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 1494770노트

반응식

HRID 1494770 반응식
[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]

참가 물질

5

반응물 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

생성물 1

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

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

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.

출처 및 근거

ORD 기록
ord-f5995ad2d4e247edbb8bc4ba1fc53a45
출처 데이터셋
uspto-grants-1991_06
특허 번호
US05026856

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