METHOD OF PRODUCING N-SULFAMINE-3-(2-GUANIDINETHIAZOL-4-YLMETHYLTHIO)-PROPIONEAMIDINE
The invention concerns heterocyclic substances, in particular reception of N- sulfamyl-3 (2- guanidinotiazol -4- ilmetiltio)- propionamidin, used in medicine as antineoplastic means. The purpose is the increase of yield and simplification of process. The process is conducted by treatment of dihydroh...
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Zusammenfassung: | The invention concerns heterocyclic substances, in particular reception of N- sulfamyl-3 (2- guanidinotiazol -4- ilmetiltio)- propionamidin, used in medicine as antineoplastic means. The purpose is the increase of yield and simplification of process. The process is conducted by treatment of dihydrohlorid S-(Z- guanidinotiazol-4- ilmetiltio)- izotiokarbamid (I) surplus of alkali (II) in the hydroalcoholic medium. Then alkylation is carried out by means of N- sulfamyl -3 hlorpropionamidin (III) at molar parity I, II and III, equal to 1: (4,1±0,2): (1-1,1). As spirit is used С1-3 - alkanol and as alkali - NaOH which is introduced under temperature from room up to 50°С, or 40 % water solution of NaOH which is introduced under temperature 20-40°С. These conditions allow to increase twice a yield of the final product and to simplify process because the final product is precipitated out in the form of crystals that excludes necessity in column chromatography. claims |
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