A gateway to a world of boundless possibilities in molecular evolution
Enamine proudly introduces the Late-Stage Functionalization Kit (LSF Kit) — a unique collection of Building Blocks equipped with specially engineered functional “handles” designed for precise and efficient late-stage transformations. This kit unlocks a new level of creative freedom for medicinal chemistry teams, enabling them to explore structure–activity relationships (SAR) and generate new analogs without altering the core molecular scaffold — faster, smarter, and more efficiently.
Key Features of the Late-Stage Functionalization Kit
- Building Blocks equipped with functional “handles” compatible with modern LSF methodologies.
- Includes activated NHPI esters — ideal substrates for mild decarboxylative C(sp³)-radical generation.
- Bonus components: two ligands and a catalyst for an immediate start to diversification workflows.
- Orthogonal compatibility with aryl and heteroaryl halides, BPin fragments, alkynes, azides, sulfonamides, nitriles, CF₃ groups, and more.
- Medicinal-chemistry-focused motifs: azetidines, pyrrolidines, piperidines, morpholines, and other high-value heterocycles.
Each building block in Enamine LSF Kit is equipped with a synthetically privileged functional group-carefully optimized for flawless transformations, including cross-coupling, C‑H activation, click chemistry, as well as photoredox and radical processes. Thanks to this, the Late-Stage Functionalization Kit integrates seamlessly into modern ligand- and medicinal-design strategies, providing researchers with unprecedented flexibility and speed.
Advantages of the Late-Stage Functionalization Kit
- Rapid SAR expansion: enables the creation of analogs without altering the core molecular architecture
- Minimal synthetic “repair”: replace parts, not the scaffold
- Support for cutting-edge chemistry: radical, photoredox, and electrochemical approaches
- Reliable supplier: Enamine offers one of the world’s largest collections of building blocks (>1.5 million compounds) with scalable logistics (enamine.net)
- Easy access: order via the Enamine catalog and online store
Examples of Enamine LSF Kit components and bonus additions — two ligands and a catalyst
Enamine LSF Kit will be an ideal solution for medicinal chemistry teams working on lead optimization and aiming to rapidly introduce saturated fragments or vary substituents without unnecessary synthetic redesign. It will also benefit researchers seeking to minimize molecular scaffold re-engineering and accelerate the progression from hit to lead. In addition, the kit is especially valuable for laboratories looking for a ready-to-use “plug-and-play” solution for late-stage transformations that is compatible with the most advanced methodologies.
Our specialists are continuously expanding and diversifying this collection of Late-Stage Functionalization Kit by introducing new classes of different compounds, thereby supporting and accelerating drug discovery workflows.
Availability
Enamine LSF Kit is available for order through the Enamine catalog and online shop. Full specifications, a list of included compounds, application examples, and instructions can be found on the Enamine website or obtained through local representatives. (For details and delivery terms, please contact the EnamineStore.com or our sales department.)
Selected publication on the use of Late-Stage Functionalization Kit
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Control of Redox-Active Ester Reactivity Enables a General Cross-Electrophile Approach to Access Arylated Strained Rings.
Daniel C. Salgueiro, Benjamin K. Chi, Ilia A. Guzei, Dr. Pablo García-Reynaga, Prof. Daniel J. Weix Angewandte Chemie 2022, 134 (33), e202205673. DOI: 10.1002/ange.202205673