abstract |
PROCEDURE FOR THE PREPARATION OF 1-(1-BENZIMIDAZOLIL)-3-N-Y2-(4-HYDROXY-3-METHOXYPHENYL)-2-HYDROXYETHYLZAMINO-BUTANE. INCLUDES THE FOLLOWING STAGES: A) CONDENSATION OF 3-AMINO-1- (1-BENZIMIDAZOLIL) BUTANE WITH (3-METHOXY-4-PHENYL-METHOXY) PHENYLGLYOXAL OR WITH 2-ETHOXY-2-HYDROXY-1-(3-METHOXY-4-PHENYL-METHOXY-PHENYL) ETHANONE, IN ALCOHOLIC MEDIUM FOR FORM AN IMINE; B) IN SITU REDUCTION OF THE IMINE WITH EXCESS SODIUM BOROHHYDRIDE TO FORM 1-(1-BENZIMIDAZOLIL)-3-N-Y2-HYDROXY-2-(3-METHO XI-4-PHENYLMETHOXY-PHENYL)ETHYLZAMINO-BUTANE, FOLLOWED OF TRANSFORMATION IN A NON-TOXIC ACID ADDITION SALT, IN CRYSTALLINE FORM, CARRIED OUT WITH SULFURIC ACID; C) HYDROGENOLISIS OF THE SALT IN THE PRESENCE OF PALLADIUM ON CHARCOAL AND HYDROGEN AT TEMPERATURES FROM 20 TO 40JC; D) TRANSFORMATION OF THE SALT INTO BASE, BY ALKALINIZATION IN AQUEOUS MEDIUM, BY MEANS OF ALKALINE CARBONATE AND E) SALIFICATION OF THE BASE OBTAINED WITH NON-TOXIC ACID TO OBTAIN THE DESIRED SALT OF GENERAL FORMULA (I). |