Synthesis 2012; 44(13): 1983-1992
DOI: 10.1055/s-0031-1290969
paper
© Georg Thieme Verlag Stuttgart · New York

Diastereocontrol in the Synthesis of 2,3,4-Trisubstituted Pyrrolidines and Tetrahydrofurans via a Palladium(II)-Catalyzed Three-Component Coupling Reaction

Sandeep Raikar
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
,
Benoy Kumar Pal
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
,
Helena C. Malinakova*
Department of Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA
Center of Excellence in Chemical Methodologies and Library Development, University of Kansas, 2034 Becker Drive, Shankel Structural Biology Center, West Campus, Lawrence, KS 66047, USA, Fax: +1(785)8645396   Email: hmalina@ku.edu
› Author Affiliations
Further Information

Publication History

Received: 31 January 2012

Accepted after revision: 23 March 2012

Publication Date:
05 June 2012 (online)


Abstract

The synthesis of trisubstituted pyrrolidines and tetrahydrofurans from boronic acids, allenes, and imines or aldehydes via a five- and a three-step protocol, respectively, is described. The assignment­ of the relative stereochemistry in the pyrrolidines and tetrahydrofurans confirmed the mechanistically significant stereochemical divergence of the palladium-catalyzed three-component coupling reaction. The methodology is applicable to the preparation of combinatorial libraries of pyrrolidines related to pharmaceutical agents and bioactive natural products.

Supporting Information