76075-21-3Relevant articles and documents
N-cyclopropyl methoxy imidazole amide derivative and application thereof in antitumor drugs
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Paragraph 0012; 0018-0021, (2021/10/27)
The invention belongs to the technical field of medicinal chemistry, and particularly relates to N-cyclopropyl methoxy imidazole amide derivatives, a preparation method and application of the N-cyclopropyl methoxy imidazole amide derivatives as an MEK inhibitor in antitumor drugs. The invention provides an N-cyclopropyl methoxy imidazole amide derivative as shown in a general formula, and geometric isomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the N-cyclopropyl methoxy imidazole amide derivative. The MEK inhibitor provided by the invention has specificity and effectiveness, and has a wider development prospect. Experimental results show that the N-cyclopropyl methoxy imidazole amide derivative synthesized by the research group has a prospect of developing targeted antitumor drugs.
Phenylethyl imidazole derivative and application thereof
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Paragraph 0081-0083, (2020/10/21)
The invention belongs to the technical field of medicines, and provides a novel phenylimidazole amide derivative shown as a general formula (I) (See the specification) and a geometrical isomer or pharmaceutically acceptable salt, hydrate, solvate and prodrug thereof, and preparation methods thereof. The compound can activate the activity of TGR5 and can be used for treating or preventing diseasesrelated to TGR5 activity regulation.
Preparation of 2'-13c-l-histidine starting from 13c-thiocyanate: Synthetic access to any site-directed stable isotope enriched l-histidine
Talab, Sarra,Taha, Kamal Khalifa,Lugtenburg, Johan
, p. 1023 - 1033 (2014/02/14)
1-Benzyl-2-(methylthio)-imidazole-5-ketone is obtained in a few simple steps starting from thiocyanate and glycine amide (glycin). Subsequent treatment with diethyl phosphorocyanidate and functional group manipulations gives 1-benzyl-5-chloromethylimidazolium chloride. This compound is converted under mild O'Donnell conditions into the corresponding L-histidine derivative. After deprotection L-histidine is obtained in good yield and 99% enantiomeric excess. 2'-13C-L-Histidine has been obtained via this new scheme with high (99%) 13C incorporation starting with commercially available 13C- thiocyanate. This synthetic scheme allows access to any isotopomer of L-histidine and many other biologically important imidazole derivatives.