- Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonis
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Some N3-substituted analogues of willardiine such as 11 and 13 are selective kainate receptor antagonists. In an attempt to improve the potency and selectivity for kainate receptors, a range of analogues of 11 and 13 were synthesized with 5-sub
- Dolman, Nigel P.,More, Julia C. A.,Alt, Andrew,Knauss, Jody L.,Pentik?inen, Olli T.,Glasser, Carla R.,Bleakman, David,Mayer, Mark L.,Collingridge, Graham L.,Jane, David E.
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p. 1558 - 1570
(2007/10/03)
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- Synthesis of tetrahydro-2-furylated pyrimidine derivatives
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The synthesis of 1-(tetrahydro-2-furyl) pyrimidine derivatives in good yields by the reaction of trimethylsilylated pyrimidine bases with 2-acetoxytetrahydrofuran using a catalytic amount of cesium chloride in acetonitrile under mild conditions is described.
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- FACILE SYNTHESIS OF TETRAHYDRO-2-FURYLATED PYRIMIDINES AND PURINES USING A NEW CATALYST OF CESIUM CHLORIDE
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1-(Tetrahydro-2-furyl)pyrimidine and 9-(tetrahydro-2-furyl)purine derivatives were successfully synthesized in good yields by the reactions of trimethylsilylated pyrimidine and purine bases with 2-acetoxytetrahydrofuran using a new catalyst of cesium chloride in acetonitrile under mild conditions.
- Lee, Chun Ho,Kim, Joong Young,Kim, Wan Joo,Kim, Yong Hae
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p. 211 - 214
(2007/10/02)
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- Method for the preparation of derivatives of uracil
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A novel and very elegant method is proposed for the preparation of N1 -(2-tetrahydrofuryl)-5-substituted or -unsubstituted uracil, especially, N1 -(2-tetrahydrofuryl)-5-fluorouracil, by the reaction of the corresponding 5-substituted uracil compound with 2,3-dihydrofuran. The reaction is performed in the presence of a chlorosilane compound, e.g. dimethyldichlorosilane, and a catalytic amount of an organic amine compound and can proceed very rapidly without disadvantageous side reactions to give the objective compound with high purity in a high yield.
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