This invention relates to the field of
peptide preparation technology, specifically to a preparation process for
terfenadine. The
terfenadine preparation process includes the following steps: (1) using resin as a
solid-phase carrier, Boc-Pip(Fmoc)-OH is loaded onto the resin to obtain Boc-Pip(Fmoc)-resin; (2) under the action of a condensing agent, Fmoc-D-Lys(Boc)-OH and Boc-D-Phe-D-Phe-D-Leu-OH are sequentially coupled onto the Boc-Pip(Fmoc)-resin to obtain
terfenadine peptide resin; (3) the terfenadine
peptide resin is lysed using a
lysis buffer, then concentrated, precipitated, and dried to obtain crude terfenadine. This invention's preparation process can effectively improve product purity while ensuring large-scale industrial production, and the steps are simple with a short reaction cycle.