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February 1, 2006
The Good New Days
I've been working on a longer post on antisense drugs (which, in case you're wondering, are different - most of the time - from nonsense drugs), but it's not quite ready yet. Home life and the Wonder Drug Factory are keeping me hopping these days.
The other day I was talking about old-fashioned reactions that we still use all the time, and I can testify to that from recent experience. I've been messing around with Grignard reagents all week, for one thing. But one of the comments to that post mentioned that I shouldn't give people the impression that those reactions are all that we use, and that's a good point.
For example, I've said before that if I had to pick one type of reaction that's run every day now that wasn't well-known when I was in graduate school, it would be a palladium-catalyzed coupling. The most commonly run is the Suzuki reaction, and we've been doing those all week, too. I would absolutely hate to do without this family of carbon-carbon bond forming methods - in fact, it's hard to imagine how we ever did.
But even though it's been around since 1979, not many people ran these reactions in the mid-1980s when I was in grad school. Palladium chemistry was seen as this exotic stuff that did weird things, and did them mostly in the hoods of organometallic chemists. As that decade wore on, though, the Suzuki and other such couplings became better known, and they just completely conquered the world in the 1990s. Now there are whole sections of the chemical catalogs devoted to them. You probably could buy about a half-dozen arylboronic acids back in 1985, but an entire industry has sprung up around such things now. And since new improvements and extensions keep coming all the time, the catalogs will surely look even stranger in another fifteen years.
My only real complaint about the Suzuki reaction is that there are so many ways to run it - solvents, catalysts, additives, temperature. You can generally get it to give you some product, no matter what conditions you choose. But in many cases, optimizing it to a reproducible high yield is like black magic. My pet theory is that any given palladium coupling reaction can be made to run in over 90% yield, if you're just willing to devote enough of your life to finding out how. Most of the time, I take what they give me and move on.
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