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A method of synthesis of 3-thiopropinyl derivatives of 5-oxo-1,3,4-benzothiadiazepine-4-acetic acid, potential antihypertensive drugs, vasopeptidase inhibitors, starting from 2-thiobenzoic acid hydrazide has been elaborated.

The accessible D-ribose mercaptoacetyl-, 3-mercaptopropionyl-, and 2-mercaprobenzoylhydrazones were used to develop a method of synthesis of gold glyconanoparticles with the average particle diameter of 10–40 nm and a low polydispersity index.

Basing on natural amino acid L-cysteine, commercially available aliphatic aldehydes, 2-acetylsulfanylbenzoyl chloride and 2,2′-disulfandiyldibenzoyl dichloride a synthesis was developed of (2R,4R)-2-alkyl-3-(2-mercaptobenzoyl)thiazolidine-4-carboxylic acids, potential antihypertensive compounds, inhibitors of angiotensin transforming enzyme.

Optically pure (2S,4S)-2-alkyl-6-oxo-3-(phenylcarbamothioyl)hexahydropyrimidine-4-carboxylic acids have been synthesized from natural L-asparagine, commercially available aldehydes, and phenyl isothiocyanate. The product structure was confirmed by 1H and 13C NMR data.

The natural amino acid L-cysteine, commercially available aldehydes, and 3-(acetylsulfanyl)propionyl chloride were used for the synthesis of 2-substituted (2R,4R)-3-(3-mercaptopropionyl)thiazolidine-4-carboxylic acids, potential antihypertensive drugs with angiotensin converting enzyme inhibiting action.

Proceeding from natural amino acid L-asparagine and commercially available aldehydes a stereoselective synthesis was developed of (2S,4S)-2-alkyl(aryl)-3-(3-sulfanylpropanoyl)-6-oxohydropyrimidine-4-carboxylic acids, potential antihypertensive drugs, inhibitors of the angiotensin converting enzyme.

A stereoselective three-step synthesis of the title thiazolidine-4-carboxylic acids (III), potential lead compounds for the development of antihypertensive drugs with angiotensin converting enzyme inhibitory activity, starting from natural L-cysteine (I) is given.