Synthesis of All Enantiomerically Pure Diastereomers of Aprepitant

Abstract

Syntheses of all eight enantiomerically pure diastereomers of aprepitant and assignment of absolute configuration at newly generated stereocenters by NMR and x-ray crystallographic analysis were achieved.

Keywords:

• ICH
• spectroscopy
• stereoisomers
• synthesis
• X-ray crystallography

ACKNOWLEDGMENTS

The authors thank management of the Dr. Reddy's Laboratories for support. We acknowledge the technical support extended by the AR&D and CRAAI divisions. We also thank the team of Dr. Moses Babu, Dr. Vishweshwar Peddy, and Mr. R. Vasu Dev of the analytical research laboratory of the Discovery Research Foundation.

Notes

IPDO Communication IPDO-IPM-00129.