol) in 1,4-dioxane (100 mL) was refluxed vigorously under Ar at 125 C. for 2 h. The reaction mixture was cooled to room temperature and concentrated. The residue was purified by silica gel chromatography (PE:EA=15:1 to 10:1) to give tert-butyl (E)-3-isothiazol-4-ylprop-2-enoate (2.7 g, 44.6% yield) as a light yellow solid. LCMS (ESI) [M+Na]+=212.1. 1H NMR (400 MHz, CDCl3): delta 8.72 (s, 1H), 8.69 (s, 1H), 7.63 (d, J=16.0 Hz, 1H), 6.36 (d, J=16.0 Hz, 1H), 1.55 (s, 9H).

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

Reference£º
Patent; Genentech, Inc.; Chan, Bryan; Daniels, Blake; Drobnick, Joy; Gazzard, Lewis; Heffron, Timothy; Huestis, Malcolm; Liang, Jun; Malhotra, Sushant; Mendonca, Rohan; Rajapaksa, Naomi; Siu, Michael; Stivala, Craig; Tellis, John; Wang, Weiru; Wei, BinQing; Zhou, Aihe; Cartwright, Matthew W.; Gancia, Emanuela; Jones, Graham; Lainchbury, Michael; Madin, Andrew; Seward, Eileen; Favor, David; Fong, Kin Chiu; Good, Andrew; Hu, Yonghan; Hu, Baihua; Lu, Aijun; US2018/282328; (2018); A1;,
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

a) 6- (Isothiazol-4-yl)-8- ((2- (trimethylsilyl)ethoxy)methoxy)-3- ((2- (trimethylsilyl)ethoxy)methyl)guinazolin-4(3H)-oneA suspension of 4-bromo-isothiazole (0.02 g, 0.1 mmol), (6- (4,4,5 ,5-tetramethyl- 1,3,2- dioxaborolan-2-yl)-8- ((2- (trimethylsilyl)ethoxy)methoxy)-3-((2-(trimethylsilyl)ethoxy)methyl)quinazolin-4(3H)-one (0.05 g, 0.08 mmol, example 28), bis (diphenylphosphino)feffocene-palladium(II)dichloride (0.01 g, 0.01 mmol), potassium carbonate (0.03 g, 0.25 mmol) and water (0.2 ml) in dimethylformamide (1 ml) was stirred in a sealed tube at 100 C for 2 hours and then at 80 C overnight. Filtration and chromatography (C18 reverse phase HPLC, methanol / water (0.1% formic acid) = 40:60 to 100:0) yielded thetitle compound as white solid (0.01 g, 16 %). MS: mle = 506.7 [M+Hf?.

24340-77-0 is used more and more widely, we look forward to future research findings about 4-Bromoisothiazole

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BISSANTZ, Caterina; BONNAFOUS, Rene; BUETTELMANN, Bernd; JAKOB-ROETNE, Roland; LERNER, Christian; RUDOLPH, Markus; WO2014/102233; (2014); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

As a common heterocyclic compound, it belongs to isothiazole compound, name is 4-Bromoisothiazole, and cas is 24340-77-0, its synthesis route is as follows.,24340-77-0

10456] 0.150 g (0.67 mmol) of 2-[6-(1H-pyrazol-4-yl)py- ridin-2-yl]pyrimidine (cf. Step 3) were initially charged, and 0.350 g (1.07 mmol) of caesium carbonate, 4.81 mg (0.03 mmol) of copper(I) oxide, 18.4mg (0.13 mmol) of salicylaldoxime, 0.165 g (1.0 mmol) of 4-bromoisothiazole and 1 ml of N,N-dimethylformamide were added successively under argon. The reaction mixture was heated at 110 C. for 24 hours. After cooling, the solvent was removed on a rotary evaporator under reduced pressure and the residue was purified by medium pressure column chromatography (MPLC) with cyclohexane/acetone (100:0 to 0:100). This gave 4.7mg (2% of theory) of2-{6-[1 -(isothiazol-4-yl)-1 H-pyrazol-4-yl] pyridin-2-yl}pyrimidine.10457] HPLC-MS: log P (HCOOH)=1.65, log P (neutral)=1.64.

With the complex challenges of chemical substances, we look forward to future research findings about 4-Bromoisothiazole

Reference£º
Patent; BAYER CROPSCIENCE AG; Koehler, Adeline; Bretschneider, Thomas; Muehlthau, Friedrich August; Fuesslein, Martin; Jeschke, Peter; Fischer, Reiner; Voerste, Arnd; Malsam, Olga; Ilg, Kerstin; US2015/284380; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com