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[求助]
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Highly efficient and regioselective acylation of pharmacologically interesting cordycepin catalyzed by lipase in the eco-friendly solvent 2-methyltetrahydrofuran A total of nine lipases and three proteases were tested for enzymatic regioselective acylation(s) of cordycepin with vinyl acetate in organic media. The highest conversion with better initial reaction rate was achieved with immobilized Candida antarctica lipase B (Novozym 435). An eco-friendly solvent 2-methyltetrahydrofuran (MeTHF) was thought to be the most suitable reaction medium. Novozym 435 was found to be a useful biocatalyst for the 25-g scale syntheses of cordycepin acetate (96.2% isolated yield), and the biocatalyst displayed excellent regioselectivity and high operational stability during the transformation. The 5′-substituted cordycepin derivative was the sole detectable product from each acylation reaction. Novozym 435 could be recycled for the synthesis of cordycepin derivative on a 25-g scale and 63% of its original activity was maintained after being reused for 7 batches. MeTHF could be considered as an eco-friendly solvent for the large scale use in biotransformation. |
至尊木蟲 (著名寫手)
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環(huán)保溶劑2-甲基四氫呋喃中脂肪酶催化的高效構(gòu)像選擇性;兴幱脙r值的蟲草素 嘗試了九種脂肪酶和三種蛋白酶在有機溶劑對蟲草素進行乙酸乙烯酯選擇性;。固定化南極假絲酵母脂肪酶 B(Novozym 435)具有較好的初始反應(yīng)速率和最高的轉(zhuǎn)化率。一種環(huán)保溶劑2-甲基四氫呋喃(methf)是最合適的反應(yīng)介質(zhì)。Novozym 435作為生物催化劑在25克級規(guī)模合成中非常有效(收率96.2%),表現(xiàn)出優(yōu)異的選擇性和轉(zhuǎn)換過程較好的穩(wěn)定性。5′取代的蟲草素衍生物是;磻(yīng)的唯一測到的產(chǎn)物。在25克的規(guī)模合物中可以回收利用, 重復(fù)利用7次后仍保持原活性的63% 。在生物轉(zhuǎn)化中methf是一種環(huán)保的,可以大量使用的溶劑。 |

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