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. 2014 Aug 11;5(10):1076–1081. doi: 10.1021/ml500238q

Scheme 1. Synthesis of 3-Cyano-3-aza-β-amino Acid Derivatives 2227.

Scheme 1

Reagents and conditions: (a) glyoxylic acid monohydrate, EtOH, RT; (b) (i) ClCO2i-Bu, NMM, THF, −25 °C; (ii) HNR2R3, THF, −25 °C to RT; (c) H2, Pd/C (10%), MeOH, 3.3 bar, RT; (d) BrCN, NaOAc, MeOH, RT.