Patent ID: 8158590

Claim:
A method of producing a compound containing a reactive moiety and a cleavable therapeutic or diagnostic moiety, said method comprising reacting a first compound containing an azide-containing or acetylene-containing group, said first compound being of formula (V) or (VI), respectively: or a pharmaceutically acceptable salt thereof, with a second compound containing an acetylene group or azide group, respectively, said second compound also containing a reactive moiety (RM), in a single step under formation of a third compound containing a triazole and a reactive moiety, said third compound being of formula (III) or (IV), respectively: or a pharmaceutically acceptable salt thereof, wherein each L 2 is independently either a bond or a linking group linking RM to one or more triazole groups; each L 1 is independently either a bond or a linking group linking the triazole, azido, or acetylene group to one or more V 1 and/or Y; each V 1 is a conditionally-cleavable moiety, optionally following prior conditional transformation, which can be cleaved or transformed by a chemical, photochemical, physical, biological, or enzymatic process, cleavage of V 1 ultimately leading to release of one or more Z moieties; each Y is independently absent or a self-eliminating spacer system which is comprised of one or more self-elimination spacers; each Z is a therapeutic or diagnostic moiety, and each Z is directly coupled to either Y or V 1 when Y is absent; q, r, and s are numbers representing degree of branching and are each independently a positive integer; z is an integer ≧1 and equal to or smaller than the total number of attachment sites for Z in the one or more V 1 —Y moieties; and each RM is independently a reactive moiety selected from wherein X 5 is selected from —Cl, —Br, —I, —F, —O—N-succinimide, —O-(4-nitrophenyl), —O-pentafluorophenyl, —O-tetrafluorophenyl, —O—C(O)—R 29 , and —O—C(O)—OR 29 ; wherein R 29 is branched or unbranched C 1 -C 10 alkyl or aryl; and X 6 is selected from —Cl, —Br, —I, —O-mesyl, —O-triflyl, and —O-tosyl.