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Synthesis of analogues for SAR studies around the lead scaffold. Reagents and conditions: a) R3CHO, NH4OAc, EtOH, 90 °C, 26–86 %, d.r. 2:1–>20:1; b) NiCl2⋅6 H2O, NaBH4, MeOH, 0 °C; c) Boc2O, 39–91 % (2 steps); d) 4, [Pd2(dba)3], Xantphos, Cs2CO3, 1,4‐dioxane, 100 °C, 2–75 %; e) 4, K3PO4, CuI, (±)‐trans‐1,2‐diaminocyclohexane, 1,4‐dioxane, 97 °C, 7–65 %; f) HCl/dioxane, 96 %; g) R2Cl, TEA, CH2Cl2 or RNCO, CH2Cl2, 12–60 %. Boc=tert‐butyloxycarbonyl, TFA=trifluoroacetic acid.
