Process research and scale-up for the pilot plant synthesis will be described. Key transformations are the establishment of the first asymmetric center by a Ru-catalyzed asymmetric transfer hydrogenation process, the enantioselective Overman rearrangement and finally setting the second asymmetric center by a diastereoselective hydrogenation reaction. Figure 1. <img src='https://acs-archive-assets2.s3.amazonaws.com/240nm/uploads/42279_abstract.jpg' alt='' />

Chemical development of an asymmetric synthesis of a glycine transporter 1 inhibitor involving an enantioselective Overman rearrangement

244th National Meeting (2012)

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