1-Aminocyclopropane-1-carboxylic acid → 1-(4-(5-(1-(2-fluorophenyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-3-yl)benzylamino)cyclopropanecarboxylic acid

HRID 219599

反応式

HRID 219599 の反応式
[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[N:8]1[C:12]([C:13]2[CH:18]=[CH:17][N:16]=[CH:15][CH:14]=2)=[C:11]([C:19]2[O:23][N:22]=[C:21]([C:24]3[CH:31]=[CH:30][C:27]([CH:28]=O)=[CH:26][CH:25]=3)[N:20]=2)[N:10]=[N:9]1.[NH2:32][C:33]1([C:36]([OH:38])=[O:37])[CH2:35][CH2:34]1>>[F:1][C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][C:3]=1[N:8]1[C:12]([C:13]2[CH:14]=[CH:15][N:16]=[CH:17][CH:18]=2)=[C:11]([C:19]2[O:23][N:22]=[C:21]([C:24]3[CH:25]=[CH:26][C:27]([CH2:28][NH:32][C:33]4([C:36]([OH:38])=[O:37])[CH2:35][CH2:34]4)=[CH:30][CH:31]=3)[N:20]=2)[N:10]=[N:9]1

参加物

3

反応物 2

HCID 5351-Aminocyclopropane-1-carboxylic acidHCID 866481594-(5-(1-(2-fluorophenyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-3-yl) benzaldehyde

生成物 1

HCID 596041541-(4-(5-(1-(2-fluorophenyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-3-yl)benzylamino)cyclopropanecarboxylic acid

実験手順

The title compound was prepared following the procedure described for Example 94, but starting from 4-(5-(1-(2-fluorophenyl)-5-(pyridin-4-yl)-1H-1,2,3-triazol-4-yl)-1,2,4-oxadiazol-3-yl)benzaldehyde, obtained as described in Example 113, Step 1, (200 mg; 0.48 mmol) and 1-aminocyclopropanecarboxylic acid (98.1 mg; 0.97 mmol) to give Example 162 as a white solid. 1H NMR: (DMSO-d6, 400 MHz) δ 8.75 (2H, dd, J=4.5, 1.6 Hz), 7.95-7.87 (3H, m), 7.76-7.69 (1H, m), 7.61 (2H, dd, J=4.5, 1.7 Hz), 7.56-7.47 (4H, m), 3.95 (2H, s), 1.18-1.14 (2H, m), 0.96-0.92 (2H, m). LC/MS (Method C): 498 (M+H)+. HPLC (Method F) Rt 2.70 min (Purity: 98.6%).

後処理

  1. customobtained

出典と根拠

ORDレコード
ord-8ca013ab337b44d2a435271978f0dc50
出典データセット
uspto-grants-2012_06
特許番号
US08202856B2

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