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(R)-1-(4-(3-fluoro-4-(7-methoxyquinolin-4-yloxy)phenylcarbamoyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydropyrazol-1-yl)propan-2-yl 2-((benzyloxycarbonyl)(methyl)-amino)acetate → (R)-1-(4-(3-fluoro-4-(7-methoxyquinolin-4-yloxy)phenylcarbamoyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydropyrazol-1-yl)propan-2-yl 2-(methylamino)acetate

HRID 1517829
ノート
印刷プレビュー

反応式

HRID 1517829 の反応式
[CH3:1][O:2][C:3]1[CH:12]=[C:11]2[C:6]([C:7]([O:13][C:14]3[CH:19]=[CH:18][C:17]([NH:20][C:21]([C:23]4[C:24](=[O:54])[N:25]([C:48]5[CH:53]=[CH:52][CH:51]=[CH:50][CH:49]=5)[N:26]([CH2:29][C@H:30]([O:32][C:33](=[O:47])[CH2:34][N:35](C(OCC5C=CC=CC=5)=O)[CH3:36])[CH3:31])[C:27]=4[CH3:28])=[O:22])=[CH:16][C:15]=3[F:55])=[CH:8][CH:9]=[N:10]2)=[CH:5][CH:4]=1>CCOC(C)=O.CO.[Pd]>[CH3:36][NH:35][CH2:34][C:33]([O:32][C@H:30]([CH3:31])[CH2:29][N:26]1[C:27]([CH3:28])=[C:23]([C:21](=[O:22])[NH:20][C:17]2[CH:18]=[CH:19][C:14]([O:13][C:7]3[C:6]4[C:11](=[CH:12][C:3]([O:2][CH3:1])=[CH:4][CH:5]=4)[N:10]=[CH:9][CH:8]=3)=[C:15]([F:55])[CH:16]=2)[C:24](=[O:54])[N:25]1[C:48]1[CH:49]=[CH:50][CH:51]=[CH:52][CH:53]=1)=[O:47]
参加物実験手順後処理出典と根拠反応ノート

参加物

5

反応物 1

HCID 66670738(R)-1-(4-(3-fluoro-4-(7-methoxyquinolin-4-yloxy)phenylcarbamoyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydropyrazol-1-yl)propan-2-yl 2-((benzyloxycarbonyl)(methyl)-amino)acetate

生成物 1

HCID 46937772(R)-1-(4-(3-fluoro-4-(7-methoxyquinolin-4-yloxy)phenylcarbamoyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydropyrazol-1-yl)propan-2-yl 2-(methylamino)acetate

試薬・触媒・溶媒 3

HCID 23938Palladium触媒HCID 887Methanol
溶媒
HCID 8857Ethyl Acetate溶媒

実験手順

To a solution of (R)-1-(4-(4-(7-methoxyquinolin-4-yloxy)-3-fluorophenylcarbamoyl)-2,3-dihydro-5-methyl-3-oxo-2-phenylpyrazol-1-yl)propan-2-yl-2-(N-benzyloxycarbo-nyl-N-methylamino)acetate (1.404 g, 1.876 mmol) in a mixture of EtOAc (100 mL) and MeOH (100 mL) was added catalytic amount of Pd/C (10%, ˜55% w/w water content, 100 mg) under N2 atmosphere. The suspension was degassed under vacuum and then purged with H2. The reaction mixture was stirred at rt for 1 h under H2 balloon. The mixture was filtered and the residue was washed with MeOH (50 mL×3). The filtrate used for the next step immediately.

後処理

  1. customThe suspension was degassed under vacuum
  2. custompurged with H2
  3. filtrationThe mixture was filtered
  4. washthe residue was washed with MeOH (50 mL×3)

出典と根拠

ORDレコード
ord-26592ac853aa4c04b6bea677ca4714ec
出典データセット
uspto-grants-2012_07
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08232294B2

反応ノート

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