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. Author manuscript; available in PMC: 2019 Aug 7.
Published in final edited form as: Bioorg Med Chem. 2018 Jun 18;26(14):3925–3938. doi: 10.1016/j.bmc.2018.06.013

Scheme 1.

Scheme 1.

Reagents and conditions: (a) malonic acid, piperidine, pyridine, reflux; (b) trimethylacety 1 chloride, Et3N, THF, 0 ºC; (c) n-BuLi, THF, −78 C; (d) Boc2O, DMAP, Et3N, CH2Cl2, −15 C; (e) Trifluoroacetic acid, CH2Cl2, rt; (f) Fe, NH4Cl, EtOH/H2O, 40–50 C; (g) Ac2O, Et3N, CH2Cl2, rt.