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A short and highly enantioselective synthesis of both enantiomers of GABA agonist baclofen in four steps with total yields of 32.8% [for (S)-isomer] and 35.1% [for (R)-isomer] is reported. The key step involved desymmetrization of cyclic anhydride with modified cinchona alkaloids.
Novel nucleobase-modified cADPR mimics were synthesized by the application of click chemistry. Cu(I)-Huisgen cycloaddition (click reaction) was used to construct 4-amide-1,2,3-triazole nucleobase and connect two building blocks efficiently. A concise protection strategy was used for the synthesis of the corresponding cyclo-pyrophosphate, and the target compounds 6a and 6b were prepared within four...
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