Ethyl isocyanatoacetate → Ethyl n-{[(1s,2r)-2-{[1-(4-fluorophenyl)-1h-indazole-5-yl]oxy}-1-methyl-2-phenylethyl]carbamoyl}glycinate

HRID 1098887

反応式

HRID 1098887 の反応式
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:16]3[C:11](=[CH:12][C:13]([O:17][C@H:18]([C:22]4[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=4)[C@H:19]([CH3:21])[NH2:20])=[CH:14][CH:15]=3)[CH:10]=[N:9]2)=[CH:4][CH:3]=1.[CH2:28]([O:30][C:31](=[O:36])[CH2:32][N:33]=[C:34]=[O:35])[CH3:29]>ClCCl>[F:1][C:2]1[CH:3]=[CH:4][C:5]([N:8]2[C:16]3[C:11](=[CH:12][C:13]([O:17][C@H:18]([C:22]4[CH:23]=[CH:24][CH:25]=[CH:26][CH:27]=4)[C@@H:19]([NH:20][C:34]([NH:33][CH2:32][C:31]([O:30][CH2:28][CH3:29])=[O:36])=[O:35])[CH3:21])=[CH:14][CH:15]=3)[CH:10]=[N:9]2)=[CH:6][CH:7]=1

参加物

4

反応物 2

HCID 76283Ethyl isocyanatoacetateHCID 59339817(alphaS,betaR)-beta-{[1-(4-Fluorophenyl)-1H-indazole-5-yl]oxy}-alpha-methylbenzeneethanamine

生成物 1

HCID 44594899Ethyl n-{[(1s,2r)-2-{[1-(4-fluorophenyl)-1h-indazole-5-yl]oxy}-1-methyl-2-phenylethyl]carbamoyl}glycinate収率 79.1%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

(αS,βR)-β-{[1-(4-Fluorophenyl)-1H-indazole-5-yl]oxy}-α-methylbenzeneethanamine (80 mg, 0.22 mmol), as described in Example 1, is dissolved in 1.42 mL dichloromethane and ethylisocyanatoacetate (28.6 mg, 0.22 mmol) is dropwise added. After stirring for 45 min at r.t. the solvent is removed and the residue purified by chromatography (silicagel, eluents: hexane/ethylacetate). 85.4 mg (78.6%) of the title compound are obtained.

後処理

  1. customis removed
  2. customthe residue purified by chromatography (silicagel, eluents: hexane/ethylacetate)

出典と根拠

ORDレコード
ord-e683cd74355d4aa98d5073f3bc8a9998
出典データセット
uspto-grants-2012_03
特許番号
US08143290B2

関連ノート

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