Hydrochloric Acid → 5-Fluoro-2-(1-isobutyl-1H-indazol-5-yloxy)-benzylamine

HRID 1897510ノート

反応式

HRID 1897510 の反応式
[F:1][C:2]1[CH:3]=[CH:4][C:5]([O:10][C:11]2[CH:12]=[C:13]3[C:17](=[CH:18][CH:19]=2)[N:16]([CH2:20][CH:21]([CH3:23])[CH3:22])[N:15]=[CH:14]3)=[C:6]([CH:9]=1)[C:7]#[N:8].N#N.Cl>CO.[OH-].[OH-].[Pd+2]>[F:1][C:2]1[CH:3]=[CH:4][C:5]([O:10][C:11]2[CH:12]=[C:13]3[C:17](=[CH:18][CH:19]=2)[N:16]([CH2:20][CH:21]([CH3:23])[CH3:22])[N:15]=[CH:14]3)=[C:6]([CH:9]=1)[CH2:7][NH2:8]

参加物

6

反応物 3

HCID 313Hydrochloric AcidHCID 947NitrogenHCID 574187715-Fluoro-2-(1-isobutyl-1H-indazol-5-yloxy)-benzonitrile

生成物 1

HCID 574841225-Fluoro-2-(1-isobutyl-1H-indazol-5-yloxy)-benzylamine収率 107.4%

試薬・触媒・溶媒 2

HCID 9942167Palladium hydroxide触媒HCID 887Methanol溶媒

実験手順

To a solution of 5-fluoro-2-(1-isobutyl-1H-indazol-5-yloxy)-benzonitrile (3.05 g, 9.86 mmol) purged with N2 in MeOH (50 mL) was added concentrated HCl (1.6 mL) and Pd(OH)2/C (15% wt, 0.457 g). The mixture was stirred at room temperature for 18 hours under H2 atmosphere. The catalyst was removed by filtration and the solution was concentrated under reduced pressure to afford 3.32 g of pale yellow foam (96% yield).

後処理

  1. customThe catalyst was removed by filtration
  2. concentrationthe solution was concentrated under reduced pressure

出典と根拠

ORDレコード
ord-ff19f9b710ec4b099e5a8996e74ad013
出典データセット
uspto-grants-2013_08
特許番号
US08518983B2

反応ノート

読み込み中…