PROCESSES FOR THE PREPARATION OF PERIPHERAL OPIOID ANTAGONIST COMPOUNDS AND INTERMEDIATES THERETO

摘要

Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.

主权项

1. A process for preparing an N-alkylpiperidine compound of Formula Ia′, or a pharmaceutically acceptable salt thereof:comprising contacting an N-alkenylpiperidine compound of Formula IIa′ or Formula IIb′ or mixture thereof:with hydrogen in the presence of a Group VIII transition metal hydrogenation catalyst and a chiral-phosphorous containing ligand for a time and under conditions effective to provide a compound of Formula Ia′.