AI Article Synopsis
- The study presents a sustainable method for hydroxymethylation or methylenation of imidazo-heteroarenes using KIO and formaldehyde generated from renewable sources like ethylene glycol and glycerol.
- This one-pot reaction yielded various 3-hydroxymethyl-imidazo-heteroarenes, important for pharmaceutical development, exemplified by Zolpidem.
- Additionally, the method allowed for the selective production of bis(imidazo[1,2-a]pyridin-3-yl)methane derivatives with good to excellent yields using glycerol.
Article Abstract
Herein, we report a KIO -mediated, sustainable and chemoselective approach for the one-pot C(sp )-H bond hydroxymethylation or methylenation of imidazo-heteroarenes with formaldehyde, generated in situ via the oxidative cleavage of ethylene glycol or glycerol (renewable reagents) through the Malaprade reaction. In the presence of ethylene glycol, a series of 3-hydroxymethyl-imidazo-heteroarenes was obtained in good to excellent yields. These compounds are important intermediates to access pharmaceutical drugs, e.g., Zolpidem. Furthermore, by using glycerol, bis(imidazo[1,2-a]pyridin-3-yl)methane derivatives were selectively obtained in good to excellent yields.
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| http://dx.doi.org/10.1002/anie.202104503 | DOI Listing |
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