More than 30 coupling reagents have been used for amide bond formation on a large scale. In practice, nine of them do almost all of the work.

More than 30 coupling reagents have been used for amide bond formation on a large scale. In practice, nine of them do almost all of the work.

We work mostly with pharma CMC teams on process development, reaction optimization, and kinetic modeling. Across that client base, a small number of reactions come up far more often than the rest: amide, Suzuki, and Buchwald-Hartwig coupling.

So we put together a cheat sheet for each one. What the realistic options are at every decision point - substrate partners, coupling agent or ligand and Pd source, base, solvent - along with typical operating ranges and a worked large-scale example from a published process.

Nothing here is secret. It's the kind of thing most process chemists assemble for themselves. We just put it on one page.

All three are downloadable on our website.

And if you run these reactions regularly and think we could add something, tell me. We'll fold the good suggestions into the next version.

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