A method for synthesizing antibody-coupled degradation agent dipeptide linkers
A seven-step synthetic route was developed using inexpensive and readily available p-aminobenzyl alcohol as a starting material, which solved the problems of low yield and complex purification in existing synthetic routes, and achieved efficient and low-cost preparation of the target product, suitable for large-scale production.
Patent Information
- Authority / Receiving Office
- CN ยท China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- WUHAN AOFEI TECH CO LTD
- Filing Date
- 2024-11-25
- Publication Date
- 2026-05-26
AI Technical Summary
The existing synthetic routes for preparing ethyl 1-[(3S)-3-{[(4-{[(2-bromophenyl)oxy]methyl}phenyl)amino]carbonyl}-8-methyl-1-oxoylide-2,8-diazanon-1-yl]cyclobutane-1-carboxylate have problems such as low yield in the third-step condensation reaction and the need for two reverse-phase purifications, which makes it difficult to meet the growing market demand.
Using readily available and inexpensive commercial raw material p-aminobenzyl alcohol as the starting material, a novel synthetic route was developed through seven conventional reactions. Each of the seven steps requires no further purification and can be directly used in the next step. The target product was successfully prepared using inexpensive and readily available reagents and mild reaction conditions.
A high-purity, high-yield preparation of ethyl 1-[(3S)-3-{[(4-{[(2-bromophenyl)oxy]methyl}phenyl)amino]carbonyl}-8-methyl-1-oxonyl-2,8-diazanon-1-yl]cyclobutane-1-carboxylate was achieved, simplifying the operation process, reducing costs, and making it suitable for large-scale production at the hundred-gram level.
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Figure CN122079809A_ABST