A phosphated p-hydroxybenzaldehyde compound and a method for assisting preparation of octreotide therefrom
By using phosphorylated p-hydroxybenzaldehyde compounds to assist in the preparation of octreotide, the problems of cumbersome separation and purification steps and environmental pollution in the existing technology are solved, realizing efficient and environmentally friendly preparation of octreotide, simplifying the process and improving yield and purity.
Patent Information
- Application Number
- CN202310844564.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2023-07-11
- Publication Date
- 2025-11-07
- Estimated Expiration
- 2043-07-11
AI Technical Summary
Existing chemical production methods for octreotide suffer from cumbersome separation and purification steps, significant waste of raw materials and solvents, and large amounts of resin solid waste that are difficult to degrade, resulting in serious environmental pollution. Furthermore, existing technologies cannot achieve high total yield and high purity under all-solid-phase synthesis conditions.
Octreotide is prepared by using phosphorylated p-hydroxybenzaldehyde compounds as auxiliary groups, condensing them with N-terminally protected aminodiols or hydroxythiols, and then performing coupling reactions and oxidative cyclization. PPHBA carriers are used for peptide synthesis, simplifying separation and purification steps, and allowing for recycling and reuse, thus reducing waste.
This method enables the simple, rapid, and efficient preparation of octreotide, reducing raw material waste and production costs, minimizing waste pollution, making it suitable for large-scale production, and improving yield and purity.