2-(1,2,3,4-Tetrahydroisoquinolin-2-yl)ethan-1-amine → N-[2-(4-Benzylpiperidin-1-yl)ethyl]-N'-(2-methylquinolin-4-yl)pyrimidine-4,6-diamine

HRID 914998

反応式

[CH2:1]1[C:10]2[C:5](=[CH:6][CH:7]=[CH:8][CH:9]=2)[CH2:4][CH2:3][N:2]1[CH2:11][CH2:12][NH2:13].Cl[C:15]1[N:20]=[CH:19][N:18]=[C:17]([NH:21][C:22]2[C:31]3[C:26](=[CH:27][CH:28]=[CH:29][CH:30]=3)[N:25]=[C:24]([CH3:32])[CH:23]=2)[CH:16]=1.[CH:33](N(C(C)C)CC)([CH3:35])[CH3:34]>CCCCO>[CH2:6]([CH:5]1[CH2:10][CH2:1][N:2]([CH2:11][CH2:12][NH:13][C:15]2[CH:16]=[C:17]([NH:21][C:22]3[C:31]4[C:26](=[CH:27][CH:28]=[CH:29][CH:30]=4)[N:25]=[C:24]([CH3:32])[CH:23]=3)[N:18]=[CH:19][N:20]=2)[CH2:3][CH2:4]1)[C:7]1[CH:8]=[CH:9][CH:35]=[CH:33][CH:34]=1

参加物

反応条件

温度: 100 °C

実験手順

To a solution of diamine 36 (0.05 g, 0.21 mmol) in n-BuOH (2 mL) were sequentially added 108 (0.05 g, 0.18 mmol) and diisopropylethylamine (37 mg, 0.27 mmol). The mixture was heated at 100° C. overnight before the volatiles were removed under reduced pressure. The residue was purified by flash chromatography (SiO2, gradient elution, 3:1 hexanes/ethyl acetate to 7:3 CH2Cl2/MeOH) to yield the desired product (20 mg, 25%) as a yellow oil.

後処理

customwere removed under reduced pressure
customThe residue was purified by flash chromatography (SiO2, gradient elution, 3:1 hexanes/ethyl acetate to 7:3 CH2Cl2/MeOH)

出典と根拠

ORDレコード: ord-e7d619599b294df088693f06ba5b1e7f
出典データセット: uspto-grants-2007_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07265122B2

反応式

参加物

反応物 3

生成物 1

試薬・触媒・溶媒 1

反応条件

実験手順

後処理

出典と根拠

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