PROCESS FOR THE PREPARATION OF N- (1-ALKYL (OR ALLYL) -2-PYRROLIDINYLMETHYL) 2-METHOXY (OR 2,3-DIMETHOXY) -5-SULFAMOYL (OR SULFAMOYL SUBSTITUTED) BENZAMIDES

摘要

Prepn. of N-(1-R1-2-pyrrolidinylmethyl) -2-methoxy-3-R2-5 (N-R3-N-R4-sulphamoyl) benzamides of formula (I) is carried out by treating the corresp. 2-methoxy-3-R2-5- (chlorosulphonyl) benzoic acid (II) with SOCl2, reacting the product with the corresp. 1-R1-2-pyrrolidinylmethylamine (III), and then reacting with HNR3R4. (where R1 is 1-4C alkyl or allyl; R2 is H or OMe; R3 and R4 are H or alkyl). Certain cpds. (I) have antiemetic and tranquillising activity (see FR 5916 M). The process is simpler than prior art processes in that it can be operated as a "one-pot" reaction.