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N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[(E)-2-(1,3-thiazol-2-yl)vinyl]-1H-1,2,3-triazole-4-carboxamide → N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[2-(1,3-thiazol-2-yl)ethyl]-1H-1,2,3-triazole-4-carboxamide

HRID 1717377
ノート
印刷プレビュー

反応式

HRID 1717377 の反応式
[CH:1]1([NH:4][C:5]([C:7]2[N:8]=[N:9][N:10]([C:19]3[CH:24]=[CH:23][C:22]([C:25]([NH:27][CH2:28][CH3:29])=[O:26])=[CH:21][CH:20]=3)[C:11]=2/[CH:12]=[CH:13]/[C:14]2[S:15][CH:16]=[CH:17][N:18]=2)=[O:6])[CH2:3][CH2:2]1>CN(C=O)C.[Pd]>[CH:1]1([NH:4][C:5]([C:7]2[N:8]=[N:9][N:10]([C:19]3[CH:20]=[CH:21][C:22]([C:25]([NH:27][CH2:28][CH3:29])=[O:26])=[CH:23][CH:24]=3)[C:11]=2[CH2:12][CH2:13][C:14]2[S:15][CH:16]=[CH:17][N:18]=2)=[O:6])[CH2:2][CH2:3]1
参加物実験手順後処理出典と根拠反応ノート

参加物

4

反応物 1

HCID 57664936N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[(E)-2-(1,3-thiazol-2-yl)vinyl]-1H-1,2,3-triazole-4-carboxamide

生成物 1

HCID 57665049N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[2-(1,3-thiazol-2-yl)ethyl]-1H-1,2,3-triazole-4-carboxamide収率 76.5%

試薬・触媒・溶媒 2

HCID 23938Palladium触媒HCID 6228Dimethylformamide溶媒

実験手順

To a solution of N-cyclopropyl-1-{4-[(ethylamino)carbonyl]phenyl}-5-[(E)-2-(1,3-thiazol-2-yl)vinyl]-1H-1,2,3-triazole-4-carboxamide (130 mg) obtained in Example 321 in DMF (10 ml) was added 10% Pd/C (50% wet, 15 mg), and the mixture was stirred for 3 days under a hydrogen atmosphere. After the reaction mixture was filtered through celite, the filtrate was evaporated under reduced pressure. The residue was purified by silica gel column (ethyl acetate to ethyl acetate/methanol=4/1) to give the title compound as a white powder (100 mg).

後処理

  1. filtrationAfter the reaction mixture was filtered through celite
  2. customthe filtrate was evaporated under reduced pressure
  3. customThe residue was purified by silica gel column (ethyl acetate to ethyl acetate/methanol=4/1)

出典と根拠

ORDレコード
ord-3ba2a3d7f1fe4795b78cd2f1afa66b1e
出典データセット
uspto-grants-2010_09
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US07803822B2

反応ノート

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