still for framstellning of bis basic ketones of xanten and xanten - 9 - one with antivirusaktivitet.

摘要

1313454 Xanthene-derived aminoketones RICHARDSON-MERRELL Inc 15 Sept 1971 [11 Dec 1970] 43026/71 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts, wherein Z is O or H 2 , A is C 1-6 alkylene, and each Y is NRSP1/SPRSP2/SP (RSP1/SP, RSP2/SP=H, C 1-6 alkyl, C 3-6 cycloalkyl or C 3-6 alkenyl), pyrrolidino, piperidino or hexamethyleneimino (any of which may be C 1-4 alkyl substituted), morpholino, piperazino or 4-C 1-4 -alkyl-piperazino. In examples, these compounds are prepared by reacting (1) a bis-(chlaroalkanoyl)xanthene with the appropriate amine; (2) a xanthenebispiperidide with a dialkylaminoalkyl Grignard compound; (3) a diacylxanthene with CH 2 O and a dialkylamine; (4) a bis-(phthalimidylalkanoyl)xanthene, or the bis-ketals of the diketones (I), with HCl; (5) the xanthene with Na 2 Cr 2 O 7 /HOAc, giving the xanthene-9- one. Intermediates otherwise prepared are 2,7- bis-(acetyl- and bromoacetyl-)xanthen-9-ones; 2,7 - bis(1,1 - diethoxy - 4 - chlorobutyl - and 3- chloropropyl- )xanthenes); and 2,7-bis(1,1-diethoxy-4-morpholinobutyl)xanthene. Therapeutic compositions having antiviral activity, and which may be administered orally, topically, bucally, parenterally or by intranasal instillation or aerosol, comprise compounds of the above formula. These compounds may also be used to treat a viral infection in viable biological material such as can be used in the production of vaccines.