With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55512-82-8,3-Bromoisothiazole,as a common compound, the synthetic route is as follows.
55512-82-8, General procedure: N-(4-Bromo-3-{[(d imethylam ino)methylene]su lfamoyl}phenyl)-2-(2-chlorophenyl)acetamide (amount as indicated in examples) was dissolved in methanol (3 mL in case of 0.59 mmol scale) and degassed with nitrogen. Bis(pinacolato)diboron (2.5 eq), mesylate[(di(1 -adamantyl)-n-butylphosphine)-2-(2?-amino-1 ,1 ?-biphenyl)]palladium(l I) (cataCXium A Pd G3, 0.05 eq) and N,N-diisoproyplethylamine (2.5 eq) were added andit was stirred for 1 hour at 50C. The catalyst was removed by filtration and the filtrate was reduced in vacuo.The crude was redissolved in n-propanol (3 mL in case of 0.59 mmol scale), followed by degassing with nitrogen. The corresponding hetarylbromide (2 eq), potassium fluoride (0.23 eq), bis(tri-tert-butylphosphine)palladium(0) (0.05 eq) and triphenylphosphine (0.05 eq) were added. It was again degassed with nitrogen and potassium phosphate (2.5 eq) was added, followed by irradiating for 1 hour at 10000 in the microwave.Any precipitate was removed by filtration and the filtrate was concentrated in vacuo andredissolved in methanol (2 mL in case of 0.59 mmol scale). Aqueous ammoniumhydroxide solution (33%, 2 mL) was added. It was stirred until UPLC-MS showed completion of deprotection. In most cases stirring overnight was sufficient, in certain cases longer stirring and addition of further aqueous ammonium hydroxide solution was necessary. The reaction mixture was then concentrated in vacuo and purified as indicatedintheexamples.
55512-82-8 3-Bromoisothiazole 15323364, aisothiazole compound, is more and more widely used in various fields.
Reference£º
Patent; BAYER PHARMA AKTIENGESELLSCHAFT; WERNER, Stefan; MESCH, Stefanie; CLEVE, Arwed; BRAeUER, Nico; HERBERT, Simon, Anthony; KOCH, Markus; DAHLLOeF, Henrik; OSMERS, Maren; HARDAKER, Elizabeth; LISHCHYNSKYI, Anton; (673 pag.)WO2017/191000; (2017); A1;,
Isothiazole – Wikipedia
Isothiazole – ScienceDirect.com