321656-73-9Relevant academic research and scientific papers
Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
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Page/Page column 16, (2008/06/13)
Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a res
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a] IMIDAZOLE-3-SULFONIC ACID
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Page/Page column 16-17, (2008/06/13)
Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
Development of a scalable process for 1-(3,5-dichlorophenyl)-5-iodo-3- methyl-(4-methylbenzyl)-1H-imidazo[1,2-a]imidazol-2-one: A key intermediate for the synthesis of LFA-1 inhibitors
Frutos, Rogelio P.,Eriksson, Magnus,Wang, Xiao-Jun,Byrne, Denis,Varsolona, Richard,Johnson, Michael D.,Nummy, Lawrence,Krishnamurthy, Dhileepkumar,Senanayake, Chris H.
, p. 137 - 140 (2012/12/24)
A safe, robust, chromatography-free and reproducible process for the multi-kilogram synthesis of vinyl iodide 2, a key intermediate for the synthesis of LFA-1 inhibitors, was developed and implemented at the pilot plant. Execution of the above process all
A practical synthesis of LFA-1 inhibitors utilizing CuCl-promoted intramolecular cyclization of thiohydantoins
Wang, Xiao-Jun,Zhang, Li,Xu, Yibo,Krishnamurthy, Dhileepkumar,Varsolona, Richard,Nummy, Laurence,Shen, Sherry,Frutos, Rogelio P.,Byrne, Denis,Chung,Farina, Vittorio,Senanayake, Chris H.
, p. 273 - 276 (2007/10/03)
An efficient and chromatography-free approach for synthesis of a new class of LFA-1 inhibitors was developed. A copper(I) chloride-promoted intramolecular cyclization of thiohydantoins 7a-b serves as a key step to highly functionalized bicyclic guanidines
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-α]imidazol-2-one derivatives
Wu, Jiang-Ping,Emeigh, Jonathan,Gao, Donghong A.,Goldberg, Daniel R.,Kuzmich, Daniel,Miao, Clara,Potocki, Ian,Qian, Kevin C.,Sorcek, Ronald J.,Jeanfavre, Deborah D.,Kishimoto, Kei,Mainolfi, Elizabeth A.,Nabozny Jr., Gerald,Peng, Charline,Reilly, Patricia,Rothlein, Robert,Sellati, Rosemarie H.,Woska Jr., Joseph R.,Chen, Shirlynn,Gunn, Jocelyn A.,O'Brien, Drane,Norris, Stephen H.,Kelly, Terence A.
, p. 5356 - 5366 (2007/10/03)
A novel class of lymphocyte function-associated antigen-1 (LFA-1) inhibitors is described. Discovered during the process to improve the physicochemical and metabolic properties of BIRT377 (1, Figure 1), a previously reported hydantoin-based LFA-1 inhibito
DERIVATIVES OF [6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-SULFONYLAMINO]-PROPIONAMIDE
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Page 13, (2008/06/13)
Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
Regiocontrolled synthesis of highly-functionalized fused imidazoles: A novel synthesis of second generation LFA-1 inhibitors
Frutos, Rogelio P.,Johnson, Michael
, p. 6509 - 6511 (2007/10/03)
A new and reliable route to a new class of LFA-1 inhibitors such as (2) has been developed. A key aspect of this route is the transformation of amino amide 5 into iodide 3 in four steps. Iodide 3 is a key advanced intermediate used in the synthesis of all
