Process and intermediates for preparing integrase inhibitors

This application claims priority under 35 U.S.C. 119(e) from U.S. Provisional Patent Application No. 60/971,395, filed 11 Sep. 2007, the contents of which are incorporated herein in their entirety.

International Patent Application Publication Number WO 2004/046115 provides certain 4-oxoquinolone compounds that are useful as HIV integrase inhibitors. The compounds are reported to be useful as anti-HIV agents.

International Patent Application Publication Number WO 2005/113508 provides certain specific crystalline forms of one of these 4-oxoquinolone compounds, 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinolone-3-carboxylic acid. The specific crystalline forms are reported to have superior physical and chemical stability compared to other physical forms of the compound.

There is currently a need for improved methods for preparing the 4-oxoquinolone compounds reported in International Patent Application Publication Number WO 2004/046115 and in International Patent Application Publication Number WO 2005/113508. In particular, there is a need for new synthetic methods that are simpler or less expensive to carry out, that provide an increased yield, or that eliminate the use of toxic or costly reagents.

The present invention provides new synthetic processes and synthetic intermediates that are useful for preparing the 4-oxoquinolone compounds reported in International Patent Application Publication Number WO 2004/046115 and in International Patent Application Publication Number WO 2005/113508.

Accordingly, in one embodiment, the present invention provides a method for preparing a compound of formula 10

or a pharmaceutically acceptable salt thereof, in which a compound of formula 4

or a salt thereof is prepared and converted into a compound of formula 10, characterized in that the compound of formula 4 is prepared from a compound of formula 15

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Industry Class:
Organic compounds -- part of the class 532-570 series

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