申请人:——
公开号:US20040151908A1
公开(公告)日:2004-08-05
Generally, and in one form, the present invention is a method of making a benzene-modified compound on solid support that includes the steps of forming an (oxy)(aryl)carbene complex, esterifying the (oxy)(aryl)carbene complex to form an (ester)(aryl)carbene complex, and contacting the (ester)(aryl)carbene complex with a solid support such that the (ester)(aryl)carbene complex is bound to the solid support. In another form, the present invention includes compositions for the resulting (ester)(aryl)carbene complexes on solid support, such as any resulting solid support compounds formed after the initial coupling as well as those from any subsequent reaction, including those with linkers and on a solid support. The method and compositions of the present invention yield stable, durable, highly efficient and cost-effective as well as potentially biologically active lead compounds on solid support.
一般来说,本发明的一种形式是在固体支持物上制造苯改性化合物的方法,该方法包括以下步骤:形成(氧)(芳基)碳烯络合物,将(氧)(芳基)碳烯络合物酯化以形成(酯)(芳基)碳烯络合物,将(酯)(芳基)碳烯络合物与固体支持物接触,使(酯)(芳基)碳烯络合物与固体支持物结合。在另一种形式中,本发明包括所得(酯)(芳基)羰基络合物在固体支持物上的组合物,例如初始偶联后形成的任何所得固体支持物化合物以及任何后续反应的化合物,包括带有连接体和在固体支持物上的化合物。本发明的方法和组合物可以在固体支持物上产生稳定、持久、高效、低成本以及具有潜在生物活性的先导化合物。