反应详情

The procedure for the preparation of [2-(3-cyclopropyl-2,4-dioxo-3,4-dihydro-2H-quinazolin-1-ylmethyl)-1-(3-methyl-butyl)-1H-benzoimidazol-5-ylmethyl]-carbamic acid tert-butyl ester was followed starting from 4-methoxy-1H-quinolin-2-one (106 mg, 0.605 mmol) and 2,2-dimethyl-propionic acid 4-[5-(tert-butoxycarbonylamino-methyl)-2-chloromethyl-benzoimidazol-1-yl]-butyl ester; HCl salt (296 mg, 0.605 mmol). Purification by flash chromatography (eluent hexane-ethyl acetate 1:1, 1:2, 0:1) afforded 2,2-dimethyl-propionic acid 4-[5-(tert-butoxycarbonylamino-methyl)-2-(4-methoxy-2-oxo-2H-quinolin-1-ylmethyl)-benzoimidazol-1-yl]-butyl ester (240 mg, 67%) as a white solid:

1. customPurification by flash chromatography (eluent hexane-ethyl acetate 1:1, 1:2, 0:1)