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Defining the Qualities of High-Quality Palladium on Carbon Catalysts for Hydrogenolysis

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (7)

Palladium-catalyzed hydrogenolysis is often the final step in challenging natural product total syntheses and a key step in industrial processes produ......

Development of a Robust Scale-Up Synthetic Route for BPR1K871: A Clinical Candidate for the Treatment of Acute Myeloid Leukemia and Solid Tumors

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (4)

Herein, a robust and scalable procedure for the synthesis of multikinase inhibitor BPR1K871 (1, a quinazoline compound bearing a substituted thiazolin......

Practical and Scalable Manufacturing Process for a Novel Dual-Acting Serotonergic Antidepressant Vilazodone

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (5)

Vilazodone combines the effects of a selective serotonin reuptake inhibitor with the 5-HT1A receptor partial agonist activity. Here, we report the dev......

Development and Scale-Up of an Improved Manufacturing Route to the ATR Inhibitor Ceralasertib

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (1)

Ceralasertib is currently being evaluated in multiple phase I/II clinical trials for the treatment of cancer. Its structure, comprising a pyrimidine c......

Understanding and Controlling the Formation of an N-Alkyl Impurity in Olmesartan Medoxomil: A Derivative via Michael-Type Addition between Tetrazole and Mesityl Oxide In Situ Generated from Acetone

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (5)

An unknown impurity was detected in olmesartan medoxomil active pharmaceutical ingredient (API), which was determined as 2-methyl-4-oxopentan-2-yl-pro......

Research on the Risk of Thermal Runaway in the Industrial Process of Styrene Solution Polymerization

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (6)

Polymerization reactions are exothermic processes that are often accompanied by viscosity changes, and they can pose hazards due to thermal runaway. T......

Development and Proof of Concept for a Large-Scale Photoredox Additive-Free Minisci Reaction

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (1)

New route development activities toward ceralasertib (AZD6738) have resulted in the discovery of an efficient, acid additive-free, photoredox Minisci ......

Progress and Opportunities for Utilizing Seeding Techniques in Crystallization Processes

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (7)

Seeding is a significant but challenging task for optimizing crystallization process operation, product quality, and process efficiency. With the deve......

Selective Oxidation of Benzylic sp(3) C-H Bonds using Molecular Oxygen in a Continuous-Flow Microreactor

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (7)

Selective aerobic oxidation of benzylic sp(3) C-H bonds to generate the corresponding ketones was achieved under continuous-flow conditions. The catal......

Highly Efficient and Practical Synthesis of the Key Intermediate of Telmisartan

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (4)

We reported herein an efficient and practical method to access 1,7'-dimethyl-2'- propyl-2,5'-bi(1H-benzimidazole) 1, a key intermediate for the synthe......

Application of Continuous Flow in Tazobactam Synthesis

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (7)

Tazobactam is a beta-lactamase inhibitor. In this work, a combination of continuous flow and batch experiments for the synthesis of tazobactam has bee......

Development of a Synthesis Process for a Novel HCV NS5A Inhibitor, Emitasvir

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (4)

A new approach to the synthesis of Emitasvir (DAG181), a small molecule hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor, is describe......

Safe Scale-Up of an N-Bromosuccinimide Involved Bromination Reaction

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (6)

Y A hazardous side reaction between N-bromosuccinimide (NBS) and 2-methyltetrahydrofuran (2-MeTHF) was identified during the thermal safety analysis t......

Development of a Robust and Scalable Process for the Large-Scale Preparation of Vadadustat

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (4)

A novel and scalable process is developed for the industrial synthesis of vadadustat. The four-step process is one step shorter compared to the report......

Three-Step One-Pot Process of 3-Methyl-5-Benzofuranol from Amine, Aldehydes, and p-Benzoquinone

期刊: ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2021; 25 (4)

3-Methyl-5-benzofuranol was prepared by a one-pot process from morpholine, propionaldehyde, and p-benzoquinone in 85-87% isolated yields. Avoiding the......

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