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


ABSTRACT: 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.

SUBMITTER: Burai R 

PROVIDER: S-EPMC2913306 | biostudies-literature | 2010 May

REPOSITORIES: biostudies-literature

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

Burai Ritwik R   Ramesh Chinnasamy C   Shorty Marvin M   Curpan Ramona R   Bologa Cristian C   Sklar Larry A LA   Oprea Tudor T   Prossnitz Eric R ER   Arterburn Jeffrey B JB  

Organic & biomolecular chemistry 20100316 9


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. ...[more]

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