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  • Analytical Chemistry

    Chiral Separations With Magnets. No, For Real.

    Now here is something I didn’t expect: what may well be a completely new way to separate enantiomers, not based in any way on shape recognition versus another chiral substance. [Quick background for those not in the field: a great many three-dimensional molecules can exist in right-handed and left-handed mirror-image forms (enantiomers), exac… Read More
  • Chemical News

    Silicon In Drug Molecules, Revisited

    Here’s an update to a post from last year about silicon in drug-like molecules. The Denmark group at Illinois has investigated a range of silicon-containing heterocycles, providing both synthetic routes into the (mostly unknown) structures, and looking at some basic pharmaceutically relevant properties. There’s a lot of work in this pap… Read More
  • Chemical News

    Diazos On Demand

    I don’t think that anyone really likes diazomethane. Organic chemists like what it can do (cyclopropane formation, cycloadditions, fast, clean methyl ester formation, etc.), but the compound itself is very hard to have warm feelings for. It’s unstable on storage, and thus has to be prepared fresh. That preparation is fairly tedious, and… Read More
  • Chemical News

    Give It to the Machines

    Here’s another paper for the automated med-chem files. A group at Merck (Boston) reports a combination of very small-scale automated synthesis with a screening assay in situ (no purification). You may be wondering how that works, or how it can possibly work, especially when you hear that the nanoscale reactions are transition-metal catalyzed. Read More
  • Current Events

    Nationalist Medicine? What Crap is This?

    I would guess that, at this point, I’ve worked with people from every region of the planet except Greenland and Antarctica. That’s how it is in drug research, and how it is in science in general. The problems and questions we’re working on are bigger than any one nationality; we’re tackling these things as a… Read More
  • Analytical Chemistry

    A New Method to Weigh Biomolecules

    I’m always happy when a new analytical technique is worked out, especially one that’s applicable to biological binding assays, doesn’t require labeling of the species involved, and is orthogonal to the existing methods. We need all the reality checks we can get, and this one (reported by a large multinational team led out of Oxfor… Read More
  • Chemical News

    Hydrogenating in a Ball Mill

    Here’s one to add to the “weird mechanosynthesis” pile. According to this paper, you can do hydrogenation reactions in a stainless-steel ball mill, without any sort of noble-metal catalyst. The hydrogen is produced when you add some n-alkane or diethyl ether to the mix (these actually get converted to gaseous methane and hydrogen… Read More
  • Chemical News

    Stop Ignoring the Sugars!

    This paper (from two groups at Yale’s chemistry department) addresses several important things that fall into the “important irritants” category in synthesis and molecular biology – or maybe that should be “irritatingly important”. We spend a lot of time thinking about proteins in terms of their primary sequence… Read More
  • Alzheimer's Disease

    Merck’s BACE-Inhibitor Alzheimer’s Wipeout

    I mentioned last year that Merck’s BACE inhibitor trial for Alzheimer’s had been stopped for futility. Now here’s the full writeup in NEJM, and futility appears to have been le mot juste. There were two treatment groups (12 mg and 40 mg), and in neither one did the ADAS-cog or ADAS-ADL scores (scales for degree… Read More
  • Drug Assays

    Pharmacokinetic Advice From Genentech

    Here’s another solid pharmacokinetics paper, this one from Genentech, with advice on how to extend drug half-life (compare this other recent one). They’re specifically addressing the “make it less lipophilic” rule of thumb that many medicinal chemists have, and they demonstrate that this isn’t exactly a universal law.… Read More
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