Piperidine → 2-Chloro-5-nitro-4-(piperidin-1-yl)pyrimidine

反応式

[Cl:1][C:2]1[N:7]=[C:6](Cl)[C:5]([N+:9]([O-:11])=[O:10])=[CH:4][N:3]=1.[NH:12]1[CH2:17][CH2:16][CH2:15][CH2:14][CH2:13]1>CCO>[Cl:1][C:2]1[N:7]=[C:6]([N:12]2[CH2:17][CH2:16][CH2:15][CH2:14][CH2:13]2)[C:5]([N+:9]([O-:11])=[O:10])=[CH:4][N:3]=1

参加物

実験手順

Method 1 was followed using 2,4-dichloro-5-nitropyrimidine (1.0 eq), and piperidine (2.0 eq) in EtOH at 0° C. to rt, yielding after washing with 1M citric acid and 1M HCl (to remove the bis addition product), 2-chloro-5-nitro-4-(piperidin-1-yl)pyrimidine (67%) LCMS (m/z): 242.9 (MH+); LC Rt=4.09 min.

後処理

customat 0° C. to rt
customyielding
washafter washing with 1M citric acid and 1M HCl (
customto remove
additionthe bis addition product), 2-chloro-5-nitro-4-(piperidin-1-yl)pyrimidine (67%) LCMS (m/z)

出典と根拠

ORDレコード: ord-e8307f40214a44f987c44c5c386c7361
出典データセット: uspto-grants-2014_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08822497B2

反応ノート

読み込み中…

参加物

反応物 2

HCID 8082Piperidine

HCID 5212662,4-Dichloro-5-nitropyrimidine

生成物 1

HCID 71472572-Chloro-5-nitro-4-(piperidin-1-yl)pyrimidine

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

後処理

customat 0° C. to rt
customyielding
washafter washing with 1M citric acid and 1M HCl (
customto remove
additionthe bis addition product), 2-chloro-5-nitro-4-(piperidin-1-yl)pyrimidine (67%) LCMS (m/z)

出典と根拠

ORDレコード: ord-e8307f40214a44f987c44c5c386c7361
出典データセット: uspto-grants-2014_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08822497B2

反応ノート

読み込み中…