反应 #1269860

ord-be0401f095054d06816e3dd8a7157f51

反应方程式

CCCCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2nc(-c3ccccc3)sc2/C=C/C(=O)O)CC1
suspension
CCCCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2nc(-c3ccccc3)sc2/C=C/C(=O)O)CC1
4-((S)-4-Carboxy-2-{[5-((E)-2-carboxy-vinyl)-2-phenyl-thiazole-4-carbonyl]-amino}-butyryl)-piperazine-1-carboxylic acid butyl ester
CCCCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2nc(-c3ccccc3)sc2CCC(=O)O)CC1
desired product
收率 33.8%
CCCCOC(=O)N1CCN(C(=O)[C@H](CCC(=O)O)NC(=O)c2nc(-c3ccccc3)sc2CCC(=O)O)CC1
4-((S)-4-Carboxy-2-{[5-(2-carboxy-ethyl)-2-phenyl-thiazole-4-carbonyl]-amino}-butyryl)-piperazine-1-carboxylic acid butyl ester
收率 33.8%

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    过滤The reaction mixture was filtrated over celite
  2. 2
    其他the filtrate evaporated to dryness

实验过程

A suspension of Example 19 (53 mg) and Pd/C (10%, 62 mg) in MeOH (2 mL) was stirred at RT under H2 atmosphere until reaction completion. The reaction mixture was filtrated over celite and the filtrate evaporated to dryness. Preparative HPLC (I) gave 18 mg of the desired product as yellow foam.

来源

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