An Atom-Economical Method to Prepare Enantiopure Benzodiazepines with N-Carboxyanhydrides

Patrick Fier and Aaron Whittaker describe an atom-economical way to prepare enantiopure benzodiazepines with NCAs.

The benzodiazepine scaffold can be found in many marketed drugs, such as Valium, Xanax, and Klonopin. Importantly, benzodiazepines are finding resurgence in medicinal chemistry with new indications such as anticancer therapeutics. As part of a Merck drug development program, Dr. Patrick Fier and Dr. Aaron Whittaker from Merck & Co. (Rahway, USA) were tasked with developing an efficient synthesis of a benzodiazepine-based molecule. They developed an atom-economical method to synthesize enantiopure benzodiazepines with N-carboxyanhydrides (NCAs).

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