74409-42-0Relevant articles and documents
An industrialized method for preparing nitro mediums of proton pump inhibitors
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Paragraph 0018; 0022; 0025; 0027; 0029; 0031; 0033; 0049, (2022/01/07)
The present invention discloses an industrial method for preparing a proton pump inhibitor intermediate nitro group, belongs to the field of chemical synthesis technology, the method comprising preparing nitrogen oxides and preparing nitro groups; the preparation of nitrogen oxides, using pyridine derivatives as starting materials, reacting with oxidants under the action of a catalyst to generate nitrogen oxides; the preparation of nitro groups, after dissolving nitrogen oxides using organic solvents, using microchannel reaction technology, using fuming nitric acid as a nitrification reagent, nitrification reaction, The method of the present invention can reduce the generation of reaction impurities, shorten the reaction time, improve product quality, and greatly improve the continuity and safety of industrial production.
Synthesis and characterization of one impurity in esomeprazole, an antiulcerative drug
Liu, Zhen-Tao,Meng, Xia,Fang, Shi-Min,Wang, Li-Zhen,Wang, Zhen-Zheng,Yang, Geng,Duan, Hong-Dong,Hao, Ai-You
, p. 867 - 877 (2019/09/06)
During drug synthesis, control of impurities is very important to get high-qualified drugs. A number of studies have devoted to synthesize the impurities and study the structures to support the method of purification. In this paper, we first synthesize one impurity in esomeprazole, rel-2-[[(3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-6-methoxy-1H-benzimidazole, with readily available raw materials, simple operation procedures and relatively mild reaction. Besides, we characterized its structure by MS, IR, 1H-NMR and HPLC analyses. The purity of target compound is as high as 99.58%, which can be used as the reference substance of the impurities of esomeprazole.
A chemical chaperone-based drug candidate is effective in a mouse model of amyotrophic lateral sclerosis (ALS)
Getter, Tamar,Zaks, Ilana,Barhum, Yael,Ben-Zur, Tali,B?selt, Sebastian,Gregoire, Simpson,Viskind, Olga,Shani, Tom,Gottlieb, Hugo,Green, Omer,Shubely, Moran,Senderowitz, Hanoch,Israelson, Adrian,Kwon, Inchan,Petri, Susanne,Offen, Daniel,Gruzman, Arie
, p. 850 - 861 (2015/05/05)
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease characterized by the selective death of motor neurons and skeletal muscle atrophy. The majority of ALS cases are acquired spontaneously, with inherited disease accounting for only 10 % of all cases. Recent studies provide compelling evidence that aggregates of misfolded proteins underlie both types of ALS. Small molecules such as artificial chaperones can prevent or even reverse the aggregation of proteins associated with various human diseases. However, their very high active concentration (micromolar range) severely limits their utility as drugs. We synthesized several ester and amide derivatives of chemical chaperones. The lead compound 14, 3-((5-((4,6-dimethylpyridin-2-yl)methoxy)-5-oxopentanoyl)oxy)-N,N-dimethylpropan-1-amine oxide shows, in the micromolar concentration range, both neuronal and astrocyte protective effects in vitro; at daily doses of 10 mg kg-1 14 improved the neurological functions and delayed body weight loss in ALS mice. Members of this new chemical chaperone derivative class are strong candidates for the development of new drugs for ALS patients.
