Fmoc-Ado-OH

Fmoc-Ado-OH is a versatile Fmoc-protected PEG-based linker widely utilized in solid-phase peptide synthesis (SPPS) and the synthesis of antibody-drug conjugates (ADCs). The compound features a hydrophilic 3,6-dioxaoctanoic acid spacer that serves as a mini-PEG linker, reducing peptide aggregation during synthesis and improving the solubility of hydrophobic peptide sequences. Fmoc-Ado-OH is particularly valuable as a spacer in peptide nucleic acid (PNA) synthesis, where the PEG linker provides the necessary flexibility and hydrophilicity. In ADC development, Fmoc-Ado-OH functions as a cleavable linker component that connects the antibody to the cytotoxic payload, enabling targeted drug delivery. Fmoc-Ado-OH is also recognized as a key intermediate for the fourth-generation anti-HIV drug Ilabot, demonstrating its significance in pharmaceutical manufacturing. As a building block, Fmoc-Ado-OH supports the synthesis of complex molecules and polymers in both research and industrial settings. The compound‘s high purity (≥95–97% by HPLC) and well-characterized physical properties make it a reliable reagent for demanding synthesis applications.

Product Parameters

Bioactivity

Fmoc-8-amino-3,6-dioxaoctanoic acid (Fmoc-NH-PEG2-CH2COOH) is a biodegradable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It also serves as a PEG-based PROTAC linker for PROTAC synthesis.

Synthetic Route

The nitrogen atom is protected by reacting benzaldehyde with diethylene glycolamine to form an imine, which then reacts with tert-butyl bromoacetate to yield an ether. Subsequent protection removal of the amino group and ester hydrolysis are accomplished in a one-pot reaction under acidic conditions with stirring overnight, ultimately yielding Fmoc-Ado-OH.

In vitro study

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker.

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.

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Need Fmoc-Ado-OH with documented purity and batch-to-batch consistency for your ADC development, peptide synthesis, or pharmaceutical manufacturing project? Cosperpharm is your trusted partner. Contact us today for pricing, technical datasheets, or to discuss your custom requirements—we’re ready to support your success.