Method for preparing FMOC-based hydrolysable linkers

摘要

Disclosed herein is a method of preparing a compound of formula 1, wherein PG is a protecting group and at least one of positions 1-8 is bound a N-maleimidyl-moiety having a structure as depicted by Y, wherein further substituents are as defined within the specification; said method comprises the step of reacting the 9-hydroxymethyl group of a compound as depicted by formula 2, wherein at least one of the positions 1-8 is bound to an amine, with a protecting group reagent introducing PG, and subsequently reacting said compound with an N-maleimidyl reagent to form the compound of formula (I).