847672-62-2Relevant academic research and scientific papers
AMINOPROPANOL DERIVATIVES
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Page/Page column 11, (2008/06/13)
Compounds of formula (I): wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer
Albert, Rainer,Hinterding, Klaus,Brinkmann, Volker,Guerini, Danilo,Müller-Hartwieg, Constanze,Knecht, Helmut,Simeon, Corinne,Streiff, Markus,Wagner, Trixie,Weizenbach, Karl,Zécri, Frédéric,Zollinger, Markus,Cooke, Nigel,Francotte, Eric
, p. 5373 - 5377 (2007/10/03)
In vivo phosphorylation of FTY720 (1) in rats and humans resulted exclusively in the biologically active (S)-configured enantiomer, which was proven by an ex vivo o-phthaldialdehyde derivatization protocol especially elaborated for phosphates of 1. Starting from the prochiral amino alcohol 1, racemic and enantiomerically pure phosphates of 1 were synthesized. Pure enantiomers were obtained after purification of a partially protected key intermediate on an enantioselective support. The absolute stereochemistry was determined by X-ray diffraction.
