Triethylamine → 8-Cyano-1-cyclopropyl-6-fluoro-7-((1S,6S)-2-oxa-5,8-diazabicyclo[4.3.0]non-yl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

HRID 2302229노트

반응식

HRID 2302229 반응식
Cl[C:2]1[C:11]([C:12]#[N:13])=[C:10]2[C:5]([C:6](=[O:20])[C:7]([C:17]([OH:19])=[O:18])=[CH:8][N:9]2[CH:14]2[CH2:16][CH2:15]2)=[CH:4][C:3]=1[F:21].[C@H:22]12[CH2:30][NH:29][CH2:28][C@@H:27]1[NH:26][CH2:25][CH2:24][O:23]2.C(N(CC)CC)C>C(#N)C>[C:12]([C:11]1[C:2]([C@:22]23[CH2:30][NH:29][CH2:28][C@@H:27]2[NH:26][CH2:25][CH2:24][O:23]3)=[C:3]([F:21])[CH:4]=[C:5]2[C:10]=1[N:9]([CH:14]1[CH2:16][CH2:15]1)[CH:8]=[C:7]([C:17]([OH:19])=[O:18])[C:6]2=[O:20])#[N:13]

참가 물질

5

반응물 3

HCID 8471TriethylamineHCID 15069982(4aS,7aS)-octahydropyrrolo[3,4-b][1,4]oxazineHCID 153471917-Chloro-8-cyano-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

생성물 1

HCID 229583728-Cyano-1-cyclopropyl-6-fluoro-7-((1S,6S)-2-oxa-5,8-diazabicyclo[4.3.0]non-yl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

시약·촉매·용매 1

HCID 6342Acetonitrile용매

실험 절차

1.00 g (3.26 mmol) of 7-chloro-8-cyano-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylicacid are stirred under argon at 40-45° C. for 25 hours with 501 mg (3.91 mmol) of (1S,6S)-2-oxa-5,8-diazabicyclo[4.3.0]nonane and 0.9 ml of triethylamine in 30 ml of acetonitrile. All volatile components are removed in vacuo and the residue is recrystallized from ethanol.

후처리

  1. customAll volatile components are removed in vacuo
  2. customthe residue is recrystallized from ethanol

출처 및 근거

ORD 기록
ord-c194f68c8e2b4d288a91e3c40c9adc5b
출처 데이터셋
uspto-grants-2002_08
특허 번호
US06432948B1

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