Hydrochloric Acid → methyl 2-[(3-{1-[(cyclopropylmethyl)amino]-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl}-1,1-dioxido-4H-1,2,4-benzothiadiazin-7-yl)oxy]ethanimidoate

反応式

Cl.[CH:2]1([CH2:5][NH:6][N:7]2[C:16]3[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=3)[C:10]([OH:17])=[C:9]([C:18]3[NH:23][C:22]4[CH:24]=[CH:25][C:26]([O:28][CH2:29][C:30]#[N:31])=[CH:27][C:21]=4[S:20](=[O:33])(=[O:32])[N:19]=3)[C:8]2=[O:34])[CH2:4][CH2:3]1.[CH3:35][OH:36]>>[CH:2]1([CH2:5][NH:6][N:7]2[C:16]3[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=3)[C:10]([OH:17])=[C:9]([C:18]3[NH:23][C:22]4[CH:24]=[CH:25][C:26]([O:28][CH2:29][C:30](=[NH:31])[O:36][CH3:35])=[CH:27][C:21]=4[S:20](=[O:33])(=[O:32])[N:19]=3)[C:8]2=[O:34])[CH2:3][CH2:4]1

参加物

反応物 3

HCID 313Hydrochloric Acid

HCID 887Methanol

HCID 136358425[(3-{1-[(cyclopropylmethyl)amino]-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl}-1,1-dioxido-4H-1,2,4-benzothiadiazin-7-yl)oxy]acetonitrile

生成物 1

HCID 136358426methyl 2-[(3-{1-[(cyclopropylmethyl)amino]-4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl}-1,1-dioxido-4H-1,2,4-benzothiadiazin-7-yl)oxy]ethanimidoate

実験手順

Hydrogen chloride gas was bubbled into a solution of the product of Example 392A (50 mg, 0.11 mmol) in methanol (10 mL) at 0° C. until saturation. The reaction was stirred at room temperature for 3 hours. The solution was evaporated under reduced pressure to give title compound (quantitative yield).