Cl.[NH:2]([C:4]([C:6]1([NH:9][C:10]([C:12]2([NH:15][C:16]([C:18]3[N:22]4[C@@:23]([CH2:36][C:37]5[CH:42]=[CH:41][C:40]([C:43]#[N:44])=[CH:39][CH:38]=5)([CH3:35])[C:24](=[O:34])[N:25]([C:26]5[CH:31]=[C:30]([Cl:32])[CH:29]=[C:28]([Cl:33])[CH:27]=5)[C:21]4=[N:20][CH:19]=3)=[O:17])[CH2:14][CH2:13]2)=[O:11])[CH2:8][CH2:7]1)=O)[NH2:3].Cl.C(O[C:49]([CH:51]1[CH2:53][CH2:52]1)=[NH:50])C.CCN(CC)CC>CN(C=O)C>[CH:51]1([C:49]2[NH:50][C:4]([C:6]3([NH:9][C:10]([C:12]4([NH:15][C:16]([C:18]5[N:22]6[C@@:23]([CH2:36][C:37]7[CH:38]=[CH:39][C:40]([C:43]#[N:44])=[CH:41][CH:42]=7)([CH3:35])[C:24](=[O:34])[N:25]([C:26]7[CH:31]=[C:30]([Cl:32])[CH:29]=[C:28]([Cl:33])[CH:27]=7)[C:21]6=[N:20][CH:19]=5)=[O:17])[CH2:13][CH2:14]4)=[O:11])[CH2:7][CH2:8]3)=[N:2][N:3]=2)[CH2:53][CH2:52]1To a solution of (R)-5-(4-cyano-benzyl)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid [1-(1-hydrazinocarbonyl-cyclopropylcarbamoyl)-cyclopropyl]-amide hydrochloride (0.080 g, 0.12 mmol) and cyclopropanecarboximidic acid ethyl ester hydrochloride (0.018 g, 0.12 mmol) in DMF (1 mL) was added Et3N (0.051 mL, 0.37 mmol). The reaction was heated in a microwave at 140° C. for 45 min and then at 180° C. for 1.5 h. The mixture was cooled to room temperature and purified via reverse-phase HPLC to give (R)-5-(4-cyano-benzyl)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid {1-[1-(5-cyclopropyl-4H-1,2,4-triazol-3-yl)-cyclopropylcarbamoyl]-cyclopropyl}-amide (0.022 g, 28%) as a white solid, m/z 670.8 [M+1]+.
불러오는 중…