Synthesis of Scaffolds

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Synthesis of Scaffolds

Almac performs the custom synthesis of scaffolds and Building blocks but has also a research program to access novel compounds.

These Building Blocks are selected for their novelty and the difficulty to be synthesised by standard chemistry. They of course present the usual MedChem features (low MW, heterocyclic structures, multiple points of diversity …) but most of all they present potential to generate IP and also fill a gap in particular chemical spaces lacking diversity.

Our catalogue currently lists 400 Building Blocks but analogues or exclusive series are also available as part of our activity.

Download Almac catalogue of Novel Scaffolds and Building Blocks from the following links:

For any enquiry regarding our catalogue, please contact scaffolds@almacgroup.com.

The following is an illustration of a C-Nucleoside library that Almac has synthesised where diazoketone derivatives of four sugar mimics were used to construct a variety of heterocycles in each case.

Further reaction with a range of aromatic and aliphatic acyl chloride-building blocks by Biofocus provided a library of more than 600 compounds.

Making Heterocycles from Diazoketones

Diazoketones Derived from Aminoacids

Almac Sciences has applied its diazoketone technology to the synthesis of a range of N-protected amino acids and peptides in multi-kilogram quantities. Selected examples, labelled by their parent amino acid, are:

These homochiral educts are ideally suited to numerous synthetic transformations, some of which are shown below:

β-Aminoacid derivatives via Arndt-Eistert homologation, for example:

α-Halogenated ketones leading to halohydrins and epoxides

High levels of diastereoselectivity can be achieved in the above reduction by chemocatalysis or biocatalysis [Link to biocatalysis section in website]

α-N-Protected aminoglyoxals via oxidation

Cyclopropane-substituted amino acids via cyclopropanation with ethyl diazoacetate

Almac

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