N1C2C(=CC=CC=2S(NC2C=CC([C:19]([OH:21])=[O:20])=CC=2)(=O)=O)C=CC=1.CCN=C=N[CH2:29][CH2:30][CH2:31]N(C)C.[CH:35]1[CH:36]=[CH:37][C:38]2[N:43](O)N=[N:41][C:39]=2[CH:40]=1.[CH3:45]CN(C(C)C)C(C)C>CN(C=O)C.O>[CH:36]12[N:41]([C:19]([O:21][C:30]([CH3:31])([CH3:45])[CH3:29])=[O:20])[CH:39]([CH2:40][CH2:35]1)[CH2:38][NH:43][CH2:37]2To a stirred solution of acid VIII (0.00021 mol, 1 eq) in DMF (5 mL), EDCI (0.048 g, 0.00024 mol, 1.1 eq), HOBt (0.038 g, 0.00024 mol, 1.1 eq) and DIPEA (0.15 mL, 0.00078 mol, 2.5 eq) were added at 0° C. and stirred for 15 minutes. A solution of amine LXXI (0.00021 mol, 1 eq) was then added at 0° C. and then the resulting mixture was allowed to stir at room temperature for overnight. After completion of the reaction, water (20 mL) was added and extracted with ethyl acetate (2×30 mL). The combined organic layer was dried over anhydrous Na2SO4 and concentrated under reduced pressure. The crude product was purified by column chromatography (silica gel, 60-120 mess, 70% ethyl acetate in hexane) to give compound in 49-55% yield.
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