Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 54, Issue 16, Pages 4945-4948Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201411728
Keywords
API synthesis; carbamates; copper; flow chemistry; homogeneous catalysis
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Funding
- Max-Planck-Society
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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.
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