A general approach to a new generation of spirocyclic molecules - oxa-spirocycles - was developed. The key synthetic step was iodocyclization. More than 150 oxa-spirocyclic compounds were prepared. Incorporation of an oxygen atom into the spirocyclic unit dramatically improved water solubility (by up to 40 times) and lowered lipophilicity. More potent oxa-spirocyclic analogues of antihypertensive drug terazosin were synthesized and studied .
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8447932 | PMC |
| http://dx.doi.org/10.1039/d1sc03615g | DOI Listing |
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