Process for making hiv protease inhibitors

Details Process for making hiv protease inhibitors Process for making hiv protease inhibitors

C - Chemistry, Metallurgy

07

D

C07D 241/04 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 403/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 487/04 (2006.01) C07D 491/04 (2006.01) C07D 491/048 (2006.01) C07D 495/04 (2006.01)

Patent

CA 2180947

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 °C. The piperazine carboxamide derivatives are key intermediates in the preparation of HIV protease inhibitor compounds, including Compound J.

L'invention se rapporte à un procédé de racémisation de pipérazine-2-tert-butylcarboxamide optiquement pur ou enrichi et de ses dérivés qui consistent à faire réagir le composé de pipérazine optiquement pur ou enrichi avec un agent de racémisation sélectionné à partir d'une base forte, un sel métallique anhydre ou un acide carboxylique, dans un solvant à une température comprise entre la température ambiante et 250 ~C. Les dérivés de carboxamide pipérazine sont des intermédiaires clés utilisés dans la préparation de composés inhibiteurs de la protéase du VIH, y compris le composé J.

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