Water → 4-Chloro-5-[3-(1-hydroxy-2-methyl-2-propylamino)propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone

HRID 21333

反応式

HRID 21333 の反応式
[Cl:1][C:2]1[C:10]([O:11][CH2:12][CH2:13][CH2:14]Cl)=[CH:9][C:8]([C:16]2[N:17]([C:32]([O:34][C:35]([CH3:38])([CH3:37])[CH3:36])=[O:33])[C:18]3[C:23]([CH:24]=2)=[CH:22][C:21]([CH2:25][N:26]2[CH2:31][CH2:30][CH2:29][CH2:28][CH2:27]2)=[CH:20][CH:19]=3)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:39].[NH2:40][C:41]([CH3:45])([CH3:44])[CH2:42][OH:43].O>CN(C)C(=O)C>[Cl:1][C:2]1[C:10]([O:11][CH2:12][CH2:13][CH2:14][NH:40][C:41]([CH3:45])([CH3:44])[CH2:42][OH:43])=[CH:9][C:8]([C:16]2[N:17]([C:32]([O:34][C:35]([CH3:38])([CH3:37])[CH3:36])=[O:33])[C:18]3[C:23]([CH:24]=2)=[CH:22][C:21]([CH2:25][N:26]2[CH2:31][CH2:30][CH2:29][CH2:28][CH2:27]2)=[CH:20][CH:19]=3)=[C:7]2[C:3]=1[CH2:4][NH:5][C:6]2=[O:39]

参加物

5

反応物 3

HCID 962WaterHCID 118072-Amino-2-methyl-1-propanolHCID 684918464-Chloro-5-(3-chloropropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone

生成物 1

HCID 684903344-Chloro-5-[3-(1-hydroxy-2-methyl-2-propylamino)propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone収率 38.2%

試薬・触媒・溶媒 1

HCID 31374Dimethylacetamide溶媒

実験手順

In a similar manner to Step 2 of Example 440, 4-chloro-5-(3-chloropropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (90.6 mg, 0.158 mmol) was dissolved in N,N-dimethylacetoamide (0.9 mL), and the solution was treated with 2-amino-2-methyl-1-propanol (0.159 mL, 1.58 mmol). The reaction mixture was added with water. The obtained solid was collected by filtration and washed with water, followed by drying under reduced pressure to obtain 4-chloro-5-[3-(1-hydroxy-2-methyl-2-propylamino)propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (37.7 mg, yield 38%).

後処理

  1. filtrationThe obtained solid was collected by filtration
  2. washwashed with water
  3. customby drying under reduced pressure

出典と根拠

ORDレコード
ord-710f0003de2c4ae298099e6e053f6013
出典データセット
uspto-grants-2010_06
特許番号
US07745641B2

関連ノート

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