Boron tribromide → (S)-4-Amino-N-(2-hydroxyphenyl)-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 1052729ノート

反応式

HRID 1052729 の反応式
[NH2:1][C:2]1[C:7]([C:8]([NH:10][C:11]2[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=2[O:17]C)=[O:9])=[C:6]([NH:19][C@H:20]([C:22]2[N:27]([C:28]3[CH:33]=[CH:32][CH:31]=[CH:30][CH:29]=3)[C:26](=[O:34])[C:25]3=[C:35]([CH3:38])[CH:36]=[CH:37][N:24]3[N:23]=2)[CH3:21])[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]=[CH:15][CH:14]=[CH:13][C:12]=2[OH:17])=[O:9])=[C:6]([NH:19][C@H:20]([C:22]2[N:27]([C:28]3[CH:29]=[CH:30][CH:31]=[CH:32][CH:33]=3)[C:26](=[O:34])[C:25]3=[C:35]([CH3:38])[CH:36]=[CH:37][N:24]3[N:23]=2)[CH3:21])[N:5]=[CH:4][N:3]=1

参加物

4

反応物 2

HCID 25134Boron tribromideHCID 118433952(S)-4-Amino-N-(2-methoxyphenyl)-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 73775677(S)-4-Amino-N-(2-hydroxyphenyl)-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 34.5%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

(S)-4-Amino-N-(2-methoxyphenyl)-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 (72 mg, 0.14 mmol) was treated with boron tribromide (1M in dichloromethane, 0.43 ml, 0.43 mmol) in dichloromethane (8 ml) according to the method described in Example 23. The crude was purified using SP1® Purification (40% to 100%, hexane-ethyl acetate) to give 24 mg (34% yield) of the title compound as a solid. Purity 99%.

後処理

  1. customThe crude was purified
  2. custom® Purification (40% to 100%, hexane-ethyl acetate)

出典と根拠

ORDレコード
ord-062e5e9039934957b54ee8319544f818
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…