1,8-Diazabicyclo(5.4.0)undec-7-ene → 7-(4-Methoxycarbonyl-2-isoindolinyl)-1-cyclopropyl-5-amino-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

HRID 1494805ノート

反応式

HRID 1494805 の反応式
[CH:1]1([N:4]2[C:13]3[C:8](=[C:9]([NH2:17])[C:10]([F:16])=[C:11](F)[C:12]=3[F:14])[C:7](=[O:18])[C:6]([C:19]([OH:21])=[O:20])=[CH:5]2)[CH2:3][CH2:2]1.Cl.[CH3:23][O:24][C:25]([C:27]1[CH:35]=[CH:34][CH:33]=[C:32]2[C:28]=1[CH2:29][NH:30][CH2:31]2)=[O:26].C1CCN2C(=NCCC2)CC1>CN(C=O)C>[CH3:23][O:24][C:25]([C:27]1[CH:35]=[CH:34][CH:33]=[C:32]2[C:28]=1[CH2:29][N:30]([C:11]1[C:12]([F:14])=[C:13]3[C:8]([C:7](=[O:18])[C:6]([C:19]([OH:21])=[O:20])=[CH:5][N:4]3[CH:1]3[CH2:3][CH2:2]3)=[C:9]([NH2:17])[C:10]=1[F:16])[CH2:31]2)=[O:26]

参加物

5

反応物 3

HCID 811841,8-Diazabicyclo(5.4.0)undec-7-eneHCID 139109475-Amino-1-cyclopropyl-6,7,8-trifluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acidHCID 19828511Methyl 2,3-dihydro-1H-isoindole-4-carboxylate--hydrogen chloride (1/1)

生成物 1

HCID 151679127-(4-Methoxycarbonyl-2-isoindolinyl)-1-cyclopropyl-5-amino-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid収率 39.8%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

298 mg of 1-cyclopropyl-5-amino-6,7,8-trifluoro-1,4- dihydro-4-oxoquinoline-3-carboxylic acid, 257 mg of 4-methoxycarbonylisoindoline hydrochloride, 532 mg of DBU, and 2ml of anhydrous DMF were processed in the same manner as in Example 20 to produce 181 mg of the target compound.

出典と根拠

ORDレコード
ord-ee07d1acd1a6408ea6d98e574fc7e241
出典データセット
uspto-grants-1991_06
特許番号
US05026856

反応ノート

読み込み中…