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A kind of swainsonine derivative and its preparation method and application

A technology of swainsonine and its derivatives, which is applied in organic chemical methods, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problems of unstable properties of swainsonine and restrictions on popularization and application, and achieve easy operation , strong antiviral activity, simple preparation process

Active Publication Date: 2021-06-01
北京中联华康科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Long-term studies have shown that swainsonine itself is unstable, which limits its clinical application

Method used

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  • A kind of swainsonine derivative and its preparation method and application
  • A kind of swainsonine derivative and its preparation method and application
  • A kind of swainsonine derivative and its preparation method and application

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Embodiment Construction

[0016] Preferred embodiments of the present invention are described below, and it should be understood that the preferred embodiments described here are only used to illustrate and explain the present invention, and are not intended to limit the present invention.

[0017] The preparation of embodiment 1 swainsonine derivatives

[0018] 1.1 Experimental part

[0019] 1.1.1 Main instruments and reagents

[0020] Avance 400 nuclear magnetic resonance spectrometer, Tensor 27 infrared spectrometer (Bruker, Germany); DSQ II mass spectrometer (Thermo, USA); X-6 precision microscopic melting point tester (Beijing Allen Electromechanical Technology Research Institute) .

[0021] Aspirin, DMF, SOCl 2 (analytical grade, Sinopharm Group Chemical Reagent Co., Ltd.); swainsonine (≥99%, industrial product, Shanghai Yiyan Biotechnology Co., Ltd.); ethyl acetate, petroleum ether (60-90°C) and other reagents are commercially available Sales of analytically pure; ordinary column chromatogra...

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Abstract

The invention discloses a swainsonine derivative, which has the following chemical structural formula: the swainsonine derivative can be obtained by reacting aspirin and swainsonine through an acid chloride esterification method. Compared with swainsonine, the derivative has stronger antiviral activity and can be used to prepare antiviral drugs, such as anti-canine distemper virus drugs.

Description

technical field [0001] The invention relates to a swainsonine derivative, a preparation method and application thereof. Background technique [0002] Locoweed, first distributed in the semi-arid west and western countries and regions, and can produce a large amount of poisonous substances that can make animals go crazy, later put Oxytropis and Astragalus in the leguminous family Toxic substances are collectively referred to as locoweed, and swainsonine SW (swainsonine) is its main toxic component. Animals eating locoweed caused chronic neurological dysfunction and poisoning symptoms, and the animals showed obvious pathological changes. In 2006, Tanaka et al. found that SW inhibited the activity of α-mannosidase in the endoplasmic reticulum through competition, destroying the function of the endoplasmic reticulum. , blocking the expression of HPIV3 surface protein fusion protein (F) and hemagglutinin-neuraminidase (HN), weakening the ability of human parainfluenza virus type...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61P31/14A61K31/437
CPCA61P31/14C07B2200/07C07D471/04
Inventor 梁剑平刘宇梁妍郝宝成王保海王学红郭文柱赵凤舞杨珍贾忠张新刚陶蕾
Owner 北京中联华康科技有限公司
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