| 摘要 |
New compounds of formula <FORM:1088531/C2/1> where R is C1- 5 alkyl, each of X, Y, and Z is hydrogen, halogen, C1- 5 alkoxy, nitro, amino, C1- 5 alkylamino, di-(C1- 5 alkyl)amino, C1- 6 acyl, C1- 6 alkanoylamino, cyano, sulphamoyl, N-(C1- 5 alkyl)sulphamoyl, N,N-di-(C1- 5 alkyl)-sulphamoyl, trihalomethyl, C1- 5 alkylthio, C1- 5 alkylsulphonyl, polyfluoro-C1- 5 alkylthio or poly fluoro-C1- 5 alkylsulphonyl, R1 is C1- 5 alkyl or allyl, m is 1, 2 or 3, and n is 0 or 1, and their quaternary ammonium salts and N-oxides, are prepared (I) by reaction of corresponding benzoyl halides and amines, or (II) by reaction of corresponding benzoyl imidazoles and amines; other benzoyl derivatives are mentioned including that obtained with Woodward's reagent, and modified procedures apply where the benzoyl compound is amino substituted; re-arrangement may occur in the heterocyclic ring, and the obtention of isomers is mentioned. Starting compounds prepared are: 2-methoxy-5-ethylthiobenzoic acid and the 5-ethylsulphonyl and 5-methylsuphinyl compounds; 2-nitro-4-trifluoromethyl benzoic acid and the 2-amino and 2-chloro compounds, 2-chloro-4-trifluoromethylbenzoic acid methyl ester, 2-methoxy - 4 - trifluoromethylbenzoic acid; 2-methoxy - 4 - sulphamoylbenzoic acid and the 4-dimethylsulphamoyl compound; 3-amino-1-ethylpyrrolidine and its picrates. Pharmaceutical compositions comprise the new compounds with carriers. Oral and parenteral preparations (tranquillizing, antiemetic) are described. |
