TRIMERIC CONJUGATES OF PEPTIDIC DERIVATIVE

摘要

The invention provides a process for forming a compound having the formula (I): from chemical entities native [A], native [B] and native [C], where native [A] has a thioester group, native [B] had a 1-amino-2-thiol group with an unoxidised sulfhydryl side chain, and native [C] had a thiol reactive function (TRF) group, wherein chemical entities [A], [B] and [C] are covalently linked by linker group L, comprising the steps of: (i) admixing native [A] and native [B] in a reaction solution; (ii) condensing the unoxidised sulfydryl side chain of native [B] with the thioester group of native [A] for producing a first intermediate compound wherein [A] and [B] are linked with a beta-aminothioester bond; (iii) rearranging the beta-aminothioester bond for producing a second intermediate compound wherein [A] and [B] are linked with an amide bond having attached thereto a free thiol group; (iv) admixing native [C] with the second intermediate compound in a reaction solution; and (v) reacting the thiol reactive function (TRF) group of native [C] with the free thiol group of the second intermediate compound for producing a compound having the formula (I).