| 摘要 |
<p>Prepn. of sulphamoylbenzamides of formula (I) is claimed: (where X is H or halogen; R is H or alkyl; R1-R3 are 1-4C alkyl or benzyl, or can be linked together or with R to form a ring; R4 is alkyl, alkenyl, aralkyl or alkoxyalkyl; R5 and R6 are H, alkyl or alkenyl, or together form a ring). The prepn. comprises (a) chlorosulphonating a salicylic acid ether (b) converting the product to the corresp. acid halide (III); (c) reacting (III) with a stoichiometric amt. of RNH-CH2-CHR1-NR2R3 to form and an amide hydrochloride (V); and (d) reacting (V) with R5R6NH. Cpds. (I) are useful as pharmaceuticals, e.g. N- (1-ethyl-2-pyrrolidinyl)-methyl -2-methoxy-5-sulphamoyl-benzam- ide (Ia) has psychotropic, spasmolytic and antiemetic activity. Intermediates (III) (which are stated to be new) are stable, easily purified crystalline cpds., giving high-purity prods. (I).</p> |
