7-[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazol-3-yl]-2-(4-methoxy-benzyl)-5-methyl-2H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one → 6-{[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazole-3-carbonyl]-amino}-2-(4-methoxy-benzyl)-5-methyl-2H-indazole-7-carboxylic acid isopropyl amide

HRID 1907147ノート

反応式

HRID 1907147 の反応式
[Cl:1][C:2]1[C:3]([N:8]2[C:12]([C:13]3[O:22][C:21](=[O:23])[C:20]4[C:19]5=[N:24][N:25]([CH2:27][C:28]6[CH:33]=[CH:32][C:31]([O:34][CH3:35])=[CH:30][CH:29]=6)[CH:26]=[C:18]5[CH:17]=[C:16]([CH3:36])[C:15]=4[N:14]=3)=[CH:11][C:10]([O:37][CH3:38])=[N:9]2)=[N:4][CH:5]=[CH:6][CH:7]=1>O1CCCC1.C(N)(C)C>[CH:12]([NH:8][C:21]([C:20]1[C:19]2[C:18](=[CH:26][N:25]([CH2:27][C:28]3[CH:29]=[CH:30][C:31]([O:34][CH3:35])=[CH:32][CH:33]=3)[N:24]=2)[CH:17]=[C:16]([CH3:36])[C:15]=1[NH:14][C:13]([C:12]1[N:8]([C:3]2[C:2]([Cl:1])=[CH:7][CH:6]=[CH:5][N:4]=2)[N:9]=[C:10]([O:37][CH3:38])[CH:11]=1)=[O:22])=[O:23])([CH3:13])[CH3:11]

参加物

4

反応物 1

HCID 585004627-[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazol-3-yl]-2-(4-methoxy-benzyl)-5-methyl-2H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one

生成物 1

HCID 585004556-{[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazole-3-carbonyl]-amino}-2-(4-methoxy-benzyl)-5-methyl-2H-indazole-7-carboxylic acid isopropyl amide

試薬・触媒・溶媒 2

HCID 6363Isopropylamine触媒HCID 8028Tetrahydrofuran溶媒

反応条件

温度
20 °C

実験手順

A solution of 7-[2-(3-chloro-pyridin-2-yl)-5-methoxy-2H-pyrazol-3-yl]-2-(4-methoxy-benzyl)-5-methyl-2H-8-oxa-1,2,6-triaza-cyclopenta[a]naphthalen-9-one (0.100 g, 0.189 mmol) in tetrahydrofurane (2 ml) was treated with 16 drops of isopropyl amine and stirred at 20° C. for three hours. The reaction mixture was evaporated and the crude product was purified by flash chromatography on silica gel using a mixture of 75% ethyl acetate 25% cyclohexane. The desired product showed the physical data reported in the corresponding table (P.34.).

後処理

  1. customThe reaction mixture was evaporated
  2. customthe crude product was purified by flash chromatography on silica gel using
  3. additiona mixture of 75% ethyl acetate 25% cyclohexane

出典と根拠

ORDレコード
ord-1f87041f4a054198808f8a7f123c1b28
出典データセット
uspto-grants-2013_12
特許番号
US08598078B2

反応ノート

読み込み中…