K

Karl Welzenbach

Novartis (Switzerland)

Publishes on Cell Adhesion Molecules Research, Monoclonal and Polyclonal Antibodies Research, Immune Response and Inflammation. 34 papers and 2.3k citations.

34Publications
2.3kTotal Citations

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Top publicationsby citations

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
Rainer Albert, Klaus Hinterding, Volker Brinkmann et al.|Journal of Medicinal Chemistry|2005
Cited by 150Open Access

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.