Category: 24340-77-0

It is a common heterocyclic compound, the isothiazole compound, 4-Bromoisothiazole, cas is 24340-77-0 its synthesis route is as follows.

4-bromoisothiazole (commercially available from Aurora, 500 mg, 3.05 mmol) was dissolved in degassed 1 ,2-Dimethoxyethane (DME) (5 ml). Pd(Ph3)4 (176 mg, 0.152 mmol) was added thereto. The reaction mixture was stirred at room temperature for 15min. [2,4-bis(methyloxy)-5-pyrimidinyl]boronic acid (commercially available from Aldrich ,1178 mg, 6.40 mmol) and 5ml_ of degassed 1 M/H2O solution of NaHCO3 were added to the reaction mixture under N2 atm. After 2h30min stirring at 900C the mixture was diluted with water and extracted with DCM. The collected organic phases were evaporated. The residue was purified by flash chromatography eluting with cyclohexane/EtOAc 5:1. 686 mg of the title compound were isolated as a yellow solid. MS (ES) {mlz): 224.06 [M+H]+.

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：
Patent; Glaxo Group Limited; WO2009/43883; (2009); 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.

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 × 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, 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：
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

It is a common heterocyclic compound, the isothiazole compound, 4-Bromoisothiazole, cas is 24340-77-0 its synthesis route is as follows.

In a nitrogen atmosphere at 100 C,(2E) -3- (4- (tributylstannyl) pyridin-3-yl) ethyl acrylate (33 mg)4-bromoisothiazole (17.41 mg),Pd (Ph3P) 4 (8.18 mg),Cuprous iodide (I) (2.70 mg),A mixture of cesium fluoride (21.50 mg) and DMF (1.5 mL) was stirred at room temperature for 13 hours.Similarly, in a nitrogen atmosphere, 100 C,(2E) -3- (4- (tributylstannyl) pyridin-3-yl) acrylate (497 mg)4-bromoisothiazole (262 mg), Pd (Ph3P) 4 (123 mg),A mixture of cuprous iodide (I) (40.6 mg), cesium fluoride (324 mg) and DMF (10 mL) was stirred for 13 hours.The reaction mixture was combined and the insoluble material was filtered.The filtrate was diluted with ethyl acetate (20 mL), water (10 mL) and saturated aqueous sodium bicarbonate (10 mL), and the aqueous layer was extracted with ethyl acetate. The extract was washed with water and brine, dried over anhydrous sodium sulfate, and the solvent was removed by distillation under reduced pressure. The residue was purified by silica gel column chromatography (ethyl acetate / hexane) to give the title compound (222 mg).

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：
Patent; TAKEDA PHARMACEUTICAL COMPANYLIMITED; HIRAYAMA, TAKAHARU; FUJIMOTO, JUN; CARY, DOUGLAS ROBERT; OKANIWA, MASANORI; HIRATA, YASUHIRO; (289 pag.)TW2017/14883; (2017); A;,
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.

l-<4-Meth l-pyridin-3-yl )-i?uda/olidin-2-one ( I- 14b: I SOiug. 0.847mmol) was reacted with 4-bromo~isothiazole ( 166tng, 1.01 nunol ). 1. 4-dioxane ( 15ml ), copper iodide ( l6.09mg. O.U847mmol). trans- 1 ,2-diamino cyciohcxane (29mg, 0.254mmol) and potassium phosphate <540mg. 2.541 mnu>? to afford the crude product. Purification by column chromatography on silica gel (2% McOH in CHCh) afforded ) 20mg of the product (54.54’J¡ã yield). 1H NMR (C DCh. 300 MI b): 6 8.82 (s, 111), 8.65-8.25 (m. 3H). 7.4-7.1 (m> H D.4.20-3.95 (in, 4H). 2.19 (s, 311)I CMS purit) : 97.95%, mi? 261.0 (M 1 1) HPl C: 96.08%

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; NOVARTIS AG; BOCK, Mark G.; GAUL, Christoph; GUMMADI, Venkateshwar Rao; SENGUPTA, Saumitra; WO2010/149755; (2010); 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.

Intermediate 58: Methyl 6-(benzenesulphonylmethyl)-3-(isothiazol-4-yl)-2-methoxybenzoate[0588] A mixture of methyl 6-(benzenesulphonylmethyl)-2-methoxy-3-(4,4,5,5- tetramethyl-l,3,2-dioxaborolan-2-yl)benzoate (Intermediate 59, 0.15g), tri-tert-butyl- phosphinium tetrafluoroborate (O.Olg), cesium carbonate (0.34g), tris-(dibenzylideneacetone)- dipalladium (0.016g), and 4-bromoisothiazole (0.06g) in dioxane (3.2ml) and water (0.4ml) was degassed and then heated in the microwave at 120C for 20 minutes. After cooling, the mixture was diluted with ether, dried (MgS04) and filtered. The filtrate was evaporated to dryness and the residue was purified by chromatography on silica, eluting with a mixture of ethyl acetate and cyclohexane with a gradient of 0-60% to give crude methyl 6- (benzenesulphonylmethyl)-3-(isothiazol-4-yl)-2-methoxy-benzoate (0..044g) as an oil. The material was used without further purification or characterisation.

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; ZAFGEN CORPORATION; DYKE, Hazel, Joan; CRAMP, Susan, Mary; PALLIN, Thomas, David; KULAGOWSKI, Janusz, Jozef; MONTANA, John, Gary; ZAHLER, Robert; WO2011/44506; (2011); A2;,
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.

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).

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; 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

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 4: 3-(6-Chloro-l-isothiazol-4-yl-2-methyl-lH-indol-3-ylsulfanyl)-benzoic acid ethyl ester[00503] 3-(6-Chloro-2-methyl-lH-indol-3-ylsulfanyl)-benzoic acid ethyl ester (0.250 g, 0.723 mmol) was combined with CuO (0.118 g, 1.48 mmol), potassium carbonate (0.130 g, 0.941 mmol) and 4- bromoisothiazole (0.250 g, 1.52 mmol) in pyridine (2 mL) and the reaction was heated to 145 C overnight. After cooling the reaction was partitioned between ?0 and DCM and the aqueous layer was extracted with DCM. The combined organics were dried over MgS04 and concentrated then submitted to silica gel chromatograp -20% EtOAc in hexanes) to yield the title compound.

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; AMIRA PHARMACEUTICALS, INC.; ROPPE, Jeffrey, Roger; PARR, Timothy, Andrew; STOCK, Nicholas, Simon; VOLKOTS, Deborah; HUTCHINSON, John, Howard; WO2012/24620; (2012); A2;,
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.

A solution of 5,7-dimethyl-N-(4-(4,4,5,5-tetramethyl-l,3,2-dioxaborolan-2- yl)phenyl)pyrazolo[l,5-a]pyrimidine-3-carboxamide 6 (286 mg, 0.73 mmol) in DMF (5 mL) was charged with 4-bromoisothiazole (100 mg, 0.60 mmol), potassium acetate (179 mg, 1.8 mmol) and Pd(dppf)Cl2DCM adduct (49 mg, 0.06 mmol) under argon at room temperature. The reaction mixture was heated to 100C for 16 h. The reaction mixture was quenched with water (5 mL), extracted with ethyl acetate (3 X 10 mL) and concentrated under vacuum to obtain crude compound. The crude compound was purified by FCC (eluent, 3-5% methanol in DCM) to afford the title compound as an off-white solid (50 mg, 23%).XH NMR (400 MHz, CDCI3) delta 10.24 (s, 1H), 8.79 (s, 1H), 8.71 (s, 1H), 8.68 (s, 1H), 7.84 (d, J=8.57 Hz, 2H), 7.61 (d, J=8.57 Hz, 2H), 6.78 (s, 1H), 2.83 (s, 3H), 2.74 (s, 3H). ES-MS m/z 350.20 (M+H)+. HPLC purity 99.1%.

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; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; LANSBURY, Peter, T.; GOOD, Andrew, C.; BOURQUE, Elyse, Marie Josee; (139 pag.)WO2016/73895; (2016); 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.

General procedure: General Procedure E: Preparation of Coupled Aryl and Heteroaryl Groups Using Buchwald Catalyzed Coupling Conditions Between an Organohalide in the Presence of a Tin Reagent (0331) [00219] A solution of organobromide (1.0 equivalent), organochloride (1.0 equivalent), hexabutylditin (1.0 equivalent) and Pd(dppf)Cl2?DCM (10 mol%) in anhydrous 1,4-dioxane (10 mL/mmol) was stirred at 100 oC under N2 overnight, then cooled and quenched with water (20 mL/mmol). The resulting mixture was extracted with EtOAc (20 mL/mmol x 3), the organic phases were separated and dried over anhydrous Na2SO4 and filtered. The filtrate was concentrated in vacuo, and the resulting residue was purified by silica gel column (0332) chromatography or preparative-TLC to afford the coupled ring system.

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; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GREENLEE, William, J.; GOOD, Andrew, C.; (309 pag.)WO2017/176961; (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.

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, 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