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Triazole compound

A compound and triazole technology, applied in the field of triazole compound and the preparation of the compound, can solve the problems of side reaction, complex composition of compound and the like

Active Publication Date: 2014-12-24
NANJING HUAWE MEDICINE TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the compound has excellent water solubility, the composition of the compound is complex and may cause a series of side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: the synthesis of compound Ia

[0033]

[0034] In a 1000mL reaction flask, fully dissolve chloromethyl-2-methoxyethyl carbonate (42g, 0.25mol) and voriconazole (69.9g, 0.2mol) with 600mL acetonitrile solution, heat to reflux and react for 10h. After TLC detection, the reaction was concentrated to dryness, dichloromethane was added to dissolve the concentrate fully under heating conditions, cooled to room temperature, filtered to dryness and vacuum dried for a period of time to obtain a white solid, namely compound Ia (82g, 85%).

[0035] MS(ESI): 483.2([M+H] + ).

Embodiment 2

[0036] Embodiment 2: the synthesis of compound Ib

[0037]

[0038] According to the operation of Example 1, replace chloromethyl-2-methoxyethyl carbonate with chloromethyl-2-[2-methoxyethoxy] ethyl carbonate, and obtain white solid (Ib , 80%).

[0039] MS (ESI): 526.5 ([M+H] + ).

Embodiment 3

[0040] Embodiment 3: the synthesis of compound Ic

[0041]

[0042] According to the operation of Example 1, replace chloromethyl-2-methoxyethyl carbonate with chloromethyl-2-[2-[2-methoxyethoxy]ethoxy]ethyl carbonate after the reaction is complete after the post-treatment A white solid (Ic, 82%) was obtained.

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Abstract

The invention discloses a triazole compound. The triazole compound has excellent water solubility. The triazole compound is obtained by introduction of a novel functional group to high efficiency and wide spectrum antifungal compound voriconazole and fluconazole drugs found in the existing clinical application and novel drug development so that the triazole compound greatly improves voriconazole and fluconazole water solubility and reduces drug toxicity.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a triazole compound and a preparation method of the compound. Background technique [0002] Triazole is a five-membered heterocyclic ring in which one carbon atom in the imidazole ring is replaced by nitrogen. As a pharmacophore, triazole has lower toxicity than imidazole and is widely used in various medicines and pesticides. [0003] For fungal diseases, especially deep fungal diseases, amphotericin B is the standard drug in the traditional treatment, but this drug has relatively high toxicity and side effects. For this reason, a liposome drug delivery system has been developed. The development and marketing of triazole antifungal drugs is a supplement to amphotericin B. The first triazole antifungal drug used clinically was Terconazole, which was launched in 1983. It pioneered the antifungal treatment of triazole compounds and aroused great interest in the rese...

Claims

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Application Information

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IPC IPC(8): C07D403/06C07D249/08A61K31/506A61K31/4196A61P31/10
CPCC07D249/08C07D403/06
Inventor 张孝清黄辉江振兴胡丹丹蒋玉伟
Owner NANJING HUAWE MEDICINE TECH DEV
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