Practical Asymmetric Synthesis of Efavirenz (DMP 266), an HIV-1 Reverse Transcriptase Inhibitor

A highly enantioselective and practical synthesis of the HIV-1 reverse transcriptase inhibitor efavirenz (1) is described. The synthesis proceeds in 62% overall yield in seven steps from 4-chloroaniline (6) to give efavirenz (1) in excellent chemical and optical purity. A novel, enantioselective add...

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Veröffentlicht in:Journal of organic chemistry 1998-11, Vol.63 (23), p.8536-8543
Hauptverfasser: Pierce, Michael E, Parsons, Rodney L, Radesca, Lilian A, Lo, Young S, Silverman, Stuart, Moore, James R, Islam, Qamrul, Choudhury, Anusuya, Fortunak, Joseph M. D, Nguyen, Dieu, Luo, Chi, Morgan, Susan J, Davis, Wayne P, Confalone, Pat N, Chen, Cheng-yi, Tillyer, Richard D, Frey, Lisa, Tan, Lushi, Xu, Feng, Zhao, Dalian, Thompson, Andrew S, Corley, Edward G, Grabowski, Edward J. J, Reamer, Robert, Reider, Paul J
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Sprache:eng
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