N-(PEG1-OH)-N-Boc-PEG2-propargyl
N-(PEG1-OH)-N-Boc-PEG2-propargyl is a branched trifunctional polyethylene glycol–based linker featuring a terminal propargyl group, a terminal hydroxyl group, and a Boc-protected amine. Structurally, it consists of PEG segments that provide aqueous solubility and conformational flexibility, connected through a Boc carbamate-bearing central nitrogen that can be deprotected under standard conditions to enable subsequent amide or urea bond formation. In PROTAC design, this type of linker is used to spatially engineer the distance and relative orientation between a target-binding ligand and an E3 ligase recruiter, while the PEG chain helps reduce nonspecific aggregation and improves handling in biological media. The propargyl handle enables efficient attachment to azide-bearing partners (e.g., via CuAAC or strain-promoted azide–alkyne cycloaddition), facilitating modular synthesis of degraders. Overall, it is valuable for constructing PROTACs with tunable linker length and improved physicochemical properties, supporting systematic structure–activity relationship studies in targeted protein degradation research.
Structure of 2100306-85-0
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N-(PEG1-OH)-N-Boc-PEG2-propargyl is a PEG-based PROTAC linker building block designed to connect targeting ligands and enable efficient ternary-complex formation. Its polyethylene glycol segments provide solubility and conformational flexibility, while the terminal propargyl handle supports orthogonal conjugation strategies. The Boc-protected amine and hydroxyl functionality offer practical sites for controlled derivatization during PROTAC assembly. The following sections describe the structure and reactivity considerations in detail.
Structure: The linker comprises PEG oligomer segments bearing an alcohol terminus and a Boc-protected amine, together with a terminal propargyl group. It contains ether linkages characteristic of PEG, a carbamate from the Boc group, and an alkyne suitable for click-type coupling.
Reactivity: Suitable PROTAC construction typically uses orthogonal functional-group chemistry: the terminal propargyl group can participate in copper-catalyzed azide–alkyne cycloaddition to install targeting or E3-ligand modules bearing azides. The Boc group enables temporary amine protection during linker functionalization and can be removed under standard acid-labile conditions to reveal an amine for subsequent coupling. PEG ether stability supports aqueous-compatible conditions, with polar solvents commonly used to maintain solubility.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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