Three New Building Block Series Advanced at Vipergen
Vipergen is pleased to announce three new publications, describing the synthesis of three series of novel bifunctional building blocks for DNA-encoded library (DEL) synthesis, developed in close collaboration with Algirdas Šačkus and his group at the Institute of Synthetic Chemistry, KTU.
The three papers address a central challenge in DEL design: expanding chemical space beyond flat, aromatic-dominated scaffolds toward novel 3D diverse frameworks that are synthetically tractable and amenable to library production.
In the first paper (Voznikaitė et al, Molecules 2026, 31, 2689), a new series of pyrimidine-based building blocks is described – combining the pyrimidine ring with a range of saturated chiral heterocycles via cyclocondensation to give novel bicyclic amino acid derivatives. The optimized synthetic routes generally provided the products in high enantiomeric excess (>90% ee)
The second paper (Jankauskas et al, Molecules 2026, 31, 2736) presents an efficient stereoselective synthesis of chiral pyrrolidine derivatives carrying indole, pyrazole, and indazole moieties – pharmacophores widely found in approved drugs. The methodology affords products in high yield with inverted configuration, and further diversification via palladium-catalysed cross-coupling extends the structural reach of the building block series.
The third paper (Voznikaitė et al, Molecules 2026, 31, 2909) introduces two complementary routes to 2,3-disubstituted propanoic acid building blocks, combining saturated cyclic amines – piperidine and azetidine – with nitrogen heterocycles via aza-Michael addition. Both routes proceed generally in high yield (>60%), with a broad substrate scope, and offer complementary structural access from a common intermediate.
“These publications reflect our ongoing investment in our DEL platforms. Novel, synthetically tractable, building blocks with high scaffold and 3D diversity ensure that our libraries continuously cover new areas of chemical space” said Rico Gerup Petersen, Senior Scientist at Vipergen. “We are also grateful to our colleagues at KTU for their outstanding synthetic chemistry expertise and dedication – this body of work is a testament to what a strong academic-industry collaboration can achieve.”
The full papers are available open access in Molecules: 2689 · 2736 · 2909
About Vipergen ApS
Vipergen is a world-leading provider of small-molecule drug discovery services based on DNA-encoded library (DEL) technologies and is the first and only company capable of screening DELs inside a living cell. Vipergen provides its proprietary suite of leading-edge DEL technologies through funded discovery partnerships with leading pharmaceutical and biotechnology companies, including top pharmaceutical companies in the USA, EU, and Japan. For more details about Vipergen and the YoctoReactor® (yR), Binder Trap Enrichment® (BTE), and Cellular Binder Trap Enrichment® (cBTE) drug discovery technology platforms, please visit https://www.vipergen.com.
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