1-Hydroxybenzotriazole → HCID 49848080, 화합물

HRID 2061720노트

반응식

HRID 2061720 반응식
C[O:2][C:3]([C:5]1[CH:6]=[C:7]([C:18]2[CH:23]=[CH:22][C:21]([CH3:24])=[CH:20][CH:19]=2)[CH:8]=[C:9]([N:11]([C:13](=[O:17])[CH:14]([CH3:16])[CH3:15])[CH3:12])[CH:10]=1)=O.[N:25]1[CH:30]=[CH:29][N:28]=[CH:27][C:26]=1[CH:31]([NH2:33])[CH3:32].C1C=CC2N(O)N=NC=2C=1>C(Cl)Cl>[N:25]1[CH:30]=[CH:29][N:28]=[CH:27][C:26]=1[CH:31]([NH:33][C:3]([C:5]1[CH:6]=[C:7]([C:18]2[CH:19]=[CH:20][C:21]([CH3:24])=[CH:22][CH:23]=2)[CH:8]=[C:9]([N:11]([C:13](=[O:17])[CH:14]([CH3:16])[CH3:15])[CH3:12])[CH:10]=1)=[O:2])[CH3:32]

참가 물질

5

반응물 3

HCID 757711-HydroxybenzotriazoleHCID 185190061-(Pyrazin-2-yl)ethanamineHCID 596275315-(Isobutyryl-methyl-amino)-4'-methyl-biphenyl-3-carboxylic acid methyl ester

생성물 1

HCID 49848080HCID 49848080, 화합물수율 34.9%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

5-(Isobutyryl-methyl-amino)-4′-methyl-biphenyl-3-carboxylic acid methyl ester (67 mg, 0.22 mmol) was added to methylene chloride (3 mL) and stirred at room temperature. TEA (0.87 g), 1-pyrazin-2-yl-ethylamine (32 mg, 0.25 mmol), HOBt (29 mg) and ECDI (54 mg) were added, and the reaction mixture was stirred overnight at room temperature. The reaction mixture was placed directly onto a silica column and eluted with 50% ethyl acetate/hexanes to give 32 mg of 5-(isobutyryl-methyl-amino)-4′-methyl-biphenyl-3-carboxylic acid (1-pyrazin-2-yl-ethyl)-amide as a white solid, MS (M+H)=417.

후처리

  1. stirringthe reaction mixture was stirred overnight at room temperature
  2. washeluted with 50% ethyl acetate/hexanes

출처 및 근거

ORD 기록
ord-263c090effb14d74a2354e93a4859146
출처 데이터셋
uspto-grants-2012_10
특허 번호
US08283383B2

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