NH-bis(PEG4-C2-NH-Boc)
NH-bis(PEG4-C2-NH-Boc) is a bifunctional polyethylene glycol–based linker building block designed for PROTAC synthesis, featuring two PEG4 arms that provide hydrophilicity and conformational flexibility, each terminated with an ethyl (C2) spacer and protected amine functionality (Boc). The “bis” architecture enables orthogonal coupling to two different PROTAC fragments—typically a ligand targeting an E3 ligase and a ligand targeting the protein of interest—while the PEG segment helps reduce steric mismatch and can improve effective encounter rates between the recruited proteins. In targeted protein degradation workflows, such PEGylated, amine-protected linkers are used to tune linker length and polarity, thereby modulating ternary complex formation and degradation potency. As a modular intermediate, it supports systematic structure–activity relationship studies and facilitates reproducible assembly of conjugates for mechanistic and optimization experiments.
Structure of 2182601-75-6
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NH-bis(PEG4-C2-NH-Boc), is designed to provide a PEG-based, flexible spacer architecture with protected amine functionality for controlled conjugation. Its hydrophilic, conformationally adaptable backbone can help tune linker length and solvation, supporting efficient formation of ternary complexes in targeted protein degradation workflows. The points below describe its structure and practical reactivity considerations for PROTAC assembly.
Structure: The linker contains a bis(amine) motif integrated into a polyethylene glycol spacer, with ethylene spacers connecting amine sites. Boc-protected nitrogen atoms provide stable carbamate protection, while ether-rich PEG segments impart hydrophilicity and conformational flexibility under typical organic synthesis conditions.
Reactivity: Boc groups are typically removed under acidic conditions to unmask primary amines prior to coupling steps. Subsequent PROTAC bond formation commonly relies on amine-reactive electrophiles such as activated esters, carbonyl diimidazoles, or isocyanates, proceeding via nucleophilic acyl substitution or related amide/urea-forming mechanisms. Mild bases and polar aprotic solvents are often used to preserve PEG integrity and minimize side reactions.
* 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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