In our current projects targeted to development of synthetic strategies applicable in the high-througput synthetic concept, we have been developing solid-phase synthesis (SPS) methodologies to access different drug-like heterocycles. In the field of drug discovery and development, SPS has been frequently used in the search for biologically active compounds and their modification due to its significant advantages, especially the rapid isolation of reaction intermediates. Consequently, only very simple equipment is required for SPS, e.g. common polypropylene fritted syringe used as the reaction/isolation vessel.
Polypropylene fritted syringe as the reaction vessel for SPS
Due to the comfortable handling with number of syringes at the same time and possible simple semi-automation using cheap and readily available instrumentation (so called Domino blocks), SPS enables parallel synthesis and quick access to compounds collection (chemical libraries) for biological screening. In this regard, our sythetic methodologies have been using only common coupling agents and conditions and readily available building blocks to extensively diversify the target compounds.