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Boron sees the light- A visible light induced organocatalytic borylation of aryl chlorides

Aryl boronates are among the most widely used synthetic intermediates in the pharmaceutical and agrochemical industries, both in R&D and commercial manufacture.1 Historically these key building blocks have been made using transition metal (Pd, Cu, Ni) catalysed cross coupling reactions between an appropriate aryl halide (usually bromide,  iodide or activated chlorides) and an alkoyboron species.2 Efforts to

Reagent of the Month- 2,2,2-Trichloro-1,1-dimethyl chloroformate

Netarsudil- a ROCK kinase inhibitor marketed by Aerie pharmaceuticals as RhopressaTM– was recently approved by the FDA for ocular hypertension.1 An asymmetric synthesis is challenging due to the aryl group lowering the pKa of the α-hydrogen, rendering it very susceptible to racemization both during synthesis of the amino acid and subsequently amide coupling to an unreactive, poorly

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