A new synthesis of the highly efficient, selective dopamine D2 agonist, 2-fluoro-N-propylnorapomorphine 1 has been accomplished, involving the transformation of thebaine 13 into 6-fluoro-6-demethoxythebaine 10, followed by sequential N-demethylation, N-alkylation, rearrangement with methanesulfonic acid into the apocodeine derivative 17, and subsequent O-demethylation with boron tribromide.
S. Berényi, S. Hosztafi and S. Makleit, J. Chem. Soc., Perkin Trans. 1, 1992, 2693 DOI: 10.1039/P19920002693
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