| 摘要 |
1,174,202. Azalicycloalkane derivatives. CIBA Ltd. 1 Jan., 1968 [30 Dec., 1966; 15 Nov., 1967], No. 44/68. Heading C2C. Novel azalicycloalkane compounds of the formula wherein Ar represents an aromatic or a monoazacyclic radical of aromatic character, R 1 and R 2 together stand for an oxo group, or R 1 represents a hydrogen atom, and R 2 represents a hydrogen, or a free or functionally converted hydroxyl group, R 3 stands for an aliphatic hydrocarbon radical, and Het represents an N- azalicycloalkyl group, and salts thereof, are produced by reacting a compound of the formula with formaldehyde and a compound of the formula H-Het, and, if desired, converting in a resulting compound having an oxo group, such group into a hydroxy group, and/or, if desired, converting in a resulting compound having a hydroxy group, such group into an oxo group or into a functionally converted hydroxy group, and/or, if desired, converting a resulting salt into the free compound or into another salt or converting a resulting free compound into an acid, and/or, if desired, separating a resulting mixture of isomers into the single isomers. p-(Z-oxy)-propiophenone is prepared by treating p-hydroxypropiophenone with a dispersion of NaH, to which mixture is added (Z)-chloride where Z is 4-fluoro-benzyl or 2-dimethylaminoethyl. 4-Benzyloxybutyrophenone is produced similarly but using p-hydroxybutyrophenone. Pharmaceutical compositions having antitussive activity and containing the compounds defined above, are administered enterally, for example orally, or parenterally.
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