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......
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......
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......
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......
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......
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......
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 ......
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......
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......
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......
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......
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......
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......
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......
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......