Patent ID: 8119375
Filing Date: 2012-02-21
Classification: C07C,C07D,C12P

Abstract:
1. A method for preparing ramipril of the formula (I) which comprises (A) hydrolyzing a compound of the formula (II) in which R is (C and then (B) converting the compound of the formula (III) by addition of penicillin G amidase into a mixture of the compounds of the formulae (IV) and (V) or a mixture of salts of the compounds of the formula (IV) and (V), or alternatively (BA′) the compound of the formula (II) being reacted with penicillin G amidase and then being hydrolyzed by addition of one or more bases or acids to a mixture of the compounds of the formulae (IV) and (V) or a mixture of salts of the compounds of the formula (IV) and (V), and then (C) converting the compound (V) or a salt of the compound (V) from the mixture of the compounds (IV) and (V) or salts thereof by catalytic hydrogenation into a compound of the formula (VI) or a salt thereof, and then either (D-A) reacting the compound of the formula (VI) with a compound of the formula (VII) to give the compound of the formula (I), or alternatively (D-B.1) reacting the compound of the formula (VI) with benzyl alcohol to give a compound of the formula (VIII) or a salt thereof, and then either (D-B.2.1) reacting the compound of the formula (VIII) either with the compound of the formula (VII) to give a compound of the formula (X) or alternatively (D-B.2.2) reacting the compound of the formula (VIII) with a compound of the formula (IX) to give a compound of the formula (X), and then (D-B.3) forming the compound of the formula (I) from the compound of the formula (X) by catalytic hydrogenation.