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

Archive for October 15th, 2006


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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