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 2302229ノート

反応式

HRID 2302229 の反応式
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]

参加物

5

反応物 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

生成物 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

試薬・触媒・溶媒 1

HCID 6342Acetonitrile溶媒

実験手順

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.

後処理

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

出典と根拠

ORDレコード
ord-c194f68c8e2b4d288a91e3c40c9adc5b
出典データセット
uspto-grants-2002_08
特許番号
US06432948B1

反応ノート

読み込み中…