Process for the preparation of 2-(r)-(1- (r)-(3,5-bis...

Details Process for the preparation of 2-(r)-(1- (r)-(3,5-bis... Process for the preparation of 2-(r)-(1- (r)-(3,5-bis...

C - Chemistry, Metallurgy

07

D

C07D 413/06 (2006.01) C07D 249/04 (2006.01)

Patent

CA 2348526

The present invention is directed to the compound 4-N,N-dimethylaminomethyl -5- formyl-1, 2,3 -triazole (I) which is a valuable intermediate in a novel convergent process for the preparation of 2-(R)-(1- (R)-(3,5-bis (trifluoromethyl) phenyl)-ethoxy) -4-(5-(dimethylamino) methyl-1,2,3-triazol - 4-yl)methyl) -3-(S)-(4- fluorophenyl) morpholine (II) which is a potent and selective substance P (or neurokinin-1) receptor antagonist useful as a therapeutic agent.

La présente invention concerne un composé 4-N,N-diméthylaminométhyl -5-formyl-1, 2,3-triazole (I) qui est un produit intermédiaire utile à un nouveau procédé convergent de préparation de 2-(R)-(1- (R)-(3,5-bis (trifluorométhyl) phényl)-éthoxy) -4-(5-(diméthylaminométhyl) -1,2,3-triazol -4-yl)méthyl) -3-(S)-(4- fluorophényl) morpholine (II), qui est un antagoniste puissant et sélectif du récepteur de la substance P (or neurokinine-1) utile comme agent thérapeutique.

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