I.[NH2:2][C:3]1[C:4]([C:11]([NH:13][C:14](=[NH:17])SC)=[O:12])=[N:5][C:6]([Cl:10])=[C:7]([NH2:9])[N:8]=1.[NH2:18][CH:19]1[CH2:24][CH2:23][N:22](C(OC(C)(C)C)=O)[CH2:21][CH2:20]1>CN(C=O)C.O>[ClH:10].[NH2:2][C:3]1[C:4]([C:11]([NH:13][C:14](=[NH:17])[NH:18][CH:19]2[CH2:24][CH2:23][NH:22][CH2:21][CH2:20]2)=[O:12])=[N:5][C:6]([Cl:10])=[C:7]([NH2:9])[N:8]=1A solution of 1-(3,5-diamino-6-chloro-pyrazine-2-carbonyl)-2-methyl-isothiourea hydroiodide (7.2 g, 18.4 mmol) and 4-amino-1-Boc-piperidine (5.5 g, 27.5 mmol) in DMF (40 mL) is stirred and heated at 50° C. for 4 hours. The mixture is diluted with water (150 mL) and sonicated for 2 hours. The resulting suspension is collected by filtration and suspended in 4 M HCl in dioxane (40 mL). MeOH (20 mL) is added and the mixture is stirred at room temperature overnight and then filtered. The solid is washed with EtOH (2×10 mL) and dried to afford the title compound. [M+H]+ 313
読み込み中…
