Methyl 3-aminopropanoate hydrochloride → Methyl N-(3-{5-[2-(methoxymethyl)-2'-methylbiphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzoyl)-beta-alaninate
反応式
[CH3:1][O:2][CH2:3][C:4]1[CH:9]=[C:8]([C:10]2[O:14][N:13]=[C:12]([C:15]3[CH:16]=[C:17]([CH:21]=[CH:22][CH:23]=3)[C:18](Cl)=[O:19])[N:11]=2)[CH:7]=[CH:6][C:5]=1[C:24]1[CH:29]=[CH:28][CH:27]=[CH:26][C:25]=1[CH3:30].Cl.[CH3:32][O:33][C:34](=[O:38])[CH2:35][CH2:36][NH2:37]>>[CH3:1][O:2][CH2:3][C:4]1[CH:9]=[C:8]([C:10]2[O:14][N:13]=[C:12]([C:15]3[CH:16]=[C:17]([CH:21]=[CH:22][CH:23]=3)[C:18]([NH:37][CH2:36][CH2:35][C:34]([O:33][CH3:32])=[O:38])=[O:19])[N:11]=2)[CH:7]=[CH:6][C:5]=1[C:24]1[CH:29]=[CH:28][CH:27]=[CH:26][C:25]=1[CH3:30]参加物
3
実験手順
The title compound was prepared following procedure described in example 121 starting from 3-{5-[2-(methoxymethyl)-2′-methylbiphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzoyl chloride, prepared as in example 130, and beta-alanine methyl ester hydrochloride. The title compound was obtained as a white foam. 1H NMR: (DMSO-d6, 300 MHz) δ 8.87 (m, 1H), 8.58 (m, 1H), 8.35 (m, 1H), 8.27 (m, 1H), 8.19 (dd, J=1.9 Hz, 7.9 Hz, 1H), 8.07 (m, 1H), 7.72 (t, J=7.9 Hz, 1H), 7.43 (d, J=7.9 Hz, 1H), 7.38-7.25 (m, 3H), 7.15 (m, 1H), 4.23 (d, J=12.9 Hz, 1H), 4.17 (d, J=12.9 Hz, 1H), 3.63 (s, 3H), 3.54 (m, 1H), 3.25 (s, 3H), 3.64 (t, J=6.9 Hz, 2H), 2.04 (s, 3H). LC/MS (Method B): 486.2 (M+H)+ 484.2 (M−H)−. HPLC (Method A) Rt: 5 min (purity: 99.3%).