Application of 1035235-27-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 1035235-27-8 name is tert-Butyl 4-bromoisoindoline-2-carboxylate, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
Example 136 r(S)-1-(2.4-Difluoro-3-phenoxy-phenyl)-propy|1-(2,3-dihydro-1 H-isoindol-4-yl)-am hydrochlorideStep 1 A solution of Key Intermediate 1 (50 mg, 0.19 mmol), fe -butyl 4- bromoisoindoline-2-carboxylate (57 mg, 0.19 mmol) and sodium fe -butoxide (26 mg, 0.27 mmol) in dioxane (1 ml) was degassed by bubbling through nitrogen for 5 mins. Tris(dibenzylideneacetone)dipalladium (0) (5 mg) and 2,2′-bis(diphenylphosphino)-1 ,1 ‘- binapthyl (5 mg) were added and the reaction mixture was heated to 120 C for 20 mins under microwave irradiation. The mixture was partitioned between sat. sodium hydrogen carbonate and ethyl acetate. The organic fractions were washed with brine, dried over magnesium sulfate, filtered and concentrated. The residue was purified by preparative hplc to give 4-[(S)-1-(2,4-difluoro-3-phenoxy-phenyl)-propylamino]-1 ,3-dihydro-isoindole-2- carboxylic acid tert-butyl ester (23 mg) as a solid.
At the same time, in my other blogs, there are other synthetic methods of this type of compound, tert-Butyl 4-bromoisoindoline-2-carboxylate, and friends who are interested can also refer to it.
Reference:
Patent; ASTEX THERAPEUTICS LIMITED; WOODHEAD, Andrew, James; CHESSARI, Gianni; BESONG, Gilbert, Ebai; CARR, Maria, Grazia; HISCOCK, Steven, Douglas; O’BRIEN, Michael, Alistair; REES, David, Charles; SAALAU-BETHELL, Susanne, Maria; WILLEMS, Hendrika, Maria, Gerarda; THOMPSON, Neil, Thomas; WO2013/64538; (2013); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem