反应详情

Using analogous procedures to those described in the second and third paragraphs of Example 12, pentafluorophenyl o-fluoro-p-[N-methyl-N-((6RS)-2-methyl-4-oxo-3-pivaloyloxymethyl-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)amino]benzoate was reacted with methyl (2S)-2-amino-4-(tetrazol-5-yl)butyrate to give methyl (2S)-2-{o-fluoro-p-[N-methyl-N-((6RS)-2-methyl-3-pivaloyloxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)amino]benzamido}-4-(tetrazol-5-yl)butyrate in 73% yield which in turn was hydrolysed with aqueous sodium hydroxide solution to give (2S)-2-{o-fluoro-p-[N-methyl-N-((6RS)-2-methyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclopenta[g]quinazolin-6-yl)amino]benzamido}-4-(tetrazol-5-yl)butyric acid in 81% yield, m.p. 203°-205° C.;