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. 2023 Feb 20;28(4):1984. doi: 10.3390/molecules28041984

Scheme 1.

Scheme 1

(a) Meldrum´s acid, AcOH, i-PrOH/EtOAc, 75 °C, 3 h; (b) NaBH4, AcOH, DCM, 0 °C–r.t., 2.25 h; (c) Eschenmoser´s salt, MeOH, 70 °C, 18 h; (d) NaOH, 100 °C, 1 h, µw; (e) 1. SOCl2, DCM/DMF, 50 °C, 3 h, 2. t-Butyl-(2R)-2-piperidinecarboxylate 19, DIPEA, DCE/DMF, 90 °C, 1 h, µw; (f) Thioacetic acid, rt, 66 h; (g) TFA, DCM, 50 °C, o.n.; (h) NH3 (25%), H2O, 0 °C–rt, 2.5 h; and (i) BBr3, DCM, −78 °C–r.t., o.n.