| 摘要 |
<p>1437170 Thiazolidinone-acetic acid derivatives WARNER-LAMBERT CO 19 March 1975 [25 March 1974 15 Feb 1975] 11411/75 Heading C2C Novel compounds I in which R 1 is C 1-4 alkyl, and pharmacologically compatible salts thereof, are prepared by reacting a corresponding C 2-6 alkyl ester at a temperature below ambient temperature with a 40 to 50% solution of hydrogen bromide in an aliphatic carboxylic acid containing up to 5 carbon atoms, and thereafter removing the acid mixture to isolate the desired amino acid which may, if desired, be converted to a pharmacologically compatible salt. t - Butyl 3 - methyl - 4 - oxo - 5 - piperidinothiazolidin - 2 - ylidene - acetate is prepared by reacting ethyl t-butyl-cyanoacetate with ethyl thioglycolate to form t-butyl 4-oxo-thiazolidin-2- ylideneacetate, reacting this with dimethyl sulphate to form t-butyl 3-methyl-4-oxo-thiazolidin-2-ylidene-acetate, reacting this with N-bromosuccinimide to give the corresponding 5-bromo derivative and then reacting this with piperidine. Pharmaceutical compositions having diuretic, anti - hypertensive and body temperatureregulating activity, for oral or parenteral administration, comprise one of the above novel compounds together with a pharmaceutical carrier.</p> |
