Process for preparing intermediates for thrombin inhibitors

Details Process for preparing intermediates for thrombin inhibitors Process for preparing intermediates for thrombin inhibitors

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) C07D 205/04 (2006.01) C07D 207/09 (2006.01) C07D 211/26 (2006.01) C07D 211/70 (2006.01) C07D 223/04 (2006.01) C07D 265/30 (2006.01) C07D 267/10 (2006.01) C07D 279/12 (2006.01) C07D 281/06 (2006.01) C07D 401/12 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2185950

A process is provided for preparing intermediates of the structure (see fig.I) wherein Rpg is preferably =CHC6H5; and P.G. is a protecting group CBZ or BOC, wherein a protected guanylpyrazole is reacted with an azacycloalkyl, azacycloalkenyl or azaheteroalkyl derivative (such as a piperidine derivative) in the presence of a DBU catalyst. The resulting intermediate may be used as a starting material for preparing thrombin inhibitors.

Méthode pour préparer des intermédiaires de structure (voir fig. I), où Rpg est de préférence =CHC6H5; P.G. est un groupe protecteur CBZ ou BOC; on fait réagir un guanylpyrazole protégé, avec un azacycloalkyle, un azacycloalcényle ou un azahétéroalkyle (comme un dérivé de la pipéridine), en présence d'un catalyseur DBU. L'intermédiaire obtenu peut servir comme produit de départ pour la préparation d'inhibiteurs de la thrombine.

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