302840-67-1Relevant 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 10; 20, (2010/11/28)
Disclosed is an improved 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
Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
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Page/Page column 15, (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
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
A practical synthesis of highly functionalized fused 1,6-dihydroimidazo-[1, 2-a]imidazole-2,5-diones, key intermediates for LFA-1 inhibitors
Wang, Xiao-Jun,Xu, Yibo,Zhang, Li,Krishnamurthy, Dhileepkumar,Nummy, Laurence,Farina, Vittorio,Senanayake, Chris H.
, p. 2800 - 2802 (2007/10/03)
An alternative and chromatography-free approach for synthesis of a new class of LFA-1 inhibitors was developed. A key feature of this process involved a transformation of thioureas 14 to acyclic guanidine derivatives 9 followed by intramolecular cyclizati
Practical synthesis of a cell adhesion inhibitor by self-regeneration of stereocenters
Yee, Nathan K.,Nummy, Laurence J.,Frutos, Rogelio P.,Song, Jinhua J.,Napolitano, Elio,Byrne, Denis P.,Jones, Paul-James,Farina, Vittorio
, p. 3495 - 3501 (2007/10/03)
An efficient enantiospecific synthesis of the cell adhesion inhibitor BIRT-377 by self-regeneration of stereocenters has been achieved in 38% overall yield in eight steps. The key transformations involve the stereoselective formation of the trans imidazol
An improved synthesis of N-aryl-hydantoin LFA-1 antagonists via the enantiospecific alkylation of an isobutyraldehyde-derived imidazolidinone template
Frutos, Rogelio P.,Stehle, Sandra,Nummy, Laurence,Yee, Nathan
, p. 101 - 104 (2007/10/03)
An improved and cost-effective process for the synthesis of N-aryl-hydantoin LFA-1 antagonists is described. Key transformations include the synthesis and stereospecific alkylation of the trans-isobutyraldehyde-derived template 4, and the one-pot hydrolys
Self-regeneration of stereocenters: A practical enantiospecific synthesis of LFA-1 antagonist BIRT-377
Yee, Nathan K.
, p. 2781 - 2783 (2007/10/03)
An efficient enantiospecific synthesis of the LFA-1 antagonist BIRT-377 has been achieved in 43percent overall yield in eight steps. The key transformations involve the stereospecific formation of the trans imidazolidinone 7, subsequent alkylation, and th
