A method of preparing a Kahalalide F

The present invention relates to a method of preparing Kahalide F, said method comprising the 2-CTC resin as the carrier, using solid phase peptide synthesis method for the synthesis of polypeptide fragments A and B, then B polypeptide fragments intramolecular esterification synthesis fragment Bi, and the polypeptide fragments A and Bi liquid phase condensation, deprotection to give Kahalide F. The method of the present invention, high yield and convenient workup, provides a new way for the industrial-scale production Kahalide F.