Category: 10271-85-9

Brief introduction of 10271-85-9

The synthetic route of 10271-85-9 has been constantly updated, and we look forward to future research findings.

10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 318 (12 mg, 0.029 mmol), isothiazole-5-carboxylic acid (7.38 mg, 0.057 mmol) and triethylamine (7.97 mul, 0.057 mmol) were suspended in toluene (1 mL) in a pressure rated 1 dram vial. Diphenylphosphoryl azide (15.73 mg, 0.057 mmol) was added to the mixture which was heated to 110 C for 3 hours. The crude reaction mixture was purified by reverse phase HPLC (Method D, 65-100% 20 min, 100% 5 min) to yield Example 621 (1.3 mg, 2.38 mmol, 8% yield). C-MS: Method H, RT = 1.25 min, MS (ESI) m/z: 546.10 (M+H)+. 1HNMR (500 MHz, DMSO-d6) delta 8.77 (s, 1H), 8.62 (s, 1H), 8.21 (s, 1H), 8.02-8.12 (m, 1H), 7.88 (s, 1H), 6.81 (s, 1H), 4.61-4.69 (m, 2H), 4.46-4.56 (m, 2H), 4.10 (s, 3H), 3.19 (s, 3H)., 10271-85-9

The synthetic route of 10271-85-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; ZHANG, Xiaojun; PRIESTLEY, Eldon Scott; BATES, J. Alex; HALPERN, Oz Scott; REZNIK, Samuel Kaye; RICHTER, Jeremy M.; (1137 pag.)WO2018/13774; (2018); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Simple exploration of 10271-85-9

10271-85-9, 10271-85-9 Isothiazole-5-carboxylic acid 5200404, aisothiazole compound, is more and more widely used in various fields.

10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The target compounds were synthesized using the procedure given in literature by refluxing aryl/heteroaryl acids with carbohydrazide 4a or 4b in phosphorous oxychloride. The reaction was monitored with the help of TLC to check its completion. After completion of reaction, the mixture was poured over crushed ice and allowed to precipitate. The precipitate was vacuum filtered, dried and recrystallized from methanol. Column chromatography was done on using n-hexane: ethylacetate mixture (7:3). Solvent was evaporated invacuo using rotary evaporator to obtain pure product.

10271-85-9, 10271-85-9 Isothiazole-5-carboxylic acid 5200404, aisothiazole compound, is more and more widely used in various fields.

Reference£º
Article; Rane, Rajesh A.; Bangalore, Pavankumar; Borhade, Sheetal D.; Khandare, Preeti K.; European Journal of Medicinal Chemistry; vol. 70; (2013); p. 49 – 58;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Simple exploration of 10271-85-9

10271-85-9 Isothiazole-5-carboxylic acid 5200404, aisothiazole compound, is more and more widely used in various.

10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of compound 117 (0.35 g, 2.67 mmol), diphenylphosphoryl azide (0.57 mL, 2.67 mmol) and triethylamine (0.37 mL, 2.67 mmol) in tert-butanol (10 mL) was heated at reflux for 5 hours, at which time thin layer chromatography (DCM/Hexanes) indicates the reaction is complete. The reaction mixture was cooled to room temperature, poured into water and extracted with diethyl ether (3¡Á). The combined ether extracts were washed with brine, dried over sodium sulfate, and concentrated to afford a beige solid. Purification by column chromatography (SiO2, 40% ethyl acetate/hexanes) afforded compound 121 as a white solid 0.245 g (46%). 1H-NMR (400 MHz, DMSO-d6) delta 8.15(d, 1H), 6.72 (d, 1H), 1.48 (s, 9H)., 10271-85-9

10271-85-9 Isothiazole-5-carboxylic acid 5200404, aisothiazole compound, is more and more widely used in various.

Reference£º
Patent; Schering Corporation; US2007/105864; (2007); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

New learning discoveries about 10271-85-9

10271-85-9, As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10271-85-9,Isothiazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of isothiazole-5-carboxylic acid (331 mg, 2.6 mmol) in DMF (21 ml) cooled to 0C was added HATU (1.0 g, 2.8 mmol) and after stirring for 30 minutes a solution ofIntermediate 7-d (1.0 g, 2.1 mmol) and DIPEA (1.1 ml, 6.4 mmol) in DMF (3 ml) was addeddropwise. The reaction was then stirred at room temperature for 1 day. A saturatedaqueous solution of ammonium chloride and ethyl acetate were then added, the organic layer was separated, washed with a saturated aqueous solution of NaHCO3 and brine, dried over anhydrous MgSO4, filtered and concentrated under reduced pressure. Purification by silica gel chromatography provided Intermediate 15-a as a beige solid.

10271-85-9, As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

Reference£º
Patent; PHARMASCIENCE INC.; LAURENT, Alain; ROSE, Yannick; MORRIS, Stephen J.; (181 pag.)WO2017/49401; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com

 

Downstream synthetic route of 10271-85-9

As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

10271-85-9, Isothiazole-5-carboxylic acid is a isothiazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-isothiazolecarboxylic acid (500 mg, 3.87 mmol, commercially available from e.g. Fluorochem or Astatech) in dry Dichloromethane (DCM) (12.9 ml) was stirred at room temperature under an atmosphere of argon. EDC (891 mg, 4.65 mmol) and HOBt (296 mg, 1.936 mmol) were added to the stirred solution. The resulting solution was stirred at room temperature under an atmosphere of argon for 1/2 hour. After this time, 1 ,1-dimethylethyl hydrazinecarboxylate (614 mg, 4.65 mmol) was added and the solution was stirred for a further 18 hours at room temperature (overnight). The solution was diluted with DCM (approx 30 ml) and washed with water (2 x 20ml). The organics were dried over MgSO4, filtered and concentrated under reduced pressure to give a brown coloured oil. The oil was chromatographed [Sitheta2, EtOAc/Hexane 0-100%] to give a thick, yellow-coloured oil which solidified on standing to afford the product in 480 mg. The residue was used directly in the next step. LCMS [M+H]+ 244.14 (at) 0.66 min (2 min run).

As the paragraph descriping shows that 10271-85-9 is playing an increasingly important role.

Reference£º
Patent; GLAXO GROUP LIMITED; DEAN, David Kenneth; MUNOZ-MURIEDAS, Jorge; SIME, Mairi; STEADMAN, Jon Graham Anthony; THEWLIS, Rachel Elizabeth Anne; TRANI, Giancarlo; WALTER, Daryl Simon; WO2010/125102; (2010); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com