The present invention provides industrially suitable processes for preparing intermediates in the production of substituted polycyclic pyridone derivatives having a cap-dependent endonuclease inhibitory activity.
In the process as shown below, wherein each symbol is as defined in the specification, an optically active substituted tricyclic pyridone derivative of the formula (VII) is obtained in high yield and high enantioselectivity by subjecting a compound of the formula (III) or (VI) to intramolecular cyclization with controlling stereochemistry to obtain a compound of the formula (IV) having a removable functional group on an asymmetric carbon, and then removing the functional group thereof.
本发明提供了在制备具有依赖CAP末端
核酸酶抑制活性的取代多环
吡啶酮衍
生物的生产中的工业适用过程。在下面所示的过程中,其中每个符号如规范中定义,通过将式(III)或(VI)的化合物经过控制立体
化学的分子内环化得到具有可移除手性
碳上的可移除官能团的式(IV)的化合物,然后去除其官能团,以高产率和高对映选择性获得式(VII)的手性取代
三环吡啶酮衍
生物。