摘要 |
<p>Cpds. of formula (I): (where R1, R2 and R3 are 1-3C alkyl), and their hydrohalides, are prepd. by reacting resorcinol with an alpha-R1CO-gamma-butyrolactone and a hydrogen halide in an anhydrous mixt. of a lower aliphatic acid (pref. glacial acetic) and H3PO3 to give a cpd. (II) of formula: (I); -CH2COOEt is H and -NR2R3 is X, in which X is Cl or Br ; reacting this with XCH2COOEt in acetone in the presence of an alkali metal carbonate and a catalyst, pref. DMF or H2O + KI, to give the ethoxycarbonylmethyl ether; reacting this with excess R2R3NH in benzene or toluene in the presence of an acid binder; washing the reaction mixt. with H2O; evaporating; dissolving in EtOH; treating with anhydrous ZnCl2 to form a complex; separating the complex; and decomposing with aq. alkali metal carbonate or NH4OH. Cpds. (I) are medicaments used for treating circulatory disorders. The overall yield is ca. 75%.</p> |