Process for the preparation of apomorphine

By using benzothiazole sulfone to replace phosphate salts, apoester was prepared by coupling reaction of C5-BTS with C10-dialdehyde and C15-BTS, solving the problems of low yield and environmental pollution in the existing technology, and realizing efficient and low-cost apoester production.

CN122102989APending Publication Date: 2026-05-29GUANGZHOU JUYUAN BIO-CHEM CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
GUANGZHOU JUYUAN BIO-CHEM CO LTD
Filing Date
2026-02-12
Publication Date
2026-05-29

AI Technical Summary

Technical Problem

Existing apoester synthesis processes suffer from low yields, high costs, and severe environmental pollution, making large-scale production difficult.

Method used

Apoester was prepared by using benzothiazole sulfone (BTS) instead of traditional phosphate salts, through the coupling reaction of C5-BTS with C10-dialdehyde and C15-BTS, thus avoiding the use of phosphorus-containing compounds and reducing the generation of waste.

Benefits of technology

It improves the synthesis yield of apoester, reduces production costs, simplifies the process, is suitable for large-scale production, and is environmentally friendly.

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Abstract

The application discloses a preparation method of arbutin, and the preparation method comprises the following steps: (1) C5-halogenated ester (II) is reacted with 2-mercaptobenzothiazole (MBT) to generate C5-BT (III), and C5-BT (III) is further oxidized to prepare C5-BTS (IV); and (2) C5-BTS (IV), C15-BTS (V) and C10-dialdehyde (VI) are coupled to prepare arbutin (I), and the specific route can be C5+C10→C15, C15+C15→C30, or C15+C10→C25, C25+C5→C30; the method has low raw material cost, avoids the use of phosphorus salt in a traditional synthesis route, and provides an efficient, economical and environmentally-friendly solution for large-scale clean production of arbutin.
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