PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF (R)-PRAZIQUANTEL

摘要

The present disclosure relates to a process and new intermediates for the synthesis of (R)-praziquantel, which is obtained through four steps in proper order, that is, condensation reaction, reduction reaction, acylation reaction and ring-closing reaction, using (1R)-2-substituted-1,2,3,4-tetrahydroisoquinoline-1-carboxylic acid as starting material. Overall, the present disclosure provides a (R)-praziquantel product with higher optical purity through a process route that is more cost effective and environmentally friendly.

主权项

1. A process for synthesis of (R)-praziquantel employing the following synthesis route: wherein, R is an amino protective group and HCl may be substituted by other acids.