tert-Butyl piperazine-1-carboxylate → 6-(4-(tert-Butoxycarbonyl)piperazin-1-yl)-5-chloronicotinic acid

反応式

[Cl:1][C:2]1[C:3](Cl)=[N:4][CH:5]=[C:6]([CH:10]=1)[C:7]([OH:9])=[O:8].[C:12]([O:16][C:17]([N:19]1[CH2:24][CH2:23][NH:22][CH2:21][CH2:20]1)=[O:18])([CH3:15])([CH3:14])[CH3:13]>>[C:12]([O:16][C:17]([N:19]1[CH2:24][CH2:23][N:22]([C:3]2[C:2]([Cl:1])=[CH:10][C:6]([C:7]([OH:9])=[O:8])=[CH:5][N:4]=2)[CH2:21][CH2:20]1)=[O:18])([CH3:15])([CH3:13])[CH3:14]

参加物

反応物 2

HCID 143452tert-Butyl piperazine-1-carboxylate

HCID 2479875,6-Dichloronicotinic acid

生成物 1

HCID 116098286-(4-(tert-Butoxycarbonyl)piperazin-1-yl)-5-chloronicotinic acid

実験手順

5,6-Dichloro-nicotinic acid (5.0 g, 0.026 mol, Aldrich) reacted with piperazine-1-carboxylic acid tert-butyl ester (4.87 g, 0.026 mol, Aldrich) under the conditions of Example 3a to give the title compound as yellow semi-solid, which was used in the next step without further purification. MS (ESI, neg. ion) m/z: 340 (M-1).

出典と根拠

ORDレコード: ord-93faf05e0c8f458a8e6acb47cfab2b9c
出典データセット: uspto-grants-2009_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07582761B2

反応ノート

読み込み中…

参加物