| 摘要 |
<p>Hypnotic and sedative 6-amino-4-oxo-4,5-dihydroisothiazolo(5,4-d)pyrimidines. M3A. are new cmpds. esp of formula (I) and their salts. (R1=aliphatic, cycloaliphatic, cyclo aliphatic-aliphatic hydrocarbon; R2=aliphatic, aromatic or araliphatic group. opt. substd. in the monocyclic aromatic ring; Am = tert. amino). Broadest claim is to 6-amino-4-oxo-4,5-dihydro-isothiazole 5,4-d pyrimidines per se Specific compound is 3,5-dimethyl-6-morpholino-4-oxo-4,5-dihydroisothiazolo 5,4-d pyrimidine. Also claimed are intermediates 6-x-4-oxo-4,5-dihydro-isothiazolo 5,4-d pyrimidines esp. those of formula and 4,6-dihalo cpds. of formula (X degree =halogen, R1, R2 as above). Use as CNS depressants e.g. as sedatives and hypnotics. Oral or i.v. dose of 0.1-0.5g/kg. are effective in mice cats and rabbits. The cmpds. may be prepared as follows:- Other conventional methods, including cyclisation of amino-substd. isothiazoles to give pyrimidine rings, may be used.</p> |
