| abstract |
NEW MATERIAL:The compound of formula (R is pyridylmethylthio, pyridylmethylsulfinyl, pyridylthiomethyl or quinolylmethylthio). EXAMPLE:2-Amino-5-(2-pyridylmethylthio)-1,3,4-thiadiazole. USE:an antitumor agent. PREPARATION:The objective compound can be produced by reacting 2-amino-5- mercapto-1,3,4-thiadiazole with a compound of formula ClCH2-X (X is pyridyl or 4-quinolyl) (e.g. 2-picolyl chloride hydrochloride) in the presence of a base (e.g. sodium hydroxide) using a phase-transfer catalyst (e.g. tetra-n- butylammonium bromide). The reaction solvent is preferably a mixture of water and a water-insoluble organic solvent such as benzene. |