p-Toluenesulfonic acid monohydrate → (S)-2-(4-bromo-8-oxo-6,7,8,10-tetrahydro-3H-oxepino[3,4-e]indazol-7-yl)acetic acid

HRID 132456ノート

反応式

HRID 132456 の反応式
[Br:1][C:2]1[CH:3]=[C:4]([CH2:13][C@@H:14]([CH2:18][C:19]([OH:21])=[O:20])[C:15]([OH:17])=[O:16])[C:5]([CH2:11]O)=[C:6]2[C:10]=1[NH:9][N:8]=[CH:7]2.O.C1(C)C=CC(S(O)(=O)=O)=CC=1>C1(C)C=CC=CC=1>[Br:1][C:2]1[C:10]2[NH:9][N:8]=[CH:7][C:6]=2[C:5]2[CH2:11][O:16][C:15](=[O:17])[C@H:14]([CH2:18][C:19]([OH:21])=[O:20])[CH2:13][C:4]=2[CH:3]=1

参加物

4

反応物 2

HCID 521998p-Toluenesulfonic acid monohydrateHCID 59732086(S)-2-((7-bromo-4-(hydroxymethyl)-1H-indazol-5-yl)methyl)succinic acid

生成物 1

HCID 59732081(S)-2-(4-bromo-8-oxo-6,7,8,10-tetrahydro-3H-oxepino[3,4-e]indazol-7-yl)acetic acid収率 99%

試薬・触媒・溶媒 1

HCID 1140Toluene溶媒

実験手順

(S)-2-((7-Bromo-4-(hydroxymethyl)-1H-indazol-5-yl)methyl)succinic acid (95 mg, 0.266 mmol) was suspended in toluene (15 mL). p-Toluenesulfonic acid monohydrate (3.5 mg, 0.018 mmol) was added to the mixture. Reaction was warmed to reflux and held with stirring for 18 hours. Mixture was concentrated to dryness. Title compound was obtained as tan solid in 99% yield. LCMS (M−H)−=339.0, 337.0.

後処理

  1. customReaction
  2. temperaturewas warmed
  3. temperatureto reflux
  4. concentrationMixture was concentrated to dryness

出典と根拠

ORDレコード
ord-7922d22c3ede4e3e9509e4effb10b728
出典データセット
uspto-grants-2008_06
特許番号
US07384931B2

反応ノート

読み込み中…