Реакция #331551

Уравнение реакции

N-isopropyl-2,2-dimethyl-3-oxo-N-[(3R)-piperidin-3-yl]-4-[2-(propionylamino)ethyl]-7-(trifluoromethyl)-3,4-dihydro-2H-1,4-benzoxazine-6-carboxamide hydrochloride

N-Boc valine

WSC

HOBt

→

desired title compound

Выход 113.1%

tert-Butyl [(1S)-1-({(3R)-3-[{[2,2-dimethyl-3-oxo-4-[2-(propionylamino)ethyl]-7-(trifluoromethyl)-3,4-dihydro-2H-1,4-benzoxazin-6-yl]carbonyl}(isopropyl)amino]piperidin-1-yl}carbonyl)-2-methylpropyl]carbamate

Выход 113.1%

Растворители

chloroform

triethylamine

Условия реакции

Обработка

1. 1
   Концентрированиеthe solvent was concentrated
2. 2
   Другоеthe obtained residue was purified by column chromatography (hexane:ethyl acetate=1:2)

Методика

To N-isopropyl-2,2-dimethyl-3-oxo-N-[(3R)-piperidin-3-yl]-4-[2-(propionylamino)ethyl]-7-(trifluoromethyl)-3,4-dihydro-2H-1,4-benzoxazine-6-carboxamide hydrochloride (300 mg) were added N-Boc valine (158 mg), WSC (210 mg), HOBt (150 mg), triethylamine (0.30 ml) and chloroform (5 ml), and the mixture was stirred at room temperature overnight. After the reaction is completed, the solvent was concentrated, and the obtained residue was purified by column chromatography (hexane:ethyl acetate=1:2) to give the desired title compound (440 mg) as white amorphous.

Источник