A process for the preparation of 2,2-disubstituted pyrroles

C - Chemistry – Metallurgy – 07 – D

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C07D 207/16 (2006.01) C07D 211/58 (2006.01) C07D 263/04 (2006.01) C07D 263/52 (2006.01)

Patent

CA 2563330

The present invention relates to the stereoselective preparation of 2,2- disubstituted-4-carbonatepyrroles from readily available chiral starting materials. Such pyrroles are useful as intermediates in the preparation of 2,2,4-trisubstituted 2,5-dihydropyrroles, that are inhibitors of mitotic kinesins and are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The product of the process of the invention may be illustrated by the Formula (I).

L'invention concerne la préparation stéréosélective de 4-carbonatepyrroles disubstitués en 2,2 à partir de matières premières chirales rapidement et facilement utilisables. Ces pyrroles sont utiles en tant qu'intermédiaires pour la préparation de 2,5-dihydropyrroles trisubstitués en 2,2,4, qui sont des inhibiteurs des kinésines mitotiques et peuvent être utilisés le traitement les maladies cellulaires prolifératives associées à l'activité kinésine KSP, et pour l'inhibition de la kinésine KSP. Le produit résultant du procédé décrit peut être illustré par la formule (I).

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