XANTHENE DERIVATIVES

摘要

1416039 Bis-basic alkoxyxanthanes RICHARDSON-MERRELL Inc 17 Dec 1973 [21 Dec 1972] 58262/73 Heading C2C Novel compounds of Formula I wherein n is an integer of from 2 to 6; Y is oxygen or sulphur; R and R 1 are each hydrogen, lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having from 3 to. 6 carbon atoms, alkenyl having from 3 to 6 carbon atoms in which the unsaturation is in a position other than in the 1-position of the alkenyl group, or when R and R 1 are taken together with the nitrogen atom to which they are attached represent the pyrrolidinyl, morpholino or piperidino radical; R 2 is hydrogen, halogen, C 1-6 alkyl or C 1-6 alkoxy; and the pharmaceutically acceptable acid addition salts thereof are prepared by dehydration of a compound of Formula III or by reaction of an R-substituted benzaldehyde and a compound of formula optionally followed by salt formation. Intermediates of Formula III above are prepared by action of the appropriate Grignard reagent with the ketone of Formula II which is formed by etherification of 3,6-dihydroxyxanthen-9-one or by reduction of the bis-thioester. 3,6 - Dihydroxyxanthen - 9 - one is prepared by cyclization of 2,21,4,41-tetrahydroxybenzophenone. 5,5 - Bis - 3,6 - (9 - oxo - xanthenyl)dimethylthiocarbamate is prepared by pyrolysis of 0,0-bis- 3,6 - (9 - oxo - xanthenyl)dimethylthiocarbamate which is prepared by reacting 3,6-dihydroxyxanthen-9-one with NaH and dimethylthiocarbamoyl chloride. Antiviral compositions in conventional forms for oral, topical and parenteral administration comprise an above novel compound and a carrier or diluent.