In the course of drug discovery programs it is common practice to iteratively install elemnets of diversity onto common scaffolds in order to establish structure actuvuty relationships (SAR). It would be highly advantageous to interrogate multiple vectors of target ligand interactions in a single parallel synthesis protocol. This approach requires orthoganol chemistries that can tolerate a diverse set of reaction conditions and ideally utilize building blocks that are readily available with the diversity required to develop meaningful and dynamic SAR. MIDA boronates hold great promise in this realm, their reagent tolerance, ease of preparation and ability to participate in slow-release cross couplings provide an excellent starting point from which to develop a platform of reactions that are capable of automated multi-dimensional analog synthesis. Herein we report a series of reaction that, taken together, begin to realize the potential of MIDA boronates in this context.

MIDA boronates for medicinal chemistry: A case study in methodology development for parallel synthesis

244th National Meeting (2012)

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