Highly efficient synthesis and characterization of the GPR30-selective agonist G-1 and related tetrahydroquinoline analogs.

Ritwik Burai Chinnasamy Ramesh Marvin Shorty Ramona Curpan Cristian Bologa Larry A Sklar Tudor Oprea Eric R Prossnitz Jeffrey B Arterburn

Org Biomol Chem

Department of Chemistry and Biochemistry MSC 3C, New Mexico State University, P.O. Box 30001, Las Cruces, New Mexico 88003, USA.

Published: May 2010

The GPR30 agonist probe G-1 and similar compounds were successfully made using a specific chemical reaction called Sc(III)-catalyzed aza-Diels-Alder cyclization.
The researchers improved their method by adjusting the solvent and the temperature during the reaction.
This optimization led to better selectivity for a specific molecular orientation, known as endo-diastereoselectivity.

The GPR30 agonist probe G-1 and structural analogs were efficiently synthesized using multicomponent or stepwise Sc(III)-catalyzed aza-Diels-Alder cyclization. Optimization of solvent and reaction temperature provided enhanced endo-diastereoselectivity.

Download full-text PDF	Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2913306	PMC
http://dx.doi.org/10.1039/c001307b	DOI Listing

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