A simple and general procedure for preparation of various phosphotyros
ine mimetics from the corresponding phenolic precursors is described.
In situ silylation of phenol acids followed by treatment with Et(3)N/C
Br4/HP(O)(OEt)(2) provides diethyl phosphate intermediates (36-96%), w
hich can be cleanly deprotected in quantitative yields upon treatment
with BSTFA/TMSI to afford novel phosphotyrosine mimetics. Copyright (C
) 1996 Elsevier Science Ltd.