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. Author manuscript; available in PMC: 2023 Sep 14.
Published in final edited form as: J Med Chem. 2021 Aug 20;64(17):12790–12807. doi: 10.1021/acs.jmedchem.1c00837

Scheme 1. General synthetic scheme.

Scheme 1.

Reagents and conditions: (i) KOAc, EtOH, 80 °C; (ii) POCl3, DMF, 80 °C; (iii) Malonic acid, piperidine, pyridine, 90 °C; (iv) method 1: NH2NH2.H2O, MeOH, 80 °C; method 2: NBSH, Et3N, THF, 45 °C; (v) method 1: CH3SO2NH2, CDI, DBU, DMF, 90 °C, method 2: CH3SO2NH2, DCC, DMAP, 0 – 45°C; (vi) NaBH4, MeOH, 25 °C; (vii) PPh3, DIAD, NaN3, H2SO4, DCM, 0 °C to 25 °C; (viii) PPh3, THF/H2O, 60 °C; (ix) CDI, methanesulfonamide, DIPEA, DCM, DCE or DMF depending on the solubility of the substrate, 25 °C – 90 °C.