Synthesis of HIV Protease Inhibitor ABT-378 (Lopinavir)

A large scale process for the synthesis of HIV protease inhibitor candidate ABT-378 has been developed which utilizes an intermediate common to the synthesis of ritonavir, Abbott's first generation compound. The synthesis relies on the sequential acylation of this intermediate which is carried...

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Bibliographic Details
Published in:Organic process research & development 2000-07, Vol.4 (4), p.264-269
Main Authors: Stoner, Eric J, Cooper, Arthur J, Dickman, Daniel A, Kolaczkowski, Lawrence, Lallaman, John E, Liu, Jih-Hua, Oliver-Shaffer, Patricia A, Patel, Ketan M, Paterson, Joseph B, Plata, Daniel J, Riley, David A, Sham, Hing. L, Stengel, Peter J, Tien, Jien-Heh J
Format: Article
Language:English
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Summary:A large scale process for the synthesis of HIV protease inhibitor candidate ABT-378 has been developed which utilizes an intermediate common to the synthesis of ritonavir, Abbott's first generation compound. The synthesis relies on the sequential acylation of this intermediate which is carried through as a mixture of diastereomers until the penultimate step. A synthesis of acid 5, derived from l-valine, is also reported.
ISSN:1083-6160
1520-586X
DOI:10.1021/op990202j