Novel indoletriazole alkaloid as well as preparation method and antifungal application thereof
A technology of indole triazole and alkaloids, which is applied in the field of medicine, and can solve problems such as the antifungal activity of indole triazole alkaloids that have not been seen.
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Embodiment 1
[0030] Example 1. Isolation and identification of compound 1 from raw Evodia rutaecarpa
[0031] Raw Evodia rutaecarpa 4Kg, first take out 200g and use a volatile oil extractor to extract about 2ml of Evodia rutaecarpa volatile oil, and prepare it for GC-MS. The dregs and the remaining raw Evodia rutaecarpa were combined and extracted 3 times with 80% ethanol under reflux, each time for 3 hours, the alcohol extract was combined, concentrated under reduced pressure to obtain about 800 g of thick extract, dissolved in water to a suspension, and successively washed with petroleum ether (60 -90°C), chloroform, ethyl acetate and water-saturated n-butanol were extracted, concentrated into extract respectively to obtain petroleum ether fraction 14g, chloroform fraction 209g, ethyl acetate fraction 26g, n-butanol fraction 210g, and water fraction 316g. The chloroform part was repeatedly passed through silica gel normal pressure (LC), low pressure (LPLC) and medium pressure column chro...
Embodiment 2
[0040] Example 2. Isolation and Identification of Compound 1 from Glycyrrhiza Evodia Evodia
[0041] Evodia rutaecarpa 9.5Kg was prepared from sugar, cold soaked in petroleum ether for 7 days to obtain 67g of petroleum ether extract; the dregs after degreasing were reflux extracted with 80% ethanol for 3 times, each time for 3 hours, combined with alcohol extracts, concentrated under reduced pressure to obtain The thick extract is about 1.5Kg; add 2% acid water and knead to dissolve to the suspension, and extract the acid water with ethyl acetate to obtain 263g of ethyl acetate extract; the extracted acid water is alkalized to PH9-10 by adding ammonia water, Extract with chloroform to obtain 126g of chloroform extract with more concentrated total alkaloids; finally adjust alkaline water to neutral and extract with n-butanol to obtain 293g of n-butanol extract. The chloroform extract was repeatedly passed through silica gel normal pressure (LC), low pressure (LPLC) and medium p...
Embodiment 3
[0042] Example 3. Preparation of new skeleton compound 2 Evodia rutaecarpa triazole base (3-[2-N-methylaniline]-triazolo[4,3-a]-3,4-dihydro-β-carboline)
[0043] Take 31.9 mg of compound 1 (Rite Xining) and place it in a 250 mL three-neck flask, add 60 mL of absolute ethanol and heat to reflux to dissolve, cool, stir in an ice bath, slowly add 10 mL of hydrazine hydrate dropwise, and drop it in about 30 minutes After the dropwise addition, continue to stir and react at 0-5°C for 5 hours, stir and react at room temperature for 24 hours, heat in an oil bath at 70-75°C, stir for 6 hours, and monitor by thin-layer chromatography until the reaction is complete. Pour the reaction solution into ice water to precipitate crystals, filter the solid, concentrate the filtrate, extract with dichloromethane (60mL×3), combine the dichloromethane extracts, wash with water (90mL) until neutral, recover the solvent to obtain a solid, Merge the solid obtained twice, and recrystallize with methan...
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