Triethylamine → 4-(2-(3,5-bis-(4-Fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetyl)-1-pyridin-2-yl-piperazin-2-one

HRID 239191ノート

反応式

HRID 239191 の反応式
Cl.Cl.[N:3]1[CH:8]=[CH:7][CH:6]=[CH:5][C:4]=1[N:9]1[CH2:14][CH2:13][NH:12][CH2:11][C:10]1=[O:15].[F:16][C:17]1[CH:22]=[CH:21][C:20]([C:23]2[N:27]=[C:26]([C:28]3[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=3)[N:25]([CH2:35][C:36](Cl)=[O:37])[N:24]=2)=[CH:19][CH:18]=1.C(N(CC)CC)C>ClCCl>[F:16][C:17]1[CH:18]=[CH:19][C:20]([C:23]2[N:27]=[C:26]([C:28]3[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=3)[N:25]([CH2:35][C:36]([N:12]3[CH2:13][CH2:14][N:9]([C:4]4[CH:5]=[CH:6][CH:7]=[CH:8][N:3]=4)[C:10](=[O:15])[CH2:11]3)=[O:37])[N:24]=2)=[CH:21][CH:22]=1

参加物

5

反応物 3

HCID 8471TriethylamineHCID 567770991-(Pyridin-2-yl)piperazin-2-one dihydrochlorideHCID 86686520(3,5-bis-(4-Fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetyl chloride

生成物 1

HCID 715865004-(2-(3,5-bis-(4-Fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetyl)-1-pyridin-2-yl-piperazin-2-one収率 30.6%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

160 mg 1-pyridin-2-yl-piperazin-2-one dihydrochloride was added to 216 mg (3,5-bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetyl chloride and 300 μL triethylamine in 10 mL dichlormethane. The reaction was stirred for 1 day at RT, the solvent was evaporated and the residue was purified by HPLC to yield 93 mg of the desired product.

後処理

  1. customthe solvent was evaporated
  2. customthe residue was purified by HPLC

出典と根拠

ORDレコード
ord-501f0628135e4bc58d060a7e62a8ea8c
出典データセット
uspto-grants-2014_02
特許番号
US08642774B2

反応ノート

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