NH2-PEG3-C2-NH-Boc

NH2-PEG3-C2-NH-Boc (PROTAC Linker 15) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs^[1][2]. In Vitro:PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins^[1].
NH2-PEG3-C2-NH-Boc can serve as an intermediate for the synthesis of Iodide ACETYL-Tailed Linker: NH2-PEG3-C2-NH-Boc is dissolved in 30 mL of dichloromethane (DCM) and reacted with Iodoacetic acid N-hydroxysuccinimide (NHS) ester (linker I) (HY-W011541) (192 mg, 0.68 mmol) and 4-methylmorpholine (77 µL, 0.68 mmol) at room temperature for 1 hour. After silica gel column chromatography and solvent removal, a brown oily liquid (linker II) is obtained. Subsequently, linker II is mixed with 10 mL of DCM/TFA solution, and upon removal of the solvent, Iodide ACETYL-Tailed Linker is obtained without further purification^[2].