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Synfacts 2011(6): 0583-0583  
DOI: 10.1055/s-0030-1259890
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a CXCR3 Antagonist

Contributor(s): Philip Kocienski
J. Chan*, B. J. Burke*, K. Baucom, K. Hansen, M. M. Bio, E. DiVirgilio, M. Faul, J. Murry
Amgen Inc., Thousand Oaks and Cambridge, USA
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Publication History

Publication Date:
19 May 2011 (online)

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Significance

The target molecule is a CXCR3 chemokine receptor antagonist that inhibits T-cell migration. It is a lead for the treatment of auto­immune diseases, such as psoriasis, rheumatoid arthritis and multiple sclerosis. Two syntheses of the target molecule are described. In the synthesis depicted, the single stereogenic center is derived from commercially available Boc-d-alanine B.