Process for the preparation of an intermediate of levocetirizine hydrochloride
By employing the reductive amination reaction of 4-chlorobenzophenone with anhydrous piperazine and the resolution method of L-di-p-methylbenzoyl tartaric acid, the problems of long preparation steps and low yield of levocetirizine hydrochloride intermediates have been solved, achieving an efficient and green production process.
CN121914037BActive Publication Date: 2026-07-24FUAN PHARM GRP NINGBO TIANHENG PHARM CO LTD
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Patent Information
- Application Number
- CN202610369481.6
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Filing Date
- 2026-03-25
- Publication Date
- 2026-07-24
- Estimated Expiration
- 2046-03-25
AI Technical Summary
Technical Problem
Existing methods for preparing levocetirizine hydrochloride intermediates suffer from lengthy steps, low yields, and a lack of environmental friendliness, especially with low yields during chiral resolution, leading to high production costs.
Method used
1-[(4-chlorophenyl)benzyl]piperazine was prepared by reductive amination of 4-chlorobenzophenone and anhydrous piperazine in the presence of a catalyst and hydrogen. Then, (R)-1-[(4-chlorophenyl)benzyl]piperazine was obtained by resolving it under alkaline conditions with L-di-p-methylbenzoyl tartaric acid as a resolving agent.
Benefits of technology
It achieves an efficient and green preparation route with high product yield, simplified process steps, reduced production costs, and is suitable for industrial production.
✦ Generated by Eureka AI based on patent content.
Abstract
The application relates to the technical field of synthesis, and particularly discloses a preparation method of a levocetirizine hydrochloride intermediate. The method comprises the following steps: 4-chlorobenzophenone and anhydrous piperazine are subjected to a reductive amination reaction in an organic solvent containing a catalyst to obtain 1-[(4-chlorophenyl)benzyl]piperazine; the 1-[(4-chlorophenyl)benzyl]piperazine is subjected to resolution in an organic solvent by using L-di-p-methylbenzoyl tartaric acid as a resolution agent, and then is subjected to isolation under alkaline conditions to obtain a levocetirizine hydrochloride intermediate (R)-1-[(4-chlorophenyl)benzyl]piperazine. The raw materials and auxiliary materials used in the application are easy to obtain, a novel, efficient and green process route is developed, the whole reaction route is short and simple to operate, the obtained levocetirizine hydrochloride intermediate (R)-1-[(4-chlorophenyl)benzyl]piperazine has high yield, the total yield reaches up to 40% calculated from 4-chlorobenzophenone, and the industrialized production can be realized.
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