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

HRID 13126

反応式

HRID 13126 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-82aaeec6ede14f6d8c1b69dc920b0408
出典データセット
uspto-grants-2010_06
特許番号
US07728030B2

関連ノート

読み込み中…