(Is)oxazole derivatives exerting ability to bind other molecules due to hydrogen or coordination bonds, weak interactions such as ion-dipole, cation-p, p-p stacking, van der Waals forces (resulting in hydrophobic effect) are considered as prime scaffold for medicinal, agricultural, supramolecular chemistry as well as materials sciences. The current trends in building blocks design for medicinal chemistry involve heterocycle decoration by low molecular weight aliphatic substituents, and such modification of (is)oxazole still remains the challenging task. The presentation will include published and unpublished results obtained in our company in the last 5 years directed to design and synthesis of MedChem relevant (is)oxazole based building blocks. For example as one of the case studies, the “biocore” concept (the concept refers to combination of (hetero)aliphatic and hydrophilic aromatic rings providing privileged structural motifs for drug discovery) applying to (is)oxazoles type <b>2</b> and <b>3 </b>will be discussed. The synthetic approaches elaborated leads to diverse (is)oxazoles based building blocks. Some of the examples are presented on Figure. The scope and limitation of approaches developed as well as scale up and cost-effectiveness issues will be analyzed.

Scalable synthesis of MedChem relevant (Is)oxazole based building blocks

2019 Fall National Meeting

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