Scheme 3. Synthetic scheme for the synthesis of covalent-allosteric inhibitor derivatives by assembling building blocks with Leuckart–Wallach-reaction. (i) Amine, formic acid, MeCN, 80 °C, ovn. (ii) 4 N HCl/1,4-dioxane, rt, 2 h. (iii) Acryloyl chloride, DIPEA, THF, rt, 3 h. (iv) Fe, NH₄Cl, MeOH/H₂O, 80 °C, 2 h.