4-Fluorobenzyl bromide → methyl 2-(1-(cyclopropylmethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)isonicotinate

反応式

BrCC1C=CC(F)=CC=1.Br[CH2:11][CH:12]1[CH2:14][CH2:13]1.[O:15]=[C:16]1[NH:20][N:19]=[CH:18][N:17]1[C:21]1[CH:22]=[C:23]([CH:28]=[CH:29][N:30]=1)[C:24]([O:26][CH3:27])=[O:25]>>[CH:14]1([CH2:13][N:20]2[C:16](=[O:15])[N:17]([C:21]3[CH:22]=[C:23]([CH:28]=[CH:29][N:30]=3)[C:24]([O:26][CH3:27])=[O:25])[CH:18]=[N:19]2)[CH2:12][CH2:11]1

参加物

反応物 3

HCID 680214-Fluorobenzyl bromide

HCID 81503Bromomethylcyclopropane

HCID 58247755methyl 2-(5-oxo-1H-1,2,4-triazol-4(5H)-yl)isonicotinate

生成物 1

HCID 58247813methyl 2-(1-(cyclopropylmethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)isonicotinate収率 65%

実験手順

Following the procedure as described in Preparation 17, making variations as required to replace 1-(bromomethyl)-4-fluorobenzene with (bromomethyl)cyclopropane to react with methyl 2-(5-oxo-1H-1,2,4-triazol-4(5H)-yl)isonicotinate, methyl 2-(1-(cyclopropylmethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)isonicotinate was obtained as a colorless solid in 65% yield: MS (ES+) m/z 275.1 (M+1).

後処理

customas described in Preparation 17

出典と根拠

ORDレコード: ord-6f69a4462ba148288c692051928d899a
出典データセット: uspto-grants-2015_11
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09187426B2

反応ノート

読み込み中…