Water → HCID 86670920、化合物

HRID 1186493ノート

反応式

HRID 1186493 の反応式
[Br:1][C:2]1[N:7]=[C:6]([C:8]2[N:12]3[CH:13]=[CH:14][N:15]=[C:16](Cl)[C:11]3=[N:10][CH:9]=2)[CH:5]=[CH:4][CH:3]=1.[N:18]1([CH2:24][CH2:25][NH2:26])[CH2:23][CH2:22][O:21][CH2:20][CH2:19]1.CCN(CC)CC.O>CC(O)C>[Br:1][C:2]1[N:7]=[C:6]([C:8]2[N:12]3[CH:13]=[CH:14][N:15]=[C:16]([NH:26][CH2:25][CH2:24][N:18]4[CH2:23][CH2:22][O:21][CH2:20][CH2:19]4)[C:11]3=[N:10][CH:9]=2)[CH:5]=[CH:4][CH:3]=1

参加物

6

反応物 4

HCID 962WaterHCID 8471TriethylamineHCID 4082852-MorpholinoethylamineHCID 86670917HCID 86670917、化合物

生成物 1

HCID 86670920HCID 86670920、化合物

試薬・触媒・溶媒 1

HCID 3776Isopropanol溶媒

実験手順

A mixture of 3-(6-bromo-pyridin-2-yl)-8-chloro-imidazo[1,2-a]pyrazine (from Example 38 supra) (3.09 g, 10.0 mmol), 2-morpholin-4-yl-ethylamine (2.6 g, 20.0 mmol), NEt3 (2.02 g, 20.0 mmol) in 2-propanol (300 mL) was stirred and heated at reflux for 16 hours. The solution was then cooled to room temperature and poured into water. The resulted solid was filtered and washed with water. The crude product was purified by chromatography (CH2Cl2:CH3OH, 20:1) to give [3-(6-bromo-pyridin-2-yl)-imidazo[1,2-a]pyrazin-8-yl]-(2-morpholin-4-yl-ethyl)-amine. (Yield 2.5 g, 62%). LC-MS: [M+H]+ 403.

後処理

  1. temperatureheated
  2. temperatureat reflux for 16 hours
  3. filtrationThe resulted solid was filtered
  4. washwashed with water
  5. customThe crude product was purified by chromatography (CH2Cl2:CH3OH, 20:1)

出典と根拠

ORDレコード
ord-487c966197a540cc8e558966c93f51ef
出典データセット
uspto-grants-2014_03
特許番号
US08673905B2

反応ノート

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