Process Research & Development at Merck & Co., Inc. encompasses a number of diverse research groups that seek to enable discovery chemistry (Discovery Process Chemistry), discover new & innovative technologies (Enabling Technologies), and/or develop the ideal process for a manufacturing route (Process Chemistry).  This presentation will exemplify my work while in the Discovery Process Chemistry group on the Soluble Guanylate Cyclase (sGC) program. Amino-pyrimidine lactams, accessed through coupling of malononitriles and amidines, represent a class of highly functionalized heterocycles of interest as sGC stimulators. One of the key bottlenecks in compound preparation was accessing highly functionalized malononitriles which had been historically prepared via a linear synthetic approach. In order to streamline compound synthesis, a more convergent, general and scalable approach to these intermediates was required. I will describe novel methods to obtain highly functionalized malononitriles, including a diastereoselective approach and subsequent manipulations as a convergent and adaptive approach to sGC stimulators.<br/>

Enabling medicinal chemistry as a process chemist

2019 Fall National Meeting

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