HCID 68563692、化合物 → 5-(R)-[2-(S)-Amino-1-(S)-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester

HRID 20351

反応式

HRID 20351 の反応式
[C:1]([O:5][C:6]([N:8]1[C@@H:13]([C@@H:14]([O:46]CC2C=CC=CC=2)[C@H:15]([N:31](CC2C=CC=CC=2)CC2C=CC=CC=2)[CH2:16][C:17]2[CH:22]=[CH:21][CH:20]=[C:19]([O:23]CC3C=CC=CC=3)[CH:18]=2)[CH2:12][O:11][C@@H:10]([O:54][CH2:55][C:56]([CH3:59])([CH3:58])[CH3:57])[C@@H:9]1[CH3:60])=[O:7])([CH3:4])([CH3:3])[CH3:2].[H][H]>C(O)(C)(C)C.[OH-].[OH-].[Pd+2]>[C:1]([O:5][C:6]([N:8]1[C@@H:13]([C@@H:14]([OH:46])[C@@H:15]([NH2:31])[CH2:16][C:17]2[CH:22]=[CH:21][CH:20]=[C:19]([OH:23])[CH:18]=2)[CH2:12][O:11][C@@H:10]([O:54][CH2:55][C:56]([CH3:59])([CH3:58])[CH3:57])[C@@H:9]1[CH3:60])=[O:7])([CH3:2])([CH3:4])[CH3:3]

参加物

5

反応物 2

HCID 68563692HCID 68563692、化合物HCID 178418361HCID 178418361、化合物

生成物 1

HCID 685615745-(R)-[2-(S)-Amino-1-(S)-hydroxy-3-(3-hydroxyphenyl)-propyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester収率 104.2%

試薬・触媒・溶媒 2

HCID 9942167Palladium hydroxide触媒HCID 6386tert-Butanol溶媒

実験手順

Dissolve 5-(R)-[1-(S)-benzyloxy-3-(3-benzyloxyphenyl)-2-(R)-dibenzylaminopropyl]-2-(R)-(2,2-dimethylpropoxy)-3-(S)-methylmorpholine-4-carboxylic acid tert-butyl ester (1.38 g, 1.70 mmol) in tert-butanol (˜50 mL). Add 20% palladium hydroxide on carbon (4 g) and hydrogenate at 50 psi hydrogen gas at 40° C. for 18 hours. Filter and concentrate to give the desired compound (802 mg).

後処理

  1. filtrationFilter
  2. concentrationconcentrate

出典と根拠

ORDレコード
ord-f603027a811c4124b583d7961476ec7f
出典データセット
uspto-grants-2010_06
特許番号
US07745438B2

関連ノート

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