申请人:Ionis Pharmaceuticals, Inc.
公开号:US10751419B2
公开(公告)日:2020-08-25
Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.
本文提供了用于合成活性共轭簇的改进方法以及用于此类方法的中间体。特别是,本文提供的改进方法通过减少所需的合成步骤,提高了活性共轭簇的合成效率。使用改进方法制备的活性共轭簇不包括使用现有方法形成的任何反式酰化杂质。与现有方法相比,改进方法还能提高总体产量和成本效益。