Yuexian Li, Mihaela Plesescu, S. Prakash
Aug 1, 2006
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[14C]-N-(6-Chloro-7-methoxy-9H-pyrido [3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide (5B), an IKK inhibitor, was synthesized from [14C]-barium carbonate in two steps in an overall radiochemical yield of 41%. The intermediate, [carboxyl-14C]-2-methylnicotinic acid, was prepared by the lithiation and carbonation of 3-bromo-2-methylpyridine. [13C4,D3]-N-(6-chloro-7-methoxy-9H-pyrido [3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide (5C) was synthesized from [1,2,3,4-13C4]-ethyl acetoacetate and [D4]-methanol in six steps in an overall yield of 2%. [13C4]-2-methylnicotic acid, was prepared by condensation of [13C4]-ethyl 3-aminocrotonate and acrolein, followed by hydrolysis with lithium hydroxide. Copyright © 2006 John Wiley & Sons, Ltd.