| 摘要 |
<p>Cpds. of formula (I) (where R1 and R2 are each H, halo, 1-3C alkyl or alkoxy, or R2 may also be -CH2OH) are used as hypnotics or sedatives in animals and have an analeptic action on the CNS. The exhibit control of cardiac rhythm and respiratory analeptic props. and have low toxicity; LD50 (mice) = ca. 1000 mg./kg. i.p. and ca. 300 mg./kg. i.v. (c.f. 820 and 280 for heptaminol.HCl), for the claimed cpd. heptaminol chromone carboxamide (Ia). (Ia) also has antiinflammatory props. shown by its activity against kaolin induced localised oedema in mice (at 100 mg./kg. i.p.) (I) are prepd. (a) by condensing heptaminol with the corresp. chromone carboxylic acid either by means of a dehydrating agent such as H2SO4 and/or polysulphuric acid, or by azeotropic distn. of water with benzene, toluene or trichloroethylene, etc. or (b) by reaction of heptaminol with the corresp. chromone carboxylic acid chloride in acetone.</p> |
