Synthesis of the major isomers of Aprepitant and Fosaprepitant

The synthesis of two isomers of Aprepitant (APT) and three isomers of Fosaprepitant (FPT), crucial components for quality control in manufacturing, is described. Herein, three chiral centers in the isomers of Aprepitant are established in high yield by induced crystallization and chiral reduction. Additionally, the isomers of Aprepitant are utilized to synthesize the isomers of Fosaprepitant with the same stereochemistry. All the target compounds were confirmed by elemental analyses, IR, NMR and MS data analysis.

Graphical abstractThe synthesis of two isomers of Aprepitant and three isomers of Fosaprepitant is described. The detailed information reported herein can provide a good reference for quality control in manufacturing.Figure optionsDownload full-size imageDownload as PowerPoint slide