Total synthesis of lasofoxifene and nafoxidine

ABSTRACT

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 (1) and lasofoxifene (2). Diketone 6 was prepared in a convenient, three-step sequence starting from 3-methoxy benzaldehyde in good yields.

GRAPHICAL ABSTRACT

KEYWORDS:

• Diketone
• lasofoxifine
• low-valent titanium
• nafoxidine
• reductive coupling process

Acknowledgment

We thank Suven Life Sciences for allowing us to publish this work and for excellent analytical services.