Suzuki–Miyaura Coupling of Aryl Nosylates with Diethanolamine Boronates
Philipp Kohler describes the Suzuki–Miyaura coupling of aryl nosylates and diethanolamine boronates.
The group of Dr. Philipp Kohler from Chemistry Process R&D at Idorsia Pharmaceuticals Ltd. (Allschwil, Switzerland) was inspired by a recent development project, in which they had to implement a Suzuki coupling of two heterocyclic entities: one with a phenolic functionality, the other featuring a boronate. Dr. Kohler explained that “in the discovery route, the building blocks were activated in the standard fashion: the phenol (Ar1) as the triflate, the other building block (Ar2) as the pinacol boronate, which was prepared through lithiation of the corresponding bromide and quenching with a suitable borylation reagent.” They were aiming to find derivatives that were prepared under ‘process-like’ conditions and purified by crystallization, identifying nosylate and diethanolamine (DABO) boronate as suitable, crystalline substrates.
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