Synthesis and Biological Activity of 9-(2,6-Difluorobenzyl)-9H-purines Bearing Chlorine
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概要
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Mitsunobu reaction of 2,6-dichloropurine with 2,6-difluorobenzyl alcohol gave 2,6-dichloro-9-(2,6-difluorobenzyl)-9H-purine and 7-benzylated congener in 73% and 10% yield, respectively. Treatment of the former compound with ammonia gave 2-chloro-9-(2,6-difluorobenzyl)adenine (1) in good yield. Also, 2-amino-6-chloro-purine was condensed with 2,6-difluorobenzyl alcohol in a similar manner to afford 2-amino-6-chloro-9-(2,6-difluorobenzyl)-9H-purine (2) as a major product. Inhibition of phosphodiesterase (PDE) isozymes by 9-(2,6-difluorobenzyl)-9H-purines was investigated and both 1 and 2 were found to be good inhibitors of PDE2 in addition to PDE4.
- 1999-04-15
著者
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KOZAI Shigetada
Faculty of Pharmaceutical Sciences, Tokushima Bunri University
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Maruyama Tokumi
Faculty Of Pharmaceutical Sciences At Kagawa Campus Tokushima Bunri University
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Maruyama Tokumi
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Kozai Shigetada
Faculty Of Pharmaceutical Sciences Tokushima Bunri University
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Kozai Shigetada
Faculty Of Pharmaceutical Science Tokushima Bunri University
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