摘要 |
<p>Cpds. of formula (I) and their salts with organic and inorganic bases: where R = C1-6 alkyl; X = O or S; Y1, Y2 = H or Me; Z1, Z2 = H, halogen of atomic number is not > 35, C1-2 alkyl or C1-2 alkoxy. Diuretics and saluretics. (V; R=Et, Y1=Y2=Z1=H, Z2=6-methyl) (see Farmdoc 41,217) (20g), paraformaldehyde (4.1g) and HNMe2.HCl (8.2g) in dioxan (125 ml) are stirred 8 hrs. at reflux and evapd. in vacuo. The crude residual (II; Am=NMe2) is treated with anhydr. CH3COONa (21g) and glacial AcOH (200 ml), stirred 2 hrs. at reflux and evapd. in vacuo. The residue is stirred with H2O (100 ml), adjusted to pH2 with conc. HCl, stirred 1 hour at 20 deg. and extracted 3 times with Et2O (150 ml). The Et2O solution is dried (Na2SO4) and evapd. The residue is crystallised from cyclohexane and xylene-cyclohexane (I; R=Et, Z1=Y1=Y2=H, Z2=6-methyl), m.p. 100-2 deg.</p> |