method for the preparation of a pharmaceutical preparation with an anti emetic effect.a 5 - (1 - hydro - carbyl - 2 - pyrrolidinylmethylcarbamoyl) - 6 - it - 1h - phenol or a salt thereof contains formed preparationobtained by application of the method and procedure for the preparation of a 5 - (1 - hydrocarbyl - 2 - pyrrolidinylmethyl - carbamoyl) - 6 - it - 1h - phenol or a salt thereof.

摘要

1475234 N - [(1 - Allyl - 2 - pyrrolidinyl)- methyl] - 2 - methoxy - 4,5 - azimidobenzamide SOC D'ETUDES SCIENTIFIQUES ET INDUSTBIELLES DE L'ILE DE FRANCE 24 Feb 1975 [11 Jan 1975] 7674/75 Heading C2C The invention comprises the title compound and acid addition and quaternary ammonium salts thereof and its preparation by nitrating a compound of the formula wherein X is OH or C 1-5 alkoxy and R and RSP1/SP each or H or carboxylic acyl or R and RSP1/SP together from a phthaloyl radical, hydrogenating and, if necessary, deacylating the corresponding 5-amino compound, diazotizing the latter to produce a 4,5-azimido compound of the formula wherein RSP11/SP is H or carboxylic acyl, and reacting this compound or a reactive derivative thereof with l-allyl-2-aminomethylpyrrolidine, or a reactive derivative thereof. Methyl 2 - methoxy - 4 - amino - 5 - nitrobenzoate, methyl 2 - methoxy - 4 - acetamido - 5- nitrobenzoate, and 2-methoxy-4-amino-5-nitrobenzoic acid are obtained by nitrating methyl 2- methoxy-4-aminobenzoate, methyl 2-methoxy- 4-acetamidobenzoate and 2-methoxy-4-aminobenzoic acid respectively. Pharmaceutical compositions, suitable for oral or parenteral administration, contain the above compound or pharmaceutically acceptable acid addition or quaternary ammonium salts thereof together with pharmaceutically acceptable diluents or carriers.