Boron tribromide → (S)-4-Amino-N-(3,5-dihydroxyphenyl)-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidine-5-carboxamide

HRID 1052736ノート

反応式

HRID 1052736 の反応式
[NH2:1][C:2]1[C:7]([C:8]([NH:10][C:11]2[CH:16]=[C:15]([O:17]C)[CH:14]=[C:13]([O:19]C)[CH:12]=2)=[O:9])=[C:6]([NH:21][C@H:22]([C:24]2[N:29]([C:30]3[CH:35]=[CH:34][CH:33]=[CH:32][CH:31]=3)[C:28](=[O:36])[C:27]3=[C:37]([CH3:40])[CH:38]=[CH:39][N:26]3[N:25]=2)[CH3:23])[N:5]=[CH:4][N:3]=1.B(Br)(Br)Br>ClCCl>[NH2:1][C:2]1[C:7]([C:8]([NH:10][C:11]2[CH:16]=[C:15]([OH:17])[CH:14]=[C:13]([OH:19])[CH:12]=2)=[O:9])=[C:6]([NH:21][C@H:22]([C:24]2[N:29]([C:30]3[CH:35]=[CH:34][CH:33]=[CH:32][CH:31]=3)[C:28](=[O:36])[C:27]3=[C:37]([CH3:40])[CH:38]=[CH:39][N:26]3[N:25]=2)[CH3:23])[N:5]=[CH:4][N:3]=1

参加物

4

反応物 2

HCID 25134Boron tribromideHCID 118433938(S)-4-Amino-N-(3,5-dimethoxyphenyl)-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidine-5-carboxamide

生成物 1

HCID 90102389(S)-4-Amino-N-(3,5-dihydroxyphenyl)-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidine-5-carboxamide収率 3%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

(S)-4-Amino-N-(3,5-dimethoxyphenyl)-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidine-5-carboxamide (720 mg, 33% purity, 0.43 mmol) was treated with boron tribromide (1M in dichloromethane, 2.60 ml, 2.6 mmol) in dichloromethane (10 ml) according to the method described in Example 23. The residue was purified by reverse phase using SP1® Purification System to give 36 mg (3% yield) as a solid. Purity 99%.

後処理

  1. customThe residue was purified by reverse phase
  2. custom® Purification System
  3. customto give 36 mg (3% yield) as a solid

出典と根拠

ORDレコード
ord-8ce144a4a6f647e79a70801509cac9cb
出典データセット
uspto-grants-2016_07
特許番号
US09388189B2

反応ノート

読み込み中…