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Synfacts 2010(9): 0980-0980  
DOI: 10.1055/s-0030-1257878
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of 5-Lipoxygenase Inhibitor MK-0633

Contributor(s): Philip Kocienski
F. Gosselin et al.*
Merck Frosst Center for Therapeutic Research, Kirkland, Canada and Merck Research Laboratories, Rahway, USA
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Publication History

Publication Date:
23 August 2010 (online)

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Significance

MK-0633 is an inhibitor of 5-lipoxygenase, a key enzyme in the cascade that transforms arachidonic acid to inflammatory leukotri­enes. A practical, chromatography-free synthesis of MK-0633 is described that features a late-stage cyclodehydration of the thiosemicarbazide I to generate the 1,3,4-oxadiazole ring.