4.6 Article

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

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 8, Issue 9, Pages 2252-2259

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c001307b

Keywords

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Funding

  1. NIH [R01 CA127731, U54MH074425, U54MH084690]
  2. University of New Mexico Cancer Research and Treatment Center NIH [P30 CA118100]
  3. New Mexico Cowboys for Cancer Research Foundation
  4. Oxnard Foundation
  5. Stranahan Foundation
  6. NATIONAL CANCER INSTITUTE [P30CA118100, R01CA127731] Funding Source: NIH RePORTER
  7. NATIONAL INSTITUTE OF MENTAL HEALTH [U54MH084690, U54MH074425] Funding Source: NIH RePORTER

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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.

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