Methylamine → Ethyl 1-[4-chloro-6-(methylamino)-1,3,5-triazin-2-yl]-4-piperidinecarboxylate

HRID 1678442ノート

反応式

HRID 1678442 の反応式
Cl[C:2]1[N:7]=[C:6]([Cl:8])[N:5]=[C:4]([N:9]2[CH2:14][CH2:13][CH:12]([C:15]([O:17][CH2:18][CH3:19])=[O:16])[CH2:11][CH2:10]2)[N:3]=1.CN.[CH:22]([N:25](C(C)C)CC)(C)C>ClCCl>[Cl:8][C:6]1[N:7]=[C:2]([NH:25][CH3:22])[N:3]=[C:4]([N:9]2[CH2:14][CH2:13][CH:12]([C:15]([O:17][CH2:18][CH3:19])=[O:16])[CH2:11][CH2:10]2)[N:5]=1

参加物

5

反応物 3

HCID 6329MethylamineHCID 81531DiisopropylethylamineHCID 2774159Ethyl 1-(4,6-dichloro-1,3,5-triazin-2-yl)piperidine-4-carboxylate

生成物 1

HCID 86644318Ethyl 1-[4-chloro-6-(methylamino)-1,3,5-triazin-2-yl]-4-piperidinecarboxylate収率 100%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒2 回

実験手順

To a solution of ethyl 1-(4,6-dichloro-1,3,5-triazin-2-yl)-4-piperidinecarboxylate (1.0 g, 3.3 mmol, 1.0 equiv) in dichloromethane (20 ml) at room temperature, a premixed solution of methylamine (1.6 ml, 3.3 mmol, 1.0 equiv) and diisopropylethylamine (DIEA, 1.7 ml, 9.8 mmol, 3.0 equiv) in dichloromethane (10 ml) was added dropwise. The reaction was stirred for 3 h at room temperature. The solvent was removed under reduced pressure to afford 983 mg (100%) of the title compound. MS (ES+): m/e 300.1 [M+H]+.

後処理

  1. customThe solvent was removed under reduced pressure

出典と根拠

ORDレコード
ord-18b04e3fc22848c891c188fbedc7753e
出典データセット
uspto-grants-2011_08
特許番号
US08008483B2

反応ノート

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