| 摘要 |
The invention relates to trifluoromethanesulfonates of the formulae II and III (II) (III) in which n = 2, R represents (C1 to C6-alkyl, (C2 to C6)-alkenyl, (C3 to C9)-cycloalkyl, (C2-C5)-acylamino-(C1- C4)-alkyl, (C7-C13)-aroylamino-(C1-C4)-alkyl, (C1-C4)-alkoxycarbonylamino-(C1-C4)-alkyl, (C6 C12)-aryl-(C1-C4)-alkoxycarbonylamino-(C1-C4)-alkyl, (C6 to C12)-aryl which can be monosubstituted, dissubstrituted or trisubstituted by one or more of (C1-C4)-alkyl, (C1 to C4)-alkoxyhydroxy, halogen, nitro, amino, (C1 to C4)-alkylamino, di-(C1 to C4)-alkylamino and methylenedioxy, or 3-indolyl, R1 represents hydrogen or (C2 to C6)-alkyl, which can be optionally substituted by amino, (C1 to C6)-acyl-amino or benzoylamino, (C2 to C6)-alkenyl, (C3 to C9)-cycloalkyl, (C5 to C9)-cycloalkenyl, (C3 to C7)-cycloalkyl-(C1 to C4)-alkyl, (C6 to C12)aryl or partially hydrogenated aryl, either of which can be substituted by (C1 to C4)-alkyl, (C1 or C2)-alkoxy or halogen, (C6 to C12)-aryl-(C2 to C4)-alkyl or (C7-C13)-aroyl-(C1-C12)-alkyl, either of which can be substituted in the aryl radical as defined above, a monocyclic or bicyclic heterocyclic radical having 5 to 7 or 8 to 10 ring atoms respectively of which 1 or 2 ring atoms represent sulfur or oxygen atoms and/or 1 to 4 ring atoms represent nitrogen atoms which can be thienyl, benzo-¢b!thienyl, furyl, pyranyl, benzofuryl, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, pyridazinyl, indazolyl, isoindolyl, indolyl, purinyl, quinolizinyl, isoquinolinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolyl, cinnolinyl, pteridinyl, oxazolyl, isoxazolyl, thiazolyl or isothiazolyl, or a side chain of a naturally occurring protected .alpha.-amino acid, R2 represents hydrogen, (C1 to C6)-alkyl, (C2 to C6)-alkenyl or (C6 to C12)-aryl- (C1 to C4)alkyl, and R3 represents hydrogen, (C1 to C6)-alkyl, (C2 to (C6)-alkenyl or (C6-C12)-aryl-(C1 to C4)-alkyl and processes for their preparation. The compounds of the formula II and III are intermediates for the preparation of inhibitors of the angiotensin converting enzyme. |
