反応式
[NH2:1][C:2](=[O:8])[CH2:3][CH2:4][C:5](O)=[O:6].[NH2:9][CH2:10][CH2:11][O:12][CH2:13][CH2:14][O:15][CH2:16][CH2:17][O:18][CH2:19][CH2:20][NH:21][S:22]([C:25]1[CH:30]=[CH:29][CH:28]=[C:27]([CH:31]2[C:40]3[C:35](=[C:36]([Cl:42])[CH:37]=[C:38]([Cl:41])[CH:39]=3)[CH2:34][N:33]([CH3:43])[CH2:32]2)[CH:26]=1)(=[O:24])=[O:23]>>[Cl:41][C:38]1[CH:39]=[C:40]2[C:35](=[C:36]([Cl:42])[CH:37]=1)[CH2:34][N:33]([CH3:43])[CH2:32][CH:31]2[C:27]1[CH:26]=[C:25]([S:22]([NH:21][CH2:20][CH2:19][O:18][CH2:17][CH2:16][O:15][CH2:14][CH2:13][O:12][CH2:11][CH2:10][NH:9][C:5](=[O:6])[CH2:4][CH2:3][C:2]([NH2:1])=[O:8])(=[O:23])=[O:24])[CH:30]=[CH:29][CH:28]=1参加物
3
反応物 2
生成物 1
実験手順
Compound 247 was prepared following the procedure outlined in Example 215 using 4-amino-4-oxobutanoic acid (7.6 mg, 0.0646 mmol) and N-(2-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)ethyl)-3-(6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)benzenesulfonamide (Compound 28, 50 mg, 0.0646 mmol). Purification by preparative HPLC gave the title compound (27.8 mg) as a TFA salt. 1H-NMR (400 MHz, CD3OD): δ 7.88 (d, 1H), 7.75 (s, 1H), 7.64 (t, 1H), 7.55 (s, 1H), 7.51 (d, 1H), 6.84 (s, 1H), 4.78-4.71 (m, 2H), 4.55-4.48 (m, 1H), 3.81-3.75 (m, 1H), 3.63-3.55 (m, 10H), 3.51-4.45 (m, 5H), 3.44-3.41 (m, 3H), 3.38-3.31 (m, 3H), 3.13 (s, 3H), 3.07-3.02 (t, 2H), 2.48-2.43 (m, 4H). MS (m/z): 645.32 [M+H]+.
後処理
- customCompound 247 was prepared
- customPurification by preparative HPLC
出典と根拠
- ORDレコード
- ord-5624e2a7625343c29fed58736d35de72
- 出典データセット
- uspto-grants-2015_03
- 特許番号
- US08969377B2
関連ノート
読み込み中…