Synthesis of Chiral Analogues of FTY720 and its Phosphate

Klaus Hinterding; Sylvain Cottens; Rainer Albert; Frederic Zecri; Peter Buehlmayer; Carsten Spanka; Volker Brinkmann; Peter Nussbaumer; Peter Ettmayer; Klemens Hoegenauer; Nathanael Gray; Shifeng Pan

doi:10.1055/s-2003-40883

PAPER

Synthesis of Chiral Analogues of FTY720 and its Phosphate

Klaus Hinterding*^a, Sylvain Cottens^a, Rainer Albert^a, Frederic Zecri^a, Peter Buehlmayer^a, Carsten Spanka^a, Volker Brinkmann^a, Peter Nussbaumer^b, Peter Ettmayer^b, Klemens Hoegenauer^b, Nathanael Gray^c, Shifeng Pan^c
^a Novartis Institutes for Biomedical Research, S507.409, 4002 Basel, Switzerland
Fax: +41(61)3246735; e-Mail: klaus.hinterding@pharma.novartis.com;
^b Novartis Forschungsinstitut GmbH, Brunner Str. 59, 1235 Wien, Austria
^c Novartis Institute for Functional Genomics Inc,, 10675 John Jay Hopkins Drive, San Diego CA 92121, USA

Abstract

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Abstract

Efficient and versatile protocols for the synthesis of chiral analogues of the novel immunomodulator FTY720 and its phosphate are described. These synthetic procedures allow for broad structural variation and deliver essential tools to further elucidate FTY720’s novel mechanism of action.

Key words

phosphates - sphingolipids - stereoselective synthesis - drugs - chiral auxiliaries

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References

These authors contributed equally to this study.

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