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

HRID 239191노트

반응식

HRID 239191 반응식
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

참가 물질

5

반응물 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

생성물 1

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

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-501f0628135e4bc58d060a7e62a8ea8c
출처 데이터셋
uspto-grants-2014_02
특허 번호
US08642774B2

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