AI Article Synopsis
- A new platform has been developed for creating 1,2-difunctionalized bicyclo[1.1.1]pentanes, which can mimic certain substituted aromatic compounds.
- This method allows for the synthesis of valuable building blocks that include alcohol, amine, and carboxylic acid functionalities from a single starting material.
- Detailed studies on the absorption, distribution, metabolism, and excretion (ADME) of these compounds, along with computational analyses, confirm their potential effectiveness as bioisosteres of aromatic compounds.
Article Abstract
The development of a versatile platform for the synthesis of 1,2-difunctionalized bicyclo[1.1.1]pentanes to potentially mimic /-substituted arenes is described. The syntheses of useful building blocks bearing alcohol, amine, and carboxylic acid functional handles have been achieved from a simple common intermediate. Several and -substituted benzene analogs, as well as simple molecular matched pairs, have also been prepared using this platform. The results of in-depth ADME (absorption, distribution, metabolism, and excretion) investigations of these systems are presented, as well as computational studies which validate the or -character of these bioisosteres.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8285974 | PMC |
| http://dx.doi.org/10.1073/pnas.2108881118 | DOI Listing |
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