Pyrinodemin A 1是一种具有细胞毒性的海洋生物碱,以一种汇聚和选择性鉴别的方式合成。关键步骤包括:将氧杂环N-氧化物进行不对称的分子内偶极环化反应,以引入分子的双环体系;通过铜盐偶联扩展饱和链;以及B-烷基铃木偶联以引入3-吡啶基部分。还原胺化反应使得第二个侧链与氮原子相连接,从而得到1。此外,还描述了通过双B-烷基铃木反应从三烯前体制备1的尝试。
Pyrinodemin A 1是一种具有细胞毒性的海洋生物碱,以一种汇聚和选择性鉴别的方式合成。关键步骤包括:将氧杂环N-氧化物进行不对称的分子内偶极环化反应,以引入分子的双环体系;通过铜盐偶联扩展饱和链;以及B-烷基铃木偶联以引入3-吡啶基部分。还原胺化反应使得第二个侧链与氮原子相连接,从而得到1。此外,还描述了通过双B-烷基铃木反应从三烯前体制备1的尝试。
申请人:University of Vermont and State Agricultural College
公开号:US06359158B1
公开(公告)日:2002-03-19
The present invention includes 16-HETE analogs which are agonists and antagonists of 16-HETE. The compositions may be formulated in pharmaceutically acceptable formulations. The invention also includes methods and products for inhibiting neutrophil adhesion and neutrophil aggregation using the 16-HETE agonists. One method of the invention involves the administration of a 16-HETE agonist in combination with a thrombolytic agent to a patient suffering from thromboembolic stroke.