中央研究院智財技轉處對外服務網

Chemical synthesis of peptides and proteins is a widely studied field, and methods have been developed for the syntheses of such compounds using sequential coupling reactions, particularly involving anchoring on solid phases such as polymers. However, sequential synthetic methods are not well suited for the preparation of larger peptides and proteins. For these, segment coupling methods have been developed whereby shorter peptides are joined in a controlled manner to produce larger molecules. The invention relates to a method for forming a peptide bond between a peptide comprising a C-terminal carboxyl thioester and a sidechain-glycosyl peptide with a free N-terminal amino group wherein the sidechain-glycosyl includes a thiol group, comprising contacting the two reagents in an aqueous medium to form the coupled product via an intramolecular S to N shift of a acyl group from a thioester formed by a step of transthioesterification.