(3-(benzyloxy)-5-fluorophenyl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine → 3-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-5-fluorophenol

HRID 237972ノート

反応式

HRID 237972 の反応式
C([O:8][C:9]1[CH:10]=[C:11]([C:16]2[C:24]3[C:19](=[N:20][CH:21]=[N:22][C:23]=3[NH2:25])[N:18]([CH:26]([CH3:28])[CH3:27])[N:17]=2)[CH:12]=[C:13]([F:15])[CH:14]=1)C1C=CC=CC=1>CO.[Pd]>[NH2:25][C:23]1[N:22]=[CH:21][N:20]=[C:19]2[N:18]([CH:26]([CH3:28])[CH3:27])[N:17]=[C:16]([C:11]3[CH:10]=[C:9]([OH:8])[CH:14]=[C:13]([F:15])[CH:12]=3)[C:24]=12

参加物

4

反応物 1

HCID 67406694(3-(benzyloxy)-5-fluorophenyl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

生成物 1

HCID 249053423-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-5-fluorophenol収率 130.5%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 887Methanol溶媒

実験手順

A solution of -(3-(benzyloxy)-5-fluorophenyl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine (15 mg, 0.04 mmol) in MeOH (0.9 ml) was flushed with argon. Pd on activated carbon (10 ml) was carefully added while keeping reaction under an argon atmosphere. Reaction was flushed with H2 gas and left under H2 atmosphere overnight at room temperature. The reaction was filtered through celite and rinsed with MeOH to yield BA22 (15 mg, 100% yield). ESI-MS (M+H)+ m/z calcd 288.1, found 288.1.

後処理

  1. customreaction under an argon atmosphere
  2. customReaction
  3. customwas flushed with H2 gas
  4. filtrationThe reaction was filtered through celite
  5. washrinsed with MeOH

出典と根拠

ORDレコード
ord-ce3f095afc9544b89e538592f8cbedab
出典データセット
uspto-grants-2014_02
特許番号
US08642604B2

反応ノート

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