An improved synthesis of 5,6,7,8‐tetrahydro‐1,7‐naphthyridine ‐ a conformationally‐restricted analog of 2‐(3‐pyridyl)ethylamine

Abstract

The 5,6,7,8-tetrahydro-1,7-naphthyridine (7) pharmacophore has the potential to serve as a conformationally-locked analog of the pharmacologically active 2-(3-pyridyl)ethylamine (1) core structure. This paper describes the synthesis of 5,6,7,8-tetrahydro-1,7-naphthyridine (7) via a five-step sequence, which affords a significant improvement over previously reported syntheses.