Water → tert-Butyl 3-difluoromethoxy-6-hydroxyindazole-1-carboxylate

HRID 1873965ノート

反応式

HRID 1873965 の反応式
C([O:8][C:9]1[CH:17]=[C:16]2[C:12]([C:13]([O:25][CH:26]([F:28])[F:27])=[N:14][N:15]2[C:18]([O:20][C:21]([CH3:24])([CH3:23])[CH3:22])=[O:19])=[CH:11][CH:10]=1)C1C=CC=CC=1.O.[H][H]>[Pd].C1COCC1>[F:28][CH:26]([F:27])[O:25][C:13]1[C:12]2[C:16](=[CH:17][C:9]([OH:8])=[CH:10][CH:11]=2)[N:15]([C:18]([O:20][C:21]([CH3:23])([CH3:22])[CH3:24])=[O:19])[N:14]=1

参加物

6

反応物 3

HCID 962WaterHCID 45280135tert-Butyl 6-(benzyloxy)-3-difluoromethoxyindazole-1-carboxylateHCID 178418361HCID 178418361、化合物

生成物 1

HCID 135869961tert-Butyl 3-difluoromethoxy-6-hydroxyindazole-1-carboxylate収率 97.7%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 8028Tetrahydrofuran溶媒

実験手順

Tert-butyl 6-(benzyloxy)-3-(difluoromethoxy)-indazole-1-carboxylate (262.5 mg) which can be prepared according to the method described in Reference example 33, etc. and 5% palladium on carbon-STD-type-50% wet with water (109.9 mg; manufactured by N. E. Chemcat Corp.) were suspended in dehydrated THF (3.4 mL; manufactured by Kanto Chemical Co., Inc.). After replacing the reaction system with hydrogen, it was stirred overnight at room temperature. After replacing the reaction solution with nitrogen, the mixture was filtered and the filtrate was concentrated under reduced pressure to obtain the title compound (197.2 mg).

後処理

  1. filtrationthe mixture was filtered
  2. concentrationthe filtrate was concentrated under reduced pressure

出典と根拠

ORDレコード
ord-b65163548ca1448b8e664a85980b1705
出典データセット
uspto-grants-2012_11
特許番号
US08304443B2

反応ノート

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