Ethylamine → 3-(Ethylamino)-1,1,1-trifluoro-2-({[1-(4-fluorophenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-2-propanol

HRID 551433

反応式

HRID 551433 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:16]3[CH:15]=[C:14]([CH3:17])[CH:13]=[C:12]([NH:18][CH2:19][C:20]4([C:23]([F:26])([F:25])[F:24])[CH2:22][O:21]4)[C:11]=3[CH:10]=[N:9]2)=[CH:4][CH:3]=1.[CH2:27]([NH2:29])[CH3:28]>ClCCl>[CH2:27]([NH:29][CH2:22][C:20]([CH2:19][NH:18][C:12]1[CH:13]=[C:14]([CH3:17])[CH:15]=[C:16]2[C:11]=1[CH:10]=[N:9][N:8]2[C:5]1[CH:4]=[CH:3][C:2]([F:1])=[CH:7][CH:6]=1)([OH:21])[C:23]([F:25])([F:24])[F:26])[CH3:28]

参加物

4

反応物 2

HCID 6341EthylamineHCID 24938054HCID 24938054、化合物

生成物 1

HCID 593241453-(Ethylamino)-1,1,1-trifluoro-2-({[1-(4-fluorophenyl)-6-methyl-1H-indazol-4-yl]amino}methyl)-2-propanol収率 85.7%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

A solution of 1-(4-fluorophenyl)-6-methyl-N-{[2-(trifluoromethyl)-2-oxiranyl]methyl}-1H-indazol-4-amine (1.52 g, 4.16 mmol) in dichloromethane (30 ml) was added to ethylamine (2M in tetrahydrofuran) (70 ml, 140 mmol). The reaction was stirred at room temperature overnight and then evaporated in vacuo. The crude product was purified on a 70 g silica Bond Elut cartridge using a 0-100% ethyl acetate in dichloromethane gradient over 60 mins to give the title compound (1.463 g).

後処理

  1. customevaporated in vacuo
  2. customThe crude product was purified on a 70 g silica Bond Elut cartridge
  3. customover 60 mins

出典と根拠

ORDレコード
ord-17c2253755db477383318d0439b5fffa
出典データセット
uspto-grants-2011_05
特許番号
US07947727B2

関連ノート

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