The first total synthesis of the novel β-adrenergic receptor antagonist MY336-a 1 and its epimer 2 has been achieved from 2,3-dimethoxytoluene, by Jackson cyclisation of Nbenzyl-N-tosylamido acetals, Lewis acid-mediated addition of silicon-based nucleophiles to p-tosyliminium ions and base-catalysed epimerisation of 1-substituted hydroxytetrahydroisoquinolines, being key steps.
T. S. Kaufman, J. Chem. Soc., Perkin Trans. 1, 1996, 2497 DOI: 10.1039/P19960002497
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