Sustainability by design: Automated nanoscale 2,3,4-trisubstituted quinazoline diversity

Mojgan Hadian, Shabnam Shaabani, Pravin Patil, Svitlana V. Shishkina, Harry Böltz, Alexander Dömling*

*Bijbehorende auteur voor dit werk

OnderzoeksoutputAcademicpeer review

4 Citaten (Scopus)
21 Downloads (Pure)


Small molecule synthesis is equally important for materials and pharmaceuticals. However, the traditional approach performed in pharmaceutical R&D including maintenance of million-sized libraries and optimization synthesis of hundreds or even thousands of chemicals on a mmol or larger scale lacks sustainability. Here, we exemplify the synthetic execution of a newly designed quinoxaline reaction towards a transformative sustainability in chemistry. This includes nanoscale synthesis, deep chemical space exploration, scalability over 6 orders of magnitude from milligram up to 10-gram resynthesis of quinazolines enabled by the simultaneous variation of four classes of building blocks. Benefits of our approach include a simple to perform, one-step procedure, mild reaction conditions and access to a very large chemical space through accessing many available building blocks. More than thousand derivatives were produced in an automated fashion on a nanoscale using positive pressure facilitated dispensing. Along with these advantages, there is a considerable reduction in synthetic effort, reagents, solvent, glass and plastic consumables and power consumption to decrease the footprint of synthetic chemistry.
Originele taal-2English
Pagina's (van-tot)2459-2467
Aantal pagina's9
TijdschriftGreen Chemistry
Nummer van het tijdschrift8
StatusPublished - 21-apr-2020

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