294181-95-6Relevant academic research and scientific papers
Synthetic method of aromatic ring group or aromatic heterocyclic tetrazole
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Paragraph 0036-0042; 0051, (2020/12/30)
The synthetic method comprises the following steps: (1) reacting 1.0 eq of ArI or HArI with 1.2 eq of ethyl 2, 2-difluoroacetate in the presence of DMSO as a solvent and 4.0 eq of Cu under the protection of nitrogen at 30 DEG C and 50 DEG C, and purifying to obtain a first intermediate compound; (2) dissolving 1.0 eq of the first intermediate compound in a mixed solvent of THF and water, adding 2.0 eq of LiOH, reacting at room temperature for 2 hours, spin-drying the solvent, adding HCl until the pH value is equal to 3, and filtering to obtain a second intermediate compound; and (3) reacting 1.0 eq of the second intermediate compound with 2.0 eq of diphenyl azide phosphate in the presence of 2.5 eq of triethylamine by taking tert-butyl alcohol as a solvent to generate aromatic ring group or aromatic heterocyclic tetrazole. The invention provides a novel synthetic method of aromatic ring group or aromatic heterocyclic tetrazole, wherein a target compound can be more conveniently obtained, and reagents participating in the reaction are low in toxicity, mild in reaction condition, simple and safe in aftertreatment, good in product quality and suitable for large-scale production.
Fungal lanosterol 14α-demethylase (CYP51) inhibitor Treatment of recurrent vulvovaginal candidiasis Treatment of onychomycosis
Chopra, S.,Dasgupta, A.,Thakare, R.
, p. 855 - 868 (2020/01/21)
Developing a rationally designed, more selective azole antifungal agent that specifically targets the fungal CYP51 over the host CYP51 is a severe unmet need considering a massive shortfall in novel antifungal agents. In this context, oteseconazole (VT-1161) represents a very exciting new development targeting serious fungal infections caused by a wide variety of fungal pathogens including multidrug-resistant Candida responsible for recurrent vulvovaginal candidiasis. This monograph details the various in vitro and in vivo properties exhibited by oteseconazole as well as its current status in clinical trials.
1,4-THIAZINE DIOXIDE AND 1,2,4-THIADIAZINE DIOXIDE DERIVATIVES AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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Page/Page column 74; 73, (2018/07/05)
The present disclosure provides a class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, X, R2, R2', R3, R4, R5, R6, and R7 of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, and other central nervous system conditions.
METALLOENZYME INHIBITOR COMPOUNDS
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Page/Page column 79; 80, (2017/07/31)
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
ANTIFUNGAL COMPOUNDS AND PROCESSES FOR MAKING
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Page/Page column 31; 32, (2017/04/11)
Provided are polymorphic forms of compound 5 or 5*, or mixtures thereof, and polymorph forms of compound 14 or 14*, or mixtures thereof. Also provided are methods of preparing compound 5 or 5*, or mixtures thereof, and methods of preparing compound of 14 or 14*, or mixtures thereof, which are useful as antifungal agents. In particular, provided is new methodology for preparing polymorphs of the compounds described and substituted derivatives thereof.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 55; 56, (2015/11/11)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 52; 53, (2015/11/10)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 82; 85; 86, (2015/11/10)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 70; 71; 72, (2015/11/10)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
ANTIFUNGAL COMPOUND PROCESS
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Page/Page column 37, (2015/11/10)
The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.
