Catalyzed process of making c-5-substituted heterocyclic...

Details Catalyzed process of making c-5-substituted heterocyclic... Catalyzed process of making c-5-substituted heterocyclic...

C - Chemistry, Metallurgy

07

D

C07D 277/54 (2006.01) C07D 207/36 (2006.01) C07D 233/66 (2006.01) C07D 263/34 (2006.01) C07D 277/34 (2006.01) C07D 277/36 (2006.01)

Patent

CA 2630558

The invention provides a process for preparing 11 ~-hydroxy steroid dehydrogenase type 1 inhibitors of formula (II) via a catalyzed reaction between a compound of formula (I) and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

La présente invention concerne un procédé de synthèse d'inhibiteurs de la 11.beta.-hydroxystéroïde déshydrogénase de type 1 de formule 2 par une réaction catalytique entre un composé de formule 1 et un composé de formule R2LG en présence d'une base : où R1, R2, X, Y et LG sont définis dans la description. Les catalyseurs exemplifiant l'invention contiennent du palladium et un ou plusieurs ligands phosphine. Le procédé peut être mené de façon stéréosélective pour aboutir à des produits énantiomériquement enrichis.

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