| 摘要 |
<p>1,236,962. Tropic acid esters. BOEHRINGER INGELHEIM G.m.b.H. 12 Sept., 1968 [12 Sept., 1967], No. 43511/68. Heading C2C. Compounds of Formula (I) where R 1 is H or acyl; R 2 is the group II or -O-A-NR 3 R 4 ; n is 1,2 or 3; A is an aliphatic chain containing at least 2C which may be branched and in which the O and N atoms are directly bonded to different C atoms; R 3 is a straight or branched chain, saturated or unsaturated aliphatic group or cycloalkyl; R 4 is as R 3 or is an alkylene group which may be branched and/or contain a hetero atom and which extends from the adjacent N of NR 3 R 4 to a C atom of A to give a 5-7 membered heterocycle; or R 3 and R 4 together represent a 4-6C alkylene group which may be branched and/or contain a hetero atom; are prepared by reduction of a compound IV to give I where R 1 is H, followed if necessary by acylation to give I where R 1 is acyl. Certain of compounds I are novel viz. those where R 1 and R 2 are as defined above with the provisos that R 4 is not as R 3 except where A has 2C atoms only; and that where R 1 is H, -ANR 3 R 4 is not an N-(straight or branched chain saturated or unsaturated aliphatic or cycloalkyl) - 3 - piperidyl, CH 2 CH 2 N(CH 3 ) 2 or CH 2 CH 2 N(C 2 H 5 ) 2 group. The acid addition salts and quaternary ammonium derivatives are also novel. Intermediates isolated are the compounds of Formula (IV) which are prepared by reaction of R 2 H with an alkylα-formylphenylacetate. Pharmaceutical compositions comprise one of the novel compounds I together with a suitable carrier or diluent, are administered orally, rectally or parenterally and have spasmolytic activity.</p> |
