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Asymmetric Synthesis of a Potent HIV-1 Integrase Inhibitor.

Asymmetric Synthesis of a Potent HIV-1 Integrase Inhibitor.
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Kuethe JT, Humphrey GR, Journet M, Peng Z, Childers KG,


Kuethe JT, Humphrey GR, Journet M, Peng Z, Childers KG, (click to view)

Kuethe JT, Humphrey GR, Journet M, Peng Z, Childers KG,

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The Journal of organic chemistry 2016 8 10()

Abstract

The development of a practical asymmetric total synthesis of the potent HIV-1 integrase inhibitor 5 is described. Key transformations include construction of the naphthridine core in a highly efficient manner followed by cyclization of the 8-membered ring. Control of the atropisomers of intermediates and final compound 5 is also described.

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