{3-(4-Chlorophenyl)-5-oxo-4-[(1E)-3,3,3-trifluoroprop-1-en-1-yl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}acetic acid → N2-{[({3-(4-Chlorophenyl)-5-oxo-4-[(1E)-3,3,3-trifluoroprop-1-en-1-yl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}acetyl)amino][2-(trifluoromethyl)phenyl]acetyl}-2-methylalaninamide

反応式

[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:12](/[CH:13]=[CH:14]/[C:15]([F:18])([F:17])[F:16])[C:11](=[O:19])[N:10]([CH2:20][C:21]([OH:23])=O)[N:9]=2)=[CH:4][CH:3]=1.Cl.[NH2:25][CH:26]([C:36]1[CH:41]=[CH:40][CH:39]=[CH:38][C:37]=1[C:42]([F:45])([F:44])[F:43])[C:27]([NH:29][C:30]([CH3:35])([C:32]([NH2:34])=[O:33])[CH3:31])=[O:28]>>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[N:12](/[CH:13]=[CH:14]/[C:15]([F:16])([F:17])[F:18])[C:11](=[O:19])[N:10]([CH2:20][C:21]([NH:25][CH:26]([C:36]3[CH:41]=[CH:40][CH:39]=[CH:38][C:37]=3[C:42]([F:43])([F:44])[F:45])[C:27]([NH:29][C:30]([CH3:35])([C:32]([NH2:34])=[O:33])[CH3:31])=[O:28])=[O:23])[N:9]=2)=[CH:6][CH:7]=1

参加物

反応物 2

HCID 59536906{3-(4-Chlorophenyl)-5-oxo-4-[(1E)-3,3,3-trifluoroprop-1-en-1-yl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}acetic acid

HCID 89780485N2-{Amino[2-(trifluoromethyl)phenyl]acetyl}-2-methylalaninamide hydrochloride

生成物 1

HCID 56932706N2-{[({3-(4-Chlorophenyl)-5-oxo-4-[(1E)-3,3,3-trifluoroprop-1-en-1-yl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}acetyl)amino][2-(trifluoromethyl)phenyl]acetyl}-2-methylalaninamide

実験手順

Analogously to Example 1, 25 mg (72 μmol) of the compound of Example 11A and 29 mg (79 μmol) of the compound of Example 62A were employed. Purification by HPLC [Method 7] gave 32 mg (70% of theory) of the title compound.

後処理

customPurification by HPLC [Method 7]

出典と根拠

ORDレコード: ord-d9b0abc1dabf471ebfc7b1f13d93afb3
出典データセット: uspto-grants-2015_05
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09034855B2

反応ノート

読み込み中…