Convenient One‐Pot Preparation of Dimethyl Bicyclo[2.2.2]octane‐1,4‐dicarbolylate, a Key Intermediate for a Novel Adenosine A₁ Receptor Antagonist

Abstract

Dimethyl bicyclo[2.2.2]octane‐1,4‐dicarboxylate (4), a key starting material for a novel adenosine A₁ receptor antagonist, was prepared in a one‐pot reaction with convenient workup and improved yield.

Keywords:

• dimethyl bicyclo[2.2.2]octane‐1,4‐dicarboxylate
• one‐pot preparation
• stoichiometry

Acknowledgment

The authors thank Richard J. Staples (X‐ray Crystallographic Laboratory, Harvard University) for performing single‐crystal X‐ray diffraction.