Development of a Two-step Route to 3-PBC and βCCt Two Agents Active Against Alcohol Self-Administration in Rodent and Primate Models

摘要

In order to gain access to 3-propoxy-β-carboline hydrochloride (3-PBC·HCl) (>1·>HCl), and β-carboline-3-carboxylate-t-butyl ester (βCCt) (>2), potential clinical agents active against alcohol self-administration, a two-step route was developed. This process involves a palladium catalyzed Buchwald-Hartwig coupling and an intramolecular Heck reaction. This two-step route provides rapid access to multigram quantities of 3-PBC (>1) and βCCt (>2), as well as analogs for studies of alcohol self-administration. The overall yield of 3-PBC (>1) was improved from 8 % to 50 % in this route.