626-00-6Relevant academic research and scientific papers
NEW COMPOUND
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Paragraph 0316; 0326, (2019/11/26)
PROBLEM TO BE SOLVED: To provide a new compound that does not have structural similarity to ceramide and has excellent CERT inhibitory activity. SOLUTION: The present invention provides a new compound of structural formula (I). A bond group -X- is cis-cyclopropyl-, R1, R2, R3, R4, and R5 independently represent a hydrogen atom, a halogen atom, a linear or branched C1-C8 alkyl group that may have a halogen atom, or OR6. SELECTED DRAWING: Figure 1 COPYRIGHT: (C)2020,JPOandINPIT
A simple and efficient two-step synthesis of 1,2,3-triiodoarenes via consecutive C-H iodination/ipso-Iododecarboxylation strategy: A potential application towards Ortho-diiodoarenes by Regioselective metal-iodine exchange reaction
Al-Zoubi, Raed M.,Al-Mughaid, Hussein,McDonald, Robert
, p. 912 - 918 (2015/06/25)
A general, robust, and efficient method for the conversion of benzoic acids to 1,2,3-triiodoarenes and 1,2,3-trihaloarenes via a two-step synthesis is reported. Commercially available benzoic acids were used that can allow the reactions to be performed on multi-gram scales with good-to-excellent yields. This report discloses a practical method for the synthesis of 1,2,3-triiodoarenes and 1,2,3-trihaloarenes that is general in scope, scalable, and easy to workup and purify. A potential application of the target compounds as precursors for novel regioselective metal-iodine exchange reaction of 1,2,3-triiodoarenes was also demonstrated. It provided ortho-diiodoaryl derivatives in a high regioselective fashion that are useful intermediates in synthesis and indeed are hard to synthesize by any other means.
Photo-induced Metal-Catalyst-Free Aromatic Finkelstein Reaction
Li, Lu,Liu, Wenbo,Zeng, Huiying,Mu, Xiaoyue,Cosa, Gonzalo,Mi, Zetian,Li, Chao-Jun
supporting information, p. 8328 - 8331 (2015/07/15)
The facile iodination of aromatic compounds under mild conditions is a great challenge for both organic and medicinal chemistry. Particularly, the synthesis of functionalized aryl iodides by light has long been considered impossible due to their photo-lability, which actually makes aryl iodides popular starting materials in many photo-substitution reactions. Herein, a photo-induced halogen exchange in aryl or vinyl halides has been discovered for the first time. A broad scope of aryl iodides can be prepared in high yields at room temperature under exceptionally mild conditions without any metal or photo-redox catalysts. The presence of a catalytic amount of elemental iodine could promote the reaction significantly.
Tetraflic acid (1,1,2,2-Tetrafluoroethanesulfonic acid, HC 2F4SO3H) and gallium tetraflate as effective catalysts in organic synthesis
Prakash, G. K. Surya,Mathew, Thomas,Panja, Chiradeep,Kulkarni, Aditya,Olah, George A.,Harmer, Mark A.
, p. 2163 - 2171 (2012/11/07)
Tetraflic acid offers ample acidity for various organic reactions that require high acidity. Its gallium(III) salt is an efficient catalyst under mild condtions for synthetic transformations such as the ketonic Strecker reaction for the synthesis of fluorinated α-amino nitriles and condensation- cyclzation reactions using suitable fluoro ketones and 1,2-disubstituted benzenes for the direct preparation of 5-membered or 6-membered fluorinated heterocycles. Copyright
Synthesis and biological evaluation of 3-aryltyramines as fragments binding to BACE-1 and BACE-2
Fehler, Stefanie K.,Pratsch, Gerald,Huber, Walter,Gast, Alain,Hochstrasser, Remo,Hennig, Michael,Heinrich, Markus R.
supporting information; experimental part, p. 2189 - 2194 (2012/05/20)
3-Aryltyramines were prepared in one single step from tyramine and various arenediazonium salts by radical arylation. Binding as well as enzyme inhibition data of the 14 compounds do not prove true interaction with BACE-1. In contrast, with BACE-2 inhibition and binding could be confirmed indicating that 3-aryltyramines are potential starting points for a drug discovery effort.
PROCESS FOR PREPARING IODINATED AROMATIC COMPOUNDS
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Page/Page column 5, (2011/10/13)
The present invention relates to a process for preparing iodinated aromatic compounds. Particularly, the present invention comprises the step of performing the iodination of a non-halogenated aromatic compound, a monoiodo aromatic compound, a diiodo aromatic compound, and iodine in the presence of a zeolite catalyst under oxygen atmosphere. In the process for preparing iodinated aromatic compounds according to the present invention, an iodination and an iodine conversion simultaneously occur, and then prevent side-reactions. Also, the lifetime of an iodination catalyst used therein can be extended by controlling the reaction temperature stably. Therefore, the process can be used for mass production of diiodo compound.
Metal-free efficient, general and facile iododecarboxylation method with biodegradable co-products
Kulbitski, Kseniya,Nisnevich, Gennady,Gandelman, Mark
supporting information; experimental part, p. 1438 - 1442 (2011/07/30)
The development of a novel, efficient and robust method for the general conversion of aliphatic and aromatic carboxylic acids to organic iodides without the use of heavy metals or strong oxidizing agents is reported. Commercially available N-iodoamides were used for both initiation and halogen donation under irradiative conditions. Isolation of the product is extremely simple and the major co-product is removed as a water-soluble biodegradable material. Copyright
PROCESS FOR THE PREPARATION OF IODIDES
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Page/Page column 35, (2012/01/05)
This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
PROCESS FOR PREPARING AROMATIC IODINE COMPOUNDS
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Page/Page column 7-8, (2011/10/19)
The present invention relates to a process for preparing iodinated aromatic compounds. Particularly, the present invention comprises the step of performing the iodination of a non-halogenated aromatic compound, a monoiodo aromatic compound, a diiodo aromatic compound, and iodine in the presence of a zeolite catalyst under oxygen atmosphere. In the process for preparing iodinated aromatic compounds according to the present invention, an iodination and an iodine conversion simultaneously occur, and then prevent side-reactions. Also, the lifetime of an iodination catalyst used therein can be extended by controlling the reaction temperature stably. Therefore, the process can be used for mass production of diiodo compound.
MANUFACTURING PROCESS FOR IODINATED AROMATIC COMPOUNDS
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Page/Page column 3, (2010/08/07)
Disclosed is a method for preparing an iodinated aromatic compound. More specifically, disclosed is a method of preparing an iodinated aromatic compound by iodinating an aromatic compound in the presence of oxygen over a zeolite catalyst, in which the aromatic compound and its monoiodo compound, as raw materials, are allowed to react with iodine. In comparison with a method in which only the aromatic compound is used as a raw material without adding the monoiodo compound, the disclosed method can increase the productivity of diiodo compounds and the selectivity to a p-diiodo compound and, at the same time, suppress side reactions, thus lengthening the life span of the catalyst.
