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. Author manuscript; available in PMC: 2015 Aug 1.
Published in final edited form as: Medchemcomm. 2014 Apr 23;5(8):1036–1047. doi: 10.1039/C4MD00117F

Table 1.

Representative reductive amination handle installation conditions

means of handle attachment reducing agent solvent and conditions rxn time yield ref
aldehyde NaCNBH3 HOAc, r.t. 1 h 80% 11
aldehyde BH3-Et3N HCl/EtOH, 0°C 5 m 65% 16
ketone BH3- tBuNH2 HCl,/EtOH/ dioxane, 0 °C 2.5 h 69% 19
ketone NaCNBH3 HOAc/DCE/ MeOH, r.t. 90 m 88% 24
glycyl linker BH3-Me3N HCl/EtOH, 0 °C 5 h 85% 15