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Synthesis of 14C- and 2H-labeled 1,3-dihydro-3,3-dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H-indol-2-one (LY195115), an orally effective positive inotrope

✍ Scribed by David W. Robertson; Joseph H. Krushinski; Don Kau

Publisher
John Wiley and Sons
Year
1986
Tongue
French
Weight
437 KB
Volume
23
Category
Article
ISSN
0022-2135

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✦ Synopsis

We have synthesized 14C-and 2H-labeled 1,3-dihydro-3,3dimethyl-5-(1,4,5,6-tetrahydro-6-oxo-3-pyridazinyl)-2H_-indol-2one (LY195115), an extremely potent, orally-effective cardiotonic with inotropic and vasodilator activities. '*C-label was introduced in the antepenultimate step by reaction of a B-chloroketone precursor with Na14CN; acid-catalyzed hydrolysis and cyclization with hydrazine provided the tetrahydropyridazinone bearing the "C-label in the 0x0-carbon. 1,3-Dihydro-3,3-di(methyl-d3)-2H-indol-2-one was prepared by exhaustive methylation of l-acetyl-l,3-dihydro-2~-indol-2-one with sodium hydride and iodomethane-dd, followed by removal of the nitrogen protecting group. This labeled material was converted in two steps to [2H6]-LY195115.

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