Process for making HIV protease inhibitors

Details Process for making HIV protease inhibitors Process for making HIV protease inhibitors

1995-06-07

1997-09-02

Bernhardt, Emily

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544360, 544362, 544390, C07D24104, C07D40106

Patent

active

056633416

ABSTRACT:
A process for racemization of optically pure or enriched piperazine-2-tert-butylcarboxamide and its derivatives comprising reacting the optically pure or enriched piperazine compound with a racemizing agent selected from a strong base, an anhydrous metal salt or a carboxylic acid, in a solvent at a temperature range of between room temperature and 250.degree. C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.

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Askin et al, Tetrahedron Letters, vol. 35, No. 5, pp. 673-676 (Jan. 31, 1994).
A. Neuberger, "Stereochemistry of Amino Acids," in M.L. Anson et al. (eds), Advances in Protein Chemistry vol. IV Academic Press 1948, pp. 344-356.

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