PL220507B1 - 3'-[3"-hydroxy-3"-methylbutyl]-4,4',2'-trihydroxy-6'-methoxy-α,β-dihydrochalcone and a method for its preparation - Google Patents
3'-[3"-hydroxy-3"-methylbutyl]-4,4',2'-trihydroxy-6'-methoxy-α,β-dihydrochalcone and a method for its preparationInfo
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- PL220507B1 PL220507B1 PL405454A PL40545413A PL220507B1 PL 220507 B1 PL220507 B1 PL 220507B1 PL 405454 A PL405454 A PL 405454A PL 40545413 A PL40545413 A PL 40545413A PL 220507 B1 PL220507 B1 PL 220507B1
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- trihydroxy
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- methylbutyl
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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Description
Opis wynalazkuDescription of the invention
Przedmiotem wynalazku jest 3'-[3”-hydroksy-3”-metylobutylo]-4,4',2'-trihydroksy-6'-metoksy-a^-dihydrochalkon, o wzorze 2, przedstawionym na rysunku oraz sposób jego wytwarzania.The present invention relates to 3 '- [3 "-hydroxy-3" -methylbutyl] -4,4', 2'-trihydroxy-6'-methoxy-α 1 -dihydro chalcone of the formula 2 shown in the drawing and a method of its preparation.
Związek ten jest biologicznie czynny i może mieć zastosowanie w przemyśle spożywczym i farmaceutycznym.This compound is biologically active and can be used in the food and pharmaceutical industries.
Dotychczas, w literaturze nie jest znany 3'-[3”-hydroksy-3”-metylobutylo]-4,4',2'-trihydroksy-6'-metoksy-a,3-dihydrochalkon ani sposób jego wytwarzania.Until now, there is no known in the literature 3 '- [3 "-hydroxy-3" -methylbutyl] -4,4', 2'-trihydroxy-6'-methoxy-a, 3-dihydrohalcone or the method of its preparation.
Istotą wynalazku jest 3'-[3”-hydroksy-3”-metylobutylo]-4,4',2'-trihydroksy-6'-metoksy-a,3-dihydrochalkon.The essence of the invention is 3 '- [3 "-hydroxy-3" -methylbutyl] -4,4', 2'-trihydroxy-6'-methoxy-a, 3-dihydroochalcone.
Natomiast istotą sposobu wytwarzania tego związku jest to, że otrzymuje się go na drodze reakcji mikrobiologicznej transformacji substratu, którym jest jakim jest 4,4',2'-trihydroksy-6'-metoksy-3'-prenylo-a,3-dihydrochalkon. Grzyby z gatunku Penicillium albidum, namnaża się w płynnym podłożu mikrobiologicznym, charakterystycznym dla grzybów, przy ciągłym mieszaniu reagentów, w temperaturze 12-40°C. Następnie do narośniętej hodowli dodaje się substrat i dalej prowadzi się proces, aż do całkowitego zużycia substratu. Po zakończeniu transformacji roztwór transformacyjny ekstrahuje się rozpuszczalnikami organicznymi niemieszającymi się z wodą, oddziela frakcję organiczną, osusza bezwodnym siarczanem magnezu, odparowuje rozpuszczalnik i tak otrzymany surowy produkt oczyszcza się pomocą technik chromatograficznych.However, the essence of the method of producing this compound is that it is obtained by microbial transformation of the substrate, which is 4,4 ', 2'-trihydroxy-6'-methoxy-3'-prenyl-a, 3-dihydroochalcone. Penicillium albidum fungi are multiplied in a liquid microbiological medium, characteristic for fungi, with constant mixing of the reagents, at a temperature of 12-40 ° C. Subsequently, a substrate is added to the grown culture and the process is continued until the substrate is completely consumed. After completion of the transformation, the transformation solution was extracted with water-immiscible organic solvents, the organic fraction was separated, dried over anhydrous magnesium sulfate, the solvent was evaporated, and the crude product thus obtained was purified by chromatographic techniques.
Korzystnie jest, gdy proces namnażania drobnoustroju prowadzi się w temperaturze 30°C.Preferably, the multiplication process of the microorganism is carried out at a temperature of 30 ° C.
Postępując zgodnie z wynalazkiem, w wyniku działania układu enzymatycznego zawartego w żywych komórkach kultury Penicillium albidum, następuje reakcja hydratacji w substracie.By following the invention, as a result of the action of the enzyme system contained in the living cells of Penicillium albidum culture, a hydration reaction takes place in the substrate.
Zasadniczą zaletą wynalazku jest otrzymanie, w łagodnych warunkach, 3'-[3”-hydroksy-3”-metylobutylo]-4,4',2'-trihydroksy-6'-metoksy-a,3-dihydrochalkon, o wzorze 2, jako głównego produktu reakcji w kulturze Penicillium albidum z wydajnością 30,1%.The main advantage of the invention is to obtain, under mild conditions, 3 '- [3 "-hydroxy-3" -methylbutyl] -4,4', 2'-trihydroxy-6'-methoxy-a, 3-dihydroochalcone of formula 2, as the main reaction product in the Penicillium albidum culture with a yield of 30.1%.
Wynalazek jest bliżej objaśniony w przykładzie wykonania.The invention is explained in more detail in an exemplary embodiment.
P r z y k ł a d 1. Do kolby o pojemności 300 cm3, w której znajduje się 100 cm3 sterylnej pożyw3 ki zawierającej 3 g glukozy i 1 g aminobaku na 1 dm wody destylowanej, wprowadza się grzyby Penicillium albidum. Po 4 dniach wzrostu drobnoustrojów w temperaturze 30°C i przy ciągłym wstrząsaniu, dodaje się 15 mg 4,4',2'-trihydroksy-6'-metoksy-3'-prenylo-a,3-dihydrochalkon, o wzorze 1, rozpuszczonego w 1 cm3 metanolu. Transformację prowadzi się przy ciągłym wstrząsaniu przez 8 dób. Następnie, uzyskany roztwór transformacyjny ekstrahuje się trzykrotnie octanem etylu, osusza bezwodnym siarczanem magnezu i odparowuje rozpuszczalnik. Otrzymuje się 21,0 mg surowego produktu, który oczyszcza się chromatograficznie, używając jako eluentu mieszaninę chloroform:metanol w stosunku objętościowym 9:1.EXAMPLE 1 To a flask of 300 cm 3, which is a 100 cm 3 three sterile sued path containing 3 g of glucose and 1 g aminobaku per 1 liter of distilled water is introduced fungus Penicillium albidum. After 4 days of microbial growth at 30 ° C and with continuous shaking, 15 mg of 4,4 ', 2'-trihydroxy-6'-methoxy-3'-prenyl-a, 3-dihydroochalcone, formula 1, dissolved in 1 cm 3 of methanol. The transformation is carried out under continuous shaking for 8 days. Then, the resulting transformation solution was extracted three times with ethyl acetate, dried with anhydrous magnesium sulfate, and the solvent was evaporated. 21.0 mg of crude product is obtained, which product is purified by chromatography using a 9: 1 by volume mixture of chloroform: methanol as eluent.
Po oczyszczeniu otrzymuje się 4,75 mg 3'-[3”-hydroksy-3”-metylobutylo]-4,4',2'-trihydroksy-6'-metoksy-a,3-dihydrochalkonu, o wzorze 2, z wydajnością 30,1%.After purification, 4.75 mg of 3 '- [3 "-hydroxy-3" -methylbutyl] -4,4', 2'-trihydroxy-6'-methoxy-a, 3-dihydroquinone of formula II are obtained with the yield 30.1%.
Uzyskany produkt charakteryzuje się następującymi danymi spektralnymi:The obtained product is characterized by the following spectral data:
1H NMR (600 MHz, aceton-d6) δ: 1,23 (6H, s, H-4”, H-5”), 1,65 (2H, m, H-2”), 2,66 (2H, m, H-1”), 2,86 (2H, m, H-β), 3,24 (2H, m, H-a), 3,85 (3H, s, C6'-OCH3), 6,08 (1H, s, H-5'), 6,75 (2H, pd, J= 8,4 Hz, H-3, H-5), 7,09 (2H, pd, J= 8,4 Hz, H-2, H-6), 14,32 (C2'-OH).1H NMR (600 MHz, acetone-d6) δ: 1.23 (6H, s, H-4 ", H-5"), 1.65 (2H, m, H-2 "), 2.66 (2H , m, H-1 "), 2.86 (2H, m, H-β), 3.24 (2H, m, Ha), 3.85 (3H, s, C6'-OCH3), 6.08 (1H, s, H-5 '), 6.75 (2H, pd, J = 8.4 Hz, H-3, H-5), 7.09 (2H, pd, J = 8.4 Hz, H-2, H-6), 14.32 (C2'-OH).
13C NMR (150 MHz, aceton-d6) δ: 17,81 (C-1”), 29,66 (C-4”, C-5”), 30,83 (C-β), 43,21 (C-2”), 46,98 (C-a), 55,94 (C6'-OCH3), 70,79 (C-3”), 91,65 (C-5'), 105,61 (C-1'), 109,92 (C-3'), 116,01 (C-3, C-5), 130,17 (C-2, C-6), 133,38 (C-1), 156,45 (C-4), 162,14 (C-6'), 163,15 (C-4'), 165,69 (C-2'), 205,47 (C=O).13C NMR (150 MHz, acetone-d6) δ: 17.81 (C-1 "), 29.66 (C-4", C-5 "), 30.83 (C-β), 43.21 ( C-2 "), 46.98 (Ca), 55.94 (C6'-OCH3), 70.79 (C-3"), 91.65 (C-5 '), 105.61 (C-1 '), 109.92 (C-3'), 116.01 (C-3, C-5), 130.17 (C-2, C-6), 133.38 (C-1), 156, 45 (C-4), 162.14 (C-6 '), 163.15 (C-4'), 165.69 (C-2 '), 205.47 (C = O).
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