Process for preparing ccr-5 receptor antagonists utilizing...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 211/98 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2673233

The present invention discloses a novel process to prepare 4-substituted 1-Cyclopropane-sulfonyl-Piperidinyl compounds, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine] compounds.

Cette invention se rapporte à un nouveau procédé permettant de préparer des composés 1-cyclopropane-sulfonyl-pipéridinyl substitués en 4, qui sont des intermédiaires utiles dans la préparation d'antagonistes des récepteurs CCR-5 et qui sont donc utiles dans le traitement des mammifères infectés par le virus HIV. L'invention concerne spécifiquement un nouveau procédé permettant de synthétiser les composés 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-pipéridinyl](3-fluorophényl)méthyl]-3(S)-méthyl-1-pipérazinyl]-1-[(4,6-diméthyl-5-pyrimidinyl)carbonyl]-4-méthylpipéridine].

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