PURPOSE: To obtain the compound useful as an intermediate for the synthesis of an antiulcerative famotidine in high yields by using a 3-substituted propionitrile and an oxonium salt as starting materials and reacting the product with a sulfamide.
CONSTITUTION: A 3-substituted propionitrile of formula I (wherein R is a halogen, mercapto, methylmercapto, isothiouronium, 5-methyl-1,3,4-thiadiazole-2- mercapto) is reacted with an oxonium salt of formula II (wherein X is Cl or Br), desirably 1.0-3.0 mol of the compound of formula I is reacted with 4.0-15.0 mol of 1.4-dioxane being a compound of the formula II at 40-70°C under a pressure of 0.5-4.0 kg/cm2 in the presence of 1.0-3.0 mol of a sulfamide to obtain a compound of formula III. The compound of formula III is reacted with a compound of formula IV (wherein R1 is a halogen or a 1-8C trialkylsilyl salt) to obtain a compound of formula V.
FURANSHISUKO KABUREE-KASUTERUB
FURANSHISUKO EUGENIO PAROMO-NI
JIYUAN KABURE-KASUTERUBI
ANTONIO RUISU PAROMO KORU