Intermediates for the preparation of n-alkylated dipeptides...

Details Intermediates for the preparation of n-alkylated dipeptides... Intermediates for the preparation of n-alkylated dipeptides...

C - Chemistry, Metallurgy

07

C

260/284, 260/317

C07C 309/70 (2006.01) C07D 209/20 (2006.01) C07D 217/26 (2006.01) C07K 5/02 (2006.01)

Patent

CA 1281330

ABSTRACT The invention relates to compounds of the formula III Image (III) in which R1 denotes hydrogen or (C1 to C6)-alkyl which can optionally be substituted by amino, (C1 to C6) acylamino or benzoylamino, (C2 to C6)-alkenyl, (C3 to C9)-cycloalkyl, (C5 to C9)-cycloalkyl, (C3 to C7)- cycloalkyl-(C1 to C4)alkyl, (C6 to C12)-aryl or partially hydrogenated aryl, each of which can be substituted by (C1 to C4) alkyl, (C1 or C2)-alkoxy or halogen, (C6 - C12)-aryl (C1 to C4)-alkyl or (C7 - C13)-aroyl-(C1 - C2)-alkyl, both of which can be substituted in the aryl radical as previously defined, a monocyclic or bicyclic heterocyclic radical having 5 to 7 or 8 to 10 ring atoms respectively, wherein 1 or 2 of these ring atoms may be sulfur or oxygen atoms and wherein 1 to 4 of of these ring atoms may be nitrogen atoms, or a side chain of a naturally occurring, optionally protected ? -aminoacid, R3 denotes hydrogen, (C1 to C6)-alkyl, (C2 to C6)alkenyl or (C6 to C12)-aryl-(C1 to C4)-alkyl, and R4 and R5, together with the atoms carrying them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 5 to 15 carbon atoms, and to a process for their preparation. The compounds of the formula are intermediates in the preparation of compounds of the formula I, which are inhibitors of angiotensin converting enzyme (ACE) or are intermediates in the preparation of inhibitors of this type.

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