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Synthesis of carbon-14 labeled LTD4 antagonist MK-571

✍ Scribed by Dennis C. Dean; David G. Melillo; Robert L. Ellsworth

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
289 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

The synthesis of (E)-5-(3-(2-(7-~hloroquinolin-2-yl)ethenyl)-phen~l)-[5-~~C]-4,6-dith~anonane dicarboxylic acid N.Ndimethylamide (I1 4C]MK-571), a high-allinity LTD4 antagonist , from sodium [ l 4C]cyanide via a five step sequence is described. Condensation of 3-[14C]cyanobenzaldehyde with 7-chloroquinaldine followed by nitrile reduction provided the [ l 4C]aldehyde 2. The pivotal formation of the penultimate unsymmetrical dithioacetal intermediate was accomplished in a selective manner from aldehyde 2 by way of an 0trimethylsilyl hemiacetal intermediate. Subsequent ester hydrolysis afforded [14C]MK-571 in 14% overall radiochemical yield.

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