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

HRID 1494773ノート

反応式

HRID 1494773 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.[Cl: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>[Cl: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 147958684-Chloro-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 147957917-(4-Chloro-2-isoindolinyl)-1-cyclopropyl-5-(2-hydroxyethylamino)-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid収率 35.1%

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, 101 mg of 4-chloroisoindoline, 182 mg of DBU, and 1.5 ml of anhydrous DMF were processed in the same manner as in Example 20 to produce 100 mg of the target compound.

出典と根拠

ORDレコード
ord-de398c9117fd4f8a8adfbafd6b7e89c8
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…