KinasePro

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

US20060252943

Posted by kinasepro on November 10, 2006

Hi GSK, Nice process route to VEGF -TIE2 inhibiting pyrimidines They aren’t terribly new (WO2002059110), still KP enjoys a good process application now and then.  Not only  do process chemists do chemistry better then the medchem folk (who’s names are on the initial applications) but nobody asks a process guy to look at the chemistry until there’s something worth making.

Nice alkylating agent.

Anhydrous conditions generally improve HCl salt precipitation.

I didn’t know this stuff did that. Cool.

Simple chemistry, good yields, no chromatography. A process guy’s dream.

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2 Responses to “US20060252943”

  1. Med_chem_workedonProject said

    Love the blog. However there has been very little “process” done to this route. With the exception of a new method for the sulfone aniline synthesis, all of the steps were worked out within the medchem stage of the project. The conditions for the initial alkylation (subject of JOC letter, 2003), the subsequent condensations, and the MeI alkylation were all verbatim with the initial route. Perhaps, we used ethyl acetate for the initial methyl Meerwein alkylation. Your right, simple chemistry, great yields, and no chromatography from the outset. Sure the initial compound application shows many routes, but that is by design — the “process” route was already in place at the beginning — check the initial “process’ or method patent. I agree process chemists do great work, but this case they had very little work to do. Perhaps you picked a bad example without doing enough homework. — thanks Med_chem_workedonProject

  2. kinasepro said

    Thanks for taking note.

    With more comments like yours this blog will become self-correcting!

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