The more cost effective alternative to HATU and one of the most popular in situ activation reagents in solid and solution phase peptide synthesis that have high reactivity with simple reaction conditions, short reaction time and limit enantiomerization during fragment condensation and during DMAP catalyzed esterification of arginine derivatives 1,2,3,4. But lower yielding couplings can become problematic on industrial scales and with long peptides. HBTU activation has been adapted for automated stepwise solid-phase peptide synthesis for both t-butoxycarbonyl (Boc) and fluorenylmethoxycarbonyl(Fmoc) strategies 5. Also a convenient agent for the synthesis of tetramethylsulfonylguanidines in basic conditions 6.
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6. Tetrahedron Lett. 2006, 47, 6087