Total synthesis of lasofoxifene and nafoxidine

Abstract

<p>An intramolecular reductive coupling process of diketone with low-valent titanium species to form a dihydronapthalene skeleton was an important step in the synthesis of nafoxidine (<b>1</b>) and lasofoxifene (<b>2</b>). Diketone <b>6</b> was prepared in a convenient, three-step sequence starting from 3-methoxy benzaldehyde in good yields.</p