ChemInform Abstract: Highly Efficient Synthesis and Characterization of the GPR30-Selective Agonist G-1 and Related Tetrahydroquinoline Analogues.

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

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 51 KB
• Volume: 41
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.201038164

✦ Synopsis

Abstract

Lewis acid‐catalyzed aza‐Diels—Alder cycloaddition of an aniline derivative (I) with cyclopentadiene (II) and various aromatic bromides (III) can be carried out in a three‐component process or by two‐step method to afford GPR30‐selective antagonist G‐1 (IVa) and derivatives (IV), (VI)/(VII), (IX), (XI)/(XII).