Diethylamine → 1H-Indolamine

HRID 966482

反応式

HRID 966482 の反応式
C([NH:3]CC)C.C(OC([C:16]1[C:24]2[C:19](=[CH:20][CH:21]=[C:22](CCOS(C)(=O)=O)[CH:23]=2)[NH:18][C:17]=1C(F)(F)F)=O)C1C=CC=CC=1>>[NH:18]1[C:19]2[C:24](=[CH:23][CH:22]=[CH:21][CH:20]=2)[CH:16]=[C:17]1[NH2:3]

参加物

3

反応物 2

HCID 8021DiethylamineHCID 233938765-(2-Methanesulfonyloxy-ethyl)-2-trifluoromethyl-1H-indole-3-carboxylic Acid Benzyl Ester

生成物 1

HCID 1220741H-Indolamine収率 20%

実験手順

Diethylamine (0.48 mL, 4.63 mmol, 3 eq) was added into the crude 5-(2-Methanesulfonyloxy-ethyl)-2-trifluoromethyl-1H-indole-3-carboxylic acid benzyl ester in dioxanes (20 mL) solution. The reaction mixture was heated to reflux overnight. After the solvent was removed, the residue was purified by gravity chromatography (SiO2, ethyl acetate-methanol-NH4OH) to yield the desire indole amine as pale yellow gel (20.0% yield). Elemental Analysis: C23H25F3N2O2.HCl: Calcd: C: 60.73; H: 5.76; N: 6.16. Found: C: 60.40; H: 5.83; N: 6.06. ESI-MS: m/z 419.73 (M+H)+.

後処理

  1. temperatureThe reaction mixture was heated
  2. temperatureto reflux overnight
  3. customAfter the solvent was removed
  4. customthe residue was purified by gravity chromatography (SiO2, ethyl acetate-methanol-NH4OH)

出典と根拠

ORDレコード
ord-43c09ca90268469c99bbc5b4ea19033f
出典データセット
uspto-grants-2005_10
特許番号
US06951848B2

関連ノート

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