📋 Workflow
Full workflow, products add-to-cart directly1
Setup and reagents
30 minPrepare anhydrous solvent, oxidant, and metal catalyst under inert atmosphere.
💡 Tip Oxidant choice governs the catalytic cycle
⚠️ Caution Often high T/P—ensure venting and safety
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2
Substrate and directing group
20 minWeigh the directing-group substrate and fix the ratio to the coupling partner.
💡 Tip Have a built-in or designed directing group
⚠️ Caution Missing directing group loses site selectivity
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3
Thermal C–H activation
4–8 hHeat in solvent (often 80–120℃) with stirring; sample periodically.
💡 Tip Sealed vial better holds temperature
⚠️ Caution High T with flammable solvent needs care
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4
Reoxidize and workup
1 hComplete the cycle with oxidant, then extract/filter to remove metal.
💡 Tip Peroxide or Ag salt serves as terminal oxidant
⚠️ Caution Pick oxidant to avoid over-oxidation
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5
Purify and confirm site
1 hPurify by column; confirm insertion site by NMR/2D (e.g. HMBC).
💡 Tip 2D NMR pins down which C–H was replaced
⚠️ Caution Carefully assign regiochemistry
🧪 Materials for this step (click to shop by spec/brand)
⚠️ 5 Common Beginner Mistakes
- ① Weak directing group loses selectivity
- ② Wrong oxidant over-oxidizes
- ③ Low T inert, high T fragments
- ④ Incomplete metal removal pollutes
- ⑤ Wrong site assignment misreads structure
❓ FAQ
+Benefits of C–H activation?
Skip pre-functionalization—high atom/step economy.
+Can directing groups be recycled?
Some are designed removable/recyclable depending on structure.
+Selectivity and scope?
Heavily dependent on directing group/catalyst; screen per substrate.