Development of a two-step route to 3-PBC and βCCt, two agents active against alcohol self-administration in rodent and primate models

OA Namjoshi, A Gryboski, GO Fonseca…

Index: Namjoshi, Ojas A.; Gryboski, Angelica; Fonseca, German O.; Van Linn, Michael L.; Wang, Zhi-Jian; Deschamps, Jeffrey R.; Cook, James M. Journal of Organic Chemistry, 2011 , vol. 76, # 11 p. 4721 - 4727

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Citation Number: 8

Abstract

To gain access to 3-propoxy-β-carboline hydrochloride (3-PBC· HCl)(1· HCl) and β- carboline-3-carboxylate-tert-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 ...

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