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Aqueous Electrochemical Synthesis of 5-Trifluoromethyluracil in Batch and Continuous Flow

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; ()

Without the use of chemical oxidants and metal catalysts, an aqueous electrochemical synthesis of 5-trifluoromethyluracil in batch and continuous flow......

Ruthenium-Catalyzed Direct Asymmetric Reductive Amination for the Synthesis of a Chiral Primary Amine Intermediate En Route to a PDE2A Inhibitor, TAK-915

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (5)

Here, we report a novel, efficient ruthenium-catalyzed direct asymmetric reductive amination of an alpha-alkoxy ketone, a structural motif for which i......

Densely Packed Chemical Synthesis Equipment by 3D Spatial Design and Additive Manufacturing: Acetylene Generation Cartridge

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (6)

Preparation of and carrying out chemicalreactions often requireconsiderable laboratory space. Miniaturization of chemical equipmentand reducing labora......

Poly(dimethylsiloxane)-Based Recyclable Tablet Catalysts Bearing Gold N-Heterocyclic Carbene Complexes for Alkyne Hydration Reactions

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (7)

The tablet-based catalytic systems offer various advantagessuchas improved stability, ease of handling, and dosage delivery of transitionmetal catalys......

One-Pot Synthesis of Menthol from Citral over Ni/H-β-38 Extrudates Containing Bentonite Clay Binder in Batch and Continuous Reactors

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; ()

Optimization of bifunctional Ni catalysts was performed to enhance the catalytic performance in the one-pot synthesis of commercially valuable menthol......

Automated Image-Based Color Analysis as an Accessible and Widely Applicable PAT Tool

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (7)

Pharmaceutical R & D is increasingly employing data-drivenapproacheswith specialized process analytical technology (PAT) tools to developprocesses......

A Proposal That Would Ban Manufacture, Supply, and Use of All Fluoropolymers and Most Fluorinated Reagents within the Entire EU

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (8)

A change to EU law is proposed that would lead to a banon manufacture,supply, and use of most per- and polyfluorinated alkyl substance (PFAS)materials......

A Synthetic Review of Eliglustat, a Drug for Gaucher's Disease

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; ()

Gaucher's disease (GD) is a rare genetic disorder that falls under the category of lysosomal storage diseases (LSDs) and is caused by the defective pr......

Optimized Kilogram-Scale Synthesis and Impurity Identification of SHEN26 (ATV014) for Treating COVID-19

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; ()

SHEN26, a 5 '-cyclohexane-carboxylate prodrug of the nucleoside analog GS-441524, is a potent RdRp inhibitor currently undergoing phase III clinical t......

Scalable and Cost-Effective Synthetic Process for the Preparation of L-3,4-Dihydroxyphenylalanine-Levodopa

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 28 (1)

We reported the development of a novel synthetic process for Levodopa (1), which involves two simple chemical steps. The first step includes the react......

A Cobalt-Containing Polysilane as an Effective Solid-State Catalyst for the Hydrosilylation of Alkenes

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (7)

A cobalt-containing polysilane was readily obtained from the treatment of poly(monohydro)silane with Co2(CO)8 at 60 degrees C. The resulting polysilan......

Scalable Synthesis of CVN424, an Inverse Agonist of the GPR6 Receptor

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (2)

CVN424 is a drug candidate, which is being investigated in clinical trials for the treatment of motor fluctuations associated with Parkinson's disease......

Continuous Flow-Facilitated CB2 Agonist Synthesis, Part 1: Azidation and [3+2] Cycloaddition

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (4)

We report the use of continuous flow processing to enable the first two steps of a new route toward a cannabinoid receptor type 2 agonist, RG7774. Fir......

Formation of N-Nitrosamine Drug Substance Related Impurities in Medicines: A Regulatory Perspective on Risk Factors and Mitigation Strategies

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2023; 27 (10)

The detection of N-nitrosamine impuritiesin medicinesand the recent emergence of nitrosamine drug substance related impurities(NDSRIs) has posed a gre......

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