KinasePro

Kinase Chemistry – Just a year and a half behind the times.

WO2006104917

Posted by kinasepro on October 15, 2006

Hi again GSK,

Looks like Kinasepro was napping again while you guys nominated your latest p38 candidate. I like your process route, and thanks for reminding me why I’ll never make a good process chemist.

You see in step 2 KP would just chuck it in the microwave with some Ac2O, precipitate with ether, and carry the crude. Sure I’d end up with a 25% yield, but I’d be half way home by lunchtime! It appears as if maybe there’s a better way to do the cyclization. I’ve never heard of this activated Horner-Emmons reagent but I can’t imagine you’d stick it in the patent if it didn’t work, eh? (Yah, these process guys are just like that) Thanks for the tip.

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