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A kind of purification method of loratadine key intermediate

A technology of loratadine and a purification method is applied in the field of purification of key intermediates of loratadine, can solve the problems of many by-products, difficult to prepare loratadine, low purity and the like, and achieves improved quality and yield , Ensure process stability, high yield and high purity effect

Active Publication Date: 2022-06-03
北京鑫开元医药科技有限公司
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Problems solved by technology

[0007] But the loratadine key intermediate with formula (1) structure that existing preparation technology makes has many by-products, low purity, it is difficult to prepare qualified loratadine

Method used

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Abstract

The invention belongs to the field of medicinal chemistry and provides a method for purifying a key intermediate of loratadine having a structure of formula (1). The structure of the formula (1) is. The purification method comprises: adding the crude product of the key intermediate of loratadine into an alcoholic solvent, stirring and dissolving, adding acid to form a salt, cooling and crystallizing, filtering, freeing, drying, and recrystallization to obtain purified loratadine key intermediates. The purification method of the key intermediate of loratadine provided by the present invention has good purification effect, and the yield and purity of the purified target product are high, which better ensures the process stability in the next step and is conducive to improving the quality of loratadine products The process of the purification process is simple, and the solvent used is common and easy to recycle, which greatly simplifies the industrial operation and is suitable for industrial large-scale production.

Description

A kind of purification method of loratadine key intermediate technical field The invention belongs to medicinal chemistry field, be specifically related to a kind of purification method of loratadine key intermediate. Background technique The chemical name of loratadine (loratadine) is 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]-cycloheptyl Alkane[1,2-b]pyridin-11-alkenyl)-1-piperidinecarboxylate, the chemical structural formula is as follows: [0003] Loratadine, as the representative of the second generation antihistamine, can competitively inhibit histamine H1 receptor and the reference of histamine It has no obvious anti-central and choline inhibitory effects, has good clinical efficacy and is safe to use. The compound with formula (1) structure is the key intermediate in the preparation process of loratadine, and the improvement of the intermediate The synthesis technique and improving the purity of the intermediate are of great significance to the production of lo...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04
CPCC07D401/04C07B2200/13Y02P20/55
Inventor 孙学涛郭文君于凯苏小庭戴信敏
Owner 北京鑫开元医药科技有限公司
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