Vibegron is a potent and selective beta-3 adrenergic receptor agonist and a drug candidate currently in clinical trials for the treatment of overactive bladder. In addition to the initial discovery chemistry route, two generations of asymmetric syntheses of vibegron are described in this presentation. The evolution of the two asymmetric routes suitable for the large scale preparation of vibegron is driven by the desire to develop a greener chemistry through the design of efficient chemical transformations / bond connections as well as process optimization. In comparison with the 1<sup>st</sup> generation route, the 2<sup>nd</sup> generation synthesis also reduces the manufacturing cost significantly.

Green by design for process evolution: Asymmetric syntheses of vibegron

251st National Meeting (2016)

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