Drug conjugate intermediate and preparation method therefor
By employing a simplified method for preparing drug conjugate intermediates, using deprotection and condensation reactions and electrochemical processes, the complexity and environmental pollution issues of ADC preparation have been resolved, enabling low-cost large-scale production.
WO2026130368A1PCT designated stage Publication Date: 2026-06-25DUALITY BIOLOGICS (SUZHOU) CO LTD
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- DUALITY BIOLOGICS (SUZHOU) CO LTD
- Filing Date
- 2025-12-16
- Publication Date
- 2026-06-25
AI Technical Summary
Technical Problem
Existing antibody-drug conjugates (ADCs) are complex to prepare, have low yields, are costly, and pose significant environmental pollution risks, making them unsuitable for large-scale production.
Method used
A method for preparing a drug conjugate intermediate is provided, which involves reacting a deprotecting agent and a condensing agent in a specific solvent, combining an electrochemical reaction and an etherification reaction, simplifying the operation and reducing environmental impact.
Benefits of technology
This method enables the preparation of drug conjugate intermediates that are simple to operate, low in cost, and environmentally friendly, making them suitable for large-scale production.
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Smart Images
Figure CN2025142981_25062026_PF_FP_ABST
Abstract
Disclosed in the present invention are a drug conjugate intermediate and a preparation method therefor. Specifically, the present invention provides a method for preparing a compound represented by formula (II) or a salt thereof, comprising the following steps: step 1, in a solvent, in the presence of a deprotection reagent, subjecting a compound represented by formula (IV) or a salt thereof to a deprotection reaction as shown below to obtain a compound represented by formula (III) or a salt thereof; and, step 2, in a solvent, in the presence of a condensation agent, subjecting the compound represented by formula (III) or the salt thereof and an amino protecting reagent to a GP3 protecting group introduction reaction as shown below to obtain a compound represented by formula (II) or a salt thereof. The preparation method of the present invention has low cost, high yield, and simpler operation and is suitable for large-scale production.
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