Synthesis, optical resolution, absolute configuration, and preliminary pharmacology of (+)-and (-)-cis-2, 3, 3a, 4, 5, 9b-hexahydro-1-methyl-1H-pyrrolo [3, 2-h] …

W Glassco, J Suchocki, C George…

Index: Glassco; Suchocki; George; Martin; May Journal of Medicinal Chemistry, 1993 , vol. 36, # 22 p. 3381 - 3385

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Citation Number: 67

Abstract

Title compound, 8, has been synthesized from isoquinolinone, 1 (an improved preparation for which is presented) and separated into its antipodes with D-and L-di-p-toluoyltartaric acids. These antipodes and the racemic precursor have been evaluated (and found active) in two in vivo systems for their effects. The most potent of the three,(+)-8, has an EDm of 7.13 pmol/kg for inhibition of spontaneous activity and 7.45 pmol/kg for antinociception ...