- Dibenzo seven-membered ring derivative as well as preparation method and application thereof
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The invention relates to a dibenzo seven-membered ring derivative as well as a preparation method and application thereof. The chemical structure of the dibenzo seven-membered ring derivative is shownas a formula (I), and X1 and X2 are respectively and independently selected from H, F, Cl, Br or I. The preparation method has easily available raw materials, and can ensure continuous supply and production; the raw materials are cheap and have the cost advantage; and thiophenol or sodium thiophenol is not used, so that the method is more environment-friendly and is also beneficial to the body health of related personnel. 7,8-difluorodibenzo[b,e]thiazepine-11(6H)-one as one of the products can further react to obtain 7,8-difluoro-6,11-dihydrobenzo[c][1]benzothiepin-11-ol, and the 7,8-difluoro-6,11-dihydrobenzo[c][1]benzothiepin-11-ol can be used as an important intermediate for preparing a drug baloxavir, so that baloxavir preparation cost is reduced.
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- 9-(2-fluorobenzyl)-6-(alkylamino)-9H-purines. A new class of anticonvulsant agents
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Several substituted aryl and 6-alkylamino analogues of the anticonvulsant purine 9-(2-fluorobenzyl)-6-(methylamino)-9H-purine were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats. Derivatives with a second fluoro substituent in the 5- or 6-position of the aryl moiety were very active with ip ED50's that ranged from 2 to 4 mg/kg. Congeners in which the purine 6-substituent was varied among a number of alkylamino groups possessed potent activity against MES that was comparable to or several times better than phenytoin.
- Kelley,Krochmal,Linn,McLean,Soroko
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p. 1005 - 1009
(2007/10/02)
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