281234-90-0Relevant articles and documents
Disubstituted 1-aryl-4-aminopiperidine library synthesis using computational drug design and high-throughput batch and flow technologies
Bryan, Marian C.,Hein, Christopher D.,Gao, Hua,Xia, Xiaoyang,Eastwood, Heather,Bruenner, Bernd A.,Louie, Steven W.,Doherty, Elizabeth M.
, p. 503 - 511 (2013/09/24)
A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member library of 1-aryl-4-aminopiperidine analogues for drug discovery screening. The application described herein demonstrates the advantages of computational library design coupled with a flexible, modular approach to library synthesis. The enabling technologies described can be readily adopted by the traditional medicinal chemist without extensive training and lengthy process development times.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 34, (2008/12/06)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
Remarkably selective palladium-catalyzed amination process: Rapid assembly of multiamino based structures
Hong, Yaping,Senanayake, Chris H.,Xiang, Tingjian,Vandenbossche, Charles P.,Tanoury, Gerald J.,Bakale, Roger P.,Wald, Stephen A.
, p. 3121 - 3124 (2007/10/03)
Palladium-catalyzed selective amination by a primary amine in the presence of a secondary amine provided up to >99:1 selectivity with high yields.