| 摘要 |
1295489 Thiopyranothienopyrimidines CIBAGEIGY AG 17 Dec 1970 [19 Dec 1969 26 Nov 1970] 59976/70 Heading C2C Compounds of the general Formula (I) (R 1,2 =halogen, CF 3 ; n=2, 3; R 3 =H, Me, Et; R 4 = Me, Et; R 5,6 = H, C 1-6 alkyl or -NR 5 R 6 = optionally C-methylated pyrrolidino, piperidino, hexamethyleneimino, morpholino, thiomorpholino, N<SP>1</SP>-(C 1-6 alkyl)piperazino, N<SP>1</SP>-(#- hydroxyethyl)piperazino) and their salts are prepared by (a) reacting a compound of the Formula (II) (X=halogen) with R 5 R 6 NH or (b) reacting a compound of the Formula (III) (X<SP>11</SP> = halogen) with R 3 R 4 N(CH 2 )nNH 2 , optionally followed in either case by isomer separation and/or salt formation. Compounds (II) and their salts are prepared by reacting a compound of the Formula (IV) with R 3 R 4 N(CH 2 ) n NH 2 , optionally followed by isomer separation and/or salt formation. Compounds (IV) are prepared by replacing the hydroxy groups in the corresponding 2, 4- dihydroxy compounds by halogen atoms, and the dihydroxy compounds are prepared by reacting a compound of the Formula (V) with an N-cyanoacetylurethane and sulphur. Compounds (I) and (II) and their salts possess antibacterial and antiparasitic activity (and are, in particular, antimalarials and anthelmintics) and may be administered in the form of pharmaceutical and veterinary preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier. |
