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Selective thionation of the lactam C\uf8feO of19using Lawesson\u2019s reagent failed (see the Supporting Information)."},{"key":"e_1_2_2_39_2","unstructured":"Debenzylation of21under H2in the presence of Pd\/C and HCl\/MeOH led to pyrazinone reduction and attempts at oxidative debenzylation with ceric ammonium nitrate (CAN) in MeCN\/H2O caused degradation."},{"key":"e_1_2_2_40_2","unstructured":"Initial pharmacological evaluation of the ligands reported here has focused on the ring\u2010extended isoquinolone3 as the first annulated cytisine and because of its structural relationship to varenicline. Using a whole\u2010brain (heteromeric) assay with 200\u2005pM[3H]epibatidine racemic isoquinolone3was a potent ligand with an IC50of 85\u2005nM(cf. (\u2212)\u2010cytisine 7.7\u2005nM; A. Kennett S. Wonnacott C. Hirschh\u00e4user C.\u2005A. Haseler T. Gallagher unpublished results). 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