PURPOSE: To obtain a novel compound useful for the treatment of diseases associated with the hyperactive behavior of α-adrenergic system on the ureter level, dysuria, pollakiurea, and benign hypertrophy of the prostate.
CONSTITUTION: There is provided a compound of formula I [wherein R is H, methyl, a phenoxyalkyl of formula II (wherein X is H, F, Cl, methyl, 1- methylethyl, or ethoxyl; and (n) is 2 or 3); (m) is 1 when (p) is 1, (m) is 0 when (p) is 2; (q) is 0 or 1; and R1 is H or methyl], for example, 2-{4-{(2-(2- methoxyphenoxy)ethyl)amino}piperidin-1-yl}pyrimidine-4-carboxamide hydrochloride. The compound of formula I can be obtained by reacting an amine compound of formula III (wherein R' is an amino protective group) with 2- chloropyrimidine-4-carboxamide in the presence of a base in an aprotic solvent to obtain an aminopyrimidine compound of formula IV, removing the protective group from the product, and optionally reacting the obtained compound with a phenoxyalkyl halide of formula V (wherein Y is Cl or Br).
KURISUCHIYAN MAROWAZERU
BENOWA MARABOO
JIYANNPIEERU MERURI