Tag: 24340-77-0

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

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]

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

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

n-Butyllithium (2.5 M solution in hexanes, 10.5 mL, 26.2 mmol) was added to a-78 00 solution of diisopropylamine (3.68 mL, 26.3 mmol) in tetrahydrofuran (80 mL).After 30 minutes, a solution of 4-bromo-1 ,2-thiazole (3.70 g, 22.5 mmol) intetrahydrofuran (20 mL) was added drop-wise, and stirring was continued at -78 00 for 30 minutes, whereupon methyl carbonocyanidate (99%, 2.15 mL, 26.8 mmol) was added. After an additional 30 minutes at -78 00 the reaction mixture was quenched via addition of saturated aqueous ammonium chloride solution, and the resulting mixturewas warmed to room temperature. After dilution with water, it was extracted with ethyl acetate; the combined organic layers were washed with saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered, and concentrated in vacuo. Purification via silica gel chromatography (Eluent: 5% ethyl acetate in heptane) provided the product as a white solid. Yield: 4.0 g, 18 mmol, 80%. 1H NMR (400 MHz, ODd3) oe8.43 (5, 1H), 3.97 (5, 3H).

With the rapid development of chemical substances, we look forward to future research findings about 24340-77-0

Reference£º
Patent; PFIZER INC.; GRAY, David Lawrence Firman; ZHANG, Lei; DAVOREN, Jennifer Elizabeth; DOUNAY, Amy Beth; EFREMOV, Ivan Viktorovich; MENTE, Scot Richard; SUBRAMANYAM, Chakrapani; WO2015/162515; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

n-Butyllithium (2.5 M solution in hexanes, 10.5 mL, 26.2 mmol) was added to a-78 00 solution of diisopropylamine (3.68 mL, 26.3 mmol) in tetrahydrofuran (80 mL).After 30 minutes, a solution of 4-bromo-1 ,2-thiazole (3.70 g, 22.5 mmol) intetrahydrofuran (20 mL) was added drop-wise, and stirring was continued at -78 00 for 30 minutes, whereupon methyl carbonocyanidate (99%, 2.15 mL, 26.8 mmol) was added. After an additional 30 minutes at -78 00 the reaction mixture was quenched via addition of saturated aqueous ammonium chloride solution, and the resulting mixturewas warmed to room temperature. After dilution with water, it was extracted with ethyl acetate; the combined organic layers were washed with saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered, and concentrated in vacuo. Purification via silica gel chromatography (Eluent: 5% ethyl acetate in heptane) provided the product as a white solid. Yield: 4.0 g, 18 mmol, 80%. 1H NMR (400 MHz, ODd3) oe8.43 (5, 1H), 3.97 (5, 3H)., 24340-77-0

The synthetic route of 24340-77-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; GRAY, David Lawrence Firman; ZHANG, Lei; DAVOREN, Jennifer Elizabeth; DOUNAY, Amy Beth; EFREMOV, Ivan Viktorovich; MENTE, Scot Richard; SUBRAMANYAM, Chakrapani; WO2015/162515; (2015); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The above oily liquid was dissolved in 10 mL of DME and 2 mL of water, and 4-bromoisothiazole (275 mg, 1.68 mmol), Pd(PPh3)4 (48 mg, 0.042 mmol) and Na2CO3 (296 mg, 2.80 mmol), and 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 72mg as a white solid powder.

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

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

24340-77-0, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 7 (497 mg, 1.07 mmol) in DMF (10 mL) were added 4-bromoisothiazole (262 mg, 1.60 mmol), CsF (324 mg, 2.13 mmol), Pd(PPh3)4 (123 mg, 0.11 mmol) and copper(I) iodide (40.6 mg, 0.21 mmol) at rt. The mixture was stirred at 100 C for 13 h. After removal of insoluble materials by filtration, the filtrate was diluted with EtOAc (20 mL), water (10 mL), and sat. aq. NaHCO3 (10 mL). The aqueous layer was extracted with EtOAc (15 mL ¡Á 3). The organic layers were combined, washed with water and brine, dried over Na2SO4, and concentrated under vacuum. The residue was purified by column chromatography (silica gel, eluted with 5-60% EtOAc/hexane) to yield 8a (208 mg, 75%) as a pale yellow solid. 1H NMR (300 MHz, DMSO-d6) delta 1.24 (3H, t, J = 7.1 Hz), 4.19 (2H, q, J = 7.1 Hz), 6.76 (1H, d, J = 16.1 Hz), 7.53-7.62 (2H, m), 8.66 (1H, d, J = 5.1 Hz), 8.77 (1H, s), 9.06 (1H, s), 9.28 (1H, s). MS (API): m/z 260.9 (M + H)+

24340-77-0, As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

Reference£º
Article; Fujimoto, Jun; Hirayama, Takaharu; Hirata, Yasuhiro; Hikichi, Yukiko; Murai, Saomi; Hasegawa, Maki; Hasegawa, Yuka; Yonemori, Kazuko; Hata, Akito; Aoyama, Kazunobu; Cary, Douglas R.; Bioorganic and Medicinal Chemistry; vol. 25; 12; (2017); p. 3018 – 3033;,
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

To a solution of 7 (497 mg, 1.07 mmol) in DMF (10 mL) were added 4-bromoisothiazole (262 mg, 1.60 mmol), CsF (324 mg, 2.13 mmol), Pd(PPh3)4 (123 mg, 0.11 mmol) and copper(I) iodide (40.6 mg, 0.21 mmol) at rt. The mixture was stirred at 100 C for 13 h. After removal of insoluble materials by filtration, the filtrate was diluted with EtOAc (20 mL), water (10 mL), and sat. aq. NaHCO3 (10 mL). The aqueous layer was extracted with EtOAc (15 mL ¡Á 3). The organic layers were combined, washed with water and brine, dried over Na2SO4, and concentrated under vacuum. The residue was purified by column chromatography (silica gel, eluted with 5-60% EtOAc/hexane) to yield 8a (208 mg, 75%) as a pale yellow solid. 1H NMR (300 MHz, DMSO-d6) delta 1.24 (3H, t, J = 7.1 Hz), 4.19 (2H, q, J = 7.1 Hz), 6.76 (1H, d, J = 16.1 Hz), 7.53-7.62 (2H, m), 8.66 (1H, d, J = 5.1 Hz), 8.77 (1H, s), 9.06 (1H, s), 9.28 (1H, s). MS (API): m/z 260.9 (M + H)+

With the rapid development of chemical substances, we look forward to future research findings about 24340-77-0

Reference£º
Article; Fujimoto, Jun; Hirayama, Takaharu; Hirata, Yasuhiro; Hikichi, Yukiko; Murai, Saomi; Hasegawa, Maki; Hasegawa, Yuka; Yonemori, Kazuko; Hata, Akito; Aoyama, Kazunobu; Cary, Douglas R.; Bioorganic and Medicinal Chemistry; vol. 25; 12; (2017); p. 3018 – 3033;,
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

To a reaction flask were added compound 22 (100 mg, 0.195 mmol), 4-bromoisothiazole (50 mg, 0.293 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 hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 42 mg of a product, yield: 46%. LC-MS(APCI): m/z = 469.5 (M+1)+. 1H NMR (400 MHz, CDCl3) delta 8.69 (d, J = 2.4 Hz, 1H), 8.58 (d, J = 9.6 Hz, 2H), 7.94 (d, J = 2.4 Hz, 1H), 7.74 (s, 1H), 7.67 (d, J = 9.0 Hz, 2H), 7.23 (s, 1H), 5.21 (d, J = 52.0 Hz, 1H), 3.56 (d, J = 3.1 Hz, 1H), 3.52 – 3.44 (m, 2H), 3.30 (t, J = 9.7 Hz, 1H), 2.26 – 2.19 (m, 1H), 2.03 – 1.97 (m, 1H).

With the rapid development of chemical substances, we look forward to future research findings about 24340-77-0

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.,24340-77-0

To a reaction flask were added compound 22 (100 mg, 0.195 mmol), 4-bromoisothiazole (50 mg, 0.293 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 hour. After TLC detected the reaction was complete, the reaction was concentrated, purified by silica gel column chromatography to afford 42 mg of a product, yield: 46%. LC-MS(APCI): m/z = 469.5 (M+1)+. 1H NMR (400 MHz, CDCl3) delta 8.69 (d, J = 2.4 Hz, 1H), 8.58 (d, J = 9.6 Hz, 2H), 7.94 (d, J = 2.4 Hz, 1H), 7.74 (s, 1H), 7.67 (d, J = 9.0 Hz, 2H), 7.23 (s, 1H), 5.21 (d, J = 52.0 Hz, 1H), 3.56 (d, J = 3.1 Hz, 1H), 3.52 – 3.44 (m, 2H), 3.30 (t, J = 9.7 Hz, 1H), 2.26 – 2.19 (m, 1H), 2.03 – 1.97 (m, 1H).

With the rapid development of chemical substances, we look forward to future research findings about 24340-77-0

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, 4-Bromoisothiazole is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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, 24340-77-0 4-Bromoisothiazole 5200358, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Shenzhen Tajirui Bio-pharmaceutical Co., Ltd.; Wang Yihan; Zhao Jiuyang; (35 pag.)CN109651359; (2019); 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.24340-77-0,4-Bromoisothiazole,as a common compound, the synthetic route is as follows.

General procedure: 2 wt% DL-alpha-Tocopherolmethoxypolyeneglycol succinate solution (1.5 mL) was added to a mixture of 5-methoxycarbonylbenzofuran-2-MIDA boronate (200 mg, 0.604 mmol), (dtbpf)PdCl2 (32 mg, 0.048 mmol) and bromobenzene (95 mg, 0.604 mmol) under N2. Et3N (0.25 mL, 1.81 mmol) was added to thesuspension under N2. The reaction mixture was vigorously stirred at 40 C for 22 h under N2. Theresulting mixture was diluted with water to form a precipitate, which was filtered, washed with water anddissolved with CHCl3. The obtained organic solutions were dried over Na2SO4 and concentrated. Theresidue was purified by flash chromatography (SiO2, AcOEt : hexane = 30 : 70) to give 143.0 mg (94%)of white powde;

As the paragraph descriping shows that 24340-77-0 is playing an increasingly important role.

Reference£º
Article; Sakurai, Yohji; Heterocycles; vol. 94; 7; (2017); p. 1322 – 1336;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com