- Reactivity of 6-halopurine analogs with glutathione as a radiotracer for assessing function of multidrug resistance-associated protein 1
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6-Bromo-7-[11C]methylpurine is reported to react with glutathione via glutathione S-transferases in the brain and to be converted into a substrate for multidrug resistance-associated protein 1 (MRP1), an efflux pump. The compound with a rapid c
- Okamura, Toshimitsu,Kikuchi, Tatsuya,Fukushi, Kiyoshi,Irie, Toshiaki
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- The new convenient synthesis of 6-fluoropurine and its 7-/9-unsubstituted analogues
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6-Fluoropurine and its 7-/9-unsubstituted analogues have good biological activity and serve as important pharmaceutical intermediates. This paper describes a new and convenient synthesis of 6-fluoropurine and its 7-/9-unsubstituted analogues, by first replacing the chlorine atoms with trimethylammonio groups through the reaction of 6-chloropurine and its 7-/9-unsubstituted analogues with trimethylamine, and then replacing the trimethylammonio groups with fluorine atoms using safe and cheap TBAF·3H2O as fluorinating agent at room temperature. Compared with reported methods, the new synthesis has milder conditions, shorter reaction times, simpler post-processing and higher (or similar) yields.
- Deng, Mei,Wang, Ningyu,Xiang, Guangming,Yu, Luoting
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p. 2999 - 3006
(2013/02/23)
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- Room-temperature nucleophilic aromatic fluorination: Experimental and theoretical studies
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(Chemical Equation Presented) Taming the reagent: The use of anhydrous tetrabutylammonium fluoride (TBAFanh) in nucleophilic aromatic substitution reactions, including variants of the selective halogen-exchange and fluorodenitration processes (see scheme), was investigated. It was shown that TBAFanh permits these reactions to be performed under surprisingly mild conditions if it is used in relatively nonpolar media.
- Sun, Haoran,DiMagno, Stephen G.
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p. 2720 - 2725
(2007/10/03)
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