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A Concise Flow Synthesis of Efavirenz

2015; Wiley; Volume: 54; Issue: 16 Linguagem: Inglês

10.1002/anie.201411728

1521-3773

Camille A. Correia, Kerry Gilmore, D. Tyler McQuade, Peter H. Seeberger,

Click Chemistry and Applications

Abstract 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.