Suzuki–Miyaura–hydrogenation targets 3D drugs

Scientists in the UK have unveiled a way to make pharmaceutical molecules with increased 3D characteristics. The single pot Suzuki–Miyaura–hydrogenation reaction results in sp2–sp3 linked pharmaceutically relevant molecules.

Source: Royal Society of Chemistry
A single pot Suzuki–Miyaura-hydrogenation can be used to furnish lead and fragment-like products in good to excellent yields

The number of tetrahedral carbon atoms, or how 3D a molecule is, is one factor that determines the success of a molecule in clinical drug trials. Molecules with a high sp3 fraction are in demand, however current methods to make them suffer drawbacks. The Suzuki–Miyaura reaction is common for the cross-coupling of sp2–sp3 systems, but alkyl boron or alkyl halides are prone to β-elimination and other side reactions, producing mixtures of products.

Read the full story by Suzanne Howson on Chemistry World.

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