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More Boronic Esters, Please
Here’s the Suzuki reaction taken down about as far as it can go: two boron groups on one carbon.
I didn’t even know that you could make those things – no doubt someone will be inspired to try the three-boron version next. Diarylmethanes aren’t the most preferred drug structures in the world (that carbon is just waiting to be oxidized), but I can’t say that I’ve always avoided them on those grounds. I was on a project where we made a whole series of the things, actually – didn’t work out so well for the intended target, but the compounds went on to hit in a completely different assay, so the company did probably get its money’s worth.
Derek Lowe is a medicinal chemist with over 20 years experience in the drug industry. He blogs daily on science and drug discovery at In The Pipeline
2012-08-22 20:12:42 Source: http://pipeline.corante.com/archives/2012/08/22/more_boronic_esters_please.php
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