Comments for TotallyMedicinal

Comment on KSP inhibitors from Merck by gurung

gurung — Thu, 03 Jul 2008 12:51:28 +0000

Yeah! u r suggestion is correct. There was excellent yield with aryl, pyridine, thiophene, furan boronic acid and faced the problem with alkyl boronic acid. Some anhydrous white solid was obtained with alkyl boronic acid as u suggested.

Thanks for ur response.

Comment on KSP inhibitors from Merck by milkshake

milkshake — Wed, 02 Jul 2008 17:41:17 +0000

also, are you aware that simple alkyl boronic acid perform very poorly in normal Suzuki (unlike vinyl, aryl and cyclopropyl)? There was report that methyl boronic acid trimer anhydride for Suzuki is feasible - but people stil prefer tin for this.

There is alkyl-transfer Suzuki variant that actually works and seems quite general - but it uses alkyl BBN boranes (generated by hydroboration of the olefin).

Comment on KSP inhibitors from Merck by milkshake

milkshake — Wed, 02 Jul 2008 16:32:20 +0000

Boronic acids spontaneously form anhydrides - cyclic trimeric ones and linear polymers also.

Dont despair - take the proton and carbon (and boron - if you have the probe) NMR in D2O with a little inorganic base and you will see that the spectra will clean up.

This is quite typical - people make boronic acid and it looks beautiful upon workup in crude but once they re-crystallise it…

You can use the whole mix, it makes no difference for Suzuki. But if it makes you nervous you can combine it with pinacol and make the pinacolada ester - those do not have this behaviour

Comment on KSP inhibitors from Merck by gurung

gurung — Wed, 02 Jul 2008 12:35:44 +0000

We bought isopropyl boronic acid (1gm) from Aldrich and n-hexyl boronic acid from Alfa recently. We set up rxn and found negative result(it did not worked). Then we analyze the chemical(eg. MP, nmr) and found that either compound is almost impure or not required one.Do you have such experience everbefore?

Comment on KSP inhibitors from Merck by santosh

santosh — Tue, 01 Jul 2008 03:53:03 +0000

Thanks dude a lot.
yes, we have google in korea.

Comment on KSP inhibitors from Merck by TotallyMedicinal

TotallyMedicinal — Mon, 30 Jun 2008 16:34:14 +0000

This might be what you are after

http://www.newscientist.com/honeywellcomp.ns

Don’t you have google in S. Korea?

http://www.google.co.uk/search?hl=en&safe=off&client=firefox-a&rls=org.mozilla%3Aen-GB%3Aofficial&hs=lPM&q=%22Chemistry+Rocks%22+New+Scientist&btnG=Search&meta=

Comment on KSP inhibitors from Merck by santosh

santosh — Mon, 30 Jun 2008 10:16:14 +0000

Hey Tot Med Chem!!!
I’v heard that newscientist has announced a competition, an essay writing on title “Chemistry Rocks”
The deadline is July 2. Could you post the url( weblink) to upload the essay.

Thanks

Santosh
S. Korea

Comment on 2-naphthylamines by DrSnowboard

DrSnowboard — Mon, 09 Jun 2008 15:47:34 +0000

Makes you wonder where they found the bottle of beta-napthylamine to use as reagent. A prohibited substance in the UK, and lame not even to mention its hazards.

Comment on Med chem stuff by TotallyMedicinal

TotallyMedicinal — Sun, 01 Jun 2008 13:42:03 +0000

Thanks Chris, that is very useful

Comment on Med chem stuff by Chris

Chris — Sun, 01 Jun 2008 08:16:15 +0000

One of the things I’m often asked for by small companies of academic groups who are looking to bring a compound forward is list of assays/properties they should evaluate.

After searching around I can’t find such guidance in the public domain so I’ve tried to put together a checklist that I hope will be useful.

http://homepage.mac.com/swain/Sites/CMC/DDResources/preclinical_checklist.html

Chris