An organic synthesis method for benzyl protecting hydroxyl groups

By using a reverse-drop addition method in the organic synthesis of benzyl protected hydroxyl groups, the problem of reaction limitation in existing technologies has been solved, achieving efficient conversion of compound (IX) to compound (XI), improving yield and reducing environmental pollution.

CN118084736BActive Publication Date: 2026-06-09WEINAN RUILIAN PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
WEINAN RUILIAN PHARM CO LTD
Filing Date
2024-02-01
Publication Date
2026-06-09

AI Technical Summary

Technical Problem

Existing technologies cannot effectively prepare compound (XI), especially organic synthesis methods for benzyl protected hydroxyl groups, which suffer from reaction limitations when preparing compound (IX).

Method used

The reaction is carried out by reverse dropping. First, benzyl chloride and iodide are dissolved in a solvent, then a strong base is added and the reaction is kept at a certain temperature. Then the substrate is added dropwise. Sodium hexamethyldisilamide or lithium hexamethylsilylaminoacetate is used as the strong base, and DMF, DMAc or DMSO is used as the solvent. The temperature is controlled during the reaction.

Benefits of technology

This method enables the simultaneous occurrence of two reactions, improving reaction efficiency and yield while reducing environmental pollution, and provides an efficient and economical method for synthesizing benzyl protected hydroxyl groups.

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Abstract

The application belongs to the technical field of organic synthesis and relates to an organic synthesis method for benzyl protection of a hydroxyl group. The application provides an organic synthesis method for benzyl protection of a hydroxyl group, which comprises the following steps: dissolving benzyl chloride and KI in DMF, adding NaH, and then adding a DMF solution containing a substrate drop by drop to perform a temperature control reaction. The application provides a new idea for protection of a non-conventional hydroxyl group.
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