Desloratadine derivative containing gamma-subunit butenolide and synthesizing method thereof

A technology of subunit butenolactone and desloratadine, which is applied in the field of novel desloratadine derivatives and their synthesis, can solve the problems of unseen desloratadine derivatives, and achieve simple and convenient preparation methods with good inhibition role, the effect of broadening the structure type
CN101735207AInactive Publication Date: 2010-06-16ZHENGZHOU UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHENGZHOU UNIV
Publication Date
2010-06-16
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a desloratadine derivative containing gamma-subunit butenolide and a synthesizing method thereof, and belongs to the technical field of organic chemical synthesis. The compounds by using desloratadine as a raw material medicament have the following structural general formula, namely the most synthesized compounds have good inhibiting effect on the shrinkage of histamine-induced isolated ileum smooth muscles of guinea pigs, and the synthesis of the derivative enriches the structural type of anti-histamine medicaments and widens the research fields of the anti-histamine medicaments. The synthesizing method provides a good foundation for the further development and utilization of medicinal molecules, and has important meanings for further developing novel anti-allergic medicaments and developing the medicaments with proprietary intellectual property rights.
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Description

technical field

[0001] The invention belongs to organic chemical synthesis. It relates to a class of desloratadine derivatives and a synthesis method thereof, in particular to a class of novel desloratadine derivatives containing γ-ylidene butenolactone groups and a synthesis method thereof Background technique

[0002] Allergic rhinitis is an allergic disease that affects human health, which can affect the work and quality of life of patients, so it has increasingly attracted global attention. Antihistamines are classified into three classes as the first-line treatment for allergic rhinitis. First-generation antihistamines, such as promethazine and ketotifen, were of limited use due to their sedative and anticholinergic side effects. Second-generation antihistamines, such as cetirizine, loratadine (1), and stin, have significantly fewer CNS and anticholinergic side effects than first-generation antihistamines. Newer generation antihistamines include fexofenadine, levocet...

Claims

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