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A class of nitrogen azole compounds and its preparation method and application

A technology for compound and azole, which is applied in the field of medicine and achieves the effects of high yield, simple preparation method and good effect

Inactive Publication Date: 2016-05-18
中国人民解放军南京军区司令部门诊部
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far no azole compound N-alkyl-N-(2-(2,4-difluorophenyl)-2-hydroxyl-3-(1H-1,2,4-trifluorophenyl) with antifungal activity Report on oxazol-1-yl))-propyl-cyclopropylaminodithiocarboxylate or its salts

Method used

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  • A class of nitrogen azole compounds and its preparation method and application
  • A class of nitrogen azole compounds and its preparation method and application
  • A class of nitrogen azole compounds and its preparation method and application

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Embodiment 1

[0030] The preparation of embodiment 1 compound of the present invention

[0031] (1) 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-cyclopropylamino)-2-ol

[0032] 1-[2-(2,4-difluorophenyl)-2,3-epoxypropyl]-1H-1,2,4-triazole mesylate 21g, with cyclopropylamine 10mL, triethylamine 20mL, heat and reflux in 300mL ethanol for 6-8 hours, distill off the solvent after the reaction is complete, extract with 200mL ethyl acetate, wash with 100mL×2 water, dry over anhydrous sodium sulfate, filter, distill off ethyl acetate to obtain oily 1- (1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-(N-cyclopropylamino)-2-ol 11.96g, yield 68.0 %.

[0033] (2) Preparation of N-methyl-N-(2-(2,4-difluorophenyl)-2-hydroxyl-3-(1H-1,2,4-triazol-1-yl))-propane Benzyl-cyclopropylcarbamate (compound 6a in Table 1):

[0034] In a 50mL single-neck bottle, put a magnet, add 10mL absolute ethanol, 0.536g 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)- 3-(N-Cyclopropylamino)-2-ol (2 mmol). After...

Embodiment 2

[0079] The pharmacological experiment of embodiment 2 compounds of the present invention

[0080] (1) Experimental method

[0081] Conventional in vitro antibacterial test methods are used, see: Antimicrob Agents Chemother 1995, 39 (5): 1169 for details.

[0082] (1) Experimental strains

[0083] In this experiment, the following 8 common human pathogenic standard fungal strains were selected as screening objects:

[0084] Deep fungi: Candida albicans, Cryptococcus neoformans, Candida glabrata, Candida parapsilosis;

[0085] Superficial fungi: Trichophyton rubrum;

[0086] Subcutaneous fungi: Microsporum gypsum, Aspergillus fumigatus.

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Abstract

The invention relates to nitrogen imidazole compounds and salts thereof. A chemical structure formula of the nitrogen imidazole compounds is as shown in the specification, wherein R is selected from hydrogen, halogen, cyanogroup and nitryl, can be located on an o-position, a meta-position and a para-position of a benzene ring, can be mono-substituted or poly-substituted. The invention further provides a preparation method and application of the compounds. The compounds are strong in antifungal activity for deep fungus, have the advantages of being efficient, low in toxicity, wide in antifungal spectrum and the like in comparison with an antifungal drug in existing clinical application, and therefore, the compounds can be used for preparing an efficient antifungal drug.

Description

【Technical field】 [0001] The present invention relates to the technical field of medicine, in particular to a class of nitrogen azole compounds and its preparation method and application. 【Background technique】 [0002] In recent years, with the widespread application of broad-spectrum antibiotics, antineoplastic drugs, and immunosuppressants, the widespread development of peritoneal dialysis, organ transplantation, and radiotherapy, and the rapid spread of immunodeficiency diseases, especially AIDS, Candida albicans, Cryptography neoformans The incidence of opportunistic deep fungal infections such as coccus and Aspergillus fumigatus has increased dramatically. Deep fungal infection has risen to the third largest infectious disease clinically, seriously threatening human life and health. Most of the antifungal drugs currently in clinical use have defects such as large toxic and side effects, narrow antibacterial spectrum, and easy to develop drug resistance. Effective anti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D249/08A61K31/4196A61P31/10
CPCC07D249/08
Inventor 陈家鲁章杰兵吴茂诚邹燕吴秋业
Owner 中国人民解放军南京军区司令部门诊部
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