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

HRID 1494774ノート

反応式

HRID 1494774 の反応式
[CH:1]1([N:4]2[C:13]3[C:8](=[C:9]([NH:17][CH2:18][CH2:19][OH:20])[C:10]([F:16])=[C:11](F)[C:12]=3[F:14])[C:7](=[O:21])[C:6]([C:22]([OH:24])=[O:23])=[CH:5]2)[CH2:3][CH2:2]1.[Br:25][C:26]1[CH:34]=[CH:33][CH:32]=[C:31]2[C:27]=1[CH2:28][NH:29][CH2:30]2.C1CCN2C(=NCCC2)CC1>CN(C=O)C>[Br:25][C:26]1[CH:34]=[CH:33][CH:32]=[C:31]2[C:27]=1[CH2:28][N:29]([C:11]1[C:12]([F:14])=[C:13]3[C:8]([C:7](=[O:21])[C:6]([C:22]([OH:24])=[O:23])=[CH:5][N:4]3[CH:1]3[CH2:2][CH2:3]3)=[C:9]([NH:17][CH2:18][CH2:19][OH:20])[C:10]=1[F:16])[CH2:30]2

参加物

5

反応物 3

HCID 811841,8-Diazabicyclo(5.4.0)undec-7-eneHCID 147958704-bromo-2,3-dihydro-1H-isoindoleHCID 198284861-Cyclopropyl-5(2-hydroxyethylamino)-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

生成物 1

HCID 147957927-(4-Bromo-2-isoindolinyl) 1-cyclopropyl-5-(2-hydroxyethylamino)-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid収率 32.7%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

205 mg of 1-cyclopropyl-5-(2-hydroxyethylamino)-6,7,8- trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, 131 mg of 4-bromoisoindoline, 182 mg of DBU, and 1.5 ml of are anhydrous DMF were processed in the same manner as in Example 20 to produce 102 mg of the target compound.

出典と根拠

ORDレコード
ord-b5dd0c5c45844d8c83152152864cbb29
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…