Piperidine → (Z)-2-[(1H-pyrrolo[2,3-b]pyridin-3-yl)methylene]-6-methoxy-7-(morpholinomethyl)benzofuran-3(2H)-one

HRID 1749829ノート

反応式

HRID 1749829 の反応式
[CH3:1][O:2][C:3]1[CH:12]=[CH:11][C:6]2[C:7](=[O:10])[CH2:8][O:9][C:5]=2[C:4]=1[CH2:13][N:14]1[CH2:19][CH2:18][O:17][CH2:16][CH2:15]1.[NH:20]1[C:28]2[C:23](=[CH:24][CH:25]=[CH:26][N:27]=2)[C:22]([CH:29]=O)=N1.N1CCCC[CH2:32]1>CO>[NH:20]1[C:28]2=[N:27][CH:26]=[CH:25][CH:24]=[C:23]2[C:22](/[CH:29]=[C:8]2\[O:9][C:5]3[C:4]([CH2:13][N:14]4[CH2:19][CH2:18][O:17][CH2:16][CH2:15]4)=[C:3]([O:2][CH3:1])[CH:12]=[CH:11][C:6]=3[C:7]\2=[O:10])=[CH:32]1

参加物

5

反応物 3

HCID 8082PiperidineHCID 712789876-methoxy-7-(morpholinomethyl)benzofuran-3(2H)-oneHCID 178520050HCID 178520050、化合物

生成物 1

HCID 71278640(Z)-2-[(1H-pyrrolo[2,3-b]pyridin-3-yl)methylene]-6-methoxy-7-(morpholinomethyl)benzofuran-3(2H)-one収率 216.9%

試薬・触媒・溶媒 1

HCID 887Methanol溶媒3 回

反応条件

温度
60 °C

実験手順

A solution of 6-methoxy-7-(morpholinomethyl)benzofuran-3(2H)-one (0.131 g, 0.500 mmol) obtained in Example A41, Step 2 in methanol (1.2 mL) was added with 7-aza-1H-indazole-3-carboxaldehyde (0.0545 g, 0.373 mmol) and piperidine (0.00265 g, 0.0311 mmol), and the mixture was stirred at 60° C. for 2 hours. The reaction mixture was cooled to room temperature, and then added with methanol (2 mL), and the precipitated solid was suspended in methanol and thereby washed to obtain the objective (Z)-2-[(1H-pyrrolo[2,3-b]pyridin-3-yl)methylene]-6-methoxy-7-(morpholinomethyl)benzofuran-3(2H)-one (0.0264 g, 21%).

後処理

  1. temperatureThe reaction mixture was cooled to room temperature
  2. washwashed

出典と根拠

ORDレコード
ord-193a30b09f3447bca49bd1cab3619f5c
出典データセット
uspto-grants-2015_10
特許番号
US09156827B2

反応ノート

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