Diisopropylethylamine → (5-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[3-chloro-4-(4-methyl-piperazin-1-yl)-phenyl]-amine

HRID 1366141

反応式

HRID 1366141 の反応式
[Br:1][C:2]1[N:7]2[CH:8]=[CH:9][N:10]=[C:6]2[C:5](Br)=[N:4][CH:3]=1.[Cl:12][C:13]1[CH:14]=[C:15]([NH2:26])[CH:16]=[CH:17][C:18]=1[N:19]1[CH2:24][CH2:23][N:22]([CH3:25])[CH2:21][CH2:20]1.CCN(C(C)C)C(C)C>CC(O)C>[NH3:4].[Br:1][C:2]1[N:7]2[CH:8]=[CH:9][N:10]=[C:6]2[C:5]([NH:26][C:15]2[CH:16]=[CH:17][C:18]([N:19]3[CH2:24][CH2:23][N:22]([CH3:25])[CH2:21][CH2:20]3)=[C:13]([Cl:12])[CH:14]=2)=[N:4][CH:3]=1

参加物

6

反応物 3

HCID 81531DiisopropylethylamineHCID 8203433-Chloro-4-(4-methylpiperazin-1-yl)anilineHCID 534859495,8-Dibromoimidazo[1,2-a]pyrazine

生成物 2

HCID 222AmmoniaHCID 59023078(5-Bromo-imidazo[1,2-a]pyrazin-8-yl)-[3-chloro-4-(4-methyl-piperazin-1-yl)-phenyl]-amine収率 39.5%

試薬・触媒・溶媒 1

HCID 3776Isopropanol溶媒

実験手順

Following the general procedure for amine displacement using 5,8-dibromoimidazo[1,2-a]pyrazine (0.20 g, 0.72 mmol), 3-chloro-4-(4-methyl-piperazin-1-yl)-phenylamine (0.263 g, 1.08 mmol) and DIPEA (0.19 mL, 1.08 mmol) in iPrOH (5 mL). Purification of the crude compound by silica gel column chromatography, eluting with 95:5 DCM:NH3 (7M in MeOH), affords the title compound (60 mg, 20%).

後処理

  1. customPurification of the crude compound by silica gel column chromatography
  2. washeluting with 95:5 DCM

出典と根拠

ORDレコード
ord-f5749447b86a4d119ab740a4cbd2925e
出典データセット
uspto-grants-2011_02
特許番号
US07893058B2

関連ノート

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