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. 2022 Aug 30;87(18):12041–12051. doi: 10.1021/acs.joc.2c01047

Scheme 1. Synthesis of Piperazinone Skeleton 4.

Scheme 1

Reagents and conditions: (i) dimethoxyacetaldehyde, H2, Pd/C 10%, MeOH, r.t., 16 h; (ii) Fmoc-Gly-OH, HATU, DIPEA, dry dimethylformamide (DMF), r.t., 16 h; (iii) TFA, TIPS, 1,2-DCE, r.t., 16 h; (iv) 5 M HCl solution in dioxane, reflux, 16 h.