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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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