哌嗪 → 5-(9-Isobutyl-6-morpholino-8-(piperazin-1-yl)-9H-purin-2-yl)pyrimidin-2-amine

HRID 1876486

反应方程式

HRID 1876486 反应方程式
[NH:1]1[CH2:6][CH2:5][NH:4][CH2:3][CH2:2]1.Cl[C:8]1[N:9]([CH2:30][CH:31]([CH3:33])[CH3:32])[C:10]2[C:15]([N:16]=1)=[C:14]([N:17]1[CH2:22][CH2:21][O:20][CH2:19][CH2:18]1)[N:13]=[C:12]([C:23]1[CH:24]=[N:25][C:26]([NH2:29])=[N:27][CH:28]=1)[N:11]=2>CN1CCCC1=O>[CH2:30]([N:9]1[C:8]([N:1]2[CH2:6][CH2:5][NH:4][CH2:3][CH2:2]2)=[N:16][C:15]2[C:10]1=[N:11][C:12]([C:23]1[CH:28]=[N:27][C:26]([NH2:29])=[N:25][CH:24]=1)=[N:13][C:14]=2[N:17]1[CH2:22][CH2:21][O:20][CH2:19][CH2:18]1)[CH:31]([CH3:33])[CH3:32]

参与物

4

反应物 2

HCID 4837哌嗪HCID 593335495-(8-Chloro-9-isobutyl-6-morpholino-9H-purin-2-yl)pyrimidin-2-amine

产物 1

HCID 593335015-(9-Isobutyl-6-morpholino-8-(piperazin-1-yl)-9H-purin-2-yl)pyrimidin-2-amine

试剂、催化剂与溶剂 1

HCID 13387N-甲基吡咯烷酮溶剂

反应条件

温度
130 °C

实验过程

Piperazine (2.0 g, 23 mmol) and N-methylpyrrolidone (10 ml) were added to 5-(8-chloro-9-isobutyl-6-morpholin-4-yl-9H-purin-2-yl)pyrimidin-2-amine (1.0 g, 2.6 mmol) and the resulting mixture was stirred at 130° C. for 4 hours. The reaction mixture was cooled and partitioned with methylene chloride and water, the organic layer was dried over magnesium sulfate, and the solvent was concentrated under reduced pressure. This compound (10 ml in liquid) was stored with N-methylpyrrolidone remaining and used for next step.

后处理

  1. temperatureThe reaction mixture was cooled
  2. custompartitioned with methylene chloride and water
  3. dry with materialthe organic layer was dried over magnesium sulfate
  4. concentrationthe solvent was concentrated under reduced pressure

来源与证据

ORD记录
ord-0beadc145db84d479a8e0c6abae201dd
来源数据集
uspto-grants-2012_11
专利号
US08309546B2

关联笔记

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