Diethylamine → {3-[3-(Diethylamino)-1,2,4-oxadiazol-5-yl]-5-(4-ethylphenyl)piperidin-1-yl}(4-hydroxypiperidin-1-yl)methanone

HRID 661278ノート

反応式

HRID 661278 の反応式
Cl[C:2]1[N:6]=[C:5]([CH:7]2[CH2:12][CH:11]([C:13]3[CH:18]=[CH:17][C:16]([CH2:19][CH3:20])=[CH:15][CH:14]=3)[CH2:10][N:9]([C:21]([N:23]3[CH2:28][CH2:27][CH:26]([OH:29])[CH2:25][CH2:24]3)=[O:22])[CH2:8]2)[O:4][N:3]=1.[CH2:30]([NH:32][CH2:33][CH3:34])[CH3:31]>C(O)C>[CH2:30]([N:32]([CH2:33][CH3:34])[C:2]1[N:6]=[C:5]([CH:7]2[CH2:12][CH:11]([C:13]3[CH:18]=[CH:17][C:16]([CH2:19][CH3:20])=[CH:15][CH:14]=3)[CH2:10][N:9]([C:21]([N:23]3[CH2:28][CH2:27][CH:26]([OH:29])[CH2:25][CH2:24]3)=[O:22])[CH2:8]2)[O:4][N:3]=1)[CH3:31]

参加物

4

反応物 2

HCID 8021Diethylamine2 回HCID 58116548[3-(3-Chloro-1,2,4-oxadiazol-5-yl)-5-(4-ethylphenyl)piperidin-1-yl](4-hydroxypiperidin-1-yl)-methanone

生成物 1

HCID 49819561{3-[3-(Diethylamino)-1,2,4-oxadiazol-5-yl]-5-(4-ethylphenyl)piperidin-1-yl}(4-hydroxypiperidin-1-yl)methanone

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

実験手順

To a solution of 45.0 mg (0.098 mmol) of the oxadiazole from Example 25A in 0.61 ml of ethanol were added 143 mg (1.96 mmol) of diethylamine, and then the reaction mixture was stirred in the microwave at 80 for 5 h. Another 143 mg (1.96 mmol) of diethylamine were added and the mixture was stirred in the microwave at 80° C. for a further 2 h. The solvent was removed under reduced pressure and the crude product was purified by means of preparative HPLC. Yield: 35.6 mg (80% of theory)

後処理

  1. stirringthe mixture was stirred in the microwave at 80° C. for a further 2 h
  2. customThe solvent was removed under reduced pressure
  3. customthe crude product was purified by means of preparative HPLC

出典と根拠

ORDレコード
ord-355168af44f2444db260efe596545500
出典データセット
uspto-grants-2011_12
特許番号
US08084469B2

反応ノート

読み込み中…