Cyclopropanemethanamine → HCID 57917614、化合物

HRID 1878439ノート

反応式

HRID 1878439 の反応式
[NH2:1][C:2]1[CH:32]=[CH:31][C:5]([C:6]([N:8]2[CH2:13][CH2:12][N:11]([CH2:14][C:15]3[CH:16]=[C:17]([CH:28]=[CH:29][CH:30]=3)[C:18]([NH:20][C:21]([C:26]#[N:27])([CH:23]3[CH2:25][CH2:24]3)[CH3:22])=[O:19])[CH2:10][CH2:9]2)=[O:7])=[CH:4][C:3]=1[F:33].C1C([N+]([O-])=O)=CC=C([Cl-][C:44]([O-])=[O:45])C=1.[CH:47]1([CH2:50][NH2:51])[CH2:49][CH2:48]1>ClCCl>[C:26]([C:21]([NH:20][C:18](=[O:19])[C:17]1[CH:28]=[CH:29][CH:30]=[C:15]([CH2:14][N:11]2[CH2:10][CH2:9][N:8]([C:6](=[O:7])[C:5]3[CH:31]=[CH:32][C:2]([NH:1][C:44]([NH:51][CH2:50][CH:47]4[CH2:49][CH2:48]4)=[O:45])=[C:3]([F:33])[CH:4]=3)[CH2:13][CH2:12]2)[CH:16]=1)([CH:23]1[CH2:25][CH2:24]1)[CH3:22])#[N:27]

参加物

4

反応物 2

HCID 75646CyclopropanemethanamineHCID 579176753-((4-(4-Amino-3-fluorobenzoyl)piperazin-1-yl)methyl)-N-(1-cyano-1-cyclopropylethyl)benzamide

生成物 1

HCID 57917614HCID 57917614、化合物収率 42%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

3-((4-(4-Amino-3-fluorobenzoyl)piperazin-1-yl)methyl)—N-(1-cyano-1-cyclopropyl-ethyl)benzamide (49 mg, 0.109 mmol) was stirred In dichloromethane at room temperature. 4-Nitrophenylchloroformate (22 mg, 0.109 mmol) was added and the reaction mixture stirred for 30 minutes. Cyclopropylmethylamine (23 mg, 0.327 mmol) was added and the reaction allowed to stir for 30 minutes at room temperature. The reaction was concentrated under reduced pressure and the resulting residue purified by silica column chromatography to afford the title compound (25 mg). MS (ESI) m/z 547.5 [M+H]+

後処理

  1. stirringto stir for 30 minutes at room temperature
  2. concentrationThe reaction was concentrated under reduced pressure
  3. customthe resulting residue purified by silica column chromatography

出典と根拠

ORDレコード
ord-1603cbe733c74f4fbe0ec3929d9fa2fa
出典データセット
uspto-grants-2012_11
特許番号
US08314091B2

反応ノート

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