Efavirenz is an essential medicine for the treatment of HIV, which is still inaccessible to millions of people worldwide. A novel, semi-continuous process provides rac-Efavirenz with an overall yield of 45 %. This streamlined proof-of-principle synthesis relies on the efficient copper-catalyzed formation of an aryl isocyanate and a subsequent intramolecular cyclization to install the carbamate core of Efavirenz in one step. The three-step method represents the shortest synthesis of this life-saving drug to date.

• Max Planck Institute of Colloids and Interfaces
• Florida State University
• Freie Universität Berlin

• API

1. API
2. copper-catalyzed formation
3. Efavirenz
4. HIV
5. intramolecular cyclization
6. proof-of-principle
7. Research Article
8. semi-continuous process