71759-89-2Relevant articles and documents
Preparation method of 4-iodo-1H-imidazole
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Paragraph 0021-0026, (2020/04/17)
The invention provides a preparation method of 4-iodo-1H-imidazole. The preparation method comprises the following steps: (1) enabling imidazole, iodine and a cosolvent for promoting the solubility ofiodine in water to react under an alkaline condition in the presence of water as a solvent, after the reaction is finished, adjusting the pH value to 7-9, filtering out precipitated white solids, performing extraction, reduced pressure distillation to remove the solvent, and recrystallization on the filtrate to recover imidazole, concentrating the recrystallized mother liquor, and mixing the obtained white solids and the precipitated white solids to obtain a 4-iodo-1H-imidazole crude product, and (2) recrystallizing the 4-iodo-1H-imidazole crude product twice to obtain a white crystal 4-iodo-1H-imidazole pure product. The method has the advantages of simple process, high reaction yield, low production cost and recyclable raw materials.
Imidazo isoindole IDO1 inhibitor as well as preparation method and application thereof
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Paragraph 0085; 0086; 0089; 0090, (2018/01/11)
The invention belongs to the field of medicine, and particularly relates to an imidazo isoindole IDO1 compound with structural characteristics of the formula (I) shown in the description as well as a three-dimensional isomer or a pharmaceutically acceptable salt thereof, a preparation method thereof and application thereof as an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. An experiment result shows that the compound of the invention has a significant inhibition effect for the activity of IDO1, can effectively promote the proliferation of cells T, prevents initial cells T from being differentiated into adjustable cells T, can invert IDO1 mediating immunosuppression, can be used for treating relevant diseases with pathological features of an IDO1 mediating kynurenine metabolic way including cancers, virus infection, neurodegenerative diseases, cataracts, organ transplant rejection, depression, autoimmune diseases and the like.
Scope and Mechanistic Limitations of a Sonogashira Coupling Reaction on an Imidazole Backbone
Sandtorv, Alexander H.,Bj?rsvik, Hans-René
, p. 4658 - 4666 (2015/08/03)
A Sonogashira coupling reaction method to join terminal alkynes to the imidazole backbone was developed and investigated. The method exhibits good functional group tolerance and provides target 4-alkynylated imidazoles in 70-93% yield. The alkyne reagents were characterized by means of DFT calculations, from which electrostatic potential surfaces (EPS) were produced. A clear correlation between the EPS of the triple bond and the success of the coupling reaction was revealed. If the EPS is in range -94 to -105 kJmol-1 the coupling is successful. An unsuccessful class of reagents (alkynols) was made compatible by means of an auxiliary group (tert-butyldimethylsilyl). EPSs of these modified reagents then resembled those of the model and these auxiliary-assisted reagents then coupled successfully in excellent yields.
