Abstract:
1-PHENYLPROPEN (1)YL(3)-OXYCARBONYL - 2'' - PIPERIDINOETHYLAMIDE AND ITS SALTS WITH PHYSIOLOGICALLY TOLERABLE ACIDS HAVING LOCAL ANAESTHETIC ACTIVITY.
Abstract:
N-ACYLATED HALOBENZENE-2,4-DISULFONAMIDE OF THE FORMULA
1-X,2-(NH2-SO2-),4-(R1-CO-N(-R)-SO2-)BENZENE
IN WHICH X IS CHLORINE OR BROMINE; R IS METHYL, ETHYL OR TETRAHYDROFURFURYL; AND R1 IS ALKYL OF UP TO 8 CARBON ATOMS, CHLOROMETHYL, BROMOMETHYL, ALLYL, FURYL, CYCLOPENTYLMETHYL, PHENYL, BENZYL OR PHENYLETHYL, HAVE BEEN FOUND TO HAVE VALUABLE DIURETIC AND SALURETIC ACTIVITY.
Abstract:
Prepn. of sulphamylanthranilic acids of formula (I) by the method given under 'PREPARATION'. Hal = Cl, Br R = benzyl, thienyl, furfuryl (I) are diuretic and saluretic agents. A mixt. of 3-sulphamyl-4-chloro-6-nitrobenzoic acid (10 g) and benzylamine (40 ml) is stirred at 100-110 deg. for 1 hr. and the hot mixt. poured into 2N-HCl (400 ml). The recovered product is dried, powdered, extd. several times with CH2Cl2 and then purified by charcoal treatment in aq. NaHCO3 soln. to yield 3-sulphamyl-4-chloro-6-benzylaminobenzoic acid (65%). m.p. 240 deg.