反応 #1269858

ord-0057e16d2eeb4504bdbacf62e8a0693f

反応方程式

CCCCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)OC(C)(C)C)NC(=O)OCc2ccccc2)CC1
4-((S)-2-benzyloxycarbonylamino-4-tert-butoxycarbonyl-butyryl)-piperazine-1-carboxylic acid butyl ester
CCCCOC(=O)N1CCN(C(=O)[C@@H](N)CCC(=O)OC(C)(C)C)CC1
desired compound
収率 94.9%
CCCCOC(=O)N1CCN(C(=O)[C@@H](N)CCC(=O)OC(C)(C)C)CC1
4-((S)-2-Amino-4-tert-butoxycarbonyl-butyryl)-piperazine-1-carboxylic acid butyl ester
収率 94.9%

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    ろ過The mixture was filtered through celite
  2. 2
    その他evaporated off
  3. 3
    その他HV drying

実験手順

A suspension of 4-((S)-2-benzyloxycarbonylamino-4-tert-butoxycarbonyl-butyryl)-piperazine-1-carboxylic acid butyl ester (4.00 g, prepared as described in WO2008050301) and Pd/C (5%, 0.42 g) in EtOH (15 mL) was hydrogenated at RT overnight. The reaction mixture was then stirred under H2 overnight. The mixture was filtered through celite and evaporated off. HV drying afforded the desired compound as light brown oil (2.79 g).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08664203B2uspto-grants-2014_03