A rapid method is reported for the preparation of biotinylated 4-amino-D-phenylalanine (D- Aph) with Fmoc as the protecting group at the α-amino. Different coupling reagents and conditions were studied to get the biotinylated compound. Coupling reagents like 1-[bis (dimethylamino) methylene]-1H-benzotriazolium 3-oxide hexafluorophosphate and BOP were found to be very efficient. Biotinylated Boc-L-Aph and biotinylated Fmoc-L-lysine ...