Analogifremgangsmaade for the preparation of racemic or optically active pairs within disubstituted derivatives or corresponding amine oxides, quaternary ammonium compounds or salts with physiologically acceptable acids

摘要

New geminally disubstituted indenes are of general formula I IMAGE (I) wherein each of R1 and R2 is hydrogen or R1 and R2 together form a direct bond or an alkylene group -(CH2)n-, in which n is an integer from 1 to 4, R3 is hydrogen, C1-3-alkoxy or halogen, and each of R4 and R5 is hydrogen or C1-4-lower alkyl, or R4 and R5 together form an alkylene group -(CH2)m-, in which m is an integer from 3 to 6; and the corresponding amine oxides, quaternary ammonium compounds and salts with physiologically acceptable acids. The indenes find use in treating incontinence, as a mucous membrane decongestant, as a blood pressure reducing agent, as vasocostrictor or as an anti-reserpine agent. The indenes may be prepared by processes known per se involving (a) synthesing the side chain -CH(OH)CH2NR4R5 by a method known per se in an indenyl precursor of a formula I compound in which the side chain is incomplete or (b) introducing the double bond into an indanyl precursor of a formula I compound in which the double bond is absent or (c) releasing the terminal amino group in a precursor of a formula I compound in which the terminal amino group is protected.