Process for preparing nucleoside prodrugs
View Patent ↗Provided are phosphoramidate nucleoside compounds of Formula (I), or pharmaceutically acceptable salts or esters or solvates thereof, useful in the treatment of cancer, viral infections and other diseases: Also provided is a process for the synthesis of the compounds of Formula (I) where a desired enantiomer, having regard to the asymmetric chiral center of the phosphorus atom P, is provided in an enriched amount. The process comprises admixing a nucleoside with a phosphorochloridate in the presence of a catalyst comprising a metal salt selected from the group consisting of salts of Cu, Fe, La and Yb.
1. A compound represented by:
wherein the ratio of the R P diastereomer to the S P diastereomer is at most 1:20.
2. The compound of claim 1 , wherein the ratio of the R P diastereomer to the S P diastereomer is 0:100.