Formamide → 10-Bromo-9-fluoro-3-[(2-methylpyrazol-3-yl)methyl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2-carboxamide

反応式

[Br:1][C:2]1[C:3]([F:27])=[CH:4][C:5]2[O:11][CH2:10][CH2:9][N:8]3[C:12]([CH2:19][C:20]4[N:24]([CH3:25])[N:23]=[CH:22][CH:21]=4)=[C:13]([C:15]([O:17]C)=O)[N:14]=[C:7]3[C:6]=2[CH:26]=1.C[O-].[Na+].C([NH2:33])=O>>[Br:1][C:2]1[C:3]([F:27])=[CH:4][C:5]2[O:11][CH2:10][CH2:9][N:8]3[C:12]([CH2:19][C:20]4[N:24]([CH3:25])[N:23]=[CH:22][CH:21]=4)=[C:13]([C:15]([NH2:33])=[O:17])[N:14]=[C:7]3[C:6]=2[CH:26]=1

参加物

反応物 3

HCID 713Formamide

HCID 10942334Sodium Methoxide

HCID 86693460Methyl 10-bromo-9-fluoro-3-((1-methyl-1H-pyrazol-5-yl)methyl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxylate

生成物 1

HCID 8669346110-Bromo-9-fluoro-3-[(2-methylpyrazol-3-yl)methyl]-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepine-2-carboxamide

実験手順

10-bromo-9-fluoro-3-((1-methyl-1H-pyrazol-5-yl)methyl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide was prepared similarly to as described in General Procedure L. Methyl 10-bromo-9-fluoro-3-((1-methyl-1H-pyrazol-5-yl)methyl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxylate was reacted with sodium methoxide and formamide to afford 11 mg (11% crude yield) of the crude title compound which was carried forward without further purification.

後処理

custom10-bromo-9-fluoro-3-((1-methyl-1H-pyrazol-5-yl)methyl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepine-2-carboxamide was prepared similarly

出典と根拠

ORDレコード: ord-16e6281abb3c4e5bb3b6367d6c728942
出典データセット: uspto-grants-2015_05
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09034866B2

反応ノート

読み込み中…