反应 #1269858

ord-0057e16d2eeb4504bdbacf62e8a0693f

反应方程式

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
收率 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
收率 94.9%

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    过滤The mixture was filtered through celite
  2. 2
    其他evaporated off
  3. 3
    其他HV drying

实验过程

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).

来源

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