Electric Literature of 959235-95-1,Some common heterocyclic compound, 959235-95-1, name is 6-(Trifluoromethoxy)indoline, molecular formula is C9H8F3NO, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
HATU (7.02 g, 18.46 mmol) was added to a mixture of 6-(trifluoromethoxy)indoline [CAS 959235-95-1 ] (2.5 g, 12.3 mmol), 2-(4-chloro-2-fluorophenyl)acetic acid [CAS 194240-75-0] (2.32 g, 12.3 mmol) and diisopropylethylamine (6.1 ml_, 36.9 mmol) in DMF (100 ml_). The resulting mixture was stirred at room temperature for 12 h. The mixture was diluted with water, the precipitate was filtered off, and washed with water. The residue was taken up with EtOAc and the organic solution was washed with a 10% aqueous solution of K2CO3, brine, dried over MgSO , filtered and the solvent was evaporated under reduced pressure. The residue product was crystallized from diisopropyl ether to give 2-(4-chloro-2- fluorophenyl)-1 -(6-(trifluoromethoxy)indolin-1 -yl)ethanone 10a (4 g).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 6-(Trifluoromethoxy)indoline, its application will become more common.