反应详情

A solution of 4-{2-[(2S,4S)-1-((S)-2-methoxycarbonylamino-3-methyl-butyryl)-4-methyl-pyrrolidin-2-yl]-3H-naphth[1,2-d]imidazol-7-yl}-3-trifluoromethoxy-benzoic acid TFA (136 mg, 0.19 mmol; Preparation 17) and HATU (86 mg, 0.23 mmol) in DMA (3 mL) was stirred for 10 min, then (R)-4-(5-amino-pyridin-2-yl)-3-methyl-piperazine-1-carboxylic acid tert-butyl ester (55 mg, 0.19 mmol), and DIPEA (98 μL, 0.56 mmol) were added. The resulting mixture was stirred at RT for 1 h, concentrated, and purified by silica gel chromatography (EtOAc/hexane 20 to 100%) to give the title intermediate (158 mg, 95% yield). (m/z): [M+H]+ calcd for C46H53F3N8O7 887.40 found 887.4.

1. concentrationconcentrated
2. custompurified by silica gel chromatography (EtOAc/hexane 20 to 100%)