4-((5-Fluoropyridin-2-yl)methoxy)pyridin-2(1H)-one → tert-Butyl 8-(4-((5-fluoropyridin-2-yl)methoxy)-2-oxopyridin-1(2H)-yl)-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylate

HRID 882063ノート

反応式

HRID 882063 の反応式
Br[C:2]1[CH:21]=[CH:20][C:5]2[N:6]3[CH2:12][CH2:11][N:10]([C:13]([O:15][C:16]([CH3:19])([CH3:18])[CH3:17])=[O:14])[CH2:9][C:7]3=[N:8][C:4]=2[CH:3]=1.[F:22][C:23]1[CH:24]=[CH:25][C:26]([CH2:29][O:30][C:31]2[CH:36]=[CH:35][NH:34][C:33](=[O:37])[CH:32]=2)=[N:27][CH:28]=1>>[F:22][C:23]1[CH:24]=[CH:25][C:26]([CH2:29][O:30][C:31]2[CH:36]=[CH:35][N:34]([C:2]3[CH:21]=[CH:20][C:5]4[N:6]5[CH2:12][CH2:11][N:10]([C:13]([O:15][C:16]([CH3:19])([CH3:18])[CH3:17])=[O:14])[CH2:9][C:7]5=[N:8][C:4]=4[CH:3]=3)[C:33](=[O:37])[CH:32]=2)=[N:27][CH:28]=1

参加物

3

反応物 2

HCID 579503414-((5-Fluoropyridin-2-yl)methoxy)pyridin-2(1H)-oneHCID 67988850tert-Butyl 8-bromo-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylate

生成物 1

HCID 67988847tert-Butyl 8-(4-((5-fluoropyridin-2-yl)methoxy)-2-oxopyridin-1(2H)-yl)-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylate収率 49.2%

実験手順

tert-Butyl 8-bromo-3,4-dihydropyrazino[1,2-a]benzimidazole-2(1H)-carboxylate (150 mg, 0.426 mmol) and 4-((5-fluoropyridin-2-yl)methoxy)pyridin-2(1H)-one (103 mg, 0.468 mmol) were reacted according to Example 18 (step g) to provide the title compound (103 mg, 47%) as a white solid: ESI MS m/z 492 [M+H]+.

出典と根拠

ORDレコード
ord-cfe8caec2ff245cda9cea16837480e6a
出典データセット
uspto-grants-2015_03
特許番号
US08993765B2

反応ノート

読み込み中…