Enantioselective Transformations in the Synthesis of Therapeutic Agents

H Yang, H Yu, IA Stolarzewicz, W Tang - Chemical Reviews, 2023 - ACS Publications
The proportion of approved chiral drugs and drug candidates under medical studies has
surged dramatically over the past two decades. As a consequence, the efficient synthesis of …

Automation isn't automatic

M Christensen, LPE Yunker, P Shiri, T Zepel… - Chemical …, 2021 - pubs.rsc.org
Automation has become an increasingly popular tool for synthetic chemists over the past
decade. Recent advances in robotics and computer science have led to the emergence of …

Data-science driven autonomous process optimization

M Christensen, LPE Yunker, F Adedeji… - Communications …, 2021 - nature.com
Autonomous process optimization involves the human intervention-free exploration of a
range process parameters to improve responses such as product yield and selectivity …

Catalytic homogeneous asymmetric hydrogenation: successes and opportunities

CSG Seo, RH Morris - Organometallics, 2018 - ACS Publications
This is an overview of successes in the realm of catalytic homogeneous asymmetric
hydrogenation of substrates primarily of interest in the synthesis of pharmaceuticals in order …

Recent advances in asymmetric hydrogenation of tetrasubstituted olefins

S Kraft, K Ryan, RB Kargbo - Journal of the American Chemical …, 2017 - ACS Publications
The asymmetric hydrogenation of tetrasubstituted olefins provides direct access to very
useful biological molecules and intermediates. The development of the technology has been …

Stereoconvergent and-divergent synthesis of tetrasubstituted alkenes by nickel-catalyzed cross-couplings

D Zell, C Kingston, J Jermaks, SR Smith… - Journal of the …, 2021 - ACS Publications
We report the development of a method to diastereoselectively access tetrasubstituted
alkenes via nickel-catalyzed Suzuki–Miyaura cross-couplings of enol tosylates and boronic …

Catalytic reductive aldol and mannich reactions of enone, acrylate, and vinyl heteroaromatic pronucleophiles

CC Meyer, E Ortiz, MJ Krische - Chemical reviews, 2020 - ACS Publications
Catalytic reductive coupling of enone, acrylate, or vinyl heteroaromatic pronucleophiles with
carbonyl or imine partners offers an alternative to base-mediated enolization in aldol-and …

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole …

T Cernak, NJ Gesmundo, K Dykstra, Y Yu… - Journal of Medicinal …, 2017 - ACS Publications
Miniaturization and parallel processing play an important role in the evolution of many
technologies. We demonstrate the application of miniaturized high-throughput …

Highly stereoselective synthesis of tetrasubstituted acyclic all-carbon olefins via enol tosylation and Suzuki–Miyaura coupling

BX Li, DN Le, KA Mack, A McClory… - Journal of the …, 2017 - ACS Publications
A highly stereocontrolled synthesis of tetrasubstituted acyclic all-carbon olefins has been
developed via a stereoselective enolization and tosylate formation, followed by a palladium …

The Catalysis Laboratory at Merck: 20 Years of Catalyzing Innovation

RT Ruck, NA Strotman, SW Krska - ACS Catalysis, 2022 - ACS Publications
The Catalysis Laboratory at Merck was established in 2002 to discover and develop
asymmetric hydrogenation transformations for application to the company's pipeline. Twenty …