A method for preparing and screening one or more compounds

C - Chemistry – Metallurgy – 07 – B

Patent

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C07B 61/00 (2006.01) B01J 19/00 (2006.01) B01J 19/12 (2006.01) C07C 45/29 (2006.01) C07C 209/62 (2006.01) C07C 211/00 (2006.01) C07C 211/27 (2006.01) C07C 227/02 (2006.01) C07C 227/20 (2006.01) C07C 229/00 (2006.01) C07C 229/24 (2006.01) C07C 231/08 (2006.01) C07C 235/00 (2006.01) C07C 235/14 (2006.01) C07C 235/34 (2006.01) C07C 235/36 (2006.01) C07C 237/00 (2006.01) C07C 237/22 (2006.01) C07C 303/38 (2006.01) C07D 211/18 (2006.01) C07D 211/22 (2006.01) C07D 211/34 (2006.01) C07D 211/60 (2006.01) C07D 211/7

Patent

CA 2385715

A method for sequentially performing a synthesis, separation and screening of chemical entities, especially a combinatorial library, is described. The method utilises a bulk of a stationary phase (e.g. silica gel, aluminium oxide, cellulose, etc. for example arranged on a backing) for the performance of the synthesis, separation and screening. The technique described enables a rapid route from synthesis to the testing of chemical compounds. Screening can be performed without need for reaction work-up. Preferred screening methods are those used to determine the biological activity of the compounds.

L'invention concerne un procédé pour effectuer de manière séquentielle la synthèse, la séparation et le criblage d'entités chimiques, notamment pour réaliser une bibliothèque combinatoire. Ce procédé consiste à utiliser un ensemble constitué d'une phase stationnaire (gel de silice, oxyde d'aluminium, cellulose, etc., par exemple placé sur un substrat) pour réaliser la synthèse, la séparation et le criblage. Cette technique permet de passer rapidement de la synthèse à l'essai des composés chimiques. Le criblage peut être réalisé sans traitement conclusif. Les méthodes de criblage préférées sont celles qui sont utilisées pour déterminer l'activité biologique de ces composés.

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