| 摘要 |
<p>New pyrimidine derivates and their manufacture. G3A. Novel compounds of the formula (I) and their addition salts:- (where R = OH, halogen or opt. substd. amino lower alkylamino amino and ring A must be substd. by at least one carbocyclic aromatic group) which have antibacterial, antiparasitic and antiinflammatory activity may be prepared by reacting an aryl substd. 2-mercapto cyclohexanone or 5(6) hexenone with cyanoacetic acid or its deriv. to give 1-mercapto-2-cyanoacarboxymethylene cyclohexane (or 5(6)ene) which is cyclised to novel 2-amino-3-carboxy-6,7-dihydro and 4,5,6,7-tetrahydro benzo b thiophenes with antiphlogistic and hypotensive activity, which are converted to (I). In an example, 4-chloro-6,8-diphenyl-5,6,7,8-tetrahydro- 1 -benzothieno pyrimidi- ne is reacted with beta-diethylaminoethylamine to give 4-(beta-diethylaminoethylamino)-6,8-diphenyl-5,6,7,8-tetrahydro- - 1 -benzothieno(2,3-d pyrimidine. are then converted to (I) (R = OH). This converted to (I) (R = halogen) and then to (I) (R = aminoalkylamino).</p> |
