1-Methylpiperazine → N-(3-Ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-3-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-acrylamide

HRID 2265983ノート

反応式

HRID 2265983 の反応式
Cl[C:2]1[C:7]([CH:8]=[CH:9][C:10]([NH:12][CH2:13][C:14]2[CH:19]=[C:18]([F:20])[C:17]([NH:21][S:22]([CH3:25])(=[O:24])=[O:23])=[C:16]([C:26]#[CH:27])[CH:15]=2)=[O:11])=[CH:6][CH:5]=[C:4]([C:28]([F:31])([F:30])[F:29])[N:3]=1.[CH3:32][N:33]1[CH2:38][CH2:37][NH:36][CH2:35][CH2:34]1>>[C:26]([C:16]1[CH:15]=[C:14]([CH:19]=[C:18]([F:20])[C:17]=1[NH:21][S:22]([CH3:25])(=[O:24])=[O:23])[CH2:13][NH:12][C:10](=[O:11])[CH:9]=[CH:8][C:7]1[C:2]([N:36]2[CH2:37][CH2:38][N:33]([CH3:32])[CH2:34][CH2:35]2)=[N:3][C:4]([C:28]([F:31])([F:30])[F:29])=[CH:5][CH:6]=1)#[CH:27]

参加物

3

反応物 2

HCID 531671-MethylpiperazineHCID 743823853-(2-Chloro-6-trifluoromethyl-pyridin-3-yl)-N-(3-ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-acrylamide

生成物 1

HCID 72335646N-(3-Ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-3-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-acrylamide収率 15%

実験手順

3-(2-Chloro-6-trifluoromethyl-pyridin-3-yl)-N-(3-ethynyl-5-fluoro-4-methanesulfonylamino-benzyl)-acrylamide (70 mg, 0.057 mmol) was reacted with N-methylpiperazine (30 μl) as in example 46 to give the title compound (13 mg, 15%) after recrystallization with Hex/EtOAc.

出典と根拠

ORDレコード
ord-0fa91f094990421e9157804d00ca55ad
出典データセット
uspto-grants-2010_12
特許番号
US07858621B2

反応ノート

読み込み中…