ANTICONVULSANTS RELATED TO U-54494 PREPARED FROM CIS-1,2-DIAMINOTETRALIN AND CIS-2,3-DIAMINOTETRALIN

[摘要] cis-Diaminotetralins 4 and 10 were converted in 4 steps to benzologs of the novel anticonvulsant U-54494. Attempted alkylation of 4 and 10 with 1,4-dibromobutane provided mixtures of the bis-pyrrolidino compounds and starting free bases together with the desired monopyrrolidino compounds 5 and 11. Treatment of these mixtures with ethyl chloroformate followed by chromatographic separation gave the carbamates 7 and 12. Reduction of these carbamates with LiAlH4 provided the N-methylamino compounds 8 and 14. Finally, benzamide formation gave rise to the analogs of U-54494, compounds 9 and 15.

[发布日期] 1991-08-05