A series of 2,3,4,(5),6-substituted pyridines containing a hydroxyphosphinyl functionally have been prepared and were evaluated for their ability to inhibit the enzyme HMG-CoA reductase. Systematic substitution of both R1-R4 and X-Y led to compounds of type 3-6 with in vitro potency greater than that of mevinolin (Na salt).
Heterocyclic Nonionic X-Ray Contrast Agents. Part 3. The Synthesis of 5-(4-(Hydroxymethyl)-2-oxo-3-oxazolidinyl)-2,4,6-triiodo-1,3benzenedicarboxamide Derivatives.-As demonstrated for (VIa) the heterocycle in the title compounds (VI) is built up by phosgene treatment of the corresponding aniline derivative, phenylmercury catalyzed addition of glycidol (III) to the isocyanate and pyridine-catalyzed intramolecular N-alkylation followed by deprotection. The intramolecular N-alkylation is highly regioselective and is not accompanied by O-alkylation products. By the use of (S)-glycidol in the reaction sequence the optically active (VIa) is obtained. The new compounds are evaluated for their potential to serve as X-ray diagnostic agents. -(PILLAI, K. M. R.; DIAMANTIDIS, G.; DUNCAN, L.; RANGANATHAN, R. S.; J.
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