Carboxamido-ethylbenzene-4-sulphonamide derivs. prepn. - by reacting beta:phenyl-ethylamine with an acid chloride, sulphochlorination and amidation

摘要

Prepn. of carboxamidoethylebzene 4-sulphonamide derivs. of formula (I), suitable for use in the prepn. of sulphonylurea derivs. with hypoglycaemic activity, comprises (a) reacting beta-phenylethylamine with a chloride of an acid RCOOH, to give an intermediate of formula (II) which is then (b) sulphochlorinated with chlorosulphonic acid and (c) amidated with concn. ammonia to give (I). In the formula, R is substd. 3,5-isoxazole. (I) are used in the prepn. of sulphonylurea derivs. which are effective hypoglycaemically at low doses, e.g. Glysolamide. (I) can be produced in only 3 steps, compared to the 6 steps necessary in previous processes and is produced in higher yields with lower prodnosts.