申请人:President and Fellows of Harvard College
公开号:US10913764B2
公开(公告)日:2021-02-09
Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
本文提供了通过东半部和西半部偶联,然后大环化来制备大环内酯的方法,以提供大环内酯,包括已知大环内酯和新型大环内酯。还提供了合成大环内酯(包括东半部和西半部)的中间体。还提供了使用本发明大环内酯类药物治疗传染性疾病和炎症的药物组合物和方法。还提供了用于合成西半部分的一般非对映选择性醛醇方法。