AI Article Synopsis
- Carbo-nucleoside derivatives are key pharmaceuticals, but few methods exist for creating new versions.
- Researchers have developed a new synthesis for specific substituted cyclopropanes that can undergo useful chemical reactions.
- This new method allows for efficient production of a variety of (carbo)nucleoside analogues in just four to five steps, facilitating the creation of bioactive compound libraries.
Article Abstract
(Carbo)nucleoside derivatives constitute an important class of pharmaceuticals, yet there are only few convergent methods to access new analogues. Here, we report the first synthesis of thymine-, uracil-, and 5-fluorouracil-substituted diester donor-acceptor cyclopropanes and their use in the indium- and tin-catalyzed [3+2] annulations with aldehydes, ketones, and enol ethers. The obtained diester products could be easily decarboxylated and reduced to the corresponding alcohols. The method gives access to a broad range of new (carbo)nucleoside analogues in only four or five steps and will be highly useful for the synthesis of libraries of bioactive compounds.
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| http://dx.doi.org/10.1002/anie.201404832 | DOI Listing |
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