| 摘要 |
<p>1,257,960. Esters of N-substituted 3-hydroxymethyl - 1,2,5,6 - tetrahydropyridine. BOEHRINGER INGELHEIM G.m.b.H. 25 June, 1969 [25 June, 1968], No. 32090/69. Heading C2C. The invention comprises compounds of formula and their acid addition salts and quaternary ammonium derivatives, wherein R 1 is C 2-10 alkyl (possibly CN- or alkyl-substituted), C 2-3 alkenyl (possibly halogen-substituted), C 2-3 alkynyl, C 3-6 cycloalkyl, or phenylalkyl; R 2 is H, Cl, Me or OH and R 3 is H, Ph or C 5-6 cycloalkyl, or CR 2 R 3 is a 5- or 6-membered cycloaliphatic ring ; and R 4 is Ph provided that when both R 3 and R 4 are Ph these groups may be joined through their o-positions either directly or via an O atom. These compounds are prepared by an esterification or N-substitution method. Details are also given for the preparation of 1-hexyl-3-hydroxymethylpyridinium bromide and 1 - hexyl - 3 - hydroxymethyl - 1,2,5,6 - tetrahydropyridine. Therapeutic compositions for oral, parenteral, rectal or topical administration, comprise compounds of the above formula, which have spasmolytic and CNS-sedative activity, in association with a pharmaceutical carrier or diluent.</p> |
