Library Synthesis

Quick access to quality compound libraries is the key driver to accelerating drug discovery. Enamine has both components required to offer efficient service:

• The stock of the building blocks. The world’s largest! Around 200k monomers are available for library designs enabling diversity, structural quality, and novelty
• Parallel synthesis capabilities. Over 1 000 compounds are produced per day, typically in 5-10 mg

This unique and powerful combination allows us to synthesize compound libraries within only three weeks and that at the price of the building blocks themselves!

Collaborative approach

Besides sharing with you an SD file with our stock building blocks, we can help you with the design of the library by advising on the reactivity of the end-capping building blocks. Most of the building blocks have been tested in-house and have been assigned reactivity scores. We can select those which, we believe, will afford products. Library enumeration can also be performed at Enamine for your convenience.

Affordability

Typically, we offer a flat price per compound in the library, often cheaper than the cost of building blocks required to prepare them.

The chemistry we perform

Parallel synthesis is enabled with over 35 validated reactions which in certain cases we can also run in a consecutive one-pot way (2-3 steps):

• All standard transformations (amidation, alkylation, arylation, reductive amination, etc.),
• Post-reaction protective group removal (Boc-, t-Bu, MOM, THP, etc.),
• Transition metal catalyzed reactions (Suzuki, Stille, Buchwald-Hartwig, etc.),
• Ring closures (1,2,4- and 1,2,3-triazoles, 1,2,4- and 1,3,4-oxadiazoles, thiazoles, imidazoles, etc.),
• Photoredox-catalyzed alkyl-aryl coupling reactions.

We have a wealth of experience in custom synthesis of scaffolds and various intermediates and can offer a full cycle of library synthesis starting from scratch.

Quality control and logistics

We perform reversed-phase preparative HPLC purification on all synthesized compounds to assure they meet purity requirements (usually 90% or 95% pure). Their quality is controlled with LCMS and up to 100% with ¹H NMR. The compounds can be delivered in virtually any containers, including those received from a customer and assay-ready plates for immediate screening.