CYANOGUANIDINE DERIVATIVE AND PRODUCTION THEREOF

摘要

NEW MATERIAL:A compound shown by formula I (R is lower alkyl; R' is H or lower alkyl). EXAMPLE:N-Cyano-N'-[2-(3-formamino-2-oxobutylthio)ethyl]-N''-methylgua nidine. USE:A synthetic intermediate for cimetidine, a remedy for gastric ulcer, showing inhibitory action on secretion of acid in the stomach based on histamine H2- acceptor antagonism. Cimetidine is obtained in a readily treatable way at a few reaction stages in high yield. PREPARATION:A haloketone derivative shown by formula II (X is Cl or Br) is reacted with an ammonium salt and a lower fatty acid salt (e.g. ammonium formate) in a double layer solvent of formamide and chloroform at 0-100 deg.C to give a compound shown by formula I.