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

HRID 909228노트

반응식

HRID 909228 반응식
[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]

참가 물질

6

반응물 3

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

생성물 1

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

시약·촉매·용매 2

HCID 9942167Palladium hydroxide촉매HCID 887Methanol용매

실험 절차

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).

후처리

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

출처 및 근거

ORD 기록
ord-c83c8dbea39244a2b8b7af3293d3cdcf
출처 데이터셋
uspto-grants-2011_09
특허 번호
US08017641B2

반응 노트

불러오는 중…