Dimethylamine → 5-Amino-1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-7-dimethylamino-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid

HRID 369257노트

반응식

HRID 369257 반응식
[NH2:1][C:2]1[C:11]([F:12])=[C:10](F)[C:9]([Cl:14])=[C:8]2[C:3]=1[C:4](=[O:27])[C:5]([C:24]([OH:26])=[O:25])=[CH:6][N:7]2[C:15]1[C:20]([F:21])=[CH:19][C:18]([F:22])=[C:17]([NH2:23])[N:16]=1.[CH3:28][NH:29][CH3:30]>N1C=CC=CC=1>[NH2:1][C:2]1[C:11]([F:12])=[C:10]([N:29]([CH3:30])[CH3:28])[C:9]([Cl:14])=[C:8]2[C:3]=1[C:4](=[O:27])[C:5]([C:24]([OH:26])=[O:25])=[CH:6][N:7]2[C:15]1[C:20]([F:21])=[CH:19][C:18]([F:22])=[C:17]([NH2:23])[N:16]=1

참가 물질

4

반응물 2

HCID 674DimethylamineHCID 221211655-Amino-1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

생성물 1

HCID 232848225-Amino-1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-7-dimethylamino-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid수율 81%

시약·촉매·용매 1

HCID 1049Pyridine용매

실험 절차

5-Amino-1-(6-amino-3, 5-difluoropyridin-2-yl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (100 mg) and an aqueous solution (about 50%; 170 mg) of dimethylamine were added to pyridine (500 mg), and the mixture was stirred at room temperature for 4 days. The reaction mixture was concentrated under reduced pressure, and ethanol (1 ml) was added to the residue. Deposits were collected by filtration and washed with ethanol and diisopropyl ether in that order to obtain the title compound (86 mg) as a yellow powder.

후처리

  1. concentrationThe reaction mixture was concentrated under reduced pressure, and ethanol (1 ml)
  2. additionwas added to the residue
  3. filtrationDeposits were collected by filtration
  4. washwashed with ethanol and diisopropyl ether in that order

출처 및 근거

ORD 기록
ord-e2ed9ef0e03546638a9f60d060aa2472
출처 데이터셋
uspto-grants-2000_10
특허 번호
US06136823

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