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

HRID 1494770ノート

反応式

HRID 1494770 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.[CH2:25]1[C:33]2[C:28](=[CH:29][CH:30]=[CH:31][CH:32]=2)[CH2:27][NH:26]1.C1CCN2C(=NCCC2)CC1>CN(C=O)C>[CH2:25]1[C:33]2[C:28](=[CH:29][CH:30]=[CH:31][CH:32]=2)[CH2:27][N:26]1[C:11]1[C:12]([F:14])=[C:13]2[C:8]([C:7](=[O:21])[C:6]([C:22]([OH:24])=[O:23])=[CH:5][N:4]2[CH:1]2[CH2:3][CH2:2]2)=[C:9]([NH:17][CH2:18][CH2:19][OH:20])[C:10]=1[F:16]

参加物

5

反応物 3

HCID 811841,8-Diazabicyclo(5.4.0)undec-7-eneHCID 422478IsoindolineHCID 198284861-Cyclopropyl-5(2-hydroxyethylamino)-6,7,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid

生成物 1

HCID 147957877-(2-Isoindolinyl)-1-cyclopropyl-5(2-hydroxyethylamino)-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid収率 42.7%

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, 119 mg of isoindoline, 182 mg of DBU, and 1.5 ml of anhydrous DMF were processed in the same manner as in Example 20 to produce 113 mg of the target compound.

出典と根拠

ORDレコード
ord-f5995ad2d4e247edbb8bc4ba1fc53a45
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…