The Petasis–Mannich reaction of allenylboronic acid with glyoxylic acid and (S)-1-phenylethylamine diastereoselectively leads to N-substituted propargylglycine of high optical purity in good yield. This product can be further subjected to… Click to show full abstract
The Petasis–Mannich reaction of allenylboronic acid with glyoxylic acid and (S)-1-phenylethylamine diastereoselectively leads to N-substituted propargylglycine of high optical purity in good yield. This product can be further subjected to esterification followed by bioconjugate synthesis using CuI-catalyzed alkyne–azide 1,3-dipolar cycloaddition reaction (‘click reaction’).
               
Click one of the above tabs to view related content.