Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

0:28

Synthesis of 4-[5-(methylthio)-1,3,4-oxadiazol-2-yl]-aniline (1)

1:15

Synthesis of Tert-butyl[18-({4-[5-(methylthio)-1,3,4-oxadiazol-2-yl]phenyl}amino)-15,18-dioxo-4,7,10-trioxa-14-azaoctadecyl] Carbamate (2)

3:00

Synthesis of Tert-butyl[18-({4-[5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl]phenyl}amino)-15,18-dioxo-4,7,10-trioxa-14-azaoctadecyl] Carbamate (3)

3:55

Synthesis of N1-(3-{2-[2-(3-aminopropoxy)ethoxy]-ethoxy}propyl)-N4-{4-[5-(methylsulfonyl)-1,3,4-oxadiazol-2-yl] phenyl}Succinamide (PODS)

4:47

Synthesis of PODS-DOTA and Bioconjugation of PODS-DOTA to Trastuzumab

6:05

Results: Synthesis of PODS and PODS-DOTA and Conjugation to Trastuzumab

8:01

Conclusion