| 摘要 |
<p>1454039 Substituted 4-oxotetrahydroquinoline 1-carboxylates PFIZER Inc 13 Sept 1974 [26 Dec 1973] 40126/74 Heading C2C The invention comprises compounds of Formula I wherein R, R 1 and R 2 are the same or different and are C 1-4 alkyl groups which may be prepared by acylation of a compound of Formula II with an appropriate agent, e.g. alkylchloroformate. Ethyl - 3 - [3,4 - dimethoxyanilino] - 2 - butenoate is prepared by reaction of 4-animoveratrole with ethylacetoacetate and is hydrogenated to obtain ethyl - 3 - [3,4 - dimethoxyanilino]- butanoate which on treatment under reflux with methanolic aqueous sodium hydroxide is hydrolysed to 3-[3,4-dimethoxyanilino]butanoic acid which is cyclized by heating with polyphosphoric acid to obtain 6,7-dimethyoxy-2-methyl- 4-oxotetrahydroquinoline. Pharmaceutical compositions having analgesic and tranquillizing activity for oral or parenteral application comprise a compound of Formula I together with a pharmaceutically acceptable carrier.</p> |
